The New Pharmacological Approaches for the Regulation of Functional Activity of G Protein-Coupled Receptors

The G protein-coupled receptors (GPCRs), a large family of the receptors that specifically interact with a number of signal molecules, play a key role in the regulation of fundamental cell processes, and the pharmacological action of over 40% of drugs is carried out through GPCRs. In the last years, a significant progress was made in the creation of selective regulators of GPCRs interacting with their allosteric sites, such as the synthetic peptides corresponding to intracellular regions of receptors (GPCR-peptides) and the low-molecular weight agonists and antagonists of GPCRs. This review describes the recent results obtained by us and other authors in the development of GPCR-peptides and low-molecular weight agonists and the prospects of their use in clinics.