Peptides Corresponding to Intracellular Regions of GPCR as a New Generation of Selective Drugs.

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.