کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1378362 | 981999 | 2005 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and evaluation of photolabile insulin prodrugs
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
We have developed two photolabile insulin prodrugs, insulin-2P and insulin-3P. These prodrugs were synthesized by protecting GlyA1 (NαA1), and one or both of the PheB1 (NαB1) and LysB29 (NεB29) amino groups in insulin using 5′-(α-methyl-nitro-piperonyl)oxy-carbonyl as the protecting group. These insulin prodrugs were efficiently activated by exposure to longwave UV light to produce insulin quantitatively. Using 2-deoxyglucose uptake assays, both di- and tri-protected compounds were less active than native insulin in the protected state, and showed comparable activity to native insulin upon photoactivation.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 17, 1 September 2005, Pages 3917–3920
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 17, 1 September 2005, Pages 3917–3920
نویسندگان
Lian-Sheng Li, Jennie L. Babendure, Subhash C. Sinha, Jerrold M. Olefsky, Richard A. Lerner,