![conference banner](/images/conference-banner.jpeg)
Abstract
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.
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:
Keywords: gnrh, lhrh, agonist, antagonist, non-peptidic
Abstract: 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 Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
![Wayfinder Image](/images/wayfinder.jpg)
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Targeted Drug Delivery and Imaging Using Mobile Milli/Microrobots: A Promising Future Towards Theranostic Pharmaceutical Design
Current Pharmaceutical Design Phosphatidylinositol 3-Kinase Isoforms as Novel Drug Targets
Current Drug Targets Advances in the Management of Brain Tumors in Infants
Current Cancer Therapy Reviews Applications of Nanomaterials for Cancer Treatment: Recent Patents Review
Recent Patents on Nanomedicine Exosome Limitations in the Treatment of Inflammatory Diseases
Current Pharmaceutical Design PI3K/Akt Signalling Pathway Specific Inhibitors: A Novel Strategy to Sensitize Cancer Cells to Anti-Cancer Drugs
Current Pharmaceutical Design Iodine Bonded with Milk Protein Inhibits Benign Prostatic Hyperplasia Development in Rats
Anti-Cancer Agents in Medicinal Chemistry Role of Calcium, Vitamin D, and the Extrarenal Vitamin D Hydroxylases in Carcinogenesis
Anti-Cancer Agents in Medicinal Chemistry Cigarette Smoking, Metabolic Activation and Carcinogenesis
Current Drug Metabolism The Potential use of Dendritic Cell-based Immunotherapy for Treatment of Pancreatic Cancer
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Role of Genomics-Based Strategies in Overcoming Chemotherapeutic Resistance
Current Pharmaceutical Biotechnology Surgical Treatment of Endometriosis
Current Women`s Health Reviews Evaluation Method of Mechanical Properties of Living NSCLC Cells Based on Nano-indentation
Current Nanoscience Gene Electrotransfer to Skin; Review of Existing Literature and Clinical Perspectives
Current Gene Therapy MicroRNA and Cancer: Tiny Molecules with Major Implications
Current Genomics Immunomodulatory Activities of Glucocorticoids: Insights from Transgenesis and Gene Targeting
Current Pharmaceutical Design Exosomes: Natural Carriers for siRNA Delivery
Current Pharmaceutical Design A Systematic Review of Decipher Genomic Classifier Risk Scores for Prostate Cancer in African-Americans
Current Pharmacogenomics and Personalized Medicine Resveratrol as an Enhancer of Apoptosis in Cancer: A Mechanistic Review
Anti-Cancer Agents in Medicinal Chemistry In Vitro, In Vivo and In Silico Analysis of the Anticancer and Estrogen-like Activity of Guava Leaf Extracts
Current Medicinal Chemistry