Discovery of potent and selective covalent inhibitors of JNK

The mitogen activated kinases JNK1/2/3 are key enzymes in signaling modules that transduce and integrate extracellular stimuli into coordinated cellular response. Here we report the discovery of the first irreversible inhibitors of JNK1/2/3. We describe two JNK3 co-crystal structures at 2.60 and 2.9...

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Bibliografiska uppgifter
Huvudupphovsmän: Zhang, Tinghu, Inesta-Vaquera, Francisco, Niepel, Mario, Zhang, Jianming, Ficarro, Scott B., Machleidt, Thomas, Xie, Ting, Marto, Jarrod A., Kim, NamDoo, Sim, Taebo, Laughlin, John D, Park, Hajeung, LoGrasso, Philip V., Patricelli, Matt, Nomanbhoy, Tyzoon K., Sorger, Peter K., Alessi, Dario R., Gray, Nathanael S.
Materialtyp: Artigo
Språk:Inglês
Publicerad: 2012
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Article
Länkar:https://ncbi.nlm.nih.gov/pmc/articles/PMC3270411/
https://ncbi.nlm.nih.gov/pubmed/22284361
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.chembiol.2011.11.010
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