کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371769 981856 2012 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Peptide-cleaving agents for human islet amyloid polypeptide containing substrate recognition site based on quinoxaline: Cleavage efficiency enhanced by lowering substrate concentration
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Peptide-cleaving agents for human islet amyloid polypeptide containing substrate recognition site based on quinoxaline: Cleavage efficiency enhanced by lowering substrate concentration
چکیده انگلیسی

Oligomers of human islet amyloid polypeptide (h-IAPP) are believed to be the pathogenic species for type 2 diabetes mellitus. Peptide-cleaving agents selective for oligomers of h-IAPP were synthesized by using quinoxaline derivatives as recognition sites attached to the Co(III) complex of cyclen in this study. When the initial concentration of h-IAPP was lowered from 4.0 to 0.20 μM, cleavage yield of the new agents was enhanced by 3 times reaching 16–22 mol %. This shows that the agents would have significant activities at subnano molar concentrations if the concentration of h-IAPP is lowered to the in vivo values. This further indicates that the peptide-cleaving agents prepared previously in this laboratory possess sufficiently high activity for application as a new therapeutic option for Alzheimer’s disease, type 2 diabetes mellitus, and Parkinson’s disease.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 4, 15 February 2012, Pages 1533–1537
نویسندگان
, , ,