کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10586551 | 981393 | 2010 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Substrate specificity and inhibitory study of human airway trypsin-like protease
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Substrate specificity and inhibitory study of human airway trypsin-like protease Substrate specificity and inhibitory study of human airway trypsin-like protease](/preview/png/10586551.png)
چکیده انگلیسی
Human airway trypsin-like protease (HAT), also referred to as TMPRSS11D, is an important physiological enzyme with the main activity pronounced in an airway. In this work we have described the substrate specificity and selectivity study of the protease, performed by the combinatorial approach. Fluorogenic/chromogenic tetrapeptide library was used for this purpose. The most efficiently hydrolyzed substrates' sequences that we selected were ABZ-Arg-Gln-Asp-Arg(Lys)-ANB-NH2. The most active inhibitor with C-terminal Arg residue underwent detectable proteolysis action in the presence of 35Â pM of HAT. Based on the selected sequences the two peptide aldehydes were synthesized and (Abz-Arg-Gln-Asp-Arg(Lys)-H) were found to be an effective HAT inhibitor, working in nanomolar range with inhibition constant 54Â nM and 112Â nM, respectively.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 15, 1 August 2010, Pages 5504-5509
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 15, 1 August 2010, Pages 5504-5509
نویسندگان
M. Wysocka, B. Spichalska, A. Lesner, M. Jaros, K. Brzozowski, A. ÅÄgowska, K. Rolka,