Allosteric modulation of G protein-coupled receptors
| Autor: | Willem Soudijn, Ad P. IJzerman, Ineke Van Wijngaarden |
|---|---|
| Rok vydání: | 2003 |
| Předmět: |
Pharmacology
Chemistry Receptors Drug Allosteric regulation Calcium-Binding Proteins Molecular Conformation Receptors Purinergic P1 General Medicine Receptors Metabotropic Glutamate Receptors Muscarinic Metabotropic receptor Receptors GABA-B Dopamine receptor Metabotropic glutamate receptor GTP-Binding Proteins Drug Discovery Muscarinic acetylcholine receptor Animals Humans Receptor 5-HT receptor G protein-coupled receptor |
| Zdroj: | Current opinion in drug discoverydevelopment. 5(5) |
| ISSN: | 1367-6733 |
| Popis: | Allosteric modulation of G-protein-coupled receptors may provide an alternative approach for selective receptor interactions. The article is an overview of allosteric modulators enhancing or diminishing the effects of (endogenous) agonists or antagonists on a variety of G-protein-coupled receptors such as muscarinic, α-adrenergic, serotoninergic, dopaminergic, adenosine, metabotropic glutamate and Ca2+ receptors. Efficacious allosteric modulators have been published for the serotonin receptor (5-HT moduline; oleamide), the dopamine receptor (cyclic analogues of the tripeptide prolyl-leucyl-glycinamide), the metabotropic glutamate receptor (CPCCOET (mglu1); MPEP (mglu5)) and the Ca2+ receptor (NPS R-568; NPS 2143). Leads are available for the muscarinic (Ach) receptor (K5720) and the α2A-adrenoceptor (agmatine). SCH-202676 and amiloride analogues are nonselective allosteric modifiers interacting with several different receptors. They may not be suitable as leads for future drugs but such compounds may be u... |
| Databáze: | OpenAIRE |
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