Journal article
G-protein-coupled receptors targeting: the allosteric approach
M.S. Médecine sciences, Vol.28(10), pp.845-851
10/2012
DOI: 10.1051/medsci/20122810012
PMID: 23067415
Abstract
G-protein-coupled receptors (GPCR) are a major family of drug targets. Essentially all drugs targeting these receptors on the market compete with the endogenous ligand (agonists or antagonists) for binding the receptor. Recently, non-competitive compounds binding to distinct sites from the cognate ligand were documented in various classes of these receptors. These compounds, called allosteric modulators, generally endowed of a better selectivity are able to modulate specifically the endogenous signaling of the receptor. To better understand the promising potential of this class of GPCRs targeting compounds, this review highlights the properties of allosteric modulators, the strategies used to identify them and the challenges associated with the development of these compounds.
Details
- Title: Subtitle
- G-protein-coupled receptors targeting: the allosteric approach
- Creators
- Julien A Sebag - Department of Molecular Physiology and Biophysics, Vanderbilt School of Medicine, Nashville, TN, USAJacques Pantel
- Resource Type
- Journal article
- Publication Details
- M.S. Médecine sciences, Vol.28(10), pp.845-851
- DOI
- 10.1051/medsci/20122810012
- PMID
- 23067415
- NLM abbreviation
- Med Sci (Paris)
- ISSN
- 0767-0974
- eISSN
- 1958-5381
- Publisher
- France
- Alternative title
- Ciblage thérapeutique des récepteurs couplés aux protéines G - La voie allostérique
- Language
- French
- Date published
- 10/2012
- Academic Unit
- Molecular Physiology and Biophysics; Iowa Neuroscience Institute
- Record Identifier
- 9984025574002771
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