Non-peptidic GnRH receptor antagonists

Keywords: gnrh, lhrh, agonist, antagonist, non-peptidic Current Medicinal Chemistry Title: Non-Peptidic GnRH Receptor Antagonists Volume: 11 Issue: 22 Author(s): Richard E. Armer and Kathryn H. Smelt Affiliation:

gnrh, lhrh, agonist, antagonist, non-peptidic

Gonadotropin-releasing hormone (GnRH) or luteinizing hormone-releasing hormone (LHRH) is a decapeptide (pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2) hypothalamic hormone that acts upon 7-trans membrane spanning GnRH receptors in the pituitary. This action leads to the secretion of the gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH) that in turn act on the reproductive organs regulating gonadal steroid production, spermatogenesis and follicular development. Peptidic agonists of the GnRH receptor have been known for many years and are currently employed therapeutically in the treatment of prostate and breast tumours, uterine fibroids, precocious puberty, endometriosis, premenstrual syndrome, contraception and infertility. Peptidic antagonists to date have only been employed commercially in the treatment of infertility during assisted reproductive therapy; however, many peptidic antagonists are currently in late stage development for many of the aforementioned indications. Whilst peptidic agonists and antagonists of the GnRH receptor have been discovered and exploited clinically, they are limited to predominantly parenteral administration due to their poor oral bioavaila bility. Recently, several small molecule GnRH antagonist series have been discovered offering the prospect of orally active therapeutics based on GnRH receptor antagonism. This article will review the current medicinal chemistry literature and structure activity relationships known for non-peptidic GnRH receptor antagonists. Export Options About this article Cite this article as: Armer E. Richard and Smelt H. Kathryn, Non-Peptidic GnRH Receptor Antagonists, Current Medicinal Chemistry 2004; 11 (22) . https://dx.doi.org/10.2174/0929867043363983 | DOI https://dx.doi.org/10.2174/0929867043363983 | Print ISSN 0929-8673 | | Publisher Name Bentham Science Publishers | Online ISSN 1875-533X | Call for Papers in Thematic Issues Advance in Novel Drug and combined Therapies for Chronic Diseases Chronic diseases such as malignant tumors and rheumatoid arthritis have long plagued a large number of patients. Currently, the management of chronic diseases has entered a new stage of targeted regulation, precise intervention and integrated treatment. The traditional diagnosis and treatment model is undergoing profound changes due to new drugs ...read more Advances in Computational Strategies for Neurodegenerative Disorders, Cancer, and Infectious Diseases” This thematic issue highlights recent advances in computational strategies applied to neurodegenerative disorders, cancer, and infectious diseases. 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