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Kisspeptin Antagonists

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Book cover Kisspeptin Signaling in Reproductive Biology

Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 784))

Abstract

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.

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Author information

Authors and Affiliations

  1. Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, Scotland, UK

    Antonia Kathryn Roseweir

  2. Institute of Cancer Sciences, School of Medicine, Veterinary Medicine and Life Sciences, University of Glasgow, Glasgow, Scotland, UK

    Antonia Kathryn Roseweir

  3. Department Zoology and Entomology, University of Pretoria, X 20, Hatfield, 0028, South Africa

    Robert P. Millar M.Sc., Ph.D., M.R.C.Path., F.R.C.P.Path.

Authors
  1. Antonia Kathryn Roseweir
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  2. Robert P. Millar M.Sc., Ph.D., M.R.C.Path., F.R.C.P.Path.
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Corresponding author

Correspondence to Robert P. Millar M.Sc., Ph.D., M.R.C.Path., F.R.C.P.Path. .

Editor information

Editors and Affiliations

  1. , Department of Reproductive Medicine, University of California, San Diego, La Jolla, 92093, California, USA

    Alexander S. Kauffman

  2. School of Anatomy, Physiology and Human Biology, The University of Western Australia, Hackett Drive, Nedlands, 6009, West Australia, Australia

    Jeremy T. Smith

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Roseweir, A.K., Millar, R.P. (2013). Kisspeptin Antagonists. In: Kauffman, A., Smith, J. (eds) Kisspeptin Signaling in Reproductive Biology. Advances in Experimental Medicine and Biology, vol 784. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-6199-9_8

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