New achievements in development and application of GPCR-peptides

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