Many or too many progesterone membrane receptors?

• Verfasst von: Wendler, Alexandra [VerfasserIn]
• Verfasst von: Wehling, Martin [VerfasserIn]
• Titel: Many or too many progesterone membrane receptors?
• Titelzusatz: clinical implications
• Verf.angabe: Alexandra Wendler and Martin Wehling
• E-Jahr: 2022
• Jahr: 14 November 2022
• Umfang: 19 S.
• Fussnoten: Gesehen am 18.01.2023
• Titel Quelle: Enthalten in: Trends in endocrinology and metabolism
• Ort Quelle: Amsterdam [u.a.] : Elsevier Science, 1989
• Jahr Quelle: 2022
• Band/Heft Quelle: 33(2022), 12, Seite 850-868
• ISSN Quelle: 1879-3061
• DOI: doi:10.1016/j.tem.2022.10.001
• Datenträger: Online-Ressource
• Sprache: eng
• Sach-SW: Mannheim classification
• Sach-SW: nongenomically initiated actions of progesterone
• Sach-SW: progesterone membrane receptor
• Sach-SW: translational success
• K10plus-PPN: 1831331756

Abstract

Several receptors for nongenomically initiated actions of progesterone (P4) exist, namely membrane-associated P4 receptors (MAPRs), membrane progestin receptors (mPRs), receptors for neurosteroids [GABAA receptor (GABAAR), NMDA receptor, sigma-1 and -2 receptors (S1R/S2R)], the classical genomic P4 receptor (PGR), and α/β hydrolase domain-containing protein 2 (ABHD2). Two drugs related to this field have been approved: brexanolone (Zulresso™) for the treatment of postpartum depression, and ganaxolone (Ztalmy™) for the treatment of CDKL5 deficiency disorder. Both are derivatives of P4 and target the GABAAR. Several other indications are in clinical testing. CT1812 (Elayta™) is also being tested for the treatment of Alzheimer’s disease (AD) in Phase 2 clinical trials, targeting the P4 receptor membrane component 1 (PGRMC1)/S2R complex. In this Review, we highlight emerging knowledge on the mechanisms of nongenomically initiated actions of P4 and its derivatives.