کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1180487 962855 2008 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Development of novel peptide inhibitor of Lipoxygenase based on biochemical and BIAcore evidences
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آنالیزی یا شیمی تجزیه
پیش نمایش صفحه اول مقاله
Development of novel peptide inhibitor of Lipoxygenase based on biochemical and BIAcore evidences
چکیده انگلیسی

Lipoxygenase (LOX) are enzymes implicated in a broad range of inflammatory diseases, cancer, asthma and atherosclerosis. These diverse biological properties lead to the interesting target for the inhibition of this metabolic pathway of LOX. The drugs available in the market against LOX reported to have various side effects. To develop potent and selective therapeutic agents against LOX, it is essential to have the knowledge of its active site. Due to the lack of structural data of human LOX, researchers are using soybean LOX (sLOX) because of their availability and similarities in the active site structure. Based on the crystal structure of sLOX-3 and its complex with known inhibitors, we have designed a tripeptide, FWY which strongly inhibits sLOX-3 activity. The inhibition by peptide has been tested with purified sLOX-3 and with LOX present in blood serum of breast cancer patients in the presence of substrate linoleic acid and arachidonic acid respectively. The dissociation constant (KD) of the peptide with sLOX-3 as determined by Surface Plasmon Resonance (SPR) was 3.59 × 10− 9 M. The kinetic constant (Ki) and IC50, as determined biochemical methods were 7.41 × 10− 8 M and 0.15 × 10− 6 M respectively.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics - Volume 1784, Issue 11, November 2008, Pages 1812–1817
نویسندگان
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