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Open AccessReview

Recent Development of Non-Peptide GnRH Antagonists

School of Pharmacy, University of Oslo, 0316 Oslo, Norway
Norsk Medisinsk Syklotronsenter AS, Postboks 4950 Nydalen, 0424 Oslo, Norway
Realomics SFI, Department of Chemistry, University of Oslo, 0316 Oslo, Norway
Department of neuropsychiatry and psychosomatic medicine, Oslo University Hospital, 4950 Oslo, Norway
Betanien Hospital, 3722 Skien, Norway
Author to whom correspondence should be addressed.
Molecules 2017, 22(12), 2188;
Received: 16 November 2017 / Revised: 4 December 2017 / Accepted: 4 December 2017 / Published: 9 December 2017
(This article belongs to the Section Medicinal Chemistry)
The decapeptide gonadotropin-releasing hormone, also referred to as luteinizing hormone-releasing hormone with the sequence (pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2) plays an important role in regulating the reproductive system. It stimulates differential release of the gonadotropins FSH and LH from pituitary tissue. To date, treatment of hormone-dependent diseases targeting the GnRH receptor, including peptide GnRH agonist and antagonists are now available on the market. The inherited issues associate with peptide agonists and antagonists have however, led to significant interest in developing orally active, small molecule, non-peptide antagonists. In this review, we will summarize all developed small molecule GnRH antagonists along with the most recent clinical data and therapeutic applications. View Full-Text
Keywords: GnRH receptor; non-peptide GnRH antagonist GnRH receptor; non-peptide GnRH antagonist
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MDPI and ACS Style

Tukun, F.-L.; Olberg, D.E.; Riss, P.J.; Haraldsen, I.; Kaass, A.; Klaveness, J. Recent Development of Non-Peptide GnRH Antagonists. Molecules 2017, 22, 2188.

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