کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10748715 1050278 2016 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Pyrithione Zn selectively inhibits hypoxia-inducible factor prolyl hydroxylase PHD3
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی زیست شیمی
پیش نمایش صفحه اول مقاله
Pyrithione Zn selectively inhibits hypoxia-inducible factor prolyl hydroxylase PHD3
چکیده انگلیسی
Increasing evidence emphasizes the role of the hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) isoforms in regulating non-HIF substrates, but isoform selective PHD inhibitors under physiological conditions have not yet been reported. Here we have identified pyrithione Zn (PZ) as a potent, isoform-selective PHD3 inhibitor. The IC50 value of PZ was determined as 0.98 μM for PHD3, while it did not show any inhibitory activity toward full length and truncated PHD2 up to 1 mM. The selective efficacy of PZ was further demonstrated at the cellular level by observing inhibition of the PHD3-dependent DNA damage response pathway without stabilization of HIF-1α.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical and Biophysical Research Communications - Volume 472, Issue 2, 1 April 2016, Pages 313-318
نویسندگان
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