{"paper_id":"04dd5212-1473-4132-86fb-f42b03fee127","body_text":"Abstract\nKeywords: gnrh, lhrh, agonist, antagonist, non-peptidic\nCurrent Medicinal Chemistry\nTitle: Non-Peptidic GnRH Receptor Antagonists\nVolume: 11 Issue: 22\nAuthor(s): Richard E. Armer and Kathryn H. Smelt\nAffiliation:\nKeywords: gnrh, lhrh, agonist, antagonist, non-peptidic\nAbstract: 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.\nExport Options\nAbout this article\nCite this article as:\nArmer E. Richard and Smelt H. Kathryn, Non-Peptidic GnRH Receptor Antagonists, Current Medicinal Chemistry 2004; 11 (22) . https://dx.doi.org/10.2174/0929867043363983\n| DOI https://dx.doi.org/10.2174/0929867043363983 |\nPrint ISSN 0929-8673 |\n| Publisher Name Bentham Science Publishers |\nOnline ISSN 1875-533X |\nCall for Papers in Thematic Issues\nAdvance in Novel Drug and combined Therapies for Chronic Diseases\nChronic 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. 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Artificial intelligence (AI) and machine learning are fundamentally reshaping the drug discovery and ...read more\n- Author Guidelines\n- Bentham Author Support Services (BASS)\n- Graphical Abstracts\n- Fabricating and Stating False Information\n- Research Misconduct\n- Post Publication Discussions and Corrections\n- Publishing Ethics and Rectitude\n- Increase Visibility of Your Article\n- Archiving Policies\n- Peer Review Workflow\n- Order Your Article Before Print\n- Promote Your Article\n- Manuscript Transfer Facility\n- Editorial Policies\n- Allegations from Whistleblowers\n- Announcements\nRelated Articles\nMini-Reviews in Medicinal Chemistry New Targeted Therapies for Anaplastic Thyroid Cancer\nAnti-Cancer Agents in Medicinal Chemistry A Review on Structures and Functions of Bcl-2 Family Proteins from Homo sapiens\nProtein & Peptide Letters Influence of Tumor Microenvironment on the Distribution and Elimination of Nano-formulations\nCurrent Drug Metabolism Liposomes Prepared in Absence of Organic Solvents: Sonication Versus Lipid Film Hydration Method\nCurrent Pharmaceutical Analysis Protective Effects of Curcumin against Iron-induced Toxicity\nCurrent Pharmaceutical Biotechnology Hormonal Effects on Drug Metabolism Through the CYP System: Perspectives on Their Potential Significance in the Era of Pharmacogenomics\nCurrent Drug Targets - Immune, Endocrine & Metabolic Disorders Aptamers: Molecular Tools for Medical Diagnosis\nCurrent Topics in Medicinal Chemistry Evolution of Novel Non-Steroidal Anti-Inflammatory Drugs with Reduced Gastrointestinal Adverse Effects\nAnti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Xeno-Cannibalism as an Exacerbation of Self-Cannibalism: A Possible Fruitful Survival Strategy for Cancer Cells\nCurrent Pharmaceutical Design Treatment of Metastases to the Vertebrae with Radiofrequency Ablation: Determination of Effectiveness by Evaluation of Tumor Necrosis – A Preliminary Result\nCurrent Radiopharmaceuticals Synthesis and Cytotoxic Activity of New β-Carboline Derivatives\nMini-Reviews in Medicinal Chemistry Properties and Recent Advantages of N,N’-dialkylimidazolium-ion Liquids Application in Electrochemistry\nCurrent Analytical Chemistry Recent Advances of Sulfonylation Reactions in Water\nCurrent Organic Synthesis Inhibitors of Vascular Endothelial Growth Factor in Cancer\nCardiovascular & Hematological Agents in Medicinal Chemistry Open Questions on Bioequivalence: An Updated Reappraisal\nCurrent Clinical Pharmacology Small Molecule Inhibitors of Stat3 Signaling Pathway\nCurrent Cancer Drug Targets Cancer Immunotherapy: The Role Regulatory T Cells Play and What Can be Done to Overcome their Inhibitory Effects\nCurrent Molecular Medicine Glycosides from Medicinal Plants as Potential Anticancer Agents: Emerging Trends Towards Future Drugs\nCurrent Medicinal Chemistry <sup>18</sup>F-labeled Bisphosphonate as an Alternative Candidate to the Gold Standard[<sup>18</sup>F]sodium fluoride ([<sup>18</sup>F]NaF) for PET Bone Imaging\nCurrent Medical Imaging","source_license":"public-domain-us","license_restricted":false}