Results 31 to 40 of about 131,252 (300)

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

The chemical diversity and structure-based discovery of allosteric modulators for the PIF-pocket of protein kinase PDK1

Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Phosphoinositide-dependent protein kinase-1 (PDK1) is an important protein in mediating the PI3K-AKT pathway and is thus identified as a promising target.
Xinyuan Xu, Yingyi Chen, Qiang Fu, Duan Ni, Jian Zhang, Xiaolong Li, Shaoyong Lu   +6 more
doaj   +1 more source

Mechanism of Allosteric Modulation of the Cys-loop Receptors

Pharmaceuticals, 2010
The cys-loop receptor family is a major family of neurotransmitter-operated ion channels. They play important roles in fast synaptic transmission, controlling neuronal excitability, and brain function.
Paul Whiteaker, Yao Huang, Yongchang Chang   +2 more
doaj   +1 more source

Allosteric Modulators of Steroid Hormone Receptors : Structural Dynamics and Gene Regulation [PDF]

, 2012
Peer ...
McEwan, Iain J, Kumar, Raj
core   +1 more source

Allosteric Modulation of Muscarinic Acetylcholine Receptors

Pharmaceuticals, 2010
An allosteric modulator is a ligand that binds to an allosteric site on the receptor and changes receptor conformation to produce increase (positive cooperativity) or decrease (negative cooperativity) in the binding or action of an orthosteric agonist (e.
Esam E. El-Fakahany, Jan Jakubík
doaj   +1 more source

Allosteric modulation of the activity of thrombin [PDF]

Biochemical Journal, 1997
Substrates containing a P3 aspartic residue are in general cleaved poorly by thrombin. This may be partly due to an unfavourable interaction between the P3 aspartate and Glu192 in the active site of thrombin. In Protein C activation and perhaps also thrombin receptor cleavage, binding of ligands at the anion-binding exosite of thrombin seems to improve
DUFFY, Edward J., ANGLIKER, Herbert, BONNIEC, Bernard F. Le, STONE, Stuart R.   +3 more
openaire   +3 more sources

Targeted NMDA Receptor Interventions for Autism: Developmentally Determined Expression of GluN2B and GluN2A-Containing Receptors and Balanced Allosteric Modulatory Approaches

Biomolecules, 2022
Various ASD risk alleles have been associated with impairment of NMDA receptor activation (i.e., NMDA Receptor Hypofunction) and/or disturbance of the careful balance between activation mediated by GluN2B-subtype and GluN2A-subtype-containing NMDA ...
Stephen I. Deutsch, Zachary N. M. Luyo, Jessica A. Burket   +2 more
doaj   +1 more source

Identification of Allosteric Modulators: Targeting ?1 Adrenoceptors [PDF]

, 2018
Despite the potential advantages of allosteric GPCR modulators, only a few compounds have been reported to modulate the ?1-adrenergic receptor (?1-AR) subtypes allosterically.
Urmi, Kaniz Fatima
core   +1 more source

Further synthesis and biological characterization of a series of 2-sulfonamidebenzamides as allosteric modulators of MrgX1 [PDF]

, 2021
The present study describes our continued efforts in the discovery and characterization of a series of 2-sulfonamidebenzamides as allosteric modulators of MrgX1.
Qi, Peng, Christopher, Aretz, Swagat, Sharma, Anish, Vadukoot, Corey, Hopkins, Alexander, Wallick, Aaron, Jensen, Xinzhong, Dong   +7 more
core   +2 more sources

Discovery of Small-Molecule Modulators of the Human Y4 Receptor. [PDF]

PLoS ONE, 2016
The human neuropeptide Y4 receptor (Y4R) and its native ligand, pancreatic polypeptide, are critically involved in the regulation of human metabolism by signaling satiety and regulating food intake, as well as increasing energy expenditure.
Gregory Sliwoski, Mario Schubert, Jan Stichel, David Weaver, Annette G Beck-Sickinger, Jens Meiler   +5 more
doaj   +1 more source