Results 41 to 50 of about 2,925,762 (288)
Biomedicines, 2021 The dopamine transporter (DAT) serves a critical role in controlling dopamine (DA)-mediated neurotransmission by regulating the clearance of DA from the synapse and extrasynaptic regions and thereby modulating DA action at postsynaptic DA receptors ...
Shaili Aggarwal +4 more
doaj +1 more source
Mechanism Reveals a Novel Site for Allosteric Inhibition of Carcinogenic Activity of Human 3-Phosphoglycerate Dehydrogenase [PDF]
, 2023 3-Phosphoglycerate Dehydrogenase (PHGDH) is primarily known for catalyzing the oxidation of 3-phosphoglycerate (3PG) to 3-phosphohydroxypyvurate (3PHP) by reducing NAD+ to NADH, an important step during L-serine biosynthesis in human cells, however, it ...
Kshatresh, Dubey +2 more
core +2 more sources
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 +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 +2 more
doaj +1 more source
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 +5 more
doaj +1 more source
Catalytic Effects of Active Site Conformational Change in the Allosteric Activation of Imidazole Glycerol Phosphate Synthase [PDF]
, 2023 Imidazole glycerol phosphate synthase (IGPS) is a class-I glutamine amidotransferase (GAT) that hydrolyzes glutamine. Ammonia is produced and transferred to a second active site, where it reacts with N1-(5′-phosphoribosyl)-formimino-5-aminoimidazole-4 ...
Alegre-Requena, Juan V. +2 more
core +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
Allosteric modulation by the fatty acid site in the glycosylated SARS-CoV-2 spike
eLifeThe 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 +9 more
doaj +1 more source