Active site inhibitors protect protein kinase C from dephosphorylation and stabilize its mature form.


Conformational changes acutely control protein kinase C (PKC). We have previously shown that the autoinhibitory pseudosubstrate must be removed from the active site in order for 1) PKC to be phosphorylated by its upstream kinase phosphoinositide-dependent kinase 1 (PDK-1), 2) the mature enzyme to bind and phosphorylate substrates, and 3) the mature enzyme… (More)
DOI: 10.1074/jbc.M111.272526


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