Mitochondria-targeted inhibitors of the human SIRT3 lysine deacetylase

Kathrin S. Troelsen, Michael Bæk, Alexander L. Nielsen, Andreas S. Madsen, Nima Rajabi and Christian A. Olsen

RSC Chem. Biol., 2021, 2, 627
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Pharmacological Advantage of SIRT2-Selective versus pan-SIRT1–3 Inhibitors

Jun Young Hong, Irma Fernandez, Ananya Anmangandla, Xuan Lu, Jessica Jingyi Bai and Hening Lin

ACS Chem. Biol., 2021, 16, 1266
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Substrates and Cyclic Peptide Inhibitors of the Oligonucleotide‐Activated Sirtuin 7**

Julie E. Bolding, Alexander L. Nielsen, Iben Jensen, Tobias N. Hansen, Line A. Ryberg, Samuel T. Jameson, Pernille Harris, Günther H. J. Peters, John M. Denu, Joseph M. Rogers and Christian A. Olsen

Angew Chem Int Ed, 2023, 62
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Efficient Crystallization of Apo Sirt2 for Small-Molecule Soaking and Structural Analysis of Ligand Interactions

Florian Friedrich, Matthias Schiedel, Sören Swyter, Lin Zhang, Wolfgang Sippl, Mike Schutkowski, Oliver Einsle and Manfred Jung

J. Med. Chem., 2025, 68, 10771
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Substrates and Cyclic Peptide Inhibitors of the Oligonucleotide‐Activated Sirtuin 7**

Julie E. Bolding, Alexander L. Nielsen, Iben Jensen, Tobias N. Hansen, Line A. Ryberg, Samuel T. Jameson, Pernille Harris, Günther H. J. Peters, John M. Denu, Joseph M. Rogers and Christian A. Olsen

Angewandte Chemie, 2023, 135
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Contemporary Applications of Thioamides and Methods for Their Synthesis

Tobias N. Hansen and Christian A. Olsen

Chemistry A European J, 2024, 30
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Recent Advances in the Discovery of SIRT1/2 Inhibitors via Computational Methods: A Perspective

Naomi Scarano, Chiara Brullo, Francesca Musumeci, Enrico Millo, Santina Bruzzone, Silvia Schenone and Elena Cichero

Pharmaceuticals, 2024, 17, 601
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SIRT2 Inhibition by AGK2 Promotes Perinuclear Cytoskeletal Organisation and Reduces Invasiveness of MDA-MB-231 Triple-Negative Breast Cancer Cells in Confined In Vitro Models

Emily Jessop, Natalie Young, Beatriz Garcia-Del-Valle, Jack T. Crusher, Boguslaw Obara and Iakowos Karakesisoglou

Cells, 2024, 13, 2023
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Investigation of Carboxylic Acid Isosteres and Prodrugs for Inhibition of the Human SIRT5 Lysine Deacylase Enzyme**

Nima Rajabi, Tobias N. Hansen, Alexander L. Nielsen, Huy T. Nguyen, Michael Bæk, Julie. E. Bolding, Oskar Ø. Bahlke, Sylvester E. G. Petersen, Christian R. O. Bartling, Kristian Strømgaard and Christian A. Olsen

Angewandte Chemie, 2022, 134
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Expanding the Accessible Chemical Space of SIRT2 Inhibitors through Exploration of Binding Pocket Dynamics

Nemanja Djokovic, Dusan Ruzic, Minna Rahnasto-Rilla, Tatjana Srdic-Rajic, Maija Lahtela-Kakkonen and Katarina Nikolic

J. Chem. Inf. Model., 2022, 62, 2571
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Synthesis of New N-[β-(Hetero)arylethyl]benzimidazole-2-carbothioamides and Their Analogues as Anti-Infective Agents and Compounds with Possible Neuro(psycho)tropic and Anticancer activity

L. N. Divaeva, A. A. Zubenko, A. S. Morkovnik, V. S. Sochnev, A. E. Svyatogorova and A. I. Klimenko

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Structural basis of SIRT7 nucleosome engagement and substrate specificity

Carlos Moreno-Yruela, Babatunde E. Ekundayo, Polina N. Foteva, Dongchun Ni, Esther Calvino-Sanles, Henning Stahlberg and Beat Fierz

Nat Commun, 2025, 16
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Structure, functions, and recent advances in the development of SIRT2 inhibitors

Junxin Xue, Xuben Hou and Hao Fang

Pharmaceutical Science Advances, 2023, 1, 100010
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Chiral Posttranslational Modification to Lysine ε-Amino Groups

Carlos Moreno-Yruela, Michael Bæk, Fabrizio Monda and Christian A. Olsen

Acc. Chem. Res., 2022, 55, 1456
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Sirtuins in Central Nervous System Tumors—Molecular Mechanisms and Therapeutic Targeting

Agnieszka Nowacka, Martyna Śniegocka, Maciej Śniegocki and Ewa Aleksandra Ziółkowska

Cells, 2025, 14, 1113
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Synthesis and modification of 7-aroyl derivatives of 4,7-dihydro-[1,2,4]triazolo-[1,5-a]-pyrimidine as potent inhibitors of sirtuin-2

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SIRT2 transgenic over‐expression does not impact lifespan in mice

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Selective SIRT2 inhibitors as promising anticancer therapeutics: An update from 2016 to 2020

Eslam Roshdy, Muhamad Mustafa, Abd El-Rahman Shaltout, Mohamed O. Radwan, Mahmoud A.A. Ibrahim, Mahmoud E. Soliman, Mikako Fujita, Masami Otsuka and Taha F.S. Ali

