کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1360785 981448 2009 16 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Current perspective of TACE inhibitors: A review
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Current perspective of TACE inhibitors: A review
چکیده انگلیسی

Rheumatoid Arthritis (RA) is one of the most common autoimmune inflammatory conditions, affecting approximately 1% of the adult population worldwide. TNF-α is a pleitropic, pro-inflammatory cytokine which plays a pivotal role in the origin and progression of RA and other immune mediated disorders. The success of anti-TNF-α biological agents proved that inhibition of TNF-α could result in effective control of RA. Since the discovery of anti-TNF-α biologicals, much efforts have gone into developing an orally bioavailable small size TNF-α antagonist. One of the ways to block TNF-α in biological fluids is to inhibit TNF-α converting enzyme (TACE). This target has been validated in preclinical trials using TACE inhibitors. But, even after more than a decade no single TACE inhibitor has passed the Phase II clinical trials. Very recently, it has been shown that TACE inhibitors could also be used for inhibition of pathogenic EGFR signaling in cancer. Hence, TACE inhibitors could perform a dual role, in curing not only RA but also certain cancerous conditions. Developments in the field have prompted us to review the research work on TACE inhibitors, especially their structure activity relationships and molecular modeling studies.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 2, 15 January 2009, Pages 444–459
نویسندگان
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