کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358477 | 981345 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Arylstibonic acids are potent and isoform-selective inhibitors of Cdc25a and Cdc25b phosphatases
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Arylstibonates structurally resemble phosphotyrosine side chains in proteins and here we addressed the ability of such compounds to act as inhibitors of a panel of mammalian tyrosine and dual-specificity phosphatases. Two arylstibonates both possessing a carboxylate side chain were identified as potent inhibitors of the protein tyrosine phosphatase PTP-ß. In addition, they inhibited the dual-specificity, cell cycle regulatory phosphatases Cdc25a and Cdc25b with sub-micromolar potency. However, the Cdc25c phosphatase was not affected demonstrating that arylstibonates may be viable leads from which to develop isoform specific Cdc25 inhibitors.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 14, 15 July 2012, Pages 4371–4376
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 14, 15 July 2012, Pages 4371–4376
نویسندگان
Lok Hang Mak, Jessica Knott, Katherine A. Scott, Claire Scott, Gillian F. Whyte, Yu Ye, David J. Mann, Oscar Ces, James Stivers, Rudiger Woscholski,