Readily functionalizable phosphonium-tagged fluorescent coumarins for enhanced detection of conjugates by mass spectrometry

Antoine Lizzul-Jurse, Laetitia Bailly, Marie Hubert-Roux, Carlos Afonso, Pierre-Yves Renard and Cyrille Sabot

Org. Biomol. Chem., 2016, 14, 7777
DOI: 10.1039/C6OB01080F

Dihydrofolate reductase inhibitory peptides screened from a structured designed β-loop peptide library displayed on phage

Hiroshi Tsutsumi, Kazuhiko Nakano and Hisakazu Mihara

Mol. BioSyst., 2015, 11, 2713
DOI: 10.1039/C5MB00316D

Structural diversity, hypothetical biosynthesis, chemical synthesis, and biological activity ofGanodermameroterpenoids

Xing-Rong Peng, Sybille B. Unsicker, Jonathan Gershenzon and Ming-Hua Qiu

Nat. Prod. Rep., 2023, 40, 1354
DOI: 10.1039/D3NP00006K

Development of 2-aminooxazoline 3-azaxanthene β-amyloid cleaving enzyme (BACE) inhibitors with improved selectivity against Cathepsin D

Jonathan D. Low, Michael D. Bartberger, Kui Chen, Yuan Cheng, Mark R. Fielden, Vijay Gore, Dean Hickman, Qingyian Liu, E. Allen Sickmier, Hugo M. Vargas, Jonathan Werner, Ryan D. White, Douglas A. Whittington, Stephen Wood and Ana E. Minatti

Med. Chem. Commun., 2017, 8, 1196
DOI: 10.1039/C7MD00106A

Synthesis of amino heterocycle aspartyl protease inhibitors

Rachel K. Chambers, Tanweer A. Khan, David B. Olsen and Brad E. Sleebs

Org. Biomol. Chem., 2016, 14, 4970
DOI: 10.1039/C5OB01842K

Hypseudone A, a hyperforin-derived polycyclic polyprenylated acylphloroglucinol with caged skeleton from Hypericum pseudohenryi

Na-Na Jiang, Yan-Song Ye and Gang Xu

Org. Chem. Front., 2025, 12, 947
DOI: 10.1039/D4QO01955E

Multifunctional inhibitors of β-amyloid aggregation based on MoS2/AuNR nanocomposites with high near-infrared absorption

Xinhuan Wang, Qiusen Han, Xueliang Liu, Chen Wang and Rong Yang

Nanoscale, 2019, 11, 9185
DOI: 10.1039/C9NR01845J

Interaction mechanism exploration of HEA derivatives as BACE1 inhibitors by in silico analysis

Qian Wu, Xianguo Li, Qingping Gao, Jinghui Wang, Yan Li and Ling Yang

Mol. BioSyst., 2016, 12, 1151
DOI: 10.1039/C5MB00859J

Asperterpenes A and B, two unprecedented meroterpenoids from Aspergillus terreus with BACE1 inhibitory activities

Changxing Qi, Jian Bao, Jianping Wang, Hucheng Zhu, Yongbo Xue, Xiaochuan Wang, Hua Li, Weiguang Sun, Weixi Gao, Yongji Lai, Jian-Guo Chen and Yonghui Zhang

Chem. Sci., 2016, 7, 6563
DOI: 10.1039/C6SC02464E

The supersaturation perspective on the amyloid hypothesis

Diana Portugal Barron and Zhefeng Guo

Chem. Sci., 2024, 15, 46
DOI: 10.1039/D3SC03981A

(±)-Spiroganoapplanin A, a complex polycyclic meroterpenoid dimer from Ganoderma applanatum displaying potential against Alzheimer's disease

Xing-Rong Peng, Rong-Can Luo, Hai-Guo Su, Lin Zhou, Xiao-Qian Ran, Ya-Rong Guo, Yong-Gang Yao and Ming-Hua Qiu

Org. Chem. Front., 2022, 9, 3093
DOI: 10.1039/D2QO00246A

The dual role of thiourea in the thiotrifluoromethylation of alkenes

Paolo Ricci, Tanatorn Khotavivattana, Lukas Pfeifer, Maurice Médebielle, John Richard Morphy and Véronique Gouverneur

Chem. Sci., 2017, 8, 1195
DOI: 10.1039/C6SC02790C

Expansion of the structure–activity relationships of BACE1 inhibitors by harnessing diverse building blocks prepared using a unified synthetic approach

Joan Mayol-Llinàs, Shiao Chow and Adam Nelson

Med. Chem. Commun., 2019, 10, 616
DOI: 10.1039/C9MD00085B

Tripeptides inhibit dual targets AChE and BACE-1: a computational study

Anh Tuan Do, Trung Hai Nguyen, Minh Quan Pham, Huy Truong Nguyen, Nguyen Phuoc Long, Van Van Vu, Huong Thi Thu Phung and Son Tung Ngo

RSC Adv., 2025, 15, 12866
DOI: 10.1039/D5RA00709G

A new G-triplex-based strategy for sensitivity enhancement of the detection of endonuclease activity and inhibition

Congcong Gao, Baoquan Che and Hong Dai

RSC Adv., 2021, 11, 28008
DOI: 10.1039/D1RA04203C

Irreversible destruction of amyloid fibril plaques by conjugated polymer based fluorogenic nanogrenades

Wei-Tao Dou, Ying Lv, Chunyan Tan, Guo-Rong Chen and Xiao-Peng He

J. Mater. Chem. B, 2016, 4, 4502
DOI: 10.1039/C6TB01351A

Current and emerging therapeutic targets of alzheimer's disease for the design of multi-target directed ligands

Laura Blaikie, Graeme Kay and Paul Kong Thoo Lin

Med. Chem. Commun., 2019, 10, 2052
DOI: 10.1039/C9MD00337A

Homo-condensation of acetophenones toward imidazothiones

Phuc Hoang Pham, Phuc Thai Thien Nguyen, Thuy Thu Bui, Hien Nhat Tra, Tung Thanh Nguyen and Nam Thanh Son Phan

RSC Adv., 2020, 10, 40225
DOI: 10.1039/D0RA03047C

Recent Advances in Antibody Therapy for Alzheimer’s Disease: Focus on Bispecific Antibodies

Han-Mo Yang

IJMS, 2025, 26, 6271
DOI: 10.3390/ijms26136271

Osthole decreases beta amyloid levels through up-regulation of miR-107 in Alzheimer’s disease

Yanan Jiao, Liang Kong, Yingjia Yao, Shaoheng Li, Zhenyu Tao, Yuhui Yan and Jingxian Yang

Neuropharmacology, 2016, 108, 332
DOI: 10.1016/j.neuropharm.2016.04.046

Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine β-Secretase (BACE1) Inhibitors via Active Conformation Stabilization

Kenji Nakahara, Kouki Fuchino, Kazuo Komano, Naoya Asada, Genta Tadano, Tsuyoshi Hasegawa, Takahiko Yamamoto, Yusuke Sako, Masayoshi Ogawa, Chie Unemura, Motoko Hosono, Hisanori Ito, Gaku Sakaguchi, Shigeru Ando, Shuichi Ohnishi, Yasuto Kido, Tamio Fukushima, Deborah Dhuyvetter, Herman Borghys, Harrie J. M. Gijsen, Yoshinori Yamano, Yasuyoshi Iso and Ken-ichi Kusakabe

J. Med. Chem., 2018, 61, 5525
DOI: 10.1021/acs.jmedchem.8b00011

Multicomponent Reactions As a Privileged Tool for Multitarget-Directed Ligand Strategies in Alzheimer’s Disease Therapy

Sylvain Grosjean, Irene Pachón-Angona, Michella Dawra, Bernard Refouvelet and Lhassane Ismaili

Future Med. Chem., 2022, 14, 1583
DOI: 10.4155/fmc-2022-0170

Beta-site APP-cleaving Enzyme-1 Inhibitory Role of Natural Flavonoids in the Treatment of Alzheimer's Disease

Sandeep Singh, Virendra Kushwaha, Shriram Sisodia, Shivendra Kumar and Kantrol Kumar Sahu

CNSAMC, 2025, 25, 39
DOI: 10.2174/0118715249315049240710063455

Interaction Prediction on BACE-1 Inhibitors Data for Alzheimer Disease using Message Passing Neural Network

Suat Toraman and Bihter Daş

Firat University Journal of Experimental and Computational Engineering, 2025, 4, 72
DOI: 10.62520/fujece.1466902

Rhizophora mucronata attenuates beta-amyloid induced cognitive dysfunction, oxidative stress and cholinergic deficit in Alzheimer’s disease animal model

Natarajan Suganthy, Dicson Sheeja Malar and Kasi Pandima Devi

Metab Brain Dis, 2016, 31, 937
DOI: 10.1007/s11011-016-9831-0

BACE-1 Inhibitors Targeting Alzheimer's Disease

Kadja Luana Chagas Monteiro, Marcone Gomes dos Santos Alcântara, Nathalia Monteiro Lins Freire, Esaú Marques Brandão, Vanessa Lima do Nascimento, Líbni Maísa dos Santos Viana, Thiago Mendonça de Aquino and Edeildo Ferreira da Silva-Júnior

CAR, 2023, 20, 131
DOI: 10.2174/1567205020666230612155953

Bioinformatic analysis reveals the molecular targets of tangeretin in overcoming the resistance of breast cancer to tamoxifen

Adam Hermawan, Herwandhani Putri and Muthi Ikawati

Gene Reports, 2020, 21, 100884
DOI: 10.1016/j.genrep.2020.100884

Design, in silico and pharmacological evaluation of a peptide inhibitor of BACE-1

Renata Boldin, Bianca Cestari Zychar, Luis Roberto C. Gonçalves and Juliana Mozer Sciani

Front. Pharmacol., 2023, 14
DOI: 10.3389/fphar.2023.1184006

Lack of β-amyloid cleaving enzyme-1 (BACE1) impairs long-term synaptic plasticity but enhances granule cell excitability and oscillatory activity in the dentate gyrus in vivo

Matej Vnencak, Marieke L. Schölvinck, Stephan W. Schwarzacher, Thomas Deller, Michael Willem and Peter Jedlicka

Brain Struct Funct, 2019, 224, 1279
DOI: 10.1007/s00429-019-01836-6

Development of novel BACE1 inhibitors with a hydroxyproline-derived N-amidinopyrrolidine scaffold

Kazuya Kobayashi, Chinami Taniguchi, Misaki Tanaka, Rani Kimura, Kaho Komurasaki, Meguru Kuwano, Mayu Ikemoto, Natsuki Kawakami, Shinya Oishi, Yasunao Hattori and Kenichi Akaji

Bioorganic & Medicinal Chemistry, 2025, 120, 118086
DOI: 10.1016/j.bmc.2025.118086

Therapeutic peptides targeting intracellular molecules

Rahela Zaman and Ezharul Hoque Chowdhury

European Polymer Journal, 2024, 219, 113386
DOI: 10.1016/j.eurpolymj.2024.113386

Alleviation of Neurological Disorders by Targeting Neurodegenerative-Associated Enzymes: Natural and Synthetic Molecules

Alka Ashok Singh, Fazlurrahman Khan and Minseok Song

IJMS, 2025, 26, 4707
DOI: 10.3390/ijms26104707

Screening Platform Based on Inductively Coupled Plasma Mass Spectrometry for β-Site Amyloid Protein Cleaving Enzyme 1 (BACE1) Inhibitors

Xin Jin, Limin Yang, Xiaowen Yan and Qiuquan Wang

ACS Chem. Neurosci., 2021, 12, 1093
DOI: 10.1021/acschemneuro.0c00816

Population density analysis for determining the protonation state of the catalytic dyad in BACE1-tertiary carbinamine-based inhibitor complex

Carlos Gueto-Tettay, Luis Pelaez-Bedoya and Juan Carlos Drosos-Ramirez

Journal of Biomolecular Structure and Dynamics, 2018, 36, 3557
DOI: 10.1080/07391102.2017.1393461

One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues

Jessica Bais, Fabio Benedetti, Federico Berti, Iole Cerminara, Sara Drioli, Maria Funicello, Giorgia Regini, Mattia Vidali and Fulvia Felluga

Molecules, 2020, 25, 4152
DOI: 10.3390/molecules25184152

Conjugated Dienones from Differently Substituted Cinnamaldehyde as Highly Potent Monoamine Oxidase-B Inhibitors: Synthesis, Biochemistry, and Computational Chemistry

Bijo Mathew, Jong Min Oh, Mohamed A. Abdelgawad, Ahmed Khames, Mohammed M. Ghoneim, Sunil Kumar, Lekshmi R. Nath, Sachithra Thazhathuveedu Sudevan, Della Grace Thomas Parambi, Clement Agoni, Mahmoud E. S. Soliman and Hoon Kim

ACS Omega, 2022, 7, 8184
DOI: 10.1021/acsomega.2c00397

Synthesis of morpholine derivatives using the Castagnoli-Cushman reaction as BACE1 inhibitors: Unexpected binding activity of cyclic thioamides

Lorenzo Calugi, Elena Lenci, Riccardo Innocenti and Andrea Trabocchi

Bioorganic & Medicinal Chemistry Letters, 2020, 30, 127211
DOI: 10.1016/j.bmcl.2020.127211

Potential Role of Venular Amyloid in Alzheimer’s Disease Pathogenesis

Christopher D. Morrone, Jossana Bishay and JoAnne McLaurin

IJMS, 2020, 21, 1985
DOI: 10.3390/ijms21061985

Secretase promotes AD progression: simultaneously cleave Notch and APP

Ke-Fan Yang, Jing-Yi Zhang, Mei Feng, Kuo Yao, Yue-Yang Liu, Ming-Sheng Zhou and Hui Jia

Front. Aging Neurosci., 2024, 16
DOI: 10.3389/fnagi.2024.1445470

Potent BACE1 inhibitory and neuroprotective activities of three lignans, styraxlignolide A, masutakeside I, and egonol, isolated from Styrax japonica

Jong Min Oh, Woong-Hee Shin, Eonmi Kim, Yoon-Ju Kwon and Hoon Kim

Fitoterapia, 2025, 186, 106789
DOI: 10.1016/j.fitote.2025.106789

Sulfonamido, amido heterocyclic adducts of tetrazole derivatives as BACE1 inhibitors: in silico exploration

Nachiket Joshi and Rajasekhar Reddy Alavala

Mol Divers, 2024, 28, 4017
DOI: 10.1007/s11030-023-10792-7

Drug Development for Alzheimer’s and Parkinson’s Disease: Where Do We Go Now?

