Results 1 to 10 of about 24,506 (124)

Notch Signal Mediates the Cross-Interaction between M2 Muscarinic Acetylcholine Receptor and Neuregulin/ErbB Pathway: Effects on Schwann Cell Proliferation

Biomolecules, 2022
The cross-talk between axon and glial cells during development and in adulthood is mediated by several molecules. Among them are neurotransmitters and their receptors, which are involved in the control of myelinating and non-myelinating glial cell ...
R. Piovesana, A. Pisano, S. Loreti, R. Ricordy, C. Talora, A. Tata   +5 more
semanticscholar   +1 more source

Importance of receptor expression in the classification of novel ligands at the M2 muscarinic acetylcholine receptor

British Journal of Pharmacology, 2022
Affinity‐based, selective orthosteric ligands for the muscarinic acetylcholine receptors (mAChRs) are difficult to develop due to high sequence homology across the five subtypes.
Ye Jiang, M. Yeasmin, Arisbel B. Gondin, A. Christopoulos, C. Valant, Wessel A. C. Burger, D. Thal   +6 more
semanticscholar   +1 more source

Vibrational spectroscopy analysis of ligand efficacy in human M2 muscarinic acetylcholine receptor (M2R)

Communications Biology, 2021
The intrinsic efficacy of ligand binding to G protein-coupled receptors (GPCRs) reflects the ability of the ligand to differentially activate its receptor to cause a physiological effect. Here we use attenuated total reflection-Fourier transform infrared
K. Katayama, Kohei Suzuki, Ryoji Suno, Ryoji Kise, Hirokazu Tsujimoto, S. Iwata, A. Inoue, Takuya Kobayashi, H. Kandori   +8 more
semanticscholar   +1 more source

Agonist-Specific Conformations of the M2 Muscarinic Acetylcholine Receptor Assessed by Molecular Dynamics

Journal of Chemical Information and Modeling, 2020
Binding of muscarinic ligands, both antagonists and agonists, and their effects on the conformation of the M2 acetylcholine receptor were modeled in silico and compared to experimental data.
Alena Randáková, Dominik Nelic, V. Doležal, E. E. El-Fakahany, John Boulos, J. Jakubík   +5 more
semanticscholar   +1 more source

Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes

Science, 2019
Choosing a partner G protein–coupled receptors (GPCRs) bind ligands outside the cell and trigger events inside the cell by selectively binding and activating specific G proteins. The selectivity occurs even among highly related GPCRs.
S. Maeda, Q. Qu, M. J. Robertson, G. Skiniotis, B. Kobilka   +4 more
semanticscholar   +1 more source

Structural and dynamic insights into supra-physiological activation and allosteric modulation of a muscarinic acetylcholine receptor

Nature Communications, 2023
Here, using cryo-electron microscopy and solution NMR, the authors reveal the structural and dynamic mechanisms underlying the signaling versatility of a muscarinic receptor regulated by orthosteric and allosteric ligands. The M2 muscarinic receptor (M2R)
Jun Xu, Qinggong Wang, H. Hübner, Yunfei Hu, Xiaogang Niu, Haoqing Wang, S. Maeda, A. Inoue, Yuyong Tao, Peter Gmeiner, Yang Du, Chang-wen Jin, B. Kobilka   +12 more
semanticscholar   +1 more source

Evidence of common and specific genetic effects: association of the muscarinic acetylcholine receptor M2 (CHRM2) gene with alcohol dependence and major depressive syndrome.

Human Molecular Genetics, 2004
Several correlated phenotypes, alcohol dependence, major depressive syndrome, and an endophenotype of electrophysiological measurements, event-related oscillations (EROs), have demonstrated linkage on the long arm of chromosome 7.
Jen C. Wang, A. Hinrichs, Heather Stock, J. Budde, Rebecca Allen, S. Bertelsen, J. Kwon, William S. Wu, D. Dick, J. Rice, K. Jones, J. Nurnberger, J. Tischfield, B. Porjesz, H. Edenberg, V. Hesselbrock, R. Crowe, M. Schuckit, H. Begleiter, T. Reich, A. Goate, L. Bierut   +21 more
semanticscholar   +1 more source

Spontaneous Lipid Binding to the Nicotinic Acetylcholine Receptor in a Native Membrane [PDF]

, 2021
The nicotinic acetylcholine receptor (nAChR) and other pentameric ligand-gated ion channels (pLGICs) are native to neuronal membranes with an unusual lipid composition. While it is well-established that these receptors can be significantly modulated by lipids, the underlying mechanisms have been primarily studied in model membranes with only a few ...
arxiv   +1 more source

Kainate receptor modulation by NETO2 [PDF]

Nature, 599(7884), 325-329 (2021), 2023
Glutamate-gated kainate receptors (KARs) are ubiquitous in the central nervous system of vertebrates, mediate synaptic transmission on post-synapse, and modulate transmitter release on pre-synapse. In the brain, the trafficking, gating kinetics, and pharmacology of KARs are tightly regulated by Neuropilin and tolloid-like proteins (Netos).
arxiv   +1 more source

Memetic Algorithms for Ligand Expulsion from Protein Cavities [PDF]

J. Chem. Phys. 143 (12), 124101, 2015, 2015
Ligand diffusion through proteins is a fundamental process governing biological signaling and enzymatic catalysis. The complex topology of protein tunnels results in difficulties with computing ligand escape pathways by standard molecular dynamics (MD) simulations. Here, two novel methods for searching of ligand exit pathways and cavity exploration are
arxiv   +1 more source