Analysing the effect caused by increasing the molecular volume in M1-AChR receptor agonists and antagonists: a structural and computational study

Wilber Montejo-López, Raúl Sampieri-Cabrera, María Inés Nicolás-Vázquez, Juan Manuel Aceves-Hernández and Rodrigo Said Razo-Hernández

RSC Adv., 2024, 14, 8615
DOI: 10.1039/D3RA07380G

Targeting glutamate synapses in schizophrenia

Julie R. Field, Adam G. Walker and P. Jeffrey Conn

Trends in Molecular Medicine, 2011, 17, 689
DOI: 10.1016/j.molmed.2011.08.004

A golden age of muscarinic acetylcholine receptor modulation in neurological diseases

Andrew B. Tobin

Nat Rev Drug Discov, 2024, 23, 743
DOI: 10.1038/s41573-024-01007-1

M1 muscarinic acetylcholine receptor in Alzheimer’s disease

Shangtong Jiang, Yanfang Li, Cuilin Zhang, Yingjun Zhao, Guojun Bu, Huaxi Xu and Yun-Wu Zhang

Neurosci. Bull., 2014, 30, 295
DOI: 10.1007/s12264-013-1406-z

The nociceptin orphanin FQ peptide receptor agonist, Ro64-6198, impairs recognition memory formation through interaction with glutamatergic but not cholinergic receptor antagonists

David Reiss, Eric P. Prinssen, Jürgen Wichmann, Brigitte L. Kieffer and Abdel-Mouttalib Ouagazzal

Neurobiology of Learning and Memory, 2012, 98, 254
DOI: 10.1016/j.nlm.2012.09.002

G Protein–Coupled Receptors in Asthma Therapy: Pharmacology and Drug Action

Stacy Gelhaus Wendell, Hao Fan and Cheng Zhang

Pharmacological Reviews, 2020, 72, 1
DOI: 10.1124/pr.118.016899

Parkinson's Disease Therapeutics: New Developments and Challenges Since the Introduction of Levodopa

Yoland Smith, Thomas Wichmann, Stewart A Factor and Mahlon R DeLong

Neuropsychopharmacol, 2012, 37, 213
DOI: 10.1038/npp.2011.212

Development of M1mAChR Allosteric and Bitopic Ligands: Prospective Therapeutics for the Treatment of Cognitive Deficits

Briana J. Davie, Arthur Christopoulos and Peter J. Scammells

ACS Chem. Neurosci., 2013, 4, 1026
DOI: 10.1021/cn400086m

Positive allosteric modulation of M 1 and M 4 muscarinic receptors as potential therapeutic treatments for schizophrenia

Samantha E. Yohn and P. Jeffrey Conn

Neuropharmacology, 2018, 136, 438
DOI: 10.1016/j.neuropharm.2017.09.012

An allosteric modulator binds to a conformational hub in the β2 adrenergic receptor

Xiangyu Liu, Jonas Kaindl, Magdalena Korczynska, Anne Stößel, Daniela Dengler, Markus Stanek, Harald Hübner, Mary J. Clark, Jake Mahoney, Rachel Ann Matt, Xinyu Xu, Kunio Hirata, Brian K. Shoichet, Roger K. Sunahara, Brian K. Kobilka and Peter Gmeiner

Nat Chem Biol, 2020, 16, 749
DOI: 10.1038/s41589-020-0549-2

Developing Chemical Genetic Approaches to Explore G Protein-Coupled Receptor Function: Validation of the Use of a Receptor Activated Solely by Synthetic Ligand (RASSL)

Elisa Alvarez-Curto, Rudi Prihandoko, Christofer S. Tautermann, Jurriaan M. Zwier, John D. Pediani, Martin J. Lohse, Carsten Hoffmann, Andrew B. Tobin and Graeme Milligan

Molecular Pharmacology, 2011, 80, 1033
DOI: 10.1124/mol.111.074674

Molekulare Allianz – von orthosterischen und allosterischen Liganden zu dualsterischen/bitopischen Agonisten G‐Protein‐gekoppelter Rezeptoren

Klaus Mohr, Jens Schmitz, Ramona Schrage, Christian Tränkle and Ulrike Holzgrabe

Angewandte Chemie, 2013, 125, 530
DOI: 10.1002/ange.201205315

Muscarinic Acetylcholine Receptors in the Retina—Therapeutic Implications

Yue Ruan, Andreas Patzak, Norbert Pfeiffer and Adrian Gericke

IJMS, 2021, 22, 4989
DOI: 10.3390/ijms22094989

Minireview: Novel Aspects of M3 Muscarinic Receptor Signaling in Pancreatic β-Cells

Kenichiro Nakajima, Shalini Jain, Inigo Ruiz de Azua, Sara M. McMillin, Mario Rossi and Jürgen Wess

