Pironetin reacts covalently with cysteine-316 of α-tubulin to destabilize microtubule

Microtubule assembly and disassembly is the target of many anticancer therapies, with β-tubulin the most-frequent target. Here, the authors used biochemical and biophysical techniques to demonstrate pironetin binds to α-tubulin and thereby inhibits microtubule polymerization providing a basis for th...

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Bibliographic Details
Main Authors: Jianhong Yang, Yuxi Wang, Taijing Wang, Jian Jiang, Catherine H. Botting, Huanting Liu, Qiang Chen, Jinliang Yang, James H. Naismith, Xiaofeng Zhu, Lijuan Chen
Format: article
Language:EN
Published: Nature Portfolio 2016
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Online Access:https://doaj.org/article/706d09f37b2b4e7daab3ae36d7438e61
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Summary:Microtubule assembly and disassembly is the target of many anticancer therapies, with β-tubulin the most-frequent target. Here, the authors used biochemical and biophysical techniques to demonstrate pironetin binds to α-tubulin and thereby inhibits microtubule polymerization providing a basis for the rational design of novel anticancer drugs.