کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1986256 1540243 2015 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Role of 13-(di)phenylalkyl berberine derivatives in the modulation of the activity of human topoisomerase IB
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی زیست شیمی
پیش نمایش صفحه اول مقاله
Role of 13-(di)phenylalkyl berberine derivatives in the modulation of the activity of human topoisomerase IB
چکیده انگلیسی

Topoisomerases IB are anticancer and antimicrobial targets whose inhibition by several natural and non-natural compounds has been documented. The inhibition effect by berberine and some 13-(di)phenylalkyl berberine derivatives has been tested towards human topoisomerase IB. Derivatives belonging to the 13-diphenylalkyl series display an efficient inhibition of the DNA relaxation and cleavage step, that increases upon pre-incubation with the enzyme. The religation step of the enzyme catalytic cycle is not affected by compounds and only slightly upon pre-incubation. The binding of the protein to the DNA substrate occurs also in the presence of the compounds, as monitored by a DNA shift assay, indicating that the compounds are not able to inhibit the formation of the enzyme–DNA complex but that they act as catalytic inhibitors.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Biological Macromolecules - Volume 77, June 2015, Pages 68–75
نویسندگان
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