Biochemistry, molecular biology and cell biology of gonadotropin-releasing hormone antagonists

Orkun Tan, Orhan Bukulmez

Research output: Contribution to journalArticle

23 Citations (Scopus)

Abstract

PURPOSE OF REVIEW: Gonadotropin-releasing hormone (GnRH) receptors are not only detected in the central nervous system but also in tissues such as ovary, endometrium, breast, gastrointestinal system, placenta and malignant tumors of ovary and breast. The direct role of GnRH-antagonists in ovarian function, implantation, cancer pathogenesis and treatment is under extensive investigation. This study reviews the biochemistry and molecular and cellular biology of GnRH-antagonists as well as GnRH types and their receptors. RECENT FINDINGS: The best clinical evidence with GnRH-antagonists has accumulated in controlled ovarian hyperstimulation protocols for prevention of premature luteinizing hormone surge (cetrorelix, ganirelix) and in the treatment of advanced-stage prostate cancer (abarelix and degarelix). GnRH-GnRH receptor pathways may have a role in the embryo implantation. The controversy still exists whether GnRH antagonist protocols result in slightly decreased clinical pregnancy rates compared with the GnRH agonist protocols. GnRH-antagonists could be used in the near future to treat some cancer types that express GnRH receptors. SUMMARY: GnRH-antagonists have various clinical applications in gynecology, reproductive medicine, urology and oncology. The emergence of well tolerated, orally active GnRH-antagonists may provide an alternative to long-term injections and is likely to have a major impact on the utility of GnRH analogues in the treatment of human diseases.

Original languageEnglish (US)
Pages (from-to)238-244
Number of pages7
JournalCurrent Opinion in Obstetrics and Gynecology
Volume23
Issue number4
DOIs
StatePublished - Aug 2011

Fingerprint

Hormone Antagonists
Gonadotropin-Releasing Hormone
Biochemistry
Cell Biology
Molecular Biology
LHRH Receptors
Ovary
Reproductive Medicine
Urology
Pregnancy Rate
Luteinizing Hormone
Endometrium
Gynecology
Placenta
Neoplasms
Prostatic Neoplasms
Breast
Therapeutics
Central Nervous System
Breast Neoplasms

Keywords

  • cell biology
  • gonadotropin-releasing hormone
  • gonadotropin-releasing hormone antagonist
  • gonadotropin-releasing hormone receptor

ASJC Scopus subject areas

  • Obstetrics and Gynecology

Cite this

Biochemistry, molecular biology and cell biology of gonadotropin-releasing hormone antagonists. / Tan, Orkun; Bukulmez, Orhan.

In: Current Opinion in Obstetrics and Gynecology, Vol. 23, No. 4, 08.2011, p. 238-244.

Research output: Contribution to journalArticle

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