KISS1R: Hallmarks of an Effective Regulator of the Neuroendocrine Axis

Neuroendocrinology
Robert P Millar, Andy V Babwah

Abstract

Kisspeptin (KP) is now well recognized as a potent stimulator of gonadotropin-releasing hormone (GnRH) secretion and thereby a major regulator of the neuroendocrine-reproductive axis. KP signals via KISS1R, a G protein-coupled receptor (GPCR) that activates the G proteins Gαq/11. Modulation of the interaction of KP with KISS1R is therefore a potential new therapeutic target for stimulating (in infertility) or inhibiting (in hormone-dependent diseases) the reproductive hormone cascade. Major efforts are underway to target KISS1R in the treatment of sex steroid hormone-dependent disorders and to stimulate endogenous hormonal responses along the neuroendocrine axis as part of in vitro fertilization protocols. The development of analogs modulating KISS1R signaling will be aided by an understanding of the intracellular pathways and dynamics of KISS1R signaling under normal and pathological conditions. This review focuses on KISS1R recruitment of intracellular signaling (Gαq/11- and β-arrestin-dependent) pathways that mediate GnRH secretion and the respective roles of rapid desensitization, internalization, and recycling of resensitized receptors in maintaining an active population of KISS1R at the cell surface to facilitate prolonge...Continue Reading

Citations

Nov 14, 2015·Journal of Pediatric Endocrinology & Metabolism : JPEM·İlker Tolga ÖzgenYaşar Cesur
Sep 20, 2015·Reproductive Biology and Endocrinology : RB&E·Mehri FayaziAndy V Babwah
Jul 18, 2015·Reproduction : the Official Journal of the Society for the Study of Fertility·Andy V Babwah
Feb 9, 2017·Molecular and Cellular Endocrinology·Eric ReiterPascale Crépieux
Sep 12, 2017·International Journal of Environmental Research and Public Health·Alberto LeonardiSusanna Esposito
Mar 8, 2019·Toxicological Sciences : an Official Journal of the Society of Toxicology·Elizabeth C BowdridgeTimothy R Nurkiewicz
Jul 4, 2019·Journal of Neuroendocrinology·Noelia P Di GiorgioVictoria Lux-Lantos
Mar 11, 2020·Cancer Metastasis Reviews·Thuc LyDanny R Welch
Aug 21, 2018·Frontiers in Endocrinology·Stephania GuzmanMoshmi M Bhattacharya
Oct 20, 2020·Frontiers in Public Health·Manoj KumarRajnarayan Tiwari
Jul 3, 2021·Trends in Molecular Medicine·Ali AbbaraWaljit S Dhillo

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