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NSAIDs: Old Drugs Reveal New Anticancer Targets

التفاصيل البيبلوغرافية
العنوان: NSAIDs: Old Drugs Reveal New Anticancer Targets
المؤلفون: Gary A. Piazza, Adam B. Keeton, Heather N. Tinsley, Jason D. Whitt, Bernard D. Gary, Bini Mathew, Raj Singh, William E. Grizzle, Robert C. Reynolds
المصدر: Pharmaceuticals, Vol 3, Iss 5, Pp 1652-1667 (2010)
بيانات النشر: MDPI AG, 2010.
سنة النشر: 2010
المجموعة: LCC:Medicine
LCC:Pharmacy and materia medica
مصطلحات موضوعية: NSAIDs, sulindac, cancer, colon, chemoprevention, Medicine, Pharmacy and materia medica, RS1-441
الوصف: There is compelling evidence that nonsteroidal anti-inflammatory drugs (NSAIDs) and cyclooxygenase-2 selective inhibitors have antineoplastic activity, but toxicity from cyclooxygenase (COX) inhibition and the suppression of physiologically important prostaglandins limits their use for cancer chemoprevention. Previous studies as reviewed here suggest that the mechanism for their anticancer properties does not require COX inhibition, but instead involves an off-target effect. In support of this possibility, recent molecular modeling studies have shown that the NSAID sulindac can be chemically modified to selectively design out its COX-1 and COX-2 inhibitory activity. Unexpectedly, certain derivatives that were synthesized based on in silico modeling displayed increased potency to inhibit tumor cell growth. Other experiments have shown that sulindac can inhibit phosphodiesterase to increase intracellular cyclic GMP levels and that this activity is closely associated with its ability to selectively induce apoptosis of tumor cells. Together, these studies suggest that COX-independent mechanisms can be targeted to develop safer and more efficacious drugs for cancer chemoprevention.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 1424-8247
Relation: http://www.mdpi.com/1424-8247/3/5/1652/; https://doaj.org/toc/1424-8247
DOI: 10.3390/ph3051652
URL الوصول: https://doaj.org/article/8f94bf6b294249a785d4a164e17fae0f
رقم الأكسشن: edsdoj.8f94bf6b294249a785d4a164e17fae0f
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:14248247
DOI:10.3390/ph3051652