Results 31 to 40 of about 81,932 (256)

Development of allosteric modulators of GPCRs for treatment of CNS disorders

Neurobiology of Disease, 2014
The discovery of allosteric modulators of G protein-coupled receptors (GPCRs) provides a promising new strategy with potential for developing novel treatments for a variety of central nervous system (CNS) disorders.
Hilary Highfield Nickols, P. Jeffrey Conn   +1 more
doaj   +1 more source

Potentiation and allosteric agonist activation of α7 nicotinic acetylcholine receptors: binding sites and hypotheses

Pharmacological Research, 2023
Considerable progress has been made in recent years towards the identification and characterisation of novel subtype-selective modulators of nicotinic acetylcholine receptors (nAChRs).
Victoria R. Sanders, Neil S. Millar
doaj   +1 more source

Structure and allosteric regulation of human NAD-dependent isocitrate dehydrogenase

Cell Discovery, 2020
Human NAD-dependent isocitrate dehydrogenase or HsIDH3 catalyzes the decarboxylation of isocitrate into α-ketoglutarate in the TCA cycle. HsIDH3 exists and functions as a heterooctamer composed of the αβ and αγ heterodimers, and is regulated ...
Pengkai Sun, Yan Liu, Tengfei Ma, Jianping Ding   +3 more
doaj   +1 more source

Unravelling the allosteric binding mode of αD-VxXXB at nicotinic acetylcholine receptors

Frontiers in Pharmacology, 2023
αD-conotoxins are 11 kDa homodimers that potently inhibit nicotinic acetylcholine receptors (nAChRs) through a non-competitive (allosteric) mechanism. In this study, we describe the allosteric binding mode of the granulin-like C-terminal (CTD) of VxXXB ...
Thao NT Ho, Nikita Abraham, Richard J. Lewis   +2 more
doaj   +1 more source

Switching Aurora‐A kinase on and off at an allosteric site [PDF]

The FEBS Journal, 2017
Protein kinases are central players in the regulation of cell cycle and signalling pathways. Their catalytic activities are strictly regulated through post‐translational modifications and protein–protein interactions that control switching between inactive and active states.
Bayliss, R, Burgess, SG, McIntyre, PJ
openaire   +4 more sources

Study of Functional and Allosteric Sites in Protein Superfamilies [PDF]

Acta Naturae, 2015
The interaction of proteins (enzymes) with a variety of low-molecular-weight compounds, as well as protein-protein interactions, is the most important factor in the regulation of their functional properties. To date, research effort has routinely focused on studying ligand binding to the functional sites of proteins (active sites of enzymes), whereas ...
SUPLATOV D., ŠVEDAS V.
openaire   +4 more sources

Conformational fingerprinting of allosteric modulators in metabotropic glutamate receptor 2

eLife, 2022
Activation of G protein-coupled receptors (GPCRs) is an allosteric process. It involves conformational coupling between the orthosteric ligand binding site and the G protein binding site. Factors that bind at non-cognate ligand binding sites to alter the
Brandon Wey-Hung Liauw, Arash Foroutan, Michael R Schamber, Weifeng Lu, Hamid Samareh Afsari, Reza Vafabakhsh   +5 more
doaj   +1 more source

Identification of the Allosteric Regulatory Site of Insulysin

PLoS ONE, 2011
Insulin degrading enzyme (IDE) is responsible for the metabolism of insulin and plays a role in clearance of the Aβ peptide associated with Alzheimer's disease. Unlike most proteolytic enzymes, IDE, which consists of four structurally related domains and exists primarily as a dimer, exhibits allosteric kinetics, being activated by both small substrate ...
Nicholas Noinaj, Sonia K Bhasin, Eun Suk Song, Kirsten E Scoggin, Maria A Juliano, Luiz Juliano, Louis B Hersh, David W Rodgers   +7 more
openaire   +3 more sources

Allosteric modulation of dextromethorphan binding sites

Neuropharmacology, 1987
The nonopioid antitussives dextromethorphan (DM), carbetapentane and caramiphen are efficacious anticonvulsant agents in the rat MES test. The findings presented strongly suggest the existence of a novel allosteric mechanism by which drugs acting at two different but interacting sites, exert their effects.
J M, Musacchio, M, Klein, L J, Santiago
openaire   +2 more sources

Allosteric modulation by the fatty acid site in the glycosylated SARS-CoV-2 spike

eLife
The spike protein is essential to the SARS-CoV-2 virus life cycle, facilitating virus entry and mediating viral-host membrane fusion. The spike contains a fatty acid (FA) binding site between every two neighbouring receptor-binding domains.
A Sofia F Oliveira, Fiona L Kearns, Mia A Rosenfeld, Lorenzo Casalino, Lorenzo Tulli, Imre Berger, Christiane Schaffitzel, Andrew D Davidson, Rommie E Amaro, Adrian J Mulholland   +9 more
doaj   +1 more source