Results 31 to 40 of about 79,838 (161)
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 +1 more
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The Allosteric Binding Sites of Sulfotransferase 1A1 [PDF]
Drug Metabolism and Disposition, 2015 Human sulfotransferases (SULTs) comprise a small, 13-member enzyme family that regulates the activities of thousands of compounds-endogenous metabolites, drugs, and other xenobiotics. SULTs transfer the sulfuryl-moiety (-SO3) from a nucleotide donor, PAPS (3'-phosphoadenosine 5'-phosphosulfate), to the hydroxyls and primary amines of acceptors. SULT1A1,
Ian, Cook +3 more
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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
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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
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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
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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
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PLOS Computational Biology, 2018 The omnipresence of allosteric regulation together with the fundamental role of structural dynamics in this phenomenon have initiated a great interest to the detection of regulatory exosites and design of corresponding effectors. However, despite a general consensus on the key role of dynamics most of the earlier efforts on the prediction of allosteric
Wei-Ven Tee +2 more
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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
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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
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Allosteric regulation of kinase activity in living cells
eLife, 2023 The dysregulation of protein kinases is associated with multiple diseases due to the kinases' involvement in a variety of cell signaling pathways. Manipulating protein kinase function, by controlling the active site, is a promising therapeutic and ...
Shivani Sujay Godbole +1 more
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