Lisa Sequeira, Sofia Benfeito, Carlos Fernandes, Inês Lima, Joana Peixoto, Catarina Alves, Cláudia Sofia Machado, Alexandra Gaspar, Fernanda Borges and Daniel Chavarria

Pharmaceutics, 2024, 16, 708
DOI: 10.3390/pharmaceutics16060708

Potent and Selective Inhibitors of Human Monoamine Oxidase A from an Endogenous Lichen Fungus Diaporthe mahothocarpus

Geum Seok Jeong, Prima F. Hillman, Myung-Gyun Kang, Sungbo Hwang, Jong-Eun Park, Sang-Jip Nam, Daeui Park and Hoon Kim

JoF, 2021, 7, 876
DOI: 10.3390/jof7100876

Synthesis of Ketones through Microwave Irradiation Promoted Metal-Free Alkylation of Aldehydes by Activation of C(sp3)–H Bond

Xinying Zhang, Zhangxin Wang, Xuesen Fan and Jianji Wang

J. Org. Chem., 2015, 80, 10660
DOI: 10.1021/acs.joc.5b01824

Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand

Arun K. Ghosh, Koena Ghosh, Margherita Brindisi, Emma K. Lendy, Yu-Chen Yen, Nagaswamy Kumaragurubaran, Xiangping Huang, Jordan Tang and Andrew D. Mesecar

Bioorganic & Medicinal Chemistry Letters, 2018, 28, 2605
DOI: 10.1016/j.bmcl.2018.06.045

Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors

Jian Liu, Wuyan Chen, Yechun Xu, Sumei Ren, Wei Zhang and Yingxia Li

Bioorganic & Medicinal Chemistry, 2015, 23, 1963
DOI: 10.1016/j.bmc.2015.03.034

Multifaceted targeting of neurodegeneration with bioactive molecules of saffron (Crocus sativus): An insilco evidence-based hypothesis

V.K.D. Krishnaswamy, Phaniendra Alugoju and Latha Periyasamy

Medical Hypotheses, 2020, 143, 109872
DOI: 10.1016/j.mehy.2020.109872

Conformational Dynamics and Binding Free Energies of Inhibitors of BACE-1: From the Perspective of Protonation Equilibria

M. Olivia Kim, Patrick G. Blachly, J. Andrew McCammon and Dennis R Livesay

PLoS Comput Biol, 2015, 11, e1004341
DOI: 10.1371/journal.pcbi.1004341

Design, synthesis, biological activity evaluation and in silico studies of new nicotinohydrazide derivatives as multi-targeted inhibitors for Alzheimer's disease

Fatih Tok, Begüm Nurpelin Sağlık, Yusuf Özkay, Zafer Asım Kaplancıklı and Bedia Koçyiğit-Kaymakçıoğlu

Journal of Molecular Structure, 2022, 1265, 133441
DOI: 10.1016/j.molstruc.2022.133441

Synthetic Analogues of Betulinic Acid as Potent Inhibitors of PS1/BACE1 Interaction to Reduce Aβ Generation

Chenlu Zhang, Xiaoyin Wang, Jin Cui, Xiaohang Li, Yangming Zhang, Xin Wang, Haifeng Gu, Wei Li, Xin Xie, Jian Zhao, Gang Pei and Fajun Nan

Chin. J. Chem., 2017, 35, 103
DOI: 10.1002/cjoc.201600611

Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation

Dawid Panek, Anna Więckowska, Tomasz Wichur, Marek Bajda, Justyna Godyń, Jakub Jończyk, Kamil Mika, Jana Janockova, Ondrej Soukup, Damijan Knez, Jan Korabecny, Stanislav Gobec and Barbara Malawska

European Journal of Medicinal Chemistry, 2017, 125, 676
DOI: 10.1016/j.ejmech.2016.09.078

Navigating the Chemical Space of Multitarget-Directed Ligands: From Hybrids to Fragments in Alzheimer’s Disease

Federica Prati, Andrea Cavalli and Maria Bolognesi

Molecules, 2016, 21, 466
DOI: 10.3390/molecules21040466

Effects of Fish Oil Combined with Selenium and Zinc on Learning and Memory Impairment in Aging Mice and Amyloid Precursor Protein Processing

Chao-xu Fu, Lin Dai, Xiu-yuan Yuan and Yan-ji Xu

Biol Trace Elem Res, 2021, 199, 1855
DOI: 10.1007/s12011-020-02280-y

Dynamic Kinetic Resolution of Allylic Azides via Asymmetric Dihydroxylation

Amy A. Ott, Charles S. Goshey and Joseph J. Topczewski

J. Am. Chem. Soc., 2017, 139, 7737
DOI: 10.1021/jacs.7b04203

Activation of CREB‐mediated autophagy by thioperamide ameliorates β‐amyloid pathology and cognition in Alzheimer’s disease

Jiangong Wang, Bin Liu, Yong Xu, Meizi Yang, Chaoyun Wang, Mengmeng Song, Jing Liu, Wentao Wang, Jingjing You, Fengjiao Sun, Dan Wang, Dunjiang Liu and Haijing Yan

Aging Cell, 2021, 20
DOI: 10.1111/acel.13333

Macrocyclic BACE1 inhibitors with hydrophobic cross-linked structures: Optimization of ring size and ring structure

Takuya Otani, Yasunao Hattori, Kenichi Akaji and Kazuya Kobayashi

Bioorganic & Medicinal Chemistry, 2021, 52, 116517
DOI: 10.1016/j.bmc.2021.116517

Rapid Identification of Tanshinone IIA Metabolites in an Amyloid-β1-42 Induced Alzherimer’s Disease Rat Model using UHPLC-Q-Exactive Qrbitrap Mass Spectrometry

Shuang Liang, Zijian Wang, Jiaqi Yuan, Jing Zhang, Xueling Dai, Fei Qin, Jiayu Zhang and Yaxuan Sun

Molecules, 2019, 24, 2584
DOI: 10.3390/molecules24142584

Structure-Based Design of Selective β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: Targeting the Flap to Gain Selectivity over BACE2

Kazuki Fujimoto, Eriko Matsuoka, Naoya Asada, Genta Tadano, Takahiko Yamamoto, Kenji Nakahara, Kouki Fuchino, Hisanori Ito, Naoki Kanegawa, Diederik Moechars, Harrie J. M. Gijsen and Ken-ichi Kusakabe

J. Med. Chem., 2019, 62, 5080
DOI: 10.1021/acs.jmedchem.9b00309

Inhibitory Effects of Macelignan on Tau Phosphorylation and Aβ Aggregation in the Cell Model of Alzheimer's Disease

Liang Gu, Nan Cai, Meiting Li, Decheng Bi, Lijun Yao, Weishan Fang, Yan Wu, Zhangli Hu, Qiong Liu, Zhijian Lin, Jun Lu and Xu Xu

Front. Nutr., 2022, 9
DOI: 10.3389/fnut.2022.892558

Strategies to target bioactive molecules to subcellular compartments. Focus on natural compounds

Lucia Biasutto, Andrea Mattarei, Martina La Spina, Michele Azzolini, Sofia Parrasia, Ildikò Szabò and Mario Zoratti

European Journal of Medicinal Chemistry, 2019, 181, 111557
DOI: 10.1016/j.ejmech.2019.07.060

Graph Theoretical Network Analysis and Pharmacoinformatics-Based Investigation of Bioactive Compounds from Semecarpus anacardium Linn. for Alzheimer’s Disease

Muniyandi Vijayalakshmi, Velmurugan Sundarapandian, Velayutham Siva Bharathi, Parasuraman Pavadai, Krishnan Sundar, Selvaraj Kunjiappan and Sureshbabu Ram Kumar Pandian

J. Comput. Biophys. Chem., 2025, 24, 287
DOI: 10.1142/S2737416523410028

The structure-based optimization of δ-sultone-fused pyrazoles as selective BuChE inhibitors

Ziwen Zhang, Jingli Min, Mengdie Chen, Xia Jiang, Yingying Xu, Huali Qin and Wenjian Tang

European Journal of Medicinal Chemistry, 2020, 201, 112273
DOI: 10.1016/j.ejmech.2020.112273

Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1′-P2′ ligands

Arun K. Ghosh, Margherita Brindisi, Yu-Chen Yen, Emilio L. Cárdenas, Jean-Rene Ella-Menye, Nagaswamy Kumaragurubaran, Xiangping Huang, Jordan Tang and Andrew D. Mesecar

Bioorganic & Medicinal Chemistry Letters, 2017, 27, 2432
DOI: 10.1016/j.bmcl.2017.04.011

Highly stereoselective asymmetric aldol routes to tert-butyl-2-(3,5-difluorophenyl)-1-oxiran-2-yl)ethyl)carbamates: Building blocks for novel protease inhibitors

Arun K. Ghosh, Emilio L. Cárdenas and Margherita Brindisi

Tetrahedron Letters, 2017, 58, 4062
DOI: 10.1016/j.tetlet.2017.09.025

Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer’s disease (1998–2018)

Pankaj Mishra, Amit Kumar and Gautam Panda

Bioorganic & Medicinal Chemistry, 2019, 27, 895
DOI: 10.1016/j.bmc.2019.01.025

Self-Assembly of Superquenched Gold Nanoparticle Nanosensors for Lighting up BACE-1 in Live Cells

Fei Ma, Qi Wang, Qinfeng Xu and Chun-yang Zhang

Anal. Chem., 2021, 93, 15124
DOI: 10.1021/acs.analchem.1c03430

Designed Multifunctional Isopeptide for Enhanced Annexin A1 Biosensing Based on Peptide–Protein Interactions in Human Blood

Rui Han, Yang Li, Wenjie Hou, Caifeng Ding and Xiliang Luo

Anal. Chem., 2023, 95, 9025
DOI: 10.1021/acs.analchem.3c01144

Deoxyschizandrin attenuates Aβ1–42-induced cognitive impairments through up-regulation of AMPA receptors in mice

Tingxu Yan, Mengjie Xu, Shutong Wan, Bo Wu, Feng Xiao, Kaishun Bi and Ying Jia

Phytochemistry Letters, 2018, 28, 24
DOI: 10.1016/j.phytol.2018.09.009

New evolutions in the BACE1 inhibitor field from 2014 to 2018

Chien-Chi Hsiao, Frederik Rombouts and Harrie J.M. Gijsen

Bioorganic & Medicinal Chemistry Letters, 2019, 29, 761
DOI: 10.1016/j.bmcl.2018.12.049

Stepping closer to treating Alzheimer’s disease patients with BACE1 inhibitor drugs

Riqiang Yan

Transl Neurodegener, 2016, 5
DOI: 10.1186/s40035-016-0061-5

Exploring the Role of Monoamine Oxidase Activity in Aging and Alzheimer’s Disease

Md. Sohanur Rahman, Md. Sahab Uddin, Md. Ataur Rahman, Md. Samsuzzaman, Tapan Behl, Abdul Hafeez, Asma Perveen, George E. Barreto and Ghulam Md. Ashraf

CPD, 2021, 27, 4017
DOI: 10.2174/1381612827666210612051713

Fragment-based virtual screening approach and molecular dynamics simulation studies for identification of BACE1 inhibitor leads

Prabu Manoharan and Nanda Ghoshal

Journal of Biomolecular Structure and Dynamics, 2018, 36, 1878
DOI: 10.1080/07391102.2017.1337590

Etiology and management of Alzheimer’s disease: Potential role of gut microbiota modulation with probiotics supplementation

Vaishali Lekchand Dasriya, Mrinal Samtiya, Tejpal Dhewa, Monica Puniya, Sanjeev Kumar, Soniya Ranveer, Vishu Chaudhary, Shilpa Vij, Pradip Behare, Namita Singh, Rotimi E. Aluko and Anil Kumar Puniya

