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15 February 2018 Gonadotropins and their receptors: coevolution, genetic variants, receptor imaging, and functional antagonists
Aaron J. Hsueh, Jiahuan He
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Abstract

Gonadotropins belong to the family of dimeric glycoprotein hormones and regulate gonadal physiology mediated by G protein-coupled, seven-transmembrane receptors. These glycoprotein hormones are widely used in the clinic to promote ovarian follicle development and for treating some cases of male infertility. We traced the coevolution of dimeric gonadotropin hormones and their receptors, together with thyrotropin and its receptor. We updated recent findings on human genetic variants of these genes and their association with dizygotic twining, polycystic ovarian syndrome, primary ovarian insufficiency, male-limited precocious puberty, and infertility. In addition to the known physiological roles of gonadotropin-receptor signaling in gonadal tissues, we also discussed emerging understanding of extragonadal functions of gonadotropins in bones and adipose tissues, together with recent advances in in vivo imaging of gonadotropin receptors in live animals. Recent development of gonadotropin receptor agonists and antagonists were summarized with an emphasis on the development of functional antagonists for FSH receptors to alleviate osteoporosis and obesity associated with menopause.

Summary Sentence

Understanding of the co-evolution of gonadotropins and their cognate receptors, together with mutant phenotypes and receptor imaging, allow future design of functional antagonists to regulate different physiological and pathological processes.

© The Author(s) 2018. Published by Oxford University Press on behalf of Society for the Study of Reproduction. All rights reserved. For permissions, please e-mail: journals.permissions@oup.com
Aaron J. Hsueh and Jiahuan He "Gonadotropins and their receptors: coevolution, genetic variants, receptor imaging, and functional antagonists," Biology of Reproduction 99(1), 3-12, (15 February 2018). https://doi.org/10.1093/biolre/ioy012
Received: 21 November 2017; Accepted: 6 February 2018; Published: 15 February 2018
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