Structure–activity relationships of inverse agonists for G-protein-coupled receptors

✍ Scribed by Willem Soudijn; Ineke van Wijngaarden; Adriaan P. Ijzerman

• Publisher: John Wiley and Sons
• Year: 2005
• Tongue: English
• Weight: 384 KB
• Volume: 25
• Category: Article
• ISSN: 0198-6325
• DOI: 10.1002/med.20031

✦ Synopsis

Abstract

It has been recently established that G‐protein‐coupled receptors (GPCRs) can be constitutively active, i.e., they can be active in the absence of an agonist. This activity can be inhibited by so‐called inverse agonists. For a number of GPCRs, such inverse agonists have been developed and studied, now enabling for the first time a study into their structure–activity relationships. © 2005 Wiley Periodicals, Inc.