Molecular Endocrinology, 2013, 27, 1208
DOI: 10.1210/me.2013-1084

Exploration of the Orthosteric/Allosteric Interface in Human M1 Muscarinic Receptors by Bitopic Fluorescent Ligands

Sandrine B. Daval, Esther Kellenberger, Dominique Bonnet, Valérie Utard, Jean-Luc Galzi and Brigitte Ilien

Molecular Pharmacology, 2013, 84, 71
DOI: 10.1124/mol.113.085670

Design, Synthesis, and Pharmacological Evaluation of Second-Generation Tetrahydroisoquinoline-Based CXCR4 Antagonists with Favorable ADME Properties

Huy H. Nguyen, Michelle B. Kim, Robert J. Wilson, Christopher J. Butch, Katie M. Kuo, Eric J. Miller, Yesim A. Tahirovic, Edgars Jecs, Valarie M. Truax, Tao Wang, Chi S. Sum, Mary E. Cvijic, Gretchen M. Schroeder, Lawrence J. Wilson and Dennis C. Liotta

J. Med. Chem., 2018, 61, 7168
DOI: 10.1021/acs.jmedchem.8b00450

LY2033298, a positive allosteric modulator at muscarinic M4 receptors, enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms

Robert L. Gannon and Mark J. Millan

Psychopharmacology, 2012, 224, 231
DOI: 10.1007/s00213-012-2743-8

Determination of Region-Specific Roles of the M3 Muscarinic Acetylcholine Receptor in Gastrointestinal Motility

Yoko Igarashi-Hisayoshi, Eikichi Ihara, Xiaopeng Bai, Chika Higashi, Hiroko Ikeda, Yoshimasa Tanaka, Mayumi Hirano, Haruei Ogino, Takatoshi Chinen, Yasushi Taguchi and Yoshihiro Ogawa

Dig Dis Sci, 2023, 68, 439
DOI: 10.1007/s10620-022-07637-y

Modulation of direct pathway striatal projection neurons by muscarinic M4-type receptors

Teresa Hernández-Flores, Omar Hernández-González, María B. Pérez-Ramírez, Esther Lara-González, Mario A. Arias-García, Mariana Duhne, Azucena Pérez-Burgos, G. Aleph Prieto, Alejandra Figueroa, Elvira Galarraga and José Bargas

Neuropharmacology, 2015, 89, 232
DOI: 10.1016/j.neuropharm.2014.09.028

Cholinergic modulation of striatal microcircuits

Nilupaer Abudukeyoumu, Teresa Hernandez‐Flores, Marianela Garcia‐Munoz and Gordon W. Arbuthnott

Eur J of Neuroscience, 2019, 49, 604
DOI: 10.1111/ejn.13949

Crystal structures of the M1 and M4 muscarinic acetylcholine receptors

David M. Thal, Bingfa Sun, Dan Feng, Vindhya Nawaratne, Katie Leach, Christian C. Felder, Mark G. Bures, David A. Evans, William I. Weis, Priti Bachhawat, Tong Sun Kobilka, Patrick M. Sexton, Brian K. Kobilka and Arthur Christopoulos

Nature, 2016, 531, 335
DOI: 10.1038/nature17188

Hippocampal place cell remapping occurs with memory storage of aversive experiences

Garrett J Blair, Changliang Guo, Shiyun Wang, Michael S Fanselow, Peyman Golshani, Daniel Aharoni and Hugh T Blair

eLife, 2023, 12
DOI: 10.7554/eLife.80661

Sphingosine-1-Phosphate and Its Receptors: Structure, Signaling, and Influence

Hugh Rosen, Raymond C. Stevens, Michael Hanson, Edward Roberts and Michael B.A. Oldstone

Annu. Rev. Biochem., 2013, 82, 637
DOI: 10.1146/annurev-biochem-062411-130916

Use of Allosteric Targets in the Discovery of Safer Drugs

Ashok Kumar Grover

Med Princ Pract, 2013, 22, 418
DOI: 10.1159/000350417

Muscarinic acetylcholine receptor modulators derived from natural toxins and diverse interaction modes

JianRong Xu, Hao Wang and HongZhuan Chen

Sci. China Chem., 2013, 56, 1333
DOI: 10.1007/s11426-013-4958-x

Allosteric Modulators of Potential Targets Related to Alzheimer's Disease: a Review

Guilherme Martins Silva, Mariana Pegrucci Barcelos, João Gabriel Curtolo Poiani, Lorane Izabel da Silva Hage‐Melim and Carlos Henrique Tomich de Paula da Silva

ChemMedChem, 2019, 14, 1467
DOI: 10.1002/cmdc.201900299

Novel Insights into M3 Muscarinic Acetylcholine Receptor Physiology and Structure

