Structure-guided optimization of small molecule c-Abl activators

c-Abl kinase is maintained in its normal inactive state in the cell through an assembled, compact conformation. We describe two chemical series that bind to the myristoyl site of the c-Abl kinase domain and stimulate c-Abl activation. We hypothesize that these molecules activate c-Abl either by bloc...

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Main Authors: Hong, Xuan, Cao, Ping, Washio, Yoshiaki, Simpson, Graham, Campobasso, Nino, Yang, Jingsong, Borthwick, Jennifer, Burton, George, Chabanet, Julien, Bertrand, Sophie, Evans, Helen, Young, Robert J., Qu, Junya, Li, Hu, Cottom, Josh, Ward, Paris, Zhang, Hong, Ho, Thau, Qin, Donghui, Christensen, Siegfried, Head, Martha S.
Formato: Artigo
Idioma:Inglês
Publicado: Springer International Publishing 2014
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC3949015/
https://ncbi.nlm.nih.gov/pubmed/24573412
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1007/s10822-014-9731-5
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