Results 31 to 40 of about 18,462 (237)

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

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

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

Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype

Journal of Pharmacological Sciences, 2004
Heterologous down-regulation of histamine H1 receptor (H1R) mediated by muscarinic acetylcholine receptor subtype was investigated using five kinds of Chinese hamster ovary (CHO) cells stably co-expressing the human H1R and one of the five (M1 –M5 ...
Katsuhiro Miyoshi, Nozomi Kawakami, Yousuke Wakayama, Norimasa Izumi, Shuhei Horio, Hiroyuki Fukui   +5 more
doaj   +1 more source

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   +4 more sources

Virtual Affinity Fingerprints for Target Fishing: A New Application of Drug Profile Matching [PDF]

, 2013
We recently introduced Drug Profile Matching (DPM), a novel virtual affinity fingerprinting bioactivity prediction method. DPM is based on the docking profiles of ca.
Czobor, P., Hári, P., Jelinek, B., Málnási Csizmadia, András, Peragovics, Á., Simon, Z., Tombor, L.   +6 more
core   +1 more source

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

Identification and Role of Muscarinic Receptor Subtypes Expressed in Rat Adrenal Medullary Cells

Journal of Pharmacological Sciences, 2011
.: The muscarinic receptor is known to be involved in the acetylcholine (ACh)-induced secretion of catecholamines in the adrenal medullary (AM) cells of various mammals.
Keita Harada, Hidetada Matsuoka, Takeyoshi Sata, Akira Warashina, Masumi Inoue   +4 more
doaj   +1 more source