2. Academic Validation
  3. Structure-activity relationships of inverse agonists for G-protein-coupled receptors

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

  • Med Res Rev. 2005 Jul;25(4):398-426. doi: 10.1002/med.20031.
Willem Soudijn 1,  Ineke van Wijngaarden,  Adriaan P Ijzerman
Affiliations

Affiliation

  • 1 Leiden/Amsterdam Center for Drug Research, PO Box 9502, 2300RA Leiden, The Netherlands.
PMID: 15816047 DOI: 10.1002/med.20031
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.

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