کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
7797451 1501074 2017 36 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Covalent binding design strategy: A prospective method for discovery of potent targeted anticancer agents
ترجمه فارسی عنوان
استراتژی طراحی اتصال چارچوب: یک روش آینده نگر برای کشف عوامل ضد سرطان هدفمند
کلمات کلیدی
سرطان، کیناز، کووالانتی، طرح، مهار کننده ها،
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی
Cancer remains the most serious disease that threatens human health. Molecularly targeted cancer therapies, specifically small-molecule protein kinase inhibitors, form an important part of cancer therapy. Targeted covalent modification represents a proven approach to drug discovery with the recent FDA approvals of afatanib, ibrutinib, and osimertinib agents, which were designed to undergo an irreversible hetero-Michael addition reaction with a unique cysteine residue of a specific protein. Covalent inhibitors possess numerous advantages, including increased biochemical efficacy, longer duration of action, the high potential for improved therapeutic index due to lower effective dose, and the potential to inhibit certain drug resistance mechanisms. In this regard, the novel targeted anticancer agents whose activity is presumably dependent upon a hetero-Michael addition reaction with thiols are summarized in this article.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 142, 15 December 2017, Pages 493-505
نویسندگان
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