Low-molecular regulators of polypeptide hormones receptors containing LGR-repeats

Abstract

During the last years the low-molecular non-peptidic regulators of the polypeptide hormones receptors containing LGR-repeats were identified. In the review the data on the structure and the molecular mechanisms of action of these regulators as agonists and antagonists of the luteinizing, follicle-stimulating and thyrotropin hormones are analyzed and systematized. The regulators interact with the serpentine domain of LGR-receptor and trigger the signaling cascades coupled with the receptor. Low-molecular agonists and antagonists of the LGR-receptors are considered as a new generation of the drugs that regulates the functional activity of sensitive to pituitary glycoprotein hormones signaling systems with high efficiency and selectivity. These regulators are more accessible compared to the hormones and can be use orally.

The stimulating influence of thienopyrimidine compounds on the adenylyl cyclase signaling systems in the rat testes

“…How ever, the practical use of glycoprotein hormones in medicine is associated with a number of problems, including their lower resistance to proteolytic degra dation, high immunogenicity, the development of resistance of the target tissues to them, and the neces sity of parenteral administration. In view of this, the search for low molecular weight agonists of glycopro tein hormone receptors is carried out in recent years, which can penetrate the transmembrane channel, where the ligand binding site of most GPCRs is located, and cause the same structural changes in it that occur upon the binding of the glycoprotein hormone to the extracellular domain of the receptor [3,4].…”