کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10588673 | 981485 | 2011 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Control of lysyl oxidase activity through site-specific deuteration of lysine
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Lysyl oxidase (LOX) is implicated in several extracellular matrix related disorders, including fibrosis and cancer. Methods of inhibition of LOX in vivo include antibodies, copper sequestration and toxic small molecules such as β-aminopropionitrile. Here, we propose a novel approach to modulation of LOX activity based on the kinetic isotope effect (KIE). We show that 6,6-d2-lysine is oxidised by LOX at substantially lower rate, with apparent deuterium effect on Vmax/Km as high as 4.35 ± 0.22. Lys is an essential nutrient, so dietary ingestion of D2Lys and its incorporation via normal Lys turnover suggests new approaches to mitigating LOX-associated pathologies.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 1, 1 January 2011, Pages 255-258
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 1, 1 January 2011, Pages 255-258
نویسندگان
Nikolay B. Pestov, Irina A. Okkelman, Vadim V. Shmanai, Alaksiej L. Hurski, Amato J. Giaccia, Mikhail S. Shchepinov,