Andrew C. Kruse, Jianhua Li, Jianxin Hu, Brian K. Kobilka and Jürgen Wess

J Mol Neurosci, 2014, 53, 316
DOI: 10.1007/s12031-013-0127-0

Crystal structure of the human angiotensin II type 2 receptor bound to an angiotensin II analog

Hidetsugu Asada, Shoichiro Horita, Kunio Hirata, Mitsunori Shiroishi, Yuki Shiimura, Hiroko Iwanari, Takao Hamakubo, Tatsuro Shimamura, Norimichi Nomura, Osamu Kusano-Arai, Tomoko Uemura, Chiyo Suno, Takuya Kobayashi and So Iwata

Nat Struct Mol Biol, 2018, 25, 570
DOI: 10.1038/s41594-018-0079-8

Muscarinic agonist, (±)-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate: High affinity, but low subtype selectivity for human M1 – M5 muscarinic acetylcholine receptors

Na-Ra Lee, Satheesh Gujarathi, Shobanbabu Bommagani, Kiranbabu Siripurapu, Guangrong Zheng and Linda P. Dwoskin

Bioorganic & Medicinal Chemistry Letters, 2019, 29, 471
DOI: 10.1016/j.bmcl.2018.12.022

Activation and allosteric modulation of a muscarinic acetylcholine receptor

Andrew C. Kruse, Aaron M. Ring, Aashish Manglik, Jianxin Hu, Kelly Hu, Katrin Eitel, Harald Hübner, Els Pardon, Celine Valant, Patrick M. Sexton, Arthur Christopoulos, Christian C. Felder, Peter Gmeiner, Jan Steyaert, William I. Weis, K. Christopher Garcia, Jürgen Wess and Brian K. Kobilka

Nature, 2013, 504, 101
DOI: 10.1038/nature12735

Drugs Interfering with Muscarinic Acetylcholine Receptors and Their Effects on Place Navigation

Jan Svoboda, Anna Popelikova and Ales Stuchlik

Front. Psychiatry, 2017, 8
DOI: 10.3389/fpsyt.2017.00215

An Antibody Biosensor Establishes the Activation of the M1 Muscarinic Acetylcholine Receptor during Learning and Memory

Adrian J. Butcher, Sophie J. Bradley, Rudi Prihandoko, Simon M. Brooke, Adrian Mogg, Julie-Myrtille Bourgognon, Timothy Macedo-Hatch, Jennifer M. Edwards, Andrew R. Bottrill, R.A.John Challiss, Lisa M. Broad, Christian C. Felder and Andrew B. Tobin

Journal of Biological Chemistry, 2016, 291, 8862
DOI: 10.1074/jbc.M115.681726

Les récepteurs couplés aux protéines G

Jean-Luc Galzi and Brigitte Ilien

Med Sci (Paris), 2012, 28, 852
DOI: 10.1051/medsci/20122810013

Chemical Modification of the M1Agonist VU0364572 Reveals Molecular Switches in Pharmacology and a Bitopic Binding Mode

Gregory J. Digby, Thomas J. Utley, Atin Lamsal, Christian Sevel, Douglas J. Sheffler, Evan P. Lebois, Thomas M. Bridges, Michael R. Wood, Colleen M. Niswender, Craig W. Lindsley and P. Jeffrey Conn

ACS Chem. Neurosci., 2012, 3, 1025
DOI: 10.1021/cn300103e

Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs

Scott A. Hollingsworth, Brendan Kelly, Celine Valant, Jordan Arthur Michaelis, Olivia Mastromihalis, Geoff Thompson, A. J. Venkatakrishnan, Samuel Hertig, Peter J. Scammells, Patrick M. Sexton, Christian C. Felder, Arthur Christopoulos and Ron O. Dror

Nat Commun, 2019, 10
DOI: 10.1038/s41467-019-11062-7

Pathophysiology and pharmacology of G protein-coupled receptors in the heart

Alyssa Grogan, Emilio Y Lucero, Haoran Jiang and Howard A Rockman

Cardiovascular Research, 2023, 119, 1117
DOI: 10.1093/cvr/cvac171

Simultaneous activation of muscarinic and GABAB receptors as a bidirectional target for novel antipsychotics

Paulina Cieślik, Monika Woźniak, Krzysztof Tokarski, Magdalena Kusek, Andrzej Pilc, Agata Płoska, Adrianna Radulska, Iwona Pelikant-Małecka, Beata Żołnowska, Jarosław Sławiński, Leszek Kalinowski and Joanna M Wierońska

Behavioural Brain Research, 2019, 359, 671
DOI: 10.1016/j.bbr.2018.09.019

Molecular Alliance—From Orthosteric and Allosteric Ligands to Dualsteric/Bitopic Agonists at G Protein Coupled Receptors

