Reversible binding of the anticancer drug KXO1 (tirbanibulin) to the colchicine-binding site of ß-tubulin explains KXO1's low clinical toxicity.

Niu, Lu; Yang, Jianhong; Yan, Wei; Yu, Yamei; Zheng, Yunhua; Ye, Haoyu; Chen, Qiang; Chen, Lijuan

Niu, Lu; Yang, Jianhong; Yan, Wei; Yu, Yamei; Zheng, Yunhua; Ye, Haoyu; Chen, Qiang; Chen, Lijuan.

Afiliação

Niu L; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital of Sichuan University and Collaborative Innovation Center of Biotherapy and Cancer, Chengdu 610041, China.
Yang J; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital of Sichuan University and Collaborative Innovation Center of Biotherapy and Cancer, Chengdu 610041, China.
Yan W; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital of Sichuan University and Collaborative Innovation Center of Biotherapy and Cancer, Chengdu 610041, China.
Yu Y; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital of Sichuan University and Collaborative Innovation Center of Biotherapy and Cancer, Chengdu 610041, China.
Zheng Y; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital of Sichuan University and Collaborative Innovation Center of Biotherapy and Cancer, Chengdu 610041, China.
Ye H; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital of Sichuan University and Collaborative Innovation Center of Biotherapy and Cancer, Chengdu 610041, China.
Chen Q; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital of Sichuan University and Collaborative Innovation Center of Biotherapy and Cancer, Chengdu 610041, China; Innovative Institute of Chinese Medicine and Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 6117
Chen L; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital of Sichuan University and Collaborative Innovation Center of Biotherapy and Cancer, Chengdu 610041, China. Electronic address: qiang_chen@scu.edu.cn.

J Biol Chem ; 294(48): 18099-18108, 2019 11 29.

Article em En | MEDLINE | ID: mdl-31628188

Assuntos

Antineoplásicos/química; Colchicina/química; Proteínas de Neoplasias/química; Tubulina (Proteína)/química; Antineoplásicos/farmacologia; Sítios de Ligação; Divisão Celular/efeitos dos fármacos; Colchicina/toxicidade; Cristalografia por Raios X; Fase G2/efeitos dos fármacos; Células HeLa; Humanos; Proteínas de Neoplasias/metabolismo; Ligação Proteica; Proto-Oncogene Mas; Tubulina (Proteína)/metabolismo

Palavras-chave

anticancer drug; drug discovery; microtubule; mitosis; tubulin; tumor therapy

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Tubulina (Proteína) / Colchicina / Proteínas de Neoplasias / Antineoplásicos Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article

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