Results 41 to 50 of about 18,227 (256)

Xanomeline displays concomitant orthosteric and allosteric binding modes at the M4 mAChR

Nature Communications, 2023
The M4 muscarinic acetylcholine receptor (M4 mAChR) has emerged as a drug target of high therapeutic interest due to its expression in regions of the brain involved in the regulation of psychosis, cognition, and addiction.
Wessel A. C. Burger, Vi Pham, Ziva Vuckovic, Alexander S. Powers, Jesse I. Mobbs, Yianni Laloudakis, Alisa Glukhova, Denise Wootten, Andrew B. Tobin, Patrick M. Sexton, Steven M. Paul, Christian C. Felder, Radostin Danev, Ron O. Dror, Arthur Christopoulos, Celine Valant, David M. Thal   +16 more
doaj   +1 more source

The structural study of mutation-induced inactivation of human muscarinic receptor M4

IUCrJ, 2020
Human muscarinic receptor M4 belongs to the class A subfamily of the G-protein-coupled receptors (GPCRs). M4 has emerged as an attractive drug target for the treatment of Alzheimer's disease and schizophrenia.
Jingjing Wang, Meng Wu, Lijie Wu, Yueming Xu, Fei Li, Yiran Wu, Petr Popov, Lin Wang, Fang Bai, Suwen Zhao, Zhi-Jie Liu, Tian Hua   +11 more
doaj   +1 more source

Live-cell microscopy or fluorescence anisotropy with budded baculoviruses—which way to go with measuring ligand binding to M4 muscarinic receptors?

Open Biology, 2022
M4 muscarinic acetylcholine receptor is a G protein-coupled receptor (GPCR) that has been associated with alcohol and cocaine abuse, Alzheimer's disease, and schizophrenia which makes it an interesting drug target.
Maris-Johanna Tahk, Jane Torp, Mohammed A. S. Ali, Dmytro Fishman, Leopold Parts, Lukas Grätz, Christoph Müller, Max Keller, Santa Veiksina, Tõnis Laasfeld, Ago Rinken   +10 more
doaj   +1 more source

Pharmaceutical Assessment Suggests Locomotion Hyperactivity in Zebrafish Triggered by Arecoline Might Be Associated with Multiple Muscarinic Acetylcholine Receptors Activation

Toxins, 2021
Arecoline is one of the nicotinic acid-based alkaloids, which is found in the betel nut. In addition to its function as a muscarinic agonist, arecoline exhibits several adverse effects, such as inducing growth retardation and causing developmental ...
Petrus Siregar, Gilbert Audira, Ling-Yi Feng, Jia-Hau Lee, Fiorency Santoso, Wen-Hao Yu, Yu-Heng Lai, Jih-Heng Li, Ying-Ting Lin, Jung-Ren Chen, Chung-Der Hsiao   +10 more
doaj   +1 more source

Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy.

ACS Pharmacology & Translational Science, 2021
Nonselective antagonists of muscarinic acetylcholine receptors (mAChRs) that broadly inhibit all five mAChR subtypes provide an efficacious treatment for some movement disorders, including Parkinson's disease and dystonia. Despite their efficacy in these
M. Moehle, Aaron M. Bender, J. Dickerson, Daniel J. Foster, Aidong Qi, Hyekyung P. Cho, Yuping Donsante, Weimin Peng, Zoey Bryant, Kaylee J Stillwell, T. Bridges, Sichen Chang, Katherine J. Watson, Jordan C. O’Neill, Julie L. Engers, Li Peng, Alice L. Rodriguez, C. Niswender, C. Lindsley, E. Hess, P. Conn, J. M. Rook   +21 more
semanticscholar   +1 more source

Light-Activated Pharmacological Tools for Exploring the Cholinergic System. [PDF]

Med Res Rev
ABSTRACT Cholinergic transmission plays a critical role in both the central and peripheral nervous systems, affecting processes such as learning, memory, and inflammation. Conventional cholinergic drugs generally suffer from poor selectivity and temporal precision, leading to undesired effects and limited therapeutic efficacy. Photopharmacology aims to
Colleoni A, Galli G, Dallanoce C, De Amici M, Gorostiza P, Matera C.   +5 more
europepmc   +2 more sources

Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]

, 2018
The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J., Broad, Lisa M., Brooke, Simon M., Bundgaard, Christoffer, Christopoulos, Arthur, Crabtree, Michael D., Dwomoh, Louis, Felder, Christian C., Langmead, Christopher J., Mogg, Adrian J., Molloy, Colin, Sanger, Helen E., Sexton, Patrick M., Thompson, Karen J., Tobin, Andrew B.   +14 more
core   +1 more source

New strategic insights into managing fungal biofilms [PDF]

, 2015
Fungal infections have dramatically increased in the last decades in parallel with an increase of populations with impaired immunity, resulting from medical conditions such as cancer, transplantation or other chronic diseases.
Borghi, Elisa, Borgo, Francesca, Morace, Giulia, Nile, Christopher, Rajendran, Ranjith, Ramage, Gordon, Sherry, Leighann   +6 more
core   +3 more sources

Discovery of VU6028418: A Highly Selective and Orally Bioavailable M4 Muscarinic Acetylcholine Receptor Antagonist.

ACS Medicinal Chemistry Letters, 2021
Herein, we report the SAR leading to the discovery of VU6028418, a potent M4 mAChR antagonist with high subtype-selectivity and attractive DMPK properties in vitro and in vivo across multiple species. VU6028418 was subsequently evaluated as a preclinical
Matthew Spock, Trever R. Carter, Katrina A. Bollinger, Changho Han, Logan A Baker, Alice L. Rodriguez, Li Peng, J. Dickerson, Aidong Qi, J. M. Rook, Jordan C. O’Neill, Katherine J. Watson, Sichen Chang, T. Bridges, Julie L. Engers, D. Engers, C. Niswender, P. Conn, C. Lindsley, Aaron M. Bender   +19 more
semanticscholar   +1 more source

Non-Neuronal Functions of the M2 Muscarinic Acetylcholine Receptor [PDF]

, 2013
Acetylcholine is an important neurotransmitter whose effects are mediated by two classes of receptors. The nicotinic acetylcholine receptors are ion channels, whereas the muscarinic receptors belong to the large family of G protein coupled seven ...
Acevedo, Antje Banning, Boman, Bonner, Caulfield, Caumont, Cheng, Claing, Coso, Crespo, Dascher, Delaney, Elorza, Ferguson, Fisher, Franco, Frucht, Grando, Grando, Hawes, Hawes, He, Hein, Hulme, Jin, Jones, Jones, Lee, Lee, Leiros, Lenhard, McCole, Michal, Miyakawa, Nguyen, Pals-Rylaarsdam, Pals-Rylaarsdam, Pitcher, Prenzel, Reiner, Ritva Tikkanen, Roseberry, Rosenblum, Shah, Simone Bocksberger, Sina Kühne, Taylor, Tohgo, Tsuga, van Biesen, van Koppen, Vogler, Vogler, Wang, Wickman, Williams, Wu, Wymke Ockenga, Zhang   +58 more
core   +3 more sources