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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Gepubliceerd in:Nat Commun
Hoofdauteurs: 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.
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: Nature Publishing Group 2017
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Article
Online toegang: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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