Results 241 to 250 of about 2,925,762 (288)

Developing the Dopamine D3 Receptor (D3R) Antagonist, (R)‐VK4‐116, as a Non‐Opioid Medication for the Treatment of Opioid Use Disorder

Medicinal Research Reviews, EarlyView.
ABSTRACT Opioid use disorder (OUD) remains a major global health challenge, and currently approved treatments (methadone, buprenorphine, and naltrexone) are all opioid receptor‐targeting drugs with limitations in access, adherence, stigma, and use in polysubstance use disorders. Because the dopamine D3 receptor (D3R) is enriched in limbic brain regions
Chia‐Kuei Wu, Yu‐Chih Lin, Junfeng Huang, Bangwei Ding, Pramod Terse, Rahul Nandre, Haksong Jin, Molly Congdon, Kun Shen, Philip Sanderson, Gregory Tawa, Stephanie Mounaud, Marta De Santis, Donald Lo, Elizabeth A. Ottinger, Amy Hauck Newman   +15 more
wiley   +1 more source

Molecular Glue Degraders in Early Development for Cancer Therapy

Medicinal Research Reviews, EarlyView.
ABSTRACT Molecular glue degraders are an emerging class of small molecule allosteric modulators that induce or stabilize protein‐protein interactions, enabling targeted degradation of previously intractable proteins. By redirecting E3 ligases to recognize neosubstrates, proteins that are not typically recognized by a specific E3 ubiquitin ligase, they ...
E. Sila Ozdemir, Hyunbum Jang, Ozlem Keskin, Attila Gursoy, Ruth Nussinov   +4 more
wiley   +1 more source

Druggable negative allosteric site of P2X3 receptors [PDF]

Proceedings of the National Academy of Sciences of the United States of America, 2018
Significance Allosteric 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 ...
Jin Wang, Ye Yu, Motoyuki Hattori
exaly   +4 more sources

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.
James A. Wells, Michael J Romanowski
exaly   +3 more sources

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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   +6 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

Correlation Between Allosteric and Orthosteric Sites

2019
Correlation between an allosteric site and its orthosteric site refers to the phenomenon that perturbations like ligand binding, mutation, or posttranslational modifications at the allosteric site leverage variation in the orthosteric site. Understanding this kind of correlation not only helps to disclose how information is transmitted in allosteric ...
Weilin, Zhang, Juan, Xie, Luhua, Lai
openaire   +2 more sources