کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10582782 | 981101 | 2011 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Tubulin photoaffinity labeling study with a plinabulin chemical probe possessing a biotin tag at the oxazole
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Tubulin photoaffinity labeling study with a plinabulin chemical probe possessing a biotin tag at the oxazole Tubulin photoaffinity labeling study with a plinabulin chemical probe possessing a biotin tag at the oxazole](/preview/png/10582782.png)
چکیده انگلیسی
A new bioactive photoaffinity probe KPU-252-B1 (4) possessing a biotin tag on the oxazole ring of a potent plinabulin derivative KPU-244 (2) was synthesized via the CuI-catalyzed Huisgen's cycloaddition reaction to understand the precise binding mode of the diketopiperazine-based anti-microtubule agent plinabulin on tubulin. Probe 4 showed significant binding affinity toward tubulin and cytotoxicity against an HT-29 cells. A photoaffinity labeling study suggested that probe 4 specifically recognizes tubulin at a binding site that binds plinabulin or colchicine, most likely near or at the colchicine binding site, which is located at the interfacial region formed by α-and β-tubulin association. The results also demonstrated that probe 4 may serve as a useful plinabulin chemical probe to investigate the molecular mechanism by which anti-microtubule diketopiperazine derivatives operate.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 1, 1 January 2011, Pages 595-602
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 1, 1 January 2011, Pages 595-602
نویسندگان
Yuri Yamazaki, Yui Kido, Koushi Hidaka, Hiroyuki Yasui, Yoshiaki Kiso, Fumika Yakushiji, Yoshio Hayashi,