Journal of Food Biochemistry, 2022, 46
DOI: 10.1111/jfbc.14043

Novel Tacrine–Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer’s Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography

Xiaoming Zha, Doriano Lamba, Lili Zhang, Yinghan Lou, Changxu Xu, Di Kang, Li Chen, Yungen Xu, Luyong Zhang, Angela De Simone, Sarah Samez, Alessandro Pesaresi, Jure Stojan, Manuela G. Lopez, Javier Egea, Vincenza Andrisano and Manuela Bartolini

J. Med. Chem., 2016, 59, 114
DOI: 10.1021/acs.jmedchem.5b01119

Prospects of β‐Secretase Inhibitors for the Treatment of Alzheimer’s Disease

Arun K. Ghosh and Jordan Tang

ChemMedChem, 2015, 10, 1463
DOI: 10.1002/cmdc.201500216

New BACE1 Chimeric Peptide Inhibitors Selectively Prevent AβPP-β Cleavage Decreasing Amyloid-β Production and Accumulation in Alzheimer’s Disease Models

Rosa Resende, Marisa Ferreira-Marques, Patrícia Moreira, Judite R.M. Coimbra, Salete J. Baptista, Ciro Isidoro, Jorge A.R. Salvador, Teresa C.P. Dinis, Cláudia F. Pereira and Armanda E. Santos

JAD, 2020, 76, 1317
DOI: 10.3233/JAD-200381

Rare Variant Analysis and Molecular Dynamics Simulation in Alzheimer’s Disease Identifies Exonic Variants in FLG

Weixue Xiong, Jiahui Cai, Ruijia Li, Canhong Wen and Haizhu Tan

Genes, 2022, 13, 838
DOI: 10.3390/genes13050838

miR-124 downregulates BACE 1 and alters autophagy in APP/PS1 transgenic mice

Xiaoxue Du, Xue Huo, Yang Yang, Zhiying Hu, Benson O.A. Botchway, Yuting Jiang and Marong Fang

Toxicology Letters, 2017, 280, 195
DOI: 10.1016/j.toxlet.2017.08.082

Rational Design of Novel 1,3-Oxazine Based β-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust Aβ Reduction in the Brain

Kouki Fuchino, Yasunori Mitsuoka, Moriyasu Masui, Noriyuki Kurose, Shuhei Yoshida, Kazuo Komano, Takahiko Yamamoto, Masayoshi Ogawa, Chie Unemura, Motoko Hosono, Hisanori Ito, Gaku Sakaguchi, Shigeru Ando, Shuichi Ohnishi, Yasuto Kido, Tamio Fukushima, Hirofumi Miyajima, Shuichi Hiroyama, Kiyotaka Koyabu, Deborah Dhuyvetter, Herman Borghys, Harrie J. M. Gijsen, Yoshinori Yamano, Yasuyoshi Iso and Ken-ichi Kusakabe

J. Med. Chem., 2018, 61, 5122
DOI: 10.1021/acs.jmedchem.8b00002

One protein, multiple pathologies: multifaceted involvement of amyloid β in neurodegenerative disorders of the brain and retina

Vivek Gupta, Veer B. Gupta, Nitin Chitranshi, Sumudu Gangoda, Roshana Vander Wall, Mojdeh Abbasi, Mojtaba Golzan, Yogita Dheer, Tejal Shah, Alberto Avolio, Roger Chung, Ralph Martins and Stuart Graham

Cell. Mol. Life Sci., 2016, 73, 4279
DOI: 10.1007/s00018-016-2295-x

Redox‐Activated Near‐Infrared‐Responsive Polyoxometalates Used for Photothermal Treatment of Alzheimer's Disease

Mengmeng Ma, Nan Gao, Yuhuan Sun, Xiubo Du, Jinsong Ren and Xiaogang Qu

Adv Healthcare Materials, 2018, 7
DOI: 10.1002/adhm.201800320

Large language models for Alzheimer's disease drug discovery

Tursun Alkam, Ebrahim Tarshizi and Andrew H Van Benschoten

Journal of Alzheimer’s Disease, 2025, 106, 799
DOI: 10.1177/13872877251346890

Advanced analytical methodologies in Alzheimer’s disease drug discovery

Angela De Simone, Marina Naldi, Daniele Tedesco, Manuela Bartolini, Lara Davani and Vincenza Andrisano

Journal of Pharmaceutical and Biomedical Analysis, 2020, 178, 112899
DOI: 10.1016/j.jpba.2019.112899

Implications of Microorganisms in Alzheimer’s Disease

Pardeep Yadav, Yeon-Hee Lee, Hrithika Panday, Shubham Kant, Neha Bajwa, Ritika Parashar, Saurabh Kumar Jha, Niraj Kumar Jha, Parma Nand, Sang-Soo Lee and Abhimanyu Kumar Jha

CIMB, 2022, 44, 4584
DOI: 10.3390/cimb44100314

Amyloid‐β in Alzheimer's disease: Structure, toxicity, distribution, treatment, and prospects

Yifan Yu, Shilong Yu, Giuseppe Battaglia and Xiaohe Tian

Ibrain, 2024
DOI: 10.1002/ibra.12155

Have there been improvements in Alzheimer’s disease drug discovery over the past 5 years?

Ramón Cacabelos

Expert Opinion on Drug Discovery, 2018, 13, 523
DOI: 10.1080/17460441.2018.1457645

Combining Virtual Screening Protocol and In Vitro Evaluation towards the Discovery of BACE1 Inhibitors

Judite R. M. Coimbra, Salete J. Baptista, Teresa C. P. Dinis, Maria M. C. Silva, Paula I. Moreira, Armanda E. Santos and Jorge A. R. Salvador

Biomolecules, 2020, 10, 535
DOI: 10.3390/biom10040535

Ameliorating Ribosylation-Induced Amyloid-β Pathology by Berberine via Inhibiting mTOR/p70S6K Signaling

Yang-Yang Wang, Qian Yan, Zhen-Ting Huang, Qian Zou, Jing Li, Ming-Hao Yuan, Liang-Qi Wu and Zhi-You Cai

JAD, 2021, 79, 833
DOI: 10.3233/JAD-200995

Quantum computational quantification of protein–ligand interactions

Josh J. M. Kirsopp, Cono Di Paola, David Zsolt Manrique, Michal Krompiec, Gabriel Greene‐Diniz, Wolfgang Guba, Agnes Meyder, Detlef Wolf, Martin Strahm and David Muñoz Ramo

Int J of Quantum Chemistry, 2022, 122
DOI: 10.1002/qua.26975

Networkodynamic approach to perceive the key phytoconstituents of E. officinalis (Amla) as natural BACE1 inhibitors: an in-silico study

Dhairiya Agarwal, Jatin Malik, Neeru Bhanwala, Ramesh Ambatwar, Sumit Kumar, Lokesh Chandrakar, Ashok Kumar Datusalia and Gopal L. Khatik

Journal of Biomolecular Structure and Dynamics, 2024, 42, 12304
DOI: 10.1080/07391102.2023.2269260

Modulating physicochemical properties of tetrahydropyridine-2-amine BACE1 inhibitors with electron-withdrawing groups: A systematic study

Frederik J.R. Rombouts, Chien-Chi Hsiao, Solène Bache, Michel De Cleyn, Pauline Heckmann, Jos Leenaerts, Carolina Martinéz-Lamenca, Sven Van Brandt, Aldo Peschiulli, Ann Vos and Harrie J.M. Gijsen

European Journal of Medicinal Chemistry, 2022, 228, 114028
DOI: 10.1016/j.ejmech.2021.114028

Advances Toward Multifunctional Cholinesterase and β-Amyloid Aggregation Inhibitors

Dawid Panek, Tomasz Wichur, Justyna Godyń , Anna Pasieka and Barbara Malawska

Future Med. Chem., 2017, 9, 1835
DOI: 10.4155/fmc-2017-0094

Molecular insight into the interaction mechanisms of amino-2H -imidazole derivatives with BACE1 protease: A QM/MM and QTAIM study

Esteban Gabriel Vega-Hissi, Rodrigo Tosso, Ricardo Daniel Enriz and Lucas Joel Gutierrez

Int. J. Quantum Chem., 2015, 115, 389
DOI: 10.1002/qua.24854

Polymethoxyflavones: Novel β-Secretase (BACE1) Inhibitors from Citrus Peels

Kumju Youn, Yoonjin Yu, Jinhyuk Lee, Woo-Sik Jeong, Chi-Tang Ho and Mira Jun

Nutrients, 2017, 9, 973
DOI: 10.3390/nu9090973

Synthesis and biological properties of amino acids and peptides containing a tetrazolyl moiety

E A Popova and R E Trifonov

Russ. Chem. Rev., 2015, 84, 891
DOI: 10.1070/RCR4527

Critical evaluation of current Alzheimer’s drug discovery (2018–19) & futuristic Alzheimer drug model approach

Atukuri Dorababu

Bioorganic Chemistry, 2019, 93, 103299
DOI: 10.1016/j.bioorg.2019.103299

Structure Dependent Differential Modulation of Aβ Fibrillization by Selenadiazole-Based Inhibitors

Umme Kalsoom, Meshari Alazmi, Hafiz Syed Usama Bin Farrukh, Ka Hang Karen Chung, Nawaf Alshammari, Aleksandr Kakinen, Ghayoor Abbas Chotana, Ibrahim Javed, Thomas Paul Davis and Rahman Shah Zaib Saleem

ACS Chem. Neurosci., 2021, 12, 3806
DOI: 10.1021/acschemneuro.1c00478

BACE1 inhibitory activity and molecular docking analysis of meroterpenoids from Sargassum serratifolium

Su Hui Seong, Md Yousof Ali, Hyeung-Rak Kim, Hyun Ah Jung and Jae Sue Choi

Bioorganic & Medicinal Chemistry, 2017, 25, 3964
DOI: 10.1016/j.bmc.2017.05.033

Chromenone Derivatives as Monoamine Oxidase Inhibitors from Marine-Derived MAR4 Clade Streptomyces sp. CNQ-031

Jong Min Oh, Chaeyoung Lee, Sang-Jip Nam and Hoon Kim

J. Microbiol. Biotechnol., 2021, 31, 1022
DOI: 10.4014/jmb.2105.05003

A phenotypic approach to the discovery of compounds that promote non-amyloidogenic processing of the amyloid precursor protein: Toward a new profile of indirect β-secretase inhibitors

Marion Gay, Caroline Evrard, Florian Descamps, Pascal Carato, Nicolas Renault, Mathilde Coevoet, Sabiha Eddarkaoui, Catherine Baud, Paul-Emmanuel Larchanché, Luc Buée, Jamal El Bakali, Valérie Vingtdeux, Nicolas Sergeant and Patricia Melnyk

European Journal of Medicinal Chemistry, 2018, 159, 104
DOI: 10.1016/j.ejmech.2018.08.092

A microfluidics-based mobility shift assay to identify new inhibitors of β-secretase for Alzheimer’s disease

Rongfeng Liu, Yu-Chih Liu, Junwei Meng, Haiyan Zhu and Xuehong Zhang

Anal Bioanal Chem, 2017, 409, 6635
DOI: 10.1007/s00216-017-0617-y

Cholinesterase inhibitory alkaloids from the rhizomes of Coptis chinensis

Thao Quyen Cao, Quynh-Mai Thi Ngo, Su Hui Seong, Ui Joung Youn, Jeong Ah Kim, Junheon Kim, Jin-Cheol Kim, Mi Hee Woo, Jae Sue Choi and Byung Sun Min

Bioorganic Chemistry, 2018, 77, 625
DOI: 10.1016/j.bioorg.2018.01.038

A simple and label-free electrochemical method for detection of beta-site amyloid precursor protein cleaving enzyme and screening of its inhibitor

Ning Xia, Youjuan Zhang, Pengpeng Guan, Yuanqiang Hao and Lin Liu

Sensors and Actuators B: Chemical, 2015, 213, 111
DOI: 10.1016/j.snb.2015.02.081

Therapeutic Potential of Targeting Regulated Intramembrane Proteolysis Mechanisms of Voltage-Gated Ion Channel Subunits and Cell Adhesion Molecules

Samantha L. Hodges, Alexandra A. Bouza and Lori L. Isom

Pharmacological Reviews, 2022, 74, 1030
DOI: 10.1124/pharmrev.121.000340

Nutrients, Phytochemicals and In Vitro Disease Prevention of Nephelium hypoleucum Kurz Fruit

Linh Khanh Luu, Sirinapa Thangsiri, Yuraporn Sahasakul, Amornrat Aursalung, Woorawee Inthachat, Piya Temviriyanukul, Nattira On-Nom, Chaowanee Chupeerach and Uthaiwan Suttisansanee

Nutrients, 2023, 15, 950
DOI: 10.3390/nu15040950

Umbelliferone and Its Synthetic Derivatives as Suitable Molecules for the Development of Agents with Biological Activities: A Review of Their Pharmacological and Therapeutic Potential

