[Novel achievements in development and application of GPCR-peptides]

One of the approaches to creating the regulators of G-protein-coupled receptors (GPCR) is the development of peptides that structurally correspond to the functionally important regions of the intracellular extracellular loops of the receptors. GPCR-peptides can selectively regulate the functional activity of homologous receptor and affect the hormonal signal transduction via the receptor. Among the peptides corresponding to the intracellular regions of GPCR, their derivatives modified with hydrophobic radicals exhibit the highest activity and selectivity of action in vitro and in vivo. Ample evidence demonstrates that lipophilic GPCR-peptides may be used to treat diseases and various abnormalities that depend on the functional activity of receptors homologous to them. In turn, the peptides corresponding to the extracellular regions of GPCR can be used as functional probes for studying the specific interaction between the receptors and their ligands, as well as for studying the etiology and pathogenesis of autoimmune diseases caused by the production of antibodies to GPCR antigenic determinants that are localized in the receptor extracellular loops. The present review focuses on the recent achievements in development and application of GPCR-peptides and on the prospects for their further use in medicine and fundamental biology.