Recent Development of Non-Peptide GnRH Antagonists

Molecules. 2017 Dec 9;22(12):2188. doi: 10.3390/molecules22122188.

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.

Keywords: GnRH receptor; non-peptide GnRH antagonist.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Drug Discovery
  • Humans
  • Molecular Structure
  • Receptors, LHRH / antagonists & inhibitors*
  • Small Molecule Libraries / administration & dosage*
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology
  • Structure-Activity Relationship

Substances

  • GNRHR protein, human
  • Receptors, LHRH
  • Small Molecule Libraries