کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10587604 981431 2013 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Calix[4]arene methylenebisphosphonic acids as inhibitors of protein tyrosine phosphatase 1B
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Calix[4]arene methylenebisphosphonic acids as inhibitors of protein tyrosine phosphatase 1B
چکیده انگلیسی
Сalix[4]arenes bearing methylenebisphosphonic or hydroxymethylenebisphosphonic acid fragments at the wide rim of the macrocycle were studied as inhibitors of PTP1B. Some of the inhibitors showed IC50 values in the micromolar range and good selectivity in comparison with other protein tyrosine phosphatases such as TC-PTP, PTPβ, LAR, and CD45. Kinetic studies indicated that the calix[4]arene derivatives influence PTP1B activity as slow-binding inhibitors. Based on molecular docking results, the binding modes of the macrocyclic bisphosphonates in the active centre of PTP1B are discussed.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 20, 15 October 2013, Pages 5619-5623
نویسندگان
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