Anita Kornicka, Łukasz Balewski, Monika Lahutta and Jakub Kokoszka

Pharmaceuticals, 2023, 16, 1732
DOI: 10.3390/ph16121732

Tetrazoles: A multi-potent motif in drug design

Ye Yuan, Muzi Li, Vasso Apostolopoulos, John Matsoukas, Wojciech M. Wolf, Mark A.T. Blaskovich, Joanna Bojarska and Zyta M. Ziora

European Journal of Medicinal Chemistry, 2024, 279, 116870
DOI: 10.1016/j.ejmech.2024.116870

Structure-based identification of potent modulators from Centella asiatica targeting BACE-1

Armin Sultana and JooHan Woo

Heliyon, 2025, 11, e42652
DOI: 10.1016/j.heliyon.2025.e42652

Preserved Transmembrane Protein Mobility in Polymer-Supported Lipid Bilayers Derived from Cell Membranes

Hudson Pace, Lisa Simonsson Nyström, Anders Gunnarsson, Elizabeth Eck, Christopher Monson, Stefan Geschwindner, Arjan Snijder and Fredrik Höök

Anal. Chem., 2015, 87, 9194
DOI: 10.1021/acs.analchem.5b01449

Lovastatin attenuates sevoflurane-induced cognitive disorder in aged rats via reducing Aβ accumulation

Ying Xu, Yunxia Dong, Cong Wang, Qian Jiang, Haichao Chu and Yue Tian

Neurochemistry International, 2021, 148, 105078
DOI: 10.1016/j.neuint.2021.105078

From AChE to BACE1 inhibitors: The role of the amine on the indanone scaffold

Angela Rampa, Francesca Mancini, Angela De Simone, Federico Falchi, Federica Belluti, Rita Maria Concetta Di Martino, Silvia Gobbi, Vincenza Andrisano, Andrea Tarozzi, Manuela Bartolini, Andrea Cavalli and Alessandra Bisi

Bioorganic & Medicinal Chemistry Letters, 2015, 25, 2804
DOI: 10.1016/j.bmcl.2015.05.002

Thiazolyl-thiadiazines as Beta Site Amyloid Precursor Protein Cleaving Enzyme-1 (BACE-1) Inhibitors and Anti-inflammatory Agents: Multitarget-Directed Ligands for the Efficient Management of Alzheimer’s Disease

Sneha R. Sagar, Devendra Pratap Singh, Nirupa B. Panchal, Rajesh D. Das, Dhaivat H. Pandya, Vasudevan Sudarsanam, Manish Nivsarkar and Kamala K. Vasu

ACS Chem. Neurosci., 2018, 9, 1663
DOI: 10.1021/acschemneuro.8b00063

Clinical Biomarkers and Novel Drug Targets to Cut Gordian Knots of Alzheimer's Disease

Abdul Jalil Shah, Roohi Mohi-ud-din, Saba Sabreen, Taha Umair Wani, Rafia Jan, Md. Noushad Javed, Prince Ahad Mir, Reyaz Hassan Mir and Mubashir Hussain Masoodi

CMP, 2023, 16, 254
DOI: 10.2174/1874467215666220903095837

Identification of BACE-1 Inhibitors against Alzheimer’s Disease through E-Pharmacophore-Based Virtual Screening and Molecular Dynamics Simulation Studies: An Insilco Approach

Kumarappan Chidambaram

Life, 2023, 13, 952
DOI: 10.3390/life13040952

Comprehensive investigation of multiple targets in the development of newer drugs for the Alzheimer's disease

Patil Ashwini, Bodhankar Subhash, Muthal Amol, Dileep Kumar, Pawar Atmaram and Kulkarni Ravindra

Acta Pharmaceutica Sinica B, 2025, 15, 1281
DOI: 10.1016/j.apsb.2024.11.016

Molecular Mechanisms of Emerging Therapeutic Targets in Alzheimer’s Disease: A Systematic Review

T. Premkumar and S. Sajitha Lulu

Neurochem. J., 2022, 16, 443
DOI: 10.1134/S1819712422040183

Discovery of δ-sultone-fused pyrazoles for treating Alzheimer's disease: Design, synthesis, biological evaluation and SAR studies

Yingying Xu, Ziwen Zhang, Xia Jiang, Xing Chen, Zhuo Wang, Hamed Alsulami, Hua-Li Qin and Wenjian Tang

European Journal of Medicinal Chemistry, 2019, 181, 111598
DOI: 10.1016/j.ejmech.2019.111598

Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors

Juraj Velcicky, Casey J. N. Mathison, Victor Nikulin, Daniel Pflieger, Robert Epple, Mihai Azimioara, Christopher Cow, Pierre-Yves Michellys, Pascal Rigollier, Daniel R. Beisner, Ursula Bodendorf, Danilo Guerini, Bo Liu, Ben Wen, Samantha Zaharevitz and Trixi Brandl

ACS Med. Chem. Lett., 2019, 10, 887
DOI: 10.1021/acsmedchemlett.9b00044

Daphnetin protects neurons in an Alzheimer disease mouse model and normal rat neurons by inhibiting BACE1 activity and activating the Nrf2/HO-1 pathway

Xin Zhang, Wen Ma, Huanyi Liu, Yuanchu Liu, Yaling Zhang, Sitong He, Xiaoli Ding, Baolin Li and Yaping Yan

Journal of Neuropathology & Experimental Neurology, 2024, 83, 670
DOI: 10.1093/jnen/nlae043

Consumption of pomegranates improves synaptic function in a transgenic mice model of Alzheimer's disease

Nady Braidy, Musthafa Mohamed Essa, Anne Poljak, Subash Selvaraju, Samir Al-Adawi, Thamilarasan Manivasagm, Arokiasamy Justin Thenmozhi, Lezanne Ooi, Perminder Sachdev and Gilles J. Guillemin

Oncotarget, 2016, 7, 64589
DOI: 10.18632/oncotarget.10905

Fluorescence Detection and Dissociation of Amyloid‐β Species for the Treatment of Alzheimer's Disease

Guanglei Lv, Yang Shen, Wubin Zheng, Jiajia Yang, Chunxia Li and Jun Lin

Advanced Therapeutics, 2019, 2
DOI: 10.1002/adtp.201900054

Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE)

Kenneth M. Boy, Jason M. Guernon, Yong-Jin Wu, Yunhui Zhang, Joe Shi, Weixu Zhai, Shirong Zhu, Samuel W. Gerritz, Jeremy H. Toyn, Jere E. Meredith, Donna M. Barten, Catherine R. Burton, Charles F. Albright, Andrew C. Good, James E. Grace, Kimberley A. Lentz, Richard E. Olson, John E. Macor and Lorin A. Thompson

Bioorganic & Medicinal Chemistry Letters, 2015, 25, 5040
DOI: 10.1016/j.bmcl.2015.10.031

Tyrosine‐Conjugation Method for Evaluating BACE1 Activity Based on Silver Nanoparticles/Metal–Organic Framework Composites as Electrochemical Tags

Yanli Zhou, Zihan Huang, Jiaxiang Liu, Hui Dong, Yintang Zhang, Maotian Xu and Yanfeng Bi

Chemistry A European J, 2023, 29
DOI: 10.1002/chem.202300450

In silico molecular studies of natural compounds as possible anti-Alzheimer’s agents: ligand-based design

Opeyemi Iwaloye, Olusola Olalekan Elekofehinti, Abiola Ibrahim Momoh, Kikiowo Babatomiwa and Esther Opeyemi Ariyo

Netw Model Anal Health Inform Bioinforma, 2020, 9
DOI: 10.1007/s13721-020-00262-7

A review on synthetic inhibitors of dual-specific tyrosine phosphorylation-regulated kinase 1A (DYRK1A) for the treatment of Alzheimer’s disease (AD)

Pinky Gehlot, Rekha Pathak, Sunil Kumar, Naveen Kumar Choudhary and Vivek Kumar Vyas

Bioorganic & Medicinal Chemistry, 2024, 113, 117925
DOI: 10.1016/j.bmc.2024.117925

Chemoproteomic profiling reveals that cathepsin D off-target activity drives ocular toxicity of β-secretase inhibitors

Andrea M. Zuhl, Charles E. Nolan, Michael A. Brodney, Sherry Niessen, Kevin Atchison, Christopher Houle, David A. Karanian, Claude Ambroise, Jeffrey W. Brulet, Elizabeth M. Beck, Shawn D. Doran, Brian T. O’Neill, Christopher W. am Ende, Cheng Chang, Kieran F. Geoghegan, Graham M. West, Joshua C. Judkins, Xinjun Hou, David R. Riddell and Douglas S. Johnson

Nat Commun, 2016, 7
DOI: 10.1038/ncomms13042

New Neurogenic Lipoic-Based Hybrids as Innovative Alzheimer'S Drugs with σ-1 Agonism and β-Secretase Inhibition

Martín Estrada, Concepción Pérez, Elena Soriano, Erik Laurini, Maurizio Romano, Sabrina Pricl, José A Morales-García, Ana Pérez-Castillo and María Isabel Rodríguez-Franco

Future Med. Chem., 2016, 8, 1191
DOI: 10.4155/fmc-2016-0036

Machine learning-based screening of in-house database to identify BACE-1 inhibitors

Ravi Singh, Asha Anand, Ankit Ganeshpurkar, Powsali Ghosh, Tushar Chaurasia, Ravi Bhushan Singh, Dileep Kumar, Sushil Kumar Singh and Ashok Kumar

Chem. Pap., 2023, 77, 6849
DOI: 10.1007/s11696-023-02982-2

Navigating the Maze of Alzheimer’s disease by exploring BACE1: Discovery, current scenario, and future prospects

Faiza Iram, Mohammad Shahid, Jaoud Ansari, Ghulam Md Ashraf, Md. Imtaiyaz Hassan and Asimul Islam

Ageing Research Reviews, 2024, 98, 102342
DOI: 10.1016/j.arr.2024.102342

Neuroprotective effect of Licochalcone A against aluminum chloride-induced neurotoxicity by reducing Aβ accumulation, oxidative stress and inflammatory reaction

Zhijuan Tang, Fang Wang, Jintao Lv, Gaohong Yang, Xinchun Shen, Fei Zeng, Lingling Meng, Wen Zhou, Libin Zhan and Zebin Weng

NeuroToxicology, 2025, 108, 295
DOI: 10.1016/j.neuro.2025.04.011

Generation of Amyloid‐β Peptides by γ‐Secretase

Rodrigo Aguayo‐Ortiz and Laura Dominguez

Israel Journal of Chemistry, 2017, 57, 574
DOI: 10.1002/ijch.201600073

Rational Design of Dual Inhibitors for Alzheimer's Disease: Insights from Computational Screening of BACE1 and GSK-3β

Magham Sai Varshini, Ramakkamma Aishwarya Reddy, Praveen Thaggikuppe Krishnamurthy and Divakar Selvaraj

CAD, 2024, 20, 998
DOI: 10.2174/0115734099270256231018072007

Trimethoxylated Halogenated Chalcones as Dual Inhibitors of MAO-B and BACE-1 for the Treatment of Neurodegenerative Disorders

Vishal Payyalot Vishal, Jong Min Oh, Ahmed Khames, Mohamed A. Abdelgawad, Aathira Sujathan Nair, Lekshmi R. Nath, Nicola Gambacorta, Fulvio Ciriaco, Orazio Nicolotti, Hoon Kim and Bijo Mathew

Pharmaceutics, 2021, 13, 850
DOI: 10.3390/pharmaceutics13060850

Tetrazoles for biomedicine

Elena A. Popova, Rostislav E. Trifonov and Vladimir A. Ostrovskii

Russ. Chem. Rev., 2019, 88, 644
DOI: 10.1070/RCR4864

Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer’s Disease

Rainer Machauer, Rainer Lueoend, Konstanze Hurth, Siem J. Veenstra, Heinrich Rueeger, Markus Voegtle, Marina Tintelnot-Blomley, Jean-Michel Rondeau, Laura H. Jacobson, Grit Laue, Karen Beltz and Ulf Neumann

J. Med. Chem., 2021, 64, 15262
DOI: 10.1021/acs.jmedchem.1c01300

Calcium channel blockers’ contribution to overcoming Current drug discovery challenges in Alzheimer’s disease

Paul J Bernard, Djamila Bellili and Lhassane Ismaili

Expert Opinion on Drug Discovery, 2024, 19, 21
DOI: 10.1080/17460441.2023.2266994

Flavonoid and Chalcone Scaffolds as Inhibitors of BACE1: Recent Updates

Anishma Payyappilliparambil Narayanan, Jayalakshmi Jayan, Sachithra Thazhathuveedu Sudevan, Archana Dhyani, Subin Mary Zachariah and Bijo Mathew

CCHTS, 2024, 27, 1243
DOI: 10.2174/1386207326666230731092409

Characterization and purification of β−secretase inhibitory peptides fraction from sea cucumber (Holothuria spinifera) enzymatic hydrolysates

Anuruddhika Udayangani Rathnayake, Racheal Abuine, Subramanian Palanisamy, Jung Kwon Lee and Hee-Guk Byun

