{"paper_id":"cba6fb9f-e16f-405f-9fcf-0290fd231d14","body_text":"Abstract\nKeywords: Aldo-keto reductases, cancer, drug discovery, enzyme inhibitors, flavonoids, non-steroidal anti-inflammatory drugs, steroids, synergistic, steroidal hormones, prostaglandins\nCurrent Medicinal Chemistry\nTitle: Inhibitors of Aldo-Keto Reductases AKR1C1-AKR1C4\nVolume: 18 Issue: 17\nAuthor(s): P. Brozic, S. Turk, T. Lanisnik Rizner and S. Gobec\nAffiliation:\nKeywords: Aldo-keto reductases, cancer, drug discovery, enzyme inhibitors, flavonoids, non-steroidal anti-inflammatory drugs, steroids, synergistic, steroidal hormones, prostaglandins\nAbstract: The AKR1C aldo-keto reductases (AKR1C1-AKR1C4) are enzymes that interconvert steroidal hormones between their active and inactive forms. In this manner, they can regulate the occupancy and trans-activation of the androgen, estrogen and progesterone receptors. The AKR1C isoforms also have important roles in the production and inactivation of neurosteroids and prostaglandins, and in the metabolism of xenobiotics. They thus represent important emerging drug targets for the development of agents for the treatment of hormone-dependent forms of cancer, like breast, prostate and endometrial cancers, and other diseases, like premenstrual syndrome, endometriosis, catamenial epilepsy and depressive disorders. We present here the physiological roles of these enzymes, along with their structural properties and an overview of the recent developments regarding their inhibitors. The most important strategies of inhibitor design are described, which include the screening of banks of natural compounds (like cinnamic acids, flavonoids, jasmonates, and related compounds), the screening of and structural modifications to non-steroidal anti-inflammatory drugs, the substrate-inspired design of steroidal and nonsteroidal inhibitors, and computer-assisted structure-based inhibitor design.\nExport Options\nAbout this article\nCite this article as:\nBrozic P., Turk S., Lanisnik Rizner T. and Gobec S., Inhibitors of Aldo-Keto Reductases AKR1C1-AKR1C4, Current Medicinal Chemistry 2011; 18 (17) . https://dx.doi.org/10.2174/092986711795933713\n| DOI https://dx.doi.org/10.2174/092986711795933713 |\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. 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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\nCurrent Vascular Pharmacology Central G-Protein Coupled Receptors (GPCR)s as Molecular Targets for the Treatment of Obesity: Assets, Liabilities and Development Status\nCurrent Drug Targets - CNS & Neurological Disorders Organometallic Complexes: New Tools for Chemotherapy\nCurrent Medicinal Chemistry Hsa_circ_0000437 Inhibits the Development of Endometrial Carcinoma through miR-626/CDKN1B Axis\nProtein & Peptide Letters Statin Intolerance: Why and What to do – With a Focus on Diabetic People\nCurrent Medicinal Chemistry Protein Phosphatase 1 and Its Complexes in Carcinogenesis\nCurrent Cancer Drug Targets Biology and Therapeutic Applications of Peroxisome Proliferator- Activated Receptors\nCurrent Topics in Medicinal Chemistry Cancer “Stemness”- Regulating MicroRNAs: Role, Mechanisms and Therapeutic Potential\nCurrent Drug Targets Progress in Synthesis and Antitumor Activities of Estradiol-linked Platinum Complex\nMini-Reviews in Medicinal Chemistry Changes in Expression Pattern of SEMA3F Depending on Endometrial Cancer Grade - Pilot Study\nCurrent Pharmaceutical Biotechnology ADAM19/Adamalysin 19 Structure, Function, and Role as a Putative Target in Tumors and Inflammatory Diseases\nCurrent Pharmaceutical Design May Endocrine Therapy be Associated with Cognitive Impairment in Breast Cancer Patients?\nClinical Cancer Drugs Inhibitory Effects of Bisphosphonates on the Proliferation of Human Ovarian Cancer Cell Lines and the Mechanism\nMedicinal Chemistry IMPDH2 Positively Impacts the Proliferation Potential of Hepatoblastoma Cells by Activating JunB Signaling Pathway\nCurrent Molecular Pharmacology Therapeutic Targeting of Cancers with Loss of PTEN Function\nCurrent Drug Targets Cancer Therapy Through Control of Cell Migration\nCurrent Cancer Drug Targets Fibroblast Growth Factor-2, Bone Homeostasis and Fracture Repair\nCurrent Pharmaceutical Design From Natural Products to Designer Drugs: Development and Molecular Mechanisms Action of Novel Anti-Microtubule Breast Cancer Therapeutics\nCurrent Topics in Medicinal Chemistry Extracellular Vesicles Isolated from Mesenchymal Stromal Cells Primed with Hypoxia: Novel Strategy in Regenerative Medicine\nCurrent Stem Cell Research & Therapy Development of an Intracellular, DNA Methyltransferase-Specific, and Gene-Specific Assay for Studying Dynamic DNA Methylation\nCurrent Pharmaceutical Design","source_license":"public-domain-us","license_restricted":false}