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

KXO1 (tirbanibulin or KX2–391) is as a non-ATP-competitive inhibitor of SRC proto-oncogene nonreceptor tyrosine kinase (SRC) and is being clinically investigated for the management of various cancers and actinic keratosis. Recently, KXO1 has also been shown to strongly inhibit tubulin. Interestingly...

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Detalhes bibliográficos
Publicado no:J Biol Chem
Main Authors: Niu, Lu, Yang, Jianhong, Yan, Wei, Yu, Yamei, Zheng, Yunhua, Ye, Haoyu, Chen, Qiang, Chen, Lijuan
Formato: Artigo
Idioma:Inglês
Publicado em: American Society for Biochemistry and Molecular Biology 2019
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6885616/
https://ncbi.nlm.nih.gov/pubmed/31628188
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1074/jbc.RA119.010732
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