A conserved protonation-dependent switch controls drug binding in the Abl kinase

In many protein kinases, a characteristic conformational change (the “DFG flip”) connects catalytically active and inactive conformations. Many kinase inhibitors—including the cancer drug imatinib—selectively target a specific DFG conformation, but the function and mechanism of the flip remain uncle...

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Bibliographic Details
Main Authors: Shan, Yibing, Seeliger, Markus A., Eastwood, Michael P., Frank, Filipp, Xu, Huafeng, Jensen, Morten Ø, Dror, Ron O., Kuriyan, John, Shaw, David E.
Format: Artigo
Language:Inglês
Published: National Academy of Sciences 2009
Subjects:
Biological Sciences
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC2610013/
https://ncbi.nlm.nih.gov/pubmed/19109437
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1073/pnas.0811223106
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