Репозиторий Университета

© 2018 Ruslania. All rights reserved. This literature review is devoted to modem notions about molecular mechanism of action of the selective modulators of progesterone receptors. The superfamily of nuclear receptors represents ligand-activated transcription factors and includes receptors for steroid hormones, lipophilic vitamins, sterols, and bile acids. These receptors serve as targets for creating numerous drugs. As a result, a new class of compounds (ligands) appeared exhibiting agonistic/partial agonistic/antagonistic functional activities depending on the context (tissue or gene target). This class of ligands is called selective modulators of nuclear receptors. Initially, mifepristone was developed as the progesterone receptor antagonist, but further it demonstrated the properties of a selective modulator of progesterone receptor and became the ancestor of this group. At present, the development of new selective modulators of progesterone receptor is aimed at obtaining higher selectivity with respect to progesterone receptors and decreasing the anti-androgenic and anti-glucocorticoid properties. Unfortunately, most of the subsequent selective modulators of progesterone receptors exhibited hepatotoxicity, which limited their wide introduction into clinical practice.