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Inhibitors paradoxically prime kinases

Journal

NATURE CHEMICAL BIOLOGY
Volume 5, Issue 7, Pages 448-449

Publisher

NATURE PUBLISHING GROUP
DOI: 10.1038/nchembio.f.11

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Funding

  1. NIDDK NIH HHS [R01 DK037871] Funding Source: Medline
  2. NIGMS NIH HHS [R01 GM030324, R01 GM068820] Funding Source: Medline

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Small-molecule inhibitors can induce phosphorylation priming of AGC kinases. Priming by ATP binding pocket conformation, rather than intrinsic kinase activity, has significant implications for drug discovery and therapeutic efficacy.

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