Process Biochemistry, 2021, 111, 86
DOI: 10.1016/j.procbio.2021.10.007

Application of Free Energy Perturbation for the Design of BACE1 Inhibitors

Myriam Ciordia, Laura Pérez-Benito, Francisca Delgado, Andrés A. Trabanco and Gary Tresadern

J. Chem. Inf. Model., 2016, 56, 1856
DOI: 10.1021/acs.jcim.6b00220

Development of coumarin–benzofuran hybrids as versatile multitargeted compounds for the treatment of Alzheimer’s Disease

Asha Hiremathad, Karam Chand and Rangappa S. Keri

Chem Biol Drug Des, 2018, 92, 1497
DOI: 10.1111/cbdd.13316

Edaravone N-benzyl pyridinium derivatives: BACE-1 inhibition, kinetics and in silico binding pose determination

L.S. Zondagh, S.F. Malan and J. Joubert

European Journal of Pharmaceutical Sciences, 2024, 201, 106869
DOI: 10.1016/j.ejps.2024.106869

Amyloid cascade in Alzheimer's disease: Recent advances in medicinal chemistry

Tarek Mohamed, Arash Shakeri and Praveen P.N. Rao

European Journal of Medicinal Chemistry, 2016, 113, 258
DOI: 10.1016/j.ejmech.2016.02.049

Consequences of Pharmacological BACE Inhibition on Synaptic Structure and Function

Kaichuan Zhu, Finn Peters, Severin Filser and Jochen Herms

Biological Psychiatry, 2018, 84, 478
DOI: 10.1016/j.biopsych.2018.04.022

Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases

David Vanda, Paweł Zajdel and Miroslav Soural

European Journal of Medicinal Chemistry, 2019, 181, 111569
DOI: 10.1016/j.ejmech.2019.111569

BACE1 inhibitors: Current status and future directions in treating Alzheimer's disease

Nour M. Moussa‐Pacha, Shifaa M. Abdin, Hany A. Omar, Hasan Alniss and Taleb H. Al‐Tel

Medicinal Research Reviews, 2020, 40, 339
DOI: 10.1002/med.21622

Effects of Gentiana delavayi Flower Extract on APP Processing in APP/PS1 CHO Cells

Min Yang, Kai-yi Zhou, Feng-feng Li, Hui-yun Yang, Ming Yin, Li-hang Zhang and Fu-sheng Wang

Biological & Pharmaceutical Bulletin, 2020, 43, 767
DOI: 10.1248/bpb.b19-00720

Biochanin-A: A Potential Candidate for the Treatment of Alzheimer’s Disease

Niraj Kumar Singh and Bharat Bhushan

CPB, 2025, 26, 1607
DOI: 10.2174/0113892010362795250223160707

Thamnolia vermicularis extract improves learning ability in APP/PS1 transgenic mice by ameliorating both Aβ and Tau pathologies

Cong Li, Xiao-dan Guo, Min Lei, Jia-yi Wu, Jia-zhen Jin, Xiao-fan Shi, Zhi-yuan Zhu, Vatcharin Rukachaisirikul, Li-hong Hu, Tie-qiao Wen and Xu Shen

Acta Pharmacol Sin, 2017, 38, 9
DOI: 10.1038/aps.2016.94

Design and synthesis of bicyclic acetals as Beta Secretase (BACE1) inhibitors

Riccardo Innocenti, Elena Lenci, Gloria Menchi, Alberto Pupi and Andrea Trabocchi

Bioorganic & Medicinal Chemistry, 2017, 25, 5077
DOI: 10.1016/j.bmc.2017.03.030

Donepezil Derivatives Targeting Amyloid-β Cascade in Alzheimer's Disease

Eva Mezeiova, Katarina Chalupova, Eugenie Nepovimova, Lukas Gorecki, Lukas Prchal, David Malinak, Kamil Kuca, Ondrej Soukup and Jan Korabecny

CAR, 2019, 16, 772
DOI: 10.2174/1567205016666190228122956

Design and synthesis of 5-cyclopropyl substituted cyclic acylguanidine compounds as BACE1 inhibitors

Jia-Kuo Liu, Wei Gu, Xiao-Rui Cheng, Jun-Ping Cheng, Ai-Hua Nie and Wen-Xia Zhou

Chinese Chemical Letters, 2016, 27, 1626
DOI: 10.1016/j.cclet.2016.05.002

Multidisciplinary approaches for targeting the secretase protein family as a therapeutic route for Alzheimer's disease

Nalini Schaduangrat, Veda Prachayasittikul, Saowapak Choomwattana, Prapimpun Wongchitrat, Kamonrat Phopin, Wilasinee Suwanjang, Aijaz Ahmad Malik, Bruno Vincent and Chanin Nantasenamat

Medicinal Research Reviews, 2019, 39, 1730
DOI: 10.1002/med.21563

Big versus small: The impact of aggregate size in disease

Brianna Hnath, Jiaxing Chen, Joshua Reynolds, Esther Choi, Jian Wang, Dongyan Zhang, Congzhou M. Sha and Nikolay V. Dokholyan

Protein Science, 2023, 32
DOI: 10.1002/pro.4686

Small-molecule drugs development for Alzheimer's disease

Weiwei Yao, Huihui Yang and Jinfei Yang

Front. Aging Neurosci., 2022, 14
DOI: 10.3389/fnagi.2022.1019412

Multitargeted Molecular Docking and Dynamic Simulation Studies of Bioactive Compounds from Rosmarinus officinalis against Alzheimer’s Disease

Fatima Javed Mirza, Saadia Zahid, Sanila Amber, Sumera Sumera, Hira Jabeen, Noreen Asim and Syed Adnan Ali Shah

Molecules, 2022, 27, 7241
DOI: 10.3390/molecules27217241

Development and comprehensive comparison of two on-line capillary electrophoretic methods for β-secretase inhibitor screening

Roman Řemínek, Lucie Slezáčková, Jan Schejbal and Zdeněk Glatz

Journal of Chromatography A, 2017, 1518, 89
DOI: 10.1016/j.chroma.2017.08.065

Synergetic effect of β-asarone and cannabidiol against Aβ aggregation in vitro and in vivo

Fangyuan Duan, Ting Ju, Chen Song, Mengyao Liu, Yi Xiong, Xue Han and Weihong Lu

Computational and Structural Biotechnology Journal, 2023, 21, 3875
DOI: 10.1016/j.csbj.2023.07.028

Guanidine-based β amyloid precursor protein cleavage enzyme 1 (BACE-1) inhibitors for the Alzheimer's disease (AD): A review

Pinky Gehlot, Sunil Kumar, Vivek Kumar Vyas, Bhanwar Singh Choudhary, Manish Sharma and Ruchi Malik

Bioorganic & Medicinal Chemistry, 2022, 74, 117047
DOI: 10.1016/j.bmc.2022.117047

Meroterpenoids with BACE1-inhibitory activity from the fruiting bodies of Suillus bovinus and Boletinus cavipes

Takamasa Yamaguchi, Hiroaki Sasaki, Genki Yatsu, Kiyotaka Koyama and Kaoru Kinoshita

J Nat Med, 2025, 79, 233
DOI: 10.1007/s11418-024-01862-7

Benzimidazole-derived Compounds Designed for Different Targets of Alzheimer’s Disease

Hayrettin Ozan Gulcan, Açelya Mavideniz, Mustafa Fethi Sahin and Ilkay Erdogan Orhan

CMC, 2019, 26, 3260
DOI: 10.2174/0929867326666190124123208

A review on flavonoid-based scaffolds as multi-target-directed ligands (MTDLs) for Alzheimer's disease

Leili Jalili-Baleh, Elaheh Babaei, Shahin Abdpour, Syed Nasir Abbas Bukhari, Alireza Foroumadi, Ali Ramazani, Mohammad Sharifzadeh, Mohammad Abdollahi and Mehdi Khoobi

European Journal of Medicinal Chemistry, 2018, 152, 570
DOI: 10.1016/j.ejmech.2018.05.004

Alzheimer's Disease and β-secretase Inhibition: An Update with a Focus on Computer-aided Inhibitor Design

Samuel C. Ugbaja, Isiaka A. Lawal, Hezekiel M. Kumalo and Monsurat M. Lawal

CDT, 2022, 23, 266
DOI: 10.2174/1389450122666210809100050

Unveiling a novel transient druggable pocket in BACE-1 through molecular simulations: Conformational analysis and binding mode of multisite inhibitors

Ornella Di Pietro, Jordi Juárez-Jiménez, Diego Muñoz-Torrero, Charles A. Laughton, F. Javier Luque and Chandra Verma

PLoS ONE, 2017, 12, e0177683
DOI: 10.1371/journal.pone.0177683

Structure–activity relationship, in vitro and in vivo evaluation of novel dienyl sulphonyl fluorides as selective BuChE inhibitors for the treatment of Alzheimer's disease

Chengyao Wu, Guijuan Zhang, Zai-Wei Zhang, Xia Jiang, Ziwen Zhang, Huanhuan Li, Hua-Li Qin and Wenjian Tang

Journal of Enzyme Inhibition and Medicinal Chemistry, 2021, 36, 1860
DOI: 10.1080/14756366.2021.1959571

Do Fragments and Crystallization Additives Bind Similarly to Drug-like Ligands?

Malgorzata N. Drwal, Célien Jacquemard, Carlos Perez, Jérémy Desaphy and Esther Kellenberger

J. Chem. Inf. Model., 2017, 57, 1197
DOI: 10.1021/acs.jcim.6b00769

A molecular dynamics study of the BACE1 conformational change from Apo to closed form induced by hydroxyethylamine derived compounds

Carlos Gueto-Tettay, Joshua Zuchniarz, Yeyson Fortich-Seca, Luis Roberto Gueto-Tettay and Juan Carlos Drosos-Ramirez

Journal of Molecular Graphics and Modelling, 2016, 70, 181
DOI: 10.1016/j.jmgm.2016.10.006

β-secretase inhibitors for Alzheimer’s disease: identification using pharmacoinformatics

Md Ataul Islam and Tahir S. Pillay

Journal of Biomolecular Structure and Dynamics, 2019, 37, 503
DOI: 10.1080/07391102.2018.1430619

Deubiquitinating enzymes (DUBs): decipher underlying basis of neurodegenerative diseases

Baohua Liu, Jing Ruan, Meng Chen, Zhongding Li, Gloria Manjengwa, Dirk Schlüter, Weihong Song and Xu Wang

Mol Psychiatry, 2022, 27, 259
DOI: 10.1038/s41380-021-01233-8

Synthesis, molecular modeling and BACE-1 inhibitory study of tetrahydrobenzo[b] pyran derivatives

Vijaya Bhaskar, Reshma Chowdary, Sheshagiri R. Dixit and Shrinivas D. Joshi

Bioorganic Chemistry, 2019, 84, 202
DOI: 10.1016/j.bioorg.2018.11.023

Discovery of isoalloxazine derivatives as a new class of potential anti-Alzheimer agents and their synthesis

Ashish M. Kanhed, Anshuman Sinha, Jatin Machhi, Ashutosh Tripathi, Zalak S. Parikh, Prakash P. Pillai, Rajani Giridhar and Mange Ram Yadav

Bioorganic Chemistry, 2015, 61, 7
DOI: 10.1016/j.bioorg.2015.05.005

Application of molecular framework-based data-mining method in the search for beta-secretase 1 inhibitors through drug repurposing

George Nicolae Daniel Ion, Dragos Paul Mihai, Gina Lupascu and George Mihai Nitulescu

Journal of Biomolecular Structure and Dynamics, 2019, 37, 3674
DOI: 10.1080/07391102.2018.1526115

Close Correlation of Monoamine Oxidase Activity with Progress of Alzheimer’s Disease in Mice, Observed by in Vivo Two-Photon Imaging

Dokyoung Kim, Sung Hoon Baik, Seokjo Kang, Seo Won Cho, Juryang Bae, Moon-Yong Cha, Michael J. Sailor, Inhee Mook-Jung and Kyo Han Ahn

ACS Cent. Sci., 2016, 2, 967
DOI: 10.1021/acscentsci.6b00309

Synthesis of N′-(4-/3-/2-/Non-substituted benzylidene)-4-[(4-methylphenyl)sulfonyloxy] Benzohydrazides and Evaluation of Their Inhibitory Activities against Monoamine Oxidases and β-Secretase

Hasan Erdinç Sellitepe, Jong Min Oh, İnci Selin Doğan, Sercan Yildirim, Ahmet Buğra Aksel, Geum Seok Jeong, Ahmed Khames, Mohamed A. Abdelgawad, Nicola Gambacorta, Orazio Nicolotti, Bijo Mathew and Hoon Kim

Applied Sciences, 2021, 11, 5830
DOI: 10.3390/app11135830

BACE1 inhibitor drugs for the treatment of Alzheimer's disease: Lessons learned, challenges to overcome, and future prospects^†

Arun K. Ghosh

GHM, 2024, 6, 164
DOI: 10.35772/ghm.2024.01033

A Novel Pectin-Like Glycopeptide Isolated from the Fruit of Fructus Mori Impedes Aggregation and Production of Aβ42

