Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

BKM120 (Buparlisib) is one of the most advanced phosphoinositide 3-kinase (PI3K) inhibitors for the treatment of cancer, but it interferes as an off-target effect with microtubule polymerization. Here, we developed two chemical derivatives that differ from BKM120 by only one atom. We show that these...

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Foilsithe in:Nat Commun
Main Authors: Bohnacker, Thomas, Prota, Andrea E., Beaufils, Florent, Burke, John E., Melone, Anna, Inglis, Alison J., Rageot, Denise, Sele, Alexander M., Cmiljanovic, Vladimir, Cmiljanovic, Natasa, Bargsten, Katja, Aher, Amol, Akhmanova, Anna, Díaz, J. Fernando, Fabbro, Doriano, Zvelebil, Marketa, Williams, Roger L., Steinmetz, Michel O., Wymann, Matthias P.
Formáid: Artigo
Teanga:Inglês
Foilsithe: Nature Publishing Group 2017
Ábhair:
Article
Rochtain Ar Líne:https://ncbi.nlm.nih.gov/pmc/articles/PMC5347140/
https://ncbi.nlm.nih.gov/pubmed/28276440
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/ncomms14683
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