To cite this record: http://ddd.uab.cat/record/67769
Pharmacogenomic and structural analysis of constitutive G-protein coupled receptor activity
Smit, Martine J. (Vrije Universiteit. Leiden/Amsterdam Center for Drug Research)
Vischer, Henry F. (Vrije Universiteit. Leiden/Amsterdam Center for Drug Research)
Bakker, Remko A. (Vrije Universiteit. Leiden/Amsterdam Center for Drug Research)
Jongejan, Aldo (Vrije Universiteit. Leiden/Amsterdam Center for Drug Research)
Timmerman, Henk (Vrije Universiteit. Leiden/Amsterdam Center for Drug Research)
Pardo, Leonardo (Universidad Autonoma de Barcelona. Dept. de Pediatria, Obstetrícia, Ginecologia i Medicina Preventiva. Unitat de Bioestadística)
Leurs, Rob (Vrije Universiteit. Leiden/Amsterdam Center for Drug Research)

Date: 2007
Abstract: G-protein coupled receptors (GPCRs) respond to a chemically diverse plethora of signal transduction molecules. The notion that GPCRs also signal without an external chemical trigger, i. e. in a constitutive or spontaneous manner, resulted in a paradigm shift in the field of GPCR pharmacology. With the recognition of constitutive GPCR activity and the fact that GPCR binding and signaling can be strongly affected by a single point mutation, GPCR pharmacogenomics obtained a lot of attention. For a variety of GPCRs, point mutations have been convincingly linked to human disease. Mutations within conserved motifs, known to be involved in GPCR activation, might explain the properties of some naturally occurring constitutively active GPCR variants linked to disease. A brief history historical introduction to the present concept of constitutive receptor activity is given and the pharmacogenomic and the structural aspects of constitutive receptor activity are described.
Note: Premi a l'excel·lència investigadora. Àmbit de les Ciències de la Salut. 2008
Rights: Tots els drets reservats
Language: Anglès.
Document: article ; altres ; article ; publishedVersion
Subject: PREI 2008 ; G-protein coupled receptors ; Constitutive activity ; Inverse agonism
Published in: The Annual Review of Pharmacology and Toxicology, Vol. 47, Núm. (2007) , p. 53-87, ISSN 0362-1642

DOI: 10.1146/annurev.pharmtox.47.120505.105126


Post-print
42 p, 2.6 MB

The record appears in these collections:
Articles > Research Excellence Awards
Articles > Published articles

 Record created 2011-02-21, last modified 2014-06-07



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