Results 41 to 50 of about 22,949 (304)

In Silico Prediction and Validation of CB2 Allosteric Binding Sites to Aid the Design of Allosteric Modulators

Molecules, 2022
Although the 3D structures of active and inactive cannabinoid receptors type 2 (CB2) are available, neither the X-ray crystal nor the cryo-EM structure of CB2-orthosteric ligand-modulator has been resolved, prohibiting the drug discovery and development ...
Jiayi Yuan, Chen Jiang, Junmei Wang, Chih-Jung Chen, Yixuan Hao, Guangyi Zhao, Zhiwei Feng, Xiang-Qun Xie   +7 more
doaj   +1 more source

Effect of γ value on binding of allosteric modulator to two allosteric sites.

, 2019
Simulation of tracer binding (ordinate) in the presence an allosteric modulator binding to two allosteric sites for various combinations of positive and negative cooperativity with the tracer indicated at headings of individual plots.
Esam E. El-Fakahany (339452), Alena Randáková (339451), Jan Jakubík (339449), Vladimír Doležal (339453)   +3 more
core   +1 more source

Modulation of the Erwinia ligand-gated ion channel (ELIC) and the 5-HT3 receptor via a common vestibule site

eLife, 2020
Pentameric ligand-gated ion channels (pLGICs) or Cys-loop receptors are involved in fast synaptic signaling in the nervous system. Allosteric modulators bind to sites that are remote from the neurotransmitter binding site, but modify coupling of ligand ...
Marijke Brams, Cedric Govaerts, Kumiko Kambara, Kerry L Price, Radovan Spurny, Anant Gharpure, Els Pardon, Genevieve L Evans, Daniel Bertrand, Sarah CR Lummis, Ryan E Hibbs, Jan Steyaert, Chris Ulens   +12 more
doaj   +1 more source

Effect of δ value on binding of allosteric modulator to two allosteric sites.

, 2019
Simulation of tracer binding (ordinate) in the presence an allosteric modulator binding to two allosteric sites for various combinations of positive and negative cooperativity with the tracer indicated at headings of individual plots.
Esam E. El-Fakahany (339452), Alena Randáková (339451), Jan Jakubík (339449), Vladimír Doležal (339453)   +3 more
core   +1 more source

Concentration dependence of binding of allosteric modulator to two allosteric sites.

, 2019
Simulation of tracer binding (ordinate) in the presence an allosteric modulator binding to two allosteric sites for various combinations of positive and negative cooperativity with the tracer indicated at headings of individual plots.
Esam E. El-Fakahany (339452), Alena Randáková (339451), Jan Jakubík (339449), Vladimír Doležal (339453)   +3 more
core   +1 more source

The antipsychotic potential of muscarinic allosteric modulation [PDF]

Drug News & Perspectives, 2010
The cholinergic hypothesis of schizophrenia emerged over 50 years ago based on clinical observations with both anticholinergics and pan-muscarinic agonists. Not until the 1990s did the cholinergic hypothesis of schizophrenia receive renewed enthusiasm based on clinical data with xanomeline, a muscarinic acetylcholine receptor M(1)/M(4)-preferring ...
Thomas M, Bridges, Evan P, LeBois, Corey R, Hopkins, Michael R, Wood, Carrie K, Jones, P Jeffrey, Conn, Craig W, Lindsley   +6 more
openaire   +2 more sources

Valosin‐containing protein counteracts ATP‐driven dissolution of FUS condensates through its ATPase activity in vitro

FEBS Letters, EarlyView.
Biomolecular condensates formed by fused in sarcoma (FUS) are dissolved by high ATP concentrations yet persist in cells. Using a reconstituted system, we demonstrate that valosin‐containing protein (VCP), an AAA+ ATPase, counteracts ATP‐driven dissolution of FUS condensates through its D2 ATPase activity.
Hitomi Kimura, Shin‐ichi Tate, Kyota Yasuda   +2 more
wiley   +1 more source

Dataset for Phase I randomized clinical trial for safety and tolerability of GET 73 in single and repeated ascending doses including preliminary pharmacokinetic parameters

Data in Brief, 2017
The data in this article outline the methods used for the administration of GET 73 in the first time-in-human manuscript entitled “Phase I randomized clinical trial for the safety, tolerability and preliminary pharmacokinetics of the mGluR5 negative ...
Carolina L. Haass-Koffler, Kimberly Goodyear, Victoria M. Long, Harrison H. Tran, Antonella Loche, Roberto Cacciaglia, Robert M. Swift, Lorenzo Leggio   +7 more
doaj   +1 more source

Generation of nanobodies acting as silent and positive allosteric modulators of the α7 nicotinic acetylcholine receptor

, 2023
International audienceThe α7 nicotinic acetylcholine receptor (nAChR), a potential drug target for treating cognitive disorders, mediates communication between neuronal and non- neuronal cells. Although many competitive antagonists, agonists, and partial-
Stéphanie Pons, Prevost, Marie, S, de la Bâtie, Gabrielle, Dejean, Nathalie Barilone, Aymé, Gabriel, Baachaoui, Rayen, Corringer, Pierre-Jean, Ákos Nemecz, Marie S. Prevost, Pons, Stéphanie, Rayen Baachaoui, Barilone, Nathalie, Gabriel Aymé, Uwe Maskos, Pierre Lafaye, Lafaye, Pierre, Qimeng Li, Nemecz, Ákos, Li, Qimeng, Gabrielle Dejean de la Bâtie, Maskos, Uwe, Pierre-Jean Corringer   +21 more
core   +1 more source

Biased Signaling and Allosteric Modulation at the FSHR [PDF]

Frontiers in Endocrinology, 2019
Knowledge on G protein-coupled receptor (GPCRs) structure and mechanism of activation has profoundly evolved over the past years. The way drugs targeting this family of receptors are discovered and used has also changed. Ligands appear to bind a growing number of GPCRs in a competitive or allosteric manner to elicit balanced signaling or biased ...
Landomiel, Flavie, de Pascali, Francesco, Raynaud, Pauline, Jean-Alphonse, Frédéric, Yvinec, Romain, Pellissier, Lucie P., Bozon, Véronique, Bruneau, Gilles, Crépieux, Pascale, Poupon, Anne, Reiter, Eric   +10 more
openaire   +5 more sources