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G‐Protein‐coupled receptor–protein interactions: Basis for new concepts on receptor structure and function
Author(s) -
Tilakaratne Nanda,
Sexton Patrick M
Publication year - 2005
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1111/j.1440-1681.2005.04295.x
Subject(s) - g protein coupled receptor , heterotrimeric g protein , rhodopsin like receptors , 5 ht5a receptor , receptor , biology , g protein coupled receptor kinase , microbiology and biotechnology , g protein , signal transduction , gtpase activating protein , computational biology , biochemistry , metabotropic receptor , agonist
SUMMARY 1. G‐Protein‐coupled receptors (GPCRs) constitute a large family of cell surface proteins. Their primary function is to transmit extracellular stimuli to intracellular signals. It is estimated that the human genome contains more than 1000 genes that code for proteins of the GPCR structure. These receptors also comprise the most important class of therapeutic drug targets. 2. The mechanism of GPCR signalling was initially envisioned as involving coupling to the heterotrimeric G‐proteins only. However, recent developments in the field suggest that such a simplistic model cannot be sustained any longer. The emerging view is that a wide range of accessory proteins are involved in the regulation of every aspect of GPCR activity. 3. G‐Protein‐coupled receptor‐interacting proteins are implicated in the regulation of several aspects of GPCR biology, including receptor targeting to the respective sites of action, receptor anchoring, signalling and receptor desensitization. In some cases (e.g. receptor activity modifying proteins), they may contribute to the receptor structure and form a part of the ligand‐binding domain. 4. These findings have contributed to new concepts of cellular organization in which modular protein–protein interactions provide a network through which signalling pathways are assembled and controlled.