Allosteric modulation of G protein-coupled receptors
- PMID: 12630295
Allosteric modulation of G protein-coupled receptors
Abstract
Allosteric modulation of G protein-coupled receptors has recently been recognized as an alternative approach for selectivity in drug action. Allosteric modulators that enhance or diminish the effects of (endogenous) agonists or antagonists on a variety of G protein-coupled receptors are described in this review, with emphasis on the latest developments in this research area. Specific examples include allosteric ligands for adenosine A1 and A3 receptors, Ca(2+)-sensing receptors, metabotropic glutamate receptor subtypes, gamma-aminobutyric acid type B and muscarinic receptors. It appears that all three major classes of G protein-coupled receptors (A, B and C) are amenable to allosteric modulation by small molecules. This constitutes an attractive and novel means to identify new leads in the drug discovery process. However, it requires a reengineering of most current assays.
Similar articles
-
Allosteric modulation of G protein-coupled receptors: perspectives and recent developments.Drug Discov Today. 2004 Sep 1;9(17):752-8. doi: 10.1016/S1359-6446(04)03220-9. Drug Discov Today. 2004. PMID: 15450241 Review.
-
Allosteric modulation of family C G-protein-coupled receptors: from molecular insights to therapeutic perspectives.Pharmacol Rev. 2011 Mar;63(1):59-126. doi: 10.1124/pr.109.002501. Epub 2011 Jan 12. Pharmacol Rev. 2011. PMID: 21228259 Review.
-
Allosteric modulators of metabotropic glutamate receptors: lessons learnt from mGlu1, mGlu2 and mGlu5 potentiators and antagonists.Biochem Soc Trans. 2004 Nov;32(Pt 5):881-7. doi: 10.1042/BST0320881. Biochem Soc Trans. 2004. PMID: 15494040 Review.
-
Positive and negative allosteric modulation of metabotropic glutamate receptors: emerging therapeutic potential.Pharmacol Ther. 2004 Dec;104(3):233-44. doi: 10.1016/j.pharmthera.2004.08.010. Pharmacol Ther. 2004. PMID: 15556676 Review.
-
Toward understanding GPCR dimers.Nat Struct Mol Biol. 2004 Aug;11(8):691-2. doi: 10.1038/nsmb0804-691. Nat Struct Mol Biol. 2004. PMID: 15280880 No abstract available.
Cited by
-
Allosteric modulation of adenosine receptors.Purinergic Signal. 2009 Mar;5(1):51-61. doi: 10.1007/s11302-008-9105-3. Epub 2008 Jul 10. Purinergic Signal. 2009. PMID: 18615273 Free PMC article.
-
Beta-ionone activates and bleaches visual pigment in salamander photoreceptors.Vis Neurosci. 2009 May-Jun;26(3):267-74. doi: 10.1017/S0952523809090105. Epub 2009 Jun 5. Vis Neurosci. 2009. PMID: 19500430 Free PMC article.
-
Discovery of an allosteric site in the caspases.Proc Natl Acad Sci U S A. 2004 Aug 24;101(34):12461-6. doi: 10.1073/pnas.0404781101. Epub 2004 Aug 16. Proc Natl Acad Sci U S A. 2004. PMID: 15314233 Free PMC article.
-
Evidence that corticotropin-releasing factor receptor type 1 couples to Gs- and Gi-proteins through different conformations of its J-domain.Br J Pharmacol. 2006 Dec;149(7):942-7. doi: 10.1038/sj.bjp.0706926. Epub 2006 Oct 23. Br J Pharmacol. 2006. PMID: 17057757 Free PMC article.
-
Allosteric modulators of glycoprotein hormone receptors: discovery and therapeutic potential.Endocrine. 2008 Aug-Dec;34(1-3):1-10. doi: 10.1007/s12020-008-9098-2. Epub 2008 Oct 28. Endocrine. 2008. PMID: 18956257 Review.
Publication types
MeSH terms
Substances
LinkOut - more resources
Other Literature Sources
Miscellaneous