Inhibitory properties of the regulatory domains of human protein kinase Calpha and mouse protein kinase Cepsilon.

The Journal of Biological Chemistry
A M ParissentiB P Schimmer

Abstract

Two fusion proteins in which the regulatory domains of human protein kinase Calpha (Ralpha; amino acids 1-270) or mouse protein kinase Cepsilon (Repsilon; amino acids 1-385) were linked in frame with glutathione S-transferase (GST) were examined for their abilities to inhibit the catalytic activities of protein kinase Calpha (PKCalpha) and other protein kinases in vitro. Both GST-Ralpha and GST-Repsilon but not GST itself potently inhibited the activities of lipid-activated rat brain PKCalpha. In contrast, the fusion proteins had little or no inhibitory effect on the activities of the Ser/Thr protein kinases cAMP-dependent protein kinase, cGMP-dependent protein kinase, casein kinase II, myosin light chain kinase, and mitogen activated protein kinase or on the src Tyr kinase. GST-Ralpha and GST-Repsilon, on a molar basis, were 100-200-fold more potent inhibitors of PKCalpha activity than was the pseudosubstrate peptide PKC19-36. In addition, a GST-Ralpha fusion protein in which the first 32 amino acids of Ralpha were deleted (including the pseudosubstrate sequence from amino acids 19-31) was an effective competitive inhibitor of PKCalpha activity. The three GST-R fusion proteins also inhibited protamine-activated PKCalpha and pr...Continue Reading

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Citations

Jul 31, 2007·Journal of Cancer Research and Clinical Oncology·D BreitkreutzT Tennenbaum
Dec 4, 2003·Journal of Experimental Therapeutics & Oncology·Jae-Won SohI Bernard Weinstein
Feb 19, 2002·The Journal of Biological Chemistry·Simon J SlaterChristopher D Stubbs
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Feb 17, 2018·Biochemical Pharmacology·Zhongwei Liu, Raouf A Khalil

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