Cevipabulin-tubulin complex reveals a novel agent binding site on α-tubulin with tubulin degradation effect

• Published in: bioRxiv
• Main Authors: Yang, Jianhong, Yu, Yamei, Li, Yong, Yan, Wei, Ye, Haoyu, Niu, Lu, Tang, Minghai, Wang, Zhoufeng, Zhuang, Yang, Heying Pei, Haoche Wei, Zhao, Min, Wen, Jiaolin, Yang, Linyu, Ouyang, Liang, Wei, Yuquan, Chen, Qiang, Li, Weimin, Chen, Lijuan
• Format: Paper
• Language: English
• Published: Cold Spring Harbor Cold Spring Harbor Laboratory Press 17.01.2021
• Subjects: Binding sites; Crystallography; Degradation; Drug delivery; Drug development; Guanosine triphosphate; Tubulin; Vinblastine; X-ray crystallography

Abstract Microtubule, composed of αβ-tubulin heterodimers, remains as one of the most popular anticancer targets for decades. To date, anti-microtubule drugs are mainly functionally divided into microtubule-destabilizing and microtubule-stabilizing agents while microtubule- or tubulin-degradation ag...