European Journal of Medicinal Chemistry, 2021, 224, 113709
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Mechanism-based inactivators of sirtuin 5: A focused structure–activity relationship study

Tobias N. Hansen, Xinyi Yuan, Marc S. I Santana and Christian A. Olsen

Bioorganic & Medicinal Chemistry Letters, 2025, 115, 130017
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Symmetrical 2,7‐disubstituted 9H‐fluoren‐9‐one as a novel and promising scaffold for selective targeting of SIRT2

Selen Gozde Kaya, Gokcen Eren, Alberto Massarotti, Habibe Beyza Gunindi, Filiz Bakar‐Ates and Erva Ozkan

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Comparison of Cellular Target Engagement Methods for the Tubulin Deacetylases Sirt2 and HDAC6: NanoBRET, CETSA, Tubulin Acetylation, and PROTACs

Anja Vogelmann, Manfred Jung, Finn K. Hansen and Matthias Schiedel

ACS Pharmacol. Transl. Sci., 2022, 5, 138
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Epigenetic meets metabolism: novel vulnerabilities to fight cancer

Domenica Scumaci and Qingfei Zheng

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Thioamides in medicinal chemistry and as small molecule therapeutic agents

Guang Huang, Tomasz Cierpicki and Jolanta Grembecka

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Sulfur(VI) Fluoride Exchange Chemistry in Solid-Phase Synthesis of Compound Arrays: Discovery of Histone Deacetylase Inhibitors

Tobias N. Hansen, Daniela Danková, Michael Bæk, Linda Grlaš and Christian A. Olsen

JACS Au, 2024, 4, 1854
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Structure–Activity Studies of 1,2,4-Oxadiazoles for the Inhibition of the NAD+-Dependent Lysine Deacylase Sirtuin 2

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A homogeneous time-resolved fluorescence screen to identify SIRT2 deacetylase and defatty-acylase inhibitors

Jie Yang, Joel Cassel, Brian C. Boyle, Daniel Oppong, Young-Hoon Ahn, Brian P. Weiser and Michael Massiah

PLoS ONE, 2024, 19, e0305000
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The (patho)physiological roles of the individual deacylase activities of a sirtuin

Weiping Zheng

Chem Biol Drug Des, 2024, 103
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Structural basis for sirtuin 2 activity and modulation: Current state and opportunities

Samuel P. Bernhard, Francesc X. Ruiz, Stacy Remiszewski, Matthew J. Todd, Thomas Shenk, John L. Kulp and Lillian W. Chiang

Journal of Biological Chemistry, 2025, 301, 110274
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Selective inhibition of SIRT2: A disputable therapeutic approach in cancer therapy

Selen Gozde Kaya and Gokcen Eren

Bioorganic Chemistry, 2024, 143, 107038
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Design, synthesis and biological evaluation of prostate-specific membrane antigen (PSMA)-targeted SIRT2 inhibitors

Junhui Yu, Zhicheng Gu, Chuang Zhang, Fei Jin, Qingqing Zhang, Shuxian Lin, Yan Li, Lei Chen and Bin He

Bioorganic Chemistry, 2024, 153, 107784
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Human Sirtuin 2 inhibitors, Their Mechanisms and Binding Modes

André Berndt Penteado, Haifa Hassanie, Renan Augusto Gomes, Flávio da Silva Emery and Gustavo Henrique Goulart Trossini

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Discovery of De Novo Macrocycle Inhibitors of Histone Deacetylase 11

Daniela Danková, Alexander L. Nielsen, Anne Zarda, Tobias N. Hansen, Marie Hesse, Michaela Benová, Athanasios Tsiris, Christian R. O. Bartling, Edward J. Will, Kristian Strømgaard, Carlos Moreno-Yruela, Christian Heinis and Christian A. Olsen

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Current Trends in Sirtuin Activator and Inhibitor Development

Karina L. Bursch, Christopher J. Goetz and Brian C. Smith

Molecules, 2024, 29, 1185
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Drug repurposing for ligand-induced rearrangement of Sirt2 active site-based inhibitors via molecular modeling and quantum mechanics calculations

Shiv Bharadwaj, Amit Dubey, Nitin Kumar Kamboj, Amaresh Kumar Sahoo, Sang Gu Kang and Umesh Yadava

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Investigation of Carboxylic Acid Isosteres and Prodrugs for Inhibition of the Human SIRT5 Lysine Deacylase Enzyme**

Nima Rajabi, Tobias N. Hansen, Alexander L. Nielsen, Huy T. Nguyen, Michael Bæk, Julie. E. Bolding, Oskar Ø. Bahlke, Sylvester E. G. Petersen, Christian R. O. Bartling, Kristian Strømgaard and Christian A. Olsen

Angew Chem Int Ed, 2022, 61
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Drugs Targeting Sirtuin 2 Exhibit Broad-Spectrum Anti-Infective Activity

Thomas Shenk, John L. Kulp III and Lillian W. Chiang

Pharmaceuticals, 2024, 17, 1298
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Hit evaluation results in 5-benzyl-1,3,4-thiadiazole-2-carboxamide based SIRT2-selective inhibitor with improved affinity and selectivity

Mahmut Gozelle, Selen Gozde Kaya, Ahmet Bugra Aksel, Erva Ozkan, Filiz Bakar-Ates, Yesim Ozkan and Gokcen Eren

Bioorganic Chemistry, 2022, 123, 105746
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SIRT2i_Predictor: A Machine Learning-Based Tool to Facilitate the Discovery of Novel SIRT2 Inhibitors

Nemanja Djokovic, Minna Rahnasto-Rilla, Nikolaos Lougiakis, Maija Lahtela-Kakkonen and Katarina Nikolic

Pharmaceuticals, 2023, 16, 127
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