Document Detail

Historical review: Negative efficacy and the constitutive activity of G-protein-coupled receptors.
MedLine Citation:
PMID:  16260046     Owner:  NLM     Status:  MEDLINE    
The idea that a receptor can produce signalling without agonist intervention and that several antagonists can be 'active' in repressing such spontaneous activity is contained in the concept of ligand-induced conformational changes. Yet, this idea was neglected by pharmacologists for many years. In this article, we review the events that brought inverse agonism and constitutive activity to general attention and made this phenomenon a topic of current research. We also suggest a classification of antagonists based on the cooperativity that links their primary site of interaction with other functional domains of the receptor.
Tommaso Costa; Susanna Cotecchia
Related Documents :
20643056 - Distribution and dynamics of rat basophilic leukemia immunoglobulin e receptors (fcepsi...
1816556 - Approaches to molecular modeling studies and specific application to serotonin ligands ...
15501046 - Design, synthesis, and evaluation of hexahydrobenz[f]isoquinolines as a novel class of ...
16530386 - Multiple receptor states are required to describe both kinetic binding and activation o...
1689476 - Autoradiographic localisation of nmda, quisqualate and kainic acid receptors in human s...
9697826 - Androgen receptors mediate hypertrophy in cardiac myocytes.
Publication Detail:
Type:  Journal Article; Review     Date:  2005-11-02
Journal Detail:
Title:  Trends in pharmacological sciences     Volume:  26     ISSN:  0165-6147     ISO Abbreviation:  Trends Pharmacol. Sci.     Publication Date:  2005 Dec 
Date Detail:
Created Date:  2005-11-21     Completed Date:  2005-12-23     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7906158     Medline TA:  Trends Pharmacol Sci     Country:  England    
Other Details:
Languages:  eng     Pagination:  618-24     Citation Subset:  IM    
Department of Pharmacology, Istituto Superiore di Sanità, Italy.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Receptors, G-Protein-Coupled / agonists,  antagonists & inhibitors,  genetics,  metabolism*
Signal Transduction*
Reg. No./Substance:
0/Ligands; 0/Receptors, G-Protein-Coupled

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  Tolerance induction through simultaneous double bone marrow transplantation with two-signal blockade...
Next Document:  A therapeutic role for cannabinoid CB1 receptor antagonists in major depressive disorders.