Peptides Corresponding to Intracellular Regions of GPCR as a New Generation of Selective Drugs
Alexander O. Shpakov *
Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, Thorez av. 44, 194223 St. Petersburg, Russia
*Author to whom correspondence should be addressed.
Abstract
In the G protein-coupled receptors (GPCRs) relatively short regions of their intracellular loops and cytoplasmic C-terminal domain are responsible for specific interaction with G-proteins. GPCR-derived peptides corresponding to these regions are able to influence the activity of signal pathways involving the cognate receptors. Modified by hydrophobic radicals, these peptides turn into their cell-penetrating analogs, pepducins, possessing the activity both in vitro and in vivo. This review is devoted to the analysis of the available data and the prospects for GPCR-peptides and their lipophilic derivatives to be used in experimental and clinical medicine in the treatment of vascular diseases, cancers, inflammation, and endocrine dysfunctions.
Keywords: Angiogenesis, cancer, G protein-coupled receptor, heterotrimeric G protein, inflammation, intracellular loop, palmitate, pepducin, peptide