A synthetic peptide inhibitor of PKA
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PKA inhibitor fragment (6-22) amide is a synthetic peptide inhibitor of cAMP-dependent protein kinase (PKA; Ki = 1.7 nM) derived from the heat-stable PKA inhibitor protein PKI.1 It is the shortest synthetic PKI peptide that retains high potency for PKA inhibition. Both the arginine-containing pseudosubstrate site of the PKI peptide in its COOH terminus and the residue Phe10 in NH2-terminal portion are required for this high affinity binding.2
1.Glass, D.B., Cheng, H.C., Mende-Mueller, L., et al.Primary structural determinants essential for potent inhibition of cAMP-dependent protein kinase by inhibitory peptides corresponding to the active portion