Saijuan Li, Can Jin, Pengcheng Gao, Wanqi Zhou, Rongrong Xiao, Zhenqiang Zhang, Wenfeng Liao and Kan Ding

J. Agric. Food Chem., 2022, 70, 9908
DOI: 10.1021/acs.jafc.2c03823

Neuroprotective Effect of β-secretase Inhibitory Peptide from Pacific Hake (Merluccius productus) Fish Protein Hydrolysate

Jung Kwon Lee, Eunice C.Y. Li-Chan, Imelda W.Y. Cheung, You-Jin Jeon, Ju-Young Ko and Hee-Guk Byun

CAR, 2019, 16, 1028
DOI: 10.2174/1567205016666191113122046

Label-free Quantitative Proteomics of Mouse Cerebrospinal Fluid Detects β-Site APP Cleaving Enzyme (BACE1) Protease Substrates In Vivo

Bastian Dislich, Felix Wohlrab, Teresa Bachhuber, Stephan A. Müller, Peer-Hendrik Kuhn, Sebastian Hogl, Melanie Meyer-Luehmann and Stefan F. Lichtenthaler

Molecular & Cellular Proteomics, 2015, 14, 2550
DOI: 10.1074/mcp.M114.041533

Increased Plasma Beta-Secretase 1 May Predict Conversion to Alzheimer’s Disease Dementia in Individuals With Mild Cognitive Impairment

Yong Shen, Haibo Wang, Qiying Sun, Hailan Yao, Andrew P. Keegan, Mike Mullan, Jeffrey Wilson, Simone Lista, Thomas Leyhe, Christoph Laske, Dan Rujescu, Allan Levey, Anders Wallin, Kaj Blennow, Rena Li and Harald Hampel

Biological Psychiatry, 2018, 83, 447
DOI: 10.1016/j.biopsych.2017.02.007

CDT2‐controlled cell cycle reentry regulates the pathogenesis of Alzheimer's disease

Fang Huang, Minghui Wang, Rong Liu, Jian‐Zhi Wang, Eric Schadt, Vahram Haroutunian, Pavel Katsel, Bin Zhang and Xiaochuan Wang

Alzheimer's & Dementia, 2019, 15, 217
DOI: 10.1016/j.jalz.2018.08.013

Synthesis and neuroprotective activity of novel 1,2,4-triazine derivatives with ethyl acetate moiety against H 2 O2 and Aβ-induced neurotoxicity

Tuba Tuylu Kucukkilinc, Kamaledin Safari Yanghagh, Beyza Ayazgok, Mohammad Ali Roknipour, Farshad Homayouni Moghadam, Alireza Moradi, Saeed Emami, Mohsen Amini and Hamid Irannejad

Med Chem Res, 2017, 26, 3057
DOI: 10.1007/s00044-017-2003-x

Structure-Based Survey of the Binding Modes of BACE1 Inhibitors

Hangchen Hu, Zhaoqiang Chen, Xiang Xu and Yechun Xu

ACS Chem. Neurosci., 2019, 10, 880
DOI: 10.1021/acschemneuro.8b00420

Peptidomimetic Modulators of BACE1

John Paul Juliano, David H. Small and Marie-Isabel Aguilar

Aust. J. Chem., 2020, 73, 366
DOI: 10.1071/CH19594

Perspectives on Inhibiting β‐Amyloid Aggregation through Structure‐Based Drug Design

Pankaj Mishra, Senthil R. Ayyannan and Gautam Panda

ChemMedChem, 2015, 10, 1467
DOI: 10.1002/cmdc.201500215

Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective β-Secretase (BACE1) Inhibitors over BACE2

Kazuki Fujimoto, Shuhei Yoshida, Genta Tadano, Naoya Asada, Kouki Fuchino, Shinji Suzuki, Eriko Matsuoka, Takahiko Yamamoto, Shiho Yamamoto, Shigeru Ando, Naoki Kanegawa, Yutaka Tonomura, Hisanori Ito, Diederik Moechars, Frederik J. R. Rombouts, Harrie J. M. Gijsen and Ken-ichi Kusakabe

J. Med. Chem., 2021, 64, 3075
DOI: 10.1021/acs.jmedchem.0c01858

Toward a Rational Design to Regulate β-Amyloid Fibrillation for Alzheimer’s Disease Treatment

Xu Han and Gefei He

ACS Chem. Neurosci., 2018, 9, 198
DOI: 10.1021/acschemneuro.7b00477

Distinguishing the Effect on the Rate and Yield of Aβ42 Aggregation by Green Tea Polyphenol EGCG

Giovanna Park, Christine Xue, Hongsu Wang and Zhefeng Guo

ACS Omega, 2020, 5, 21497
DOI: 10.1021/acsomega.0c02063

Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry

Patrick Mäder and Lars Kattner

J. Med. Chem., 2020, 63, 14243
DOI: 10.1021/acs.jmedchem.0c00960

Nutraceuticals: An emerging therapeutic approach against the pathogenesis of Alzheimer’s disease

Pritam Sadhukhan, Sukanya Saha, Sayanta Dutta, Sushweta Mahalanobish and Parames C. Sil

Pharmacological Research, 2018, 129, 100
DOI: 10.1016/j.phrs.2017.11.028

Novel Multitarget-Directed Ligands Aiming at Symptoms and Causes of Alzheimer’s Disease

Anna Więckowska, Tomasz Wichur, Justyna Godyń, Adam Bucki, Monika Marcinkowska, Agata Siwek, Krzysztof Więckowski, Paula Zaręba, Damijan Knez, Monika Głuch-Lutwin, Grzegorz Kazek, Gniewomir Latacz, Kamil Mika, Marcin Kołaczkowski, Jan Korabecny, Ondrej Soukup, Marketa Benkova, Katarzyna Kieć-Kononowicz, Stanislav Gobec and Barbara Malawska

ACS Chem. Neurosci., 2018, 9, 1195
DOI: 10.1021/acschemneuro.8b00024

Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates

Mihirbaran Mandal, Yusheng Wu, Jeffrey Misiaszek, Guoqing Li, Alexei Buevich, John P. Caldwell, Xiaoxiang Liu, Robert D. Mazzola, Peter Orth, Corey Strickland, Johannes Voigt, Hongwu Wang, Zhaoning Zhu, Xia Chen, Michael Grzelak, Lynn A. Hyde, Reshma Kuvelkar, Prescott T. Leach, Giuseppe Terracina, Lili Zhang, Qi Zhang, Maria S. Michener, Brad Smith, Kathleen Cox, Diane Grotz, Leonard Favreau, Kaushik Mitra, Irina Kazakevich, Brian A. McKittrick, William Greenlee, Matthew E. Kennedy, Eric M. Parker, Jared N. Cumming and Andrew W. Stamford

J. Med. Chem., 2016, 59, 3231
DOI: 10.1021/acs.jmedchem.5b01995

Fas Apoptosis Inhibitory Molecule Blocks and Dissolves Pathological Amyloid-β Species

Hiroaki Kaku, Alexander V. Ludlow, Michael F. Gutknecht and Thomas L. Rothstein

Front. Mol. Neurosci., 2021, 14
DOI: 10.3389/fnmol.2021.750578

Evaluation of Selected Plant Phenolics via Beta-Secretase-1 Inhibition, Molecular Docking, and Gene Expression Related to Alzheimer’s Disease

Tugba Uçar Akyürek, Ilkay Erdogan Orhan, F. Sezer Şenol Deniz, Gokcen Eren, Busra Acar and Alaattin Sen

Pharmaceuticals, 2024, 17, 1441
DOI: 10.3390/ph17111441

Active Site Mapping of an Aspartic Protease by Multiple Fragment Crystal Structures: Versatile Warheads To Address a Catalytic Dyad

Nedyalka Radeva, Johannes Schiebel, Xiaojie Wang, Stefan G. Krimmer, Kan Fu, Martin Stieler, Frederik R. Ehrmann, Alexander Metz, Thomas Rickmeyer, Michael Betz, Johan Winquist, Ah Young Park, Franziska U. Huschmann, Manfred S. Weiss, Uwe Mueller, Andreas Heine and Gerhard Klebe

J. Med. Chem., 2016, 59, 9743
DOI: 10.1021/acs.jmedchem.6b01195

Optimization of Hydroxyethylamine Transition State Isosteres as Aspartic Protease Inhibitors by Exploiting Conformational Preferences

Ana B. Bueno, Javier Agejas, Howard Broughton, Robert Dally, Timothy B. Durham, Juan Félix Espinosa, Rosario González, Patric J. Hahn, Alicia Marcos, Ramón Rodríguez, Gema Sanz, José F. Soriano, David Timm, Paloma Vidal, Hsiu-Chiung Yang and James R. McCarthy

J. Med. Chem., 2017, 60, 9807
DOI: 10.1021/acs.jmedchem.7b01304

Myeloid ectopic viral integration site 2 accelerates the progression of Alzheimer's disease

Yuting Cui, Xiaomin Zhang, Jing Liu, Yuli Hou, Qiao Song, Min Cao, Jingjing Zhang, Xiaoling Wang, Congcong Liu, Peichang Wang and Yaqi Wang

Aging Cell, 2024, 23
DOI: 10.1111/acel.14260

Protease inhibitor from Streptomyces pulveraceus strain VITSSAB as a potential therapeutic agent against BACE1 in Alzheimer's disease: A molecular docking and dynamics simulations study

Shatakshi Mishra, B. Stany, Aparana Kumari and K.V. Bhaskara Rao

Biocatalysis and Agricultural Biotechnology, 2025, 65, 103559
DOI: 10.1016/j.bcab.2025.103559

Structure-based design, synthesis and biological evaluation of novel β-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand

Arun K. Ghosh, Margherita Brindisi, Yu-Chen Yen, Xiaoming Xu, Xiangping Huang, Thippeswamy Devasamudram, Geoffrey Bilcer, Hui Lei, Gerald Koelsch, Andrew D. Mesecar and Jordan Tang

Bioorganic & Medicinal Chemistry Letters, 2015, 25, 668
DOI: 10.1016/j.bmcl.2014.11.087

Icariside II Ameliorates Cognitive Impairments Induced by Chronic Cerebral Hypoperfusion by Inhibiting the Amyloidogenic Pathway: Involvement of BDNF/TrkB/CREB Signaling and Up-Regulation of PPARα and PPARγ in Rats

Caixia Yin, Yuanyuan Deng, Yuangui Liu, Jianmei Gao, Lingli Yan and Qihai Gong

Front. Pharmacol., 2018, 9
DOI: 10.3389/fphar.2018.01211

Long Non-coding RNA: Insight Into Mechanisms of Alzheimer's Disease

Zhen Lan, Yanting Chen, Jiali Jin, Yun Xu and Xiaolei Zhu

Front. Mol. Neurosci., 2022, 14
DOI: 10.3389/fnmol.2021.821002

BACE1 Function and Inhibition: Implications of Intervention in the Amyloid Pathway of Alzheimer’s Disease Pathology

Gerald Koelsch

Molecules, 2017, 22, 1723
DOI: 10.3390/molecules22101723

Alzheimer’s therapy targeting the β-secretase enzyme BACE1: Benefits and potential limitations from the perspective of animal model studies

Masuo Ohno

Brain Research Bulletin, 2016, 126, 183
DOI: 10.1016/j.brainresbull.2016.04.007

3,4-Dihydro-1,3,5-triazin-2(1H)-ones as the First Dual BACE-1/GSK-3β Fragment Hits against Alzheimer’s Disease

Federica Prati, Angela De Simone, Andrea Armirotti, Maria Summa, Daniela Pizzirani, Rita Scarpelli, Sine Mandrup Bertozzi, Daniel I. Perez, Vincenza Andrisano, Ana Perez-Castillo, Barbara Monti, Francesca Massenzio, Letizia Polito, Marco Racchi, Piera Sabatino, Giovanni Bottegoni, Ana Martinez, Andrea Cavalli and Maria L. Bolognesi

ACS Chem. Neurosci., 2015, 6, 1665
DOI: 10.1021/acschemneuro.5b00121

Highly Diastereoselective Metal-Free Catalytic Synthesis of Drug-Like Spiroimidazolidinone

A. M. Jassem, A. H. Raheemah, W. A. Radhi, A. M. Alid and H. A. Jaber

Russ J Org Chem, 2019, 55, 1598
DOI: 10.1134/S107042801910021X

Reducing Aβ load and tau phosphorylation: Emerging perspective for treating Alzheimer's disease

Jaspreet Kalra and Aamir Khan

European Journal of Pharmacology, 2015, 764, 571
DOI: 10.1016/j.ejphar.2015.07.043

A PM7 dynamic residue-ligand interactions energy landscape of the BACE1 inhibitory pathway by hydroxyethylamine compounds. Part I: The flap closure process

Carlos Gueto-Tettay, Alejandro Martinez-Consuegra, Joshua Zuchniarz, Luis Roberto Gueto-Tettay and Juan Carlos Drosos-Ramírez

Journal of Molecular Graphics and Modelling, 2017, 76, 274
DOI: 10.1016/j.jmgm.2017.07.010

Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362

Martin A. Lowe, Alvaro Cardenas, Jean-Pierre Valentin, Zhaoning Zhu, Jan Abendroth, Jose L. Castro, Reiner Class, Annie Delaunois, Renaud Fleurance, Helga Gerets, Vitalina Gryshkova, Lloyd King, Donald D. Lorimer, Malcolm MacCoss, Julian H. Rowley, Marie-Luce Rosseels, Leandro Royer, Richard D. Taylor, Melanie Wong, Oliver Zaccheo, Vishal P. Chavan, Gokul A. Ghule, Bapusaheb K. Tapkir, Jeremy N. Burrows, Maëlle Duffey, Matthias Rottmann, Sergio Wittlin, Iñigo Angulo-Barturen, María Belén Jiménez-Díaz, Josefine Striepen, Kate J. Fairhurst, Tomas Yeo, David A. Fidock, Alan F. Cowman, Paola Favuzza, Benigno Crespo-Fernandez, Francisco Javier Gamo, Daniel E. Goldberg, Dominique Soldati-Favre, Benoît Laleu and Teresa de Haro

J. Med. Chem., 2022, 65, 14121
DOI: 10.1021/acs.jmedchem.2c01336

Alzheimer Hastalığı ve Anti-Alzheimer Etkili Bileşiklerin Yapılarının Araştırılması

Özden TARI and Ramazan YAĞMURTAŞAN

HUJPHARM, 2023
DOI: 10.52794/hujpharm.1175099

Disease-modifying therapies for Alzheimer’s disease: Clinical trial progress and opportunity

Yujie Zhang, Jie Chen, Yanru Li, Bin Jiao and Shilin Luo

Ageing Research Reviews, 2025, 103, 102595
DOI: 10.1016/j.arr.2024.102595

Inhibiting and Remodeling Toxic Amyloid-Beta Oligomer Formation Using a Computationally Designed Drug Molecule That Targets Alzheimer’s Disease

Matthew A. Downey, Maxwell J. Giammona, Christian A. Lang, Steven K. Buratto, Ambuj Singh and Michael T. Bowers

J. Am. Soc. Mass Spectrom., 2019, 30, 85
DOI: 10.1007/s13361-018-1975-1

Challenges in the treatment of Alzheimer’s disease: recent progress and treatment strategies of pharmaceuticals targeting notable pathological factors

Yung-Chih Kuo and Rajendiran Rajesh

Expert Review of Neurotherapeutics, 2019, 19, 623
DOI: 10.1080/14737175.2019.1621750

Organic Carbamates in Drug Design and Medicinal Chemistry

Arun K. Ghosh and Margherita Brindisi

J. Med. Chem., 2015, 58, 2895
DOI: 10.1021/jm501371s

Resveratrol and neuroprotection: an insight into prospective therapeutic approaches against Alzheimer’s disease from bench to bedside

Fahadul Islam, Mohamed H. Nafady, Md. Rezaul Islam, Susmita Saha, Salma Rashid, Aklima Akter, Md. Harun- Or-Rashid, Muhammad Furqan Akhtar, Asma Perveen, Ghulam Md. Ashraf, Md. Habibur Rahman and Sherouk Hussein Sweilam

Mol Neurobiol, 2022, 59, 4384
DOI: 10.1007/s12035-022-02859-7

Recent therapeutic strategies targeting beta amyloid and tauopathies in Alzheimer's disease

Yamini Madav, Sarika Wairkar and Bala Prabhakar

Brain Research Bulletin, 2019, 146, 171
DOI: 10.1016/j.brainresbull.2019.01.004

Protective Roles of Monsonia angustifolia and Its Active Compounds in Experimental Models of Alzheimer’s Disease

Yoon Sun Chun, Joonki Kim, Sungkwon Chung, Eric Khorombi, Dashnie Naidoo, Rudzani Nthambeleni, Nial Harding, Vinesh Maharaj, Gerda Fouche and Hyun Ok Yang

J. Agric. Food Chem., 2017, 65, 3133
DOI: 10.1021/acs.jafc.6b04451

Lead discovery of a guanidinyl tryptophan derivative on amyloid cascade inhibition

Piyapan Suwanttananuruk, Jutamas Jiaranaikulwanitch, Pornthip Waiwut and Opa Vajragupta

Open Chemistry, 2020, 18, 546
DOI: 10.1515/chem-2020-0067

Synthesis and structure-activity relationship study of multi-target triazine derivatives as innovative candidates for treatment of Alzheimer's disease

Aida Iraji, Omidreza Firuzi, Mehdi Khoshneviszadeh, Hamid Nadri, Najmeh Edraki and Ramin Miri

Bioorganic Chemistry, 2018, 77, 223
DOI: 10.1016/j.bioorg.2018.01.017

Transcriptional Regulation of BACE1 by NFAT3 Leads to Enhanced Amyloidogenic Processing

Zhengrong Mei, Pengke Yan, Xiangping Tan, Shiming Zheng and Bing Situ

Neurochem Res, 2015, 40, 829
DOI: 10.1007/s11064-015-1533-1

Design, Synthesis and Enzymatic Inhibition of Novel Unusual Amino Acids as a Transition State Analogue of Amyloid Precursor Protein Peptide

Atefe Ghodrati, Loghman Firoozpour, Saeed Balalaie, Faezeh Sadat Hosseini, Sorour Ramezanpour, Najme Edraki, Naser Mohtavinejad and Massoud Amanlou

Int J Pept Res Ther, 2020, 26, 2169
DOI: 10.1007/s10989-020-10015-9

Management of Alzheimer’s disease—An insight of the enzymatic and other novel potential targets

Badar ul Islam and Shams Tabrez

International Journal of Biological Macromolecules, 2017, 97, 700
DOI: 10.1016/j.ijbiomac.2017.01.076

A graphene oxide-based fluorescent scheme for the determination of the activity of the β-site amyloid precursor protein (BACE1) and its inhibitors

Lin Liu, Ning Xia and Jie Yu

Microchim Acta, 2016, 183, 265
DOI: 10.1007/s00604-015-1647-9

A computational study of buckyballs as potential inhibitors of BACE1 in Alzheimer’s treatment

Thi-Thuy-Huong Le, Minh Quan Pham, Nguyen Minh Tam, Huong Thi Thu Phung and Son Tung Ngo

Chemical Physics Letters, 2024, 854, 141553
DOI: 10.1016/j.cplett.2024.141553

Aberrant proteolytic processing and therapeutic strategies in Alzheimer disease

Taisuke Tomita

Advances in Biological Regulation, 2017, 64, 33
DOI: 10.1016/j.jbior.2017.01.001

A molecular approach in drug development for Alzheimer’s disease

Snezana Agatonovic-Kustrin, Christine Kettle and David W. Morton

Biomedicine & Pharmacotherapy, 2018, 106, 553
DOI: 10.1016/j.biopha.2018.06.147

Hypothesis on ontogenesis and pathophysiology of Alzheimer’s disease

Eduarda Dal Pisol Schwab, Ruliam Queiroz, Anne Karine Bosetto Fiebrantz, Murilo Bastos, Juliana Sartori Bonini and Weber Cláudio Francisco Nunes da Silva

einstein (São Paulo), 2022, 20
DOI: 10.31744/einstein_journal/2022RW0170

α‐Mangostin decreases β‐amyloid peptides production via modulation of amyloidogenic pathway

Lan‐Xue Zhao, Yan Wang, Ting Liu, Yan‐Xia Wang, Hong‐Zhuan Chen, Jian‐Rong Xu and Yu Qiu

CNS Neurosci Ther, 2017, 23, 526
DOI: 10.1111/cns.12699

Structure–activity relationship study of hydroxyethylamine isostere and P1′ site structure of peptide mimetic BACE1 inhibitors

Kazuya Kobayashi, Takuya Otani, Saki Ijiri, Yuki Kawasaki, Hiroki Matsubara, Takahiro Miyagi, Taishi Kitajima, Risa Iseki, Katsuyasu Ishizawa, Naoka Shindo, Kouta Okawa, Kouta Ueda, Syun Ando, Momoka Kawakita, Yasunao Hattori and Kenichi Akaji

Bioorganic & Medicinal Chemistry, 2021, 50, 116459
DOI: 10.1016/j.bmc.2021.116459

Evaluation of Inhibitory Activities of Sophora flavescens and Angelica gigas Nakai Root Extracts against Monoamine Oxidases, Cholinesterases, and β-Secretase

Jong Eun Park, Seul-Ki Mun, Sung-Tae Yee and Hoon Kim

Processes, 2022, 10, 880
DOI: 10.3390/pr10050880

Explore peptides extracted from gliadin hydrolysates suppressing BACE1 activity and restraining Aβ protein deposition

Kuo-Chiang Hsu, Shang-Ming Huang, Jhih-Yi Shen, Long Yi Chan, Pei-Yu Lai and Chin-Yu Lin

International Journal of Biological Macromolecules, 2025, 307, 141932
DOI: 10.1016/j.ijbiomac.2025.141932

A signal-on electrochemical strategy for protease detection based on the formation of ATCUN-Cu(II)

Ning Xia, Peizhen Peng, Shasha Wang, Jiaying Du, Gaihong Zhu, Weimin Du and Lin Liu

Sensors and Actuators B: Chemical, 2016, 232, 557
DOI: 10.1016/j.snb.2016.03.144

Meroterpenoids with BACE1 Inhibitory Activity from the Fruiting Body of Boletinus asiaticus

Genki Yatsu, Yoshihiro Kino, Hiroaki Sasaki, Jun-ichi Satoh, Kaoru Kinoshita and Kiyotaka Koyama

J. Nat. Prod., 2019, 82, 1797
DOI: 10.1021/acs.jnatprod.8b01092

Dual functional liposomes carrying antioxidants against tau hyperphosphorylation and apoptosis of neurons

Yung-Chih Kuo, Yung-I Lou and Rajendiran Rajesh

Journal of Drug Targeting, 2020, 28, 949
DOI: 10.1080/1061186X.2020.1761819

Alzheimer’s Disease: A Suitable Case for Treatment with Precision Medicine?

Ernest K.J. Pauwels and Gerard J. Boer

Med Princ Pract, 2024, 33, 301
DOI: 10.1159/000538251

Alzheimer’s Disease Pharmacotherapy in Relation to Cholinergic System Involvement

Gabriela Dumitrita Stanciu, Andrei Luca, Razvan Nicolae Rusu, Veronica Bild, Sorin Ioan Beschea Chiriac, Carmen Solcan, Walther Bild and Daniela Carmen Ababei

Biomolecules, 2019, 10, 40
DOI: 10.3390/biom10010040

Discovery of Sulforaphane as a Potent BACE1 Inhibitor Based on Kinetics and Computational Studies

Kumju Youn, Jeong-Hyun Yoon, Nayoung Lee, Gyutae Lim, Jinhyuk Lee, Shengmin Sang, Chi-Tang Ho and Mira Jun

Nutrients, 2020, 12, 3026
DOI: 10.3390/nu12103026

1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads

Frederik J. R. Rombouts, Gary Tresadern, Oscar Delgado, Carolina Martínez-Lamenca, Michiel Van Gool, Aránzazu García-Molina, Sergio A. Alonso de Diego, Daniel Oehlrich, Hana Prokopcova, José Manuel Alonso, Nigel Austin, Herman Borghys, Sven Van Brandt, Michel Surkyn, Michel De Cleyn, Ann Vos, Richard Alexander, Gregor Macdonald, Dieder Moechars, Harrie Gijsen and Andrés A. Trabanco

J. Med. Chem., 2015, 58, 8216
DOI: 10.1021/acs.jmedchem.5b01101

Crosstalk between peripheral immunity and central nervous system in Alzheimer’s disease

Hanchen Yang, Qi Qin, Meng Wang, Yunsi Yin, Ruiyang Li and Yi Tang

Cellular Immunology, 2023, 391-392, 104743
DOI: 10.1016/j.cellimm.2023.104743

Recent Studies on Design and Development of Drugs Against Alzheimer’s Disease (AD) Based on Inhibition of BACE-1 and Other AD-causative Agents

Satya P. Gupta and Vaishali M. Patil

CTMC, 2020, 20, 1195
DOI: 10.2174/1568026620666200416091623

Swedish mutant APP-based BACE1 binding site peptide reduces APP β-cleavage and cerebral Aβ levels in Alzheimer’s mice

Song Li, Huayan Hou, Takashi Mori, Darrell Sawmiller, Adam Smith, Jun Tian, Yanjiang Wang, Brian Giunta, Paul R. Sanberg, Sheqing Zhang and Jun Tan

Sci Rep, 2015, 5
DOI: 10.1038/srep11322

Hypoxia-Induced Degenerative Protein Modifications Associated with Aging and Age-Associated Disorders

Sunil S Adav and Siu Kwan Sze

Aging and disease, 2020, 11, 341
DOI: 10.14336/AD.2019.0604

A capillary electrophoresis-mass spectrometry based method for the screening of β-secretase inhibitors as potential Alzheimer's disease therapeutics

