Results 51 to 60 of about 4,452,404 (339)

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

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

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   +3 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

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, Nikolay V Dokholyan   +1 more
doaj   +1 more source

Dissecting a novel allosteric mechanism of cruzain: A computer-aided approach.

PLoS ONE, 2019
Trypanosoma cruzi is the causative agent of Chagas disease, a neglected infection affecting millions of people in tropical regions. There are several chemotherapeutic agents for the treatment of this disease, but most of them are highly toxic and ...
Lilian Hernández Alvarez, Diego Enry Barreto Gomes, Jorge Enrique Hernández González, Pedro Geraldo Pascutti   +3 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

The role of the allosteric B site in the fumarase reaction [PDF]

Proceedings of the National Academy of Sciences, 2004
The role of a malate binding site in a concavity external to the more deeply situated active site has been a major mystery of the fumarase reaction. The malate, within 12 Å of the active site, was bound by hydrogen bonds to two main-chain amides and to two basic residues, H129 and R126. Mutation of the His of this so-called B site of
Irwin A, Rose, Todd M, Weaver
openaire   +2 more sources