Kisspeptin antagonists

Roseweir, A. K. and Millar, R. P. (2013) Kisspeptin antagonists. In: Kisspeptin Signaling in Reproductive Biology. Series: Advances in Experimental Medicine and Biology, 784 (784). Springer New York: New York, NY, pp. 159-186. ISBN 9781461461982 (doi: 10.1007/978-1-4614-6199-9_8)

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Kisspeptin is now known to be an important regulator of the hypothalamic-­pituitary-gonadal axis and is the target of a range of regulators, such as steroid hormone feedback, nutritional and metabolic regulation. Kisspeptin binds to its cognate receptor, KISS1R (also called GPR54), on GnRH neurons and stimulates their activity, which in turn provides an obligatory signal for GnRH secretion—thus gating down-stream events supporting reproduction. The development of peripherally active kisspeptin antagonists could offer a unique therapeutic agent for treating hormone-dependent disorders of reproduction, including precocious puberty, endometriosis, and metastatic prostate cancer. The following chapter discusses the advances made in the search for both peptide and small molecule kisspeptin antagonists and their use in delineating the role of kisspeptin within the reproductive system. To date, four peptide antagonists and one small molecule antagonist have been designed.

Item Type:Book Sections
Glasgow Author(s) Enlighten ID:Roseweir, Dr Antonia
Authors: Roseweir, A. K., and Millar, R. P.
College/School:College of Medical Veterinary and Life Sciences > School of Cancer Sciences
Journal Name:Advances in Experimental Medicine and Biology
Publisher:Springer New York
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