Recent Development of Non-Peptide GnRH Antagonists

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2017 Dec 14

PMID 29232843

Citations 14

Authors

Feng-Ling Tukun

Dag Erlend Olberg

Patrick J Riss

Ira Haraldsen

Anita Kaass

Jo Klaveness

Affiliations

Soon will be listed here.

Abstract

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.

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