Biochemistry

Two photoaffinity analogues of the tripeptide, hemiasterlin, exclusively label α-tubulin

…, Y Qiu, F Loganzo, S Ayral-Kaloustian, A Zask…

文献索引：Yamashita, Ayako; Norton, Emily B.; Kaplan, Joshua A.; Niu, Chuan; Loganzo, Frank; Hernandez, Richard; Beyer, Carl F.; Annable, Tami; Musto, Sylvia; Discafani, Carolyn; Zask, Arie; Ayral-Kaloustian, Semiramis Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 21 p. 5317 - 5322

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被引用次数: 28

摘要

A synthetic analogue of the tripeptide hemiasterlin, designated HTI-286, depolymerizes microtubules, is a poor substrate for P-glycoprotein, and inhibits the growth of paclitaxel- resistant tumors in xenograft models. Two radiolabeled photoaffinity analogues of HTI-286, designated 4-benzoyl-N, β, β-trimethyl-l-phenylalanyl-N 1-[(1 S, 2 E)-3-carboxy-1- isopropylbut-2-enyl]-N 1, 3-dimethyl-l-valinamide (probe 1) and N, β, β-trimethyl-l- ...