Results 211 to 220 of about 81,932 (256)

The amino terminal domain of the human α7 nicotinic acetylcholine receptor subunit leads to the functional expression of human/insect receptors

British Journal of Pharmacology, EarlyView.
Human α7 receptors have been characterised in terms of pharmacological properties. Insertion of the N‐terminal domain of the human α7 subunit leads to honeybee and cockroach chimeric receptors activated by ACh and inhibited by α‐Bgt. Insertion of the human cys‐loop leads to cockroach chimeric receptors modulated by PNU.
Alison Cartereau, Chloé Veront, Alexandra Cremades, Priscilla Martin, Remi Gojard, Nicolas Galland, Emiliane Taillebois, Dieudonnée Togbé, Jean‐Yves Le Questel, Steeve H. Thany   +9 more
wiley   +1 more source

Flecainide binding dynamics in voltage‐gated sodium channels: A comparative isoform analysis of the state‐dependent block

British Journal of Pharmacology, EarlyView.
Background and Purpose Local anaesthetics and class I anti‐arrhythmic drugs block voltage‐gated Na+ channels, but the molecular basis for the isoform differences in drug sensitivity remains unclear. Understanding these mechanisms is essential for optimizing therapeutic efficacy and safety.
Tatsuo Munakata, Etsuko Kumada, Nao Katayama, Hiroki Nakagawa, Akihiko Sunami   +4 more
wiley   +1 more source

A common allosteric site and mechanism in caspases [PDF]

Proceedings of the National Academy of Sciences of the United States of America, 2006
We present a common allosteric mechanism for control of inflammatory and apoptotic caspases. Highly specific thiol-containing inhibitors of the human inflammatory caspase-1 were identified by using disulfide trapping, a method for site-directed small-molecule discovery.
Justin M Scheer, Michael J Romanowski, James A Wells   +2 more
exaly   +3 more sources

Druggable negative allosteric site of P2X3 receptors [PDF]

Proceedings of the National Academy of Sciences of the United States of America, 2018
SignificanceAllosteric regulation, produced by the binding of a ligand at an allosteric site topographically distinct from the orthosteric site, represents a direct and efficient means for modulation of biological macromolecule function. Because allosteric modulators have advantages over classic orthosteric ligands as therapeutic agents, understanding ...
Jin Wang, Yichen Huang, Peng Cao
exaly   +3 more sources

Some of the next articles are maybe not open access.

Related searches:

Crosslinking Allosteric Sites on the Nucleosome

Angewandte Chemie International Edition, 2019
AbstractTargeting defined histone protein sites in chromatin is an emerging therapeutic approach that can potentially be enhanced by allosteric effects within the nucleosome. Here we characterized a novel hetero‐bimetallic compound with a design based on a nucleosomal allostery effect observed earlier for two unrelated drugs—the RuII antimetastasis ...
Lucinda K. Batchelor, Louis De Falco, Thibaud von Erlach, Deepti Sharma, Zenita Adhireksan, Ursula Roethlisberger, Curt A. Davey, Paul J. Dyson   +7 more
openaire   +4 more sources

Multiple allosteric sites on muscarinic receptors

Life Sciences, 2001
Proteins and small molecules are capable of regulating the agonist binding and function of G-protein coupled receptors by multiple allosteric mechanisms. In the case of muscarinic receptors, there is the well-characterised allosteric site that binds, for example, gallamine and brucine. The protein kinase inhibitor, KT5720, has now been shown to bind to
N J, Birdsall, S, Lazareno, A, Popham, J, Saldanha   +3 more
openaire   +2 more sources

Searching for new allosteric sites in enzymes

Current Opinion in Structural Biology, 2004
The discovery of new allosteric sites generates opportunities for the identification of novel pharmaceuticals and increases our understanding of basic biological processes. Increasingly, allosteric sites are being discovered in various families of proteins by several methods, paving the way for the development of entirely new classes of drugs with a ...
Jeanne A, Hardy, James A, Wells
openaire   +2 more sources

Advances in NMR Methods to Identify Allosteric Sites and Allosteric Ligands

2019
NMR allows assessment of protein structure in solution. Unlike conventional X-ray crystallography that provides snapshots of protein conformations, all conformational states are simultaneously accessible to analysis by NMR. This is a significant advantage for discovery and characterization of allosteric effects.
Hazem, Abdelkarim, Ben, Hitchinson, Avik, Banerjee, Vadim, Gaponenko   +3 more
openaire   +2 more sources

Fishing for allosteric sites on GABAA receptors

Biochemical Pharmacology, 2004
GABA(A) receptors have structural and functional homology with a super-family of cys-loop ligand-gated ion channel receptors including the nicotinic acetylcholine receptors. Amino acid residues involved in ligand-binding pockets are homologous among super-family members, leading to the multiple-loop model of binding sites situated at subunit interfaces,
Richard W, Olsen, Chang-Sheng S, Chang, Guodong, Li, H Jacob, Hanchar, Martin, Wallner   +4 more
openaire   +2 more sources

Discovery of hidden allosteric sites as novel targets for allosteric drug design

Drug Discovery Today, 2018
Hidden allosteric sites, as a novel type of allosteric site, are invisible in ligand-unbound (apo) crystal structures, but can emerge in ligand-bound (holo) crystal structures when a specific ligand binds to, and stabilizes, a unique conformation favored by the ligand. However, the identification of these sites is a significant challenge.
Shaoyong, Lu, Mingfei, Ji, Duan, Ni, Jian, Zhang   +3 more
openaire   +2 more sources