학술논문
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders.
Document Type
Journal Article
Source
Subject
*DRUG development
*DRUG analysis
*CENTRAL nervous system stimulants
*CELL receptors
*ALLOSTERIC regulation
*G proteins
*LIGANDS (Biochemistry)
*ANIMALS
*BIOCHEMISTRY
*CENTRAL nervous system diseases
*DRUG design
*CLINICAL drug trials
*PHENOMENOLOGY
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Language
ISSN
1474-1776
Abstract
Despite G-protein-coupled receptors (GPCRs) being among the most fruitful targets for marketed drugs, intense discovery efforts for several GPCR subtypes have failed to deliver selective drug candidates. Historically, drug discovery programmes for GPCR ligands have been dominated by efforts to develop agonists and antagonists that act at orthosteric sites for endogenous ligands. However, in recent years, there have been tremendous advances in the discovery of novel ligands for GPCRs that act at allosteric sites to regulate receptor function. These compounds provide high selectivity, novel modes of efficacy and may lead to novel therapeutic agents for the treatment of multiple psychiatric and neurological human disorders. [ABSTRACT FROM AUTHOR]