Jan Schejbal, Lucie Slezáčková, Roman Řemínek and Zdeněk Glatz

Journal of Chromatography A, 2017, 1487, 235
DOI: 10.1016/j.chroma.2017.01.057

Protocol for fast screening of multi-target drug candidates: Application to Alzheimer’s disease

Nguyen Quoc Thai, Hoang Linh Nguyen, Huynh Quang Linh and Mai Suan Li

Journal of Molecular Graphics and Modelling, 2017, 77, 121
DOI: 10.1016/j.jmgm.2017.08.002

Computer-Aided Drug Design of β-Secretase, γ-Secretase and Anti-Tau Inhibitors for the Discovery of Novel Alzheimer’s Therapeutics

Varnavas D. Mouchlis, Georgia Melagraki, Lefteris C. Zacharia and Antreas Afantitis

IJMS, 2020, 21, 703
DOI: 10.3390/ijms21030703

Synthesis of the Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor NB-360

Heinrich Rueeger, Rainer Lueoend, Rainer Machauer, Siem J. Veenstra, Philipp Holzer, Konstanze Hurth, Markus Voegtle, Mathias Frederiksen, Jean-Michel Rondeau, Marina Tintelnot-Blomley, Laura H. Jacobson, Matthias Staufenbiel, Grit Laue and Ulf Neumann

J. Med. Chem., 2021, 64, 4677
DOI: 10.1021/acs.jmedchem.0c02143

Insights into the Pathophysiology of Alzheimer’s Disease and Potential Therapeutic Targets: A Current Perspective

Kesevan Rajah Kumaran, Suleiman Yunusa, Enoch Perimal, Habibah Wahab, Christian P. Müller, Zurina Hassan and Madeleine Hackney

JAD, 2023, 91, 507
DOI: 10.3233/JAD-220666

Drug Discovery to Drug Development of BACE1 Inhibitor as Antialzheimer’s: A Review

Sonali Mehendale Munj and Pooja Bhagwan Patil

CTMC, 2023, 23, 77
DOI: 10.2174/1568026623666221228140450

N-Cyclohexylimidazo[1,2-a]pyridine derivatives as multi-target-directed ligands for treatment of Alzheimer's disease

Zahra Haghighijoo, Sara Akrami, Mina Saeedi, Afsaneh Zonouzi, Aida Iraji, Bagher Larijani, Hossein Fakherzadeh, Farshad Sharifi, Seyed Masoud Arzaghi, Mohammad Mahdavi and Najmeh Edraki

Bioorganic Chemistry, 2020, 103, 104146
DOI: 10.1016/j.bioorg.2020.104146

Application of computational methods in the drug discovery and development of Alzheimer's disease

Qianqian Zhang, Xiaoqing Gong, Huanxiang Liu and Xiaojun Yao

Acta Pharmaceutica Sinica B, 2025
DOI: 10.1016/j.apsb.2025.07.038

Targeting protein aggregation for the treatment of degenerative diseases

Yvonne S. Eisele, Cecilia Monteiro, Colleen Fearns, Sandra E. Encalada, R. Luke Wiseman, Evan T. Powers and Jeffery W. Kelly

Nat Rev Drug Discov, 2015, 14, 759
DOI: 10.1038/nrd4593

Modulating Conformation of Aβ-Peptide: An Effective Way to Prevent Protein-Misfolding Disease

Xiang Ma, Jiai Hua, Kun Wang, Hongmei Zhang, Changli Zhang, Yafeng He, Zijian Guo and Xiaoyong Wang

Inorg. Chem., 2018, 57, 13533
DOI: 10.1021/acs.inorgchem.8b02115

A Close Look at BACE1 Inhibitors for Alzheimer’s Disease Treatment

Brati Das and Riqiang Yan

CNS Drugs, 2019, 33, 251
DOI: 10.1007/s40263-019-00613-7

Neuritogenic activity of bi-functional bis-tryptoline triazole

Jutamas Jiaranaikulwanitch, Sarin Tadtong, Piyarat Govitrapong, Valery V. Fokin and Opa Vajragupta

Bioorganic & Medicinal Chemistry, 2017, 25, 1195
DOI: 10.1016/j.bmc.2016.12.027

Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based β-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial

Yuji Koriyama, Akihiro Hori, Hisanori Ito, Shuji Yonezawa, Yoshiyasu Baba, Norihiko Tanimoto, Tatsuhiko Ueno, Shiho Yamamoto, Takahiko Yamamoto, Naoya Asada, Kenji Morimoto, Shunsuke Einaru, Katsunori Sakai, Takushi Kanazu, Akihiro Matsuda, Yoshitaka Yamaguchi, Takuya Oguma, Maarten Timmers, Luc Tritsmans, Ken-ichi Kusakabe, Akira Kato and Gaku Sakaguchi

J. Med. Chem., 2021, 64, 1873
DOI: 10.1021/acs.jmedchem.0c01917

BACE1 Inhibitory Meroterpenoids from Aspergillus terreus

Changxing Qi, Mengting Liu, Qun Zhou, Weixi Gao, Chunmei Chen, Yongji Lai, Zhengxi Hu, Yongbo Xue, Jinwen Zhang, Dongyan Li, Xiao-Nian Li, Qing Zhang, Jianping Wang, Hucheng Zhu and Yonghui Zhang

J. Nat. Prod., 2018, 81, 1937
DOI: 10.1021/acs.jnatprod.7b01050

Genetic architecture of hippocampus subfields volumes in Alzheimer’s disease

Jiahui Cai, Weixue Xiong, Xueqin Wang and Haizhu Tan

CNS Neurosci Ther, 2024, 30
DOI: 10.1111/cns.14110

Inhibition of the mitochondrial pyruvate carrier in astrocytes reduces amyloid and tau accumulation in the 3xTgAD mouse model of Alzheimer's disease

Kelly Ceyzériat, Aurélien M. Badina, Francesco Petrelli, Sylvie Montessuit, Alekos Nicolaides, Philippe Millet, Armand Savioz, Jean-Claude Martinou and Benjamin B. Tournier

Neurobiology of Disease, 2024, 200, 106623
DOI: 10.1016/j.nbd.2024.106623

Discovery of Extremely Selective Fused Pyridine-Derived β-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions

Tatsuhiko Ueno, Eriko Matsuoka, Naoya Asada, Shiho Yamamoto, Naoki Kanegawa, Mana Ito, Hisanori Ito, Diederik Moechars, Frederik J. R. Rombouts, Harrie J. M. Gijsen and Ken-ichi Kusakabe

J. Med. Chem., 2021, 64, 14165
DOI: 10.1021/acs.jmedchem.1c00359

Small Molecules N-Phenylbenzofuran-2-carboxamide and N-Phenylbenzo[b]thiophene-2-carboxamide Promote Beta-Amyloid (Aβ42) Aggregation and Mitigate Neurotoxicity

Yusheng Zhao and Praveen P. N. Rao

ACS Chem. Neurosci., 2023, 14, 4185
DOI: 10.1021/acschemneuro.3c00576

Synthesis, Molecular Docking, and Preliminary Evaluation of 2‐(1,2,3‐Triazoyl)benzaldehydes As Multifunctional Agents for the Treatment of Alzheimer's Disease

Gabriel P. Costa, Rodolfo S. M. Baldinotti, Mariana G. Fronza, José Edmilson R. Nascimento, Ítalo F. C. Dias, Mariana Souza Sonego, Fabiana Kömmling Seixas, Tiago Collares, Gelson Perin, Raquel G. Jacob, Lucielli Savegnago and Diego Alves

ChemMedChem, 2020, 15, 610
DOI: 10.1002/cmdc.201900622

FLZ attenuates learning and memory deficits via suppressing neuroinflammation induced by LPS in mice

Liang-Yu Wu, Xiu-Qi Bao, Hong-Yan Pang, Hua Sun and Dan Zhang

Journal of Asian Natural Products Research, 2015, 17, 306
DOI: 10.1080/10286020.2014.1003183

Physiological Functions of the β-Site Amyloid Precursor Protein Cleaving Enzyme 1 and 2

Riqiang Yan

Front. Mol. Neurosci., 2017, 10
DOI: 10.3389/fnmol.2017.00097

Multifunctional iminochromene-2H-carboxamide derivatives containing different aminomethylene triazole with BACE1 inhibitory, neuroprotective and metal chelating properties targeting Alzheimer's disease

Aida Iraji, Omidreza Firuzi, Mehdi Khoshneviszadeh, Marjan Tavakkoli, Mohammad Mahdavi, Hamid Nadri, Najmeh Edraki and Ramin Miri

European Journal of Medicinal Chemistry, 2017, 141, 690
DOI: 10.1016/j.ejmech.2017.09.057

Understanding the Binding Mechanism of Antagonist (AZD3293) Against BACE-1: Molecular Insights into Alzheimer’s Drug Discovery

Sphelele Sosibo, Daniel Gyamfi Amoako, Anou Moise Somboro, Darren Delai Sun, Jane Catherine Ngila and Hezekiel Kumalo

LDDD, 2020, 17, 850
DOI: 10.2174/1570180816666191029142640

Route Design in the 21st Century: The ICSYNTH Software Tool as an Idea Generator for Synthesis Prediction

Anders Bøgevig, Hans-Jürgen Federsel, Fernando Huerta, Michael G. Hutchings, Hans Kraut, Thomas Langer, Peter Löw, Christoph Oppawsky, Tobias Rein and Heinz Saller

Org. Process Res. Dev., 2015, 19, 357
DOI: 10.1021/op500373e

Amyloid β-Protein Assembly: The Effect of Molecular Tweezers CLR01 and CLR03

Xueyun Zheng, Deyu Liu, Frank-Gerrit Klärner, Thomas Schrader, Gal Bitan and Michael T. Bowers

J. Phys. Chem. B, 2015, 119, 4831
DOI: 10.1021/acs.jpcb.5b00692

Unlocking the potential: Woodfordia fruticosa Kurz in Alzheimer's disease management - A concise review

Sanjukta Sen, Shreyasi Meur, Gouranga Nandi and Dipanjan Karati

Brain Disorders, 2024, 16, 100171
DOI: 10.1016/j.dscb.2024.100171

Highlights in BACE1 Inhibitors for Alzheimer's Disease Treatment

Judite R. M. Coimbra, Daniela F. F. Marques, Salete J. Baptista, Cláudia M. F. Pereira, Paula I. Moreira, Teresa C. P. Dinis, Armanda E. Santos and Jorge A. R. Salvador

Front. Chem., 2018, 6
DOI: 10.3389/fchem.2018.00178

Computational analysis of BACE1-ligand complex crystal structures and linear discriminant analysis for identification of BACE1 inhibitors with anti P-glycoprotein binding property

Prabu Manoharan, Kiranmai Chennoju and Nanda Ghoshal

Journal of Biomolecular Structure and Dynamics, 2018, 36, 262
DOI: 10.1080/07391102.2016.1276477

Selected Class of Enamides Bearing Nitro Functionality as Dual-Acting with Highly Selective Monoamine Oxidase-B and BACE1 Inhibitors

Anusree Venkidath, Jong Min Oh, Sanal Dev, Elham Amin, Shebina P. Rasheed, Ajeesh Vengamthodi, Nicola Gambacorta, Ahmed Khames, Mohamed A. Abdelgawad, Ginson George, Orazio Nicolotti, Hoon Kim and Bijo Mathew

Molecules, 2021, 26, 6004
DOI: 10.3390/molecules26196004

Exploring new avenues for modifying course of progression of Alzheimer's disease: The rise of natural medicine

Sarah Lye, Caitlin E. Aust, Lyn R. Griffiths and Francesca Fernandez

Journal of the Neurological Sciences, 2021, 422, 117332
DOI: 10.1016/j.jns.2021.117332

BACE1 Inhibitors for Alzheimer’s Disease: Current Challenges and Future Perspectives

Judite R.M. Coimbra, Rosa Resende, José B.A. Custódio, Jorge A.R. Salvador, Armanda E. Santos, Paula I. Moreira, Jesus Avila, Daniela Galimberti, Miguel A. Pappolla, Germán Plascencia-Villa, Aaron A. Sorensen, Xiongwei Zhu and George Perry

JAD, 2024, 101, S53
DOI: 10.3233/JAD-240146

Natural products against Alzheimer's disease: Pharmaco-therapeutics and biotechnological interventions

Abhijit Dey, Raktim Bhattacharya, Anuradha Mukherjee and Devendra Kumar Pandey

Biotechnology Advances, 2017, 35, 178
DOI: 10.1016/j.biotechadv.2016.12.005

BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer’s Disease

Federica Prati, Giovanni Bottegoni, Maria Laura Bolognesi and Andrea Cavalli

J. Med. Chem., 2018, 61, 619
DOI: 10.1021/acs.jmedchem.7b00393

Donepezil structure-based hybrids as potential multifunctional anti-Alzheimer’s drug candidates

Luca Piemontese, Daniel Tomás, Asha Hiremathad, Vito Capriati, Emanuel Candeias, Sandra M. Cardoso, Sílvia Chaves and M. Amélia Santos

Journal of Enzyme Inhibition and Medicinal Chemistry, 2018, 33, 1212
DOI: 10.1080/14756366.2018.1491564