Effects and therapeutic potentials of kisspeptin analogs: regulation of the hypothalamic-pituitary-gonadal axis

Neuroendocrinology
Hisanori Matsui, Taiji Asami

Abstract

The hypothalamic peptide kisspeptin (metastin), the endogenous ligand of the G protein-coupled receptor KISS1R, plays a critical role in controlling GnRH release from hypothalamic GnRH neurons and thereby regulates hypothalamic-pituitary-gonadal functions. Although the therapeutic potential of kisspeptin is attractive, its susceptibility to proteolytic degradation limits its utility. To overcome this, KISS1R agonists or antagonists as peptide analogs or small molecules have been investigated. Kisspeptin analogs have been most extensively studied by reducing the length of the peptide from the original 54 amino acids to 10 amino acids or less and by substituting key amino acid residues. Also, 2 investigational kisspeptin agonist analogs have been evaluated in clinical studies in men; in agreement with animal studies, abrupt elevations in gonadotropin and testosterone levels were observed as an acute effect, followed by rapid reductions in these hormones as a chronic effect. Some studies of small-molecule KISS1R antagonists have also been published. In this review, we present a brief overview on kisspeptin/KISS1R physiology in reproductive functions and summarize the available knowledge of both agonists and antagonists. We also fo...Continue Reading

Citations

Apr 14, 2016·Journal of the Chinese Medical Association : JCMA·Kuan-Hao TsuiPeng-Hui Wang
Jun 11, 2016·Journal of Peptide Science : an Official Publication of the European Peptide Society·M A CamerinoP E Thompson
Dec 5, 2017·International Journal of Endocrinology and Metabolism·Sareh Zeydabadi NejadAzita Zadeh-Vakili
Nov 17, 2020·The Journal of Clinical Investigation·Ali AbbaraWaljit S Dhillo
Oct 13, 2020·Frontiers in Neuroendocrinology·Hsien-Ming WuPeter C K Leung
Jun 8, 2021·Chemical Science·Samuel D MeltonDavid M Chenoweth

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