Article

Dynamics of human protein kinases linked to drug selectivity

2018-03-21

Abstract excerpt

Protein kinases are major drug targets, but the development of highly-selective inhibitors has been challenging due to the similarity of their active sites. The observation of distinct structural states of the fully-conserved Asp-Phe-Gly (DFG) loop has put the concept of conformational selection for the DFG-state at the center of kinase drug discovery. Recently, it was shown that Gleevec selectivity for the Tyr-ki...

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Literature Corpus work: 647b113d-f98b-5674-8808-62964da384fb
DOI: 10.1101/286310

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