کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
190126 459692 2011 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Electrochemical investigations of sarcoma-related protein kinase inhibition
موضوعات مرتبط
مهندسی و علوم پایه مهندسی شیمی مهندسی شیمی (عمومی)
پیش نمایش صفحه اول مقاله
Electrochemical investigations of sarcoma-related protein kinase inhibition
چکیده انگلیسی

An electrochemical biosensor was developed for the determination of sarcoma (Src)-related protein kinase-catalyzed phosphorylation reactions in the presence of adenosine 5′-γ-ferrocenoyl triphosphate (Fc-ATP). The sensing platform is based on a highly specific amino acid sequence Glu-Gly-Ile-Tyr-Asp-Val-Pro (EGIYDVP), to which a Fc-PO2 moiety can be transferred from Fc-ATP by the action of the Src kinase. The enzyme kinetics and kinase inhibition were investigated by square wave voltammetry (SWV). The kinetic parameters Km and Vmax were determined for Src protein kinase with respect to Fc-ATP co-substrate and were found to be 200 μM and 115 μA cm−2 min, for phosphorylation of the EGIYDVP peptide substrate. Furthermore, the Src-catalyzed phosphorylation of Tyr was investigated in the presence of the small molecule inhibitors PP1, PP2, SU6656, and roscovitine. PP3 does not inhibit Src activity and was used as a control. The percent inhibition at half concentration, IC50, values were determined for all inhibitors under the study and were estimated to be in the 5–30 nM range. The electrochemical study suggests that the increase in inhibition efficiency was in the order PP3 < SU6656 < roscovitine < PP2 < PP1.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Electrochimica Acta - Volume 56, Issue 28, 1 December 2011, Pages 10676–10682
نویسندگان
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