Klaus Mohr, Jens Schmitz, Ramona Schrage, Christian Tränkle and Ulrike Holzgrabe

Angew Chem Int Ed, 2013, 52, 508
DOI: 10.1002/anie.201205315

Cholinergic interneurons in the dorsal and ventral striatum: anatomical and functional considerations in normal and diseased conditions

Kalynda K. Gonzales and Yoland Smith

Annals of the New York Academy of Sciences, 2015, 1349, 1
DOI: 10.1111/nyas.12762

Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration

Joseph D. Panarese, Hykeyung P. Cho, Jeffrey J. Adams, Kellie D. Nance, Pedro M. Garcia-Barrantes, Sichen Chang, Ryan D. Morrison, Anna L. Blobaum, Colleen M. Niswender, Shaun R. Stauffer, P. Jeffrey Conn and Craig W. Lindsley

Bioorganic & Medicinal Chemistry Letters, 2016, 26, 3822
DOI: 10.1016/j.bmcl.2016.04.083

Targeting Selective Activation of M1 for the Treatment of Alzheimer’s Disease: Further Chemical Optimization and Pharmacological Characterization of the M1 Positive Allosteric Modulator ML169

James C. Tarr, Mark L. Turlington, Paul R. Reid, Thomas J. Utley, Douglas J. Sheffler, Hyekyung P. Cho, Rebecca Klar, Tristano Pancani, Michael T. Klein, Thomas M. Bridges, Ryan D. Morrison, Anna L. Blobaum, Zixui Xiang, J. Scott Daniels, Colleen M. Niswender, P. Jeffrey Conn, Michael R. Wood and Craig W. Lindsley

ACS Chem. Neurosci., 2012, 3, 884
DOI: 10.1021/cn300068s

Structural determinants for the interactions between muscarinic toxin 7 and muscarinic acetylcholine receptors

Jianrong Xu, Hengyi Zhao, Zhaoxi Zheng, Yu Wang, Yinyao Niu, Hao Wang, Jun Xu, Yang Lu and Hongzhuan Chen

J of Molecular Recognition, 2015, 28, 239
DOI: 10.1002/jmr.2438

Diagnostic significance of measuring antibodies to cyclic type 3 muscarinic acetylcholine receptor peptides in primary Sjogren's syndrome

J. He, J.-p. Guo, Y. Ding, Y.-n. Li, S.-s. Pan, Y. Liu and Z.-g. Li

Rheumatology, 2011, 50, 879
DOI: 10.1093/rheumatology/keq420

Fluorescent Derivatives of AC-42 To Probe Bitopic Orthosteric/Allosteric Binding Mechanisms on Muscarinic M1 Receptors

Sandrine B. Daval, Céline Valant, Dominique Bonnet, Esther Kellenberger, Marcel Hibert, Jean-Luc Galzi and Brigitte Ilien

J. Med. Chem., 2012, 55, 2125
DOI: 10.1021/jm201348t

Employing novel animal models in the design of clinically efficacious GPCR ligands

Sophie J Bradley, Sajjad A Riaz and Andrew B Tobin

Current Opinion in Cell Biology, 2014, 27, 117
DOI: 10.1016/j.ceb.2013.12.002

Muscarinic acetylcholine receptor X-ray structures: potential implications for drug development

Andrew C Kruse, Jianxin Hu, Brian K Kobilka and Jürgen Wess

Current Opinion in Pharmacology, 2014, 16, 24
DOI: 10.1016/j.coph.2014.02.006

The role of the second and third extracellular loops of the adenosine A1 receptor in activation and allosteric modulation

M.C. Peeters, L.E. Wisse, A. Dinaj, B. Vroling, G. Vriend and A.P. IJzerman

Biochemical Pharmacology, 2012, 84, 76
DOI: 10.1016/j.bcp.2012.03.008

Alzheimer's Therapeutics: Translation of Preclinical Science to Clinical Drug Development

Alena V Savonenko, Tatiana Melnikova, Andrew Hiatt, Tong Li, Paul F Worley, Juan C Troncoso, Phil C Wong and Don L Price

Neuropsychopharmacol, 2012, 37, 261
DOI: 10.1038/npp.2011.211

Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease

Bruce J. Melancon, James C. Tarr, Joseph D. Panarese, Michael R. Wood and Craig W. Lindsley

Drug Discovery Today, 2013, 18, 1185
DOI: 10.1016/j.drudis.2013.09.005

Muscarinic and nicotinic acetylcholine receptor agonists: current scenario in Alzheimer's disease therapy

Stuti Verma, Ashwini Kumar, Timir Tripathi and Awanish Kumar

Journal of Pharmacy and Pharmacology, 2018, 70, 985
DOI: 10.1111/jphp.12919