APE/REF-1 as a Drug Target for Acne and Development of Potential APE/REF-1 Inhibitors for Prevention and Therapy of Acne Vulgarsis
Background: Acne vulgarisis the most common skin disorder, and while it usually appears in adolescence, adults can get it too. The pathogenesis of acne is complex and multifactorial. According to the American Academy of Dermatology, the four basic mechanisms contributing to acne are hormones, increased sebum production, changes inside hair follicles, and bacteria. Acne occurs when hair follicles and the sebaceous glands inside the follicles are inflamed. Sebaceous glands make an oily substance called sebum. Too much sebum can clog the follicles and then bacteria contaminate the skin cell and sebum mixture and grow, leading to inflammation.
Several compounds are used for acne, either in topical or systemic form, including different topical retinoids, tretinoin (all-trans-retinoic acid), isotretinoin (1 3-cis-retinoic acid), adapalene (derived from naphthoic acid), and tazarotene (acetylenic retinoid). They act mainly as comedolytics, but anti-inflammatory actions have also been discovered recently. The retinoids have great beneficial effects, but also some adverse effects, the main one being teratogenicity. Novel and safer anti-acne compounds are extremely needed. Technology: Virtual screen can be used to sample the entire virtual chemical marketplace of drug-like molecules, thereby eliminating the tasks of synthesizing and experimentally testing every molecule. VS has been shown to be as efficient as experimental high-throughput screening (HTS) in hit identification, while much faster and less expensive. Moreover, a virtual experiment can be easily designed to preselect for a particular binding site or receptor. Compared to HTS and ligand-based screening, receptor-based VS by fast ligand docking has the additional benefit of providing details of binding mode to facilitate rational lead optimization. VS enables diverse compounds to be identified which would never have been identified or tested in a traditional laboratory high-throughput screen. Therefore, new classes of binders can be identified. Application: Novel and safer anti-acne compounds
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