Inhibitors of aldo-keto reductases AKR1C1-AKR1C4

Keywords: Aldo-keto reductases, cancer, drug discovery, enzyme inhibitors, flavonoids, non-steroidal anti-inflammatory drugs, steroids, synergistic, steroidal hormones, prostaglandins Current Medicinal Chemistry Title: Inhibitors of Aldo-Keto Reductases AKR1C1-AKR1C4 Volume: 18 Issue: 17 Author(s): P. Brozic, S. Turk, T. Lanisnik Rizner and S. Gobec Affiliation:

Aldo-keto reductases, cancer, drug discovery, enzyme inhibitors, flavonoids, non-steroidal anti-inflammatory drugs, steroids, synergistic, steroidal hormones, prostaglandins

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. Export Options About this article Cite this article as: Brozic 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 | DOI https://dx.doi.org/10.2174/092986711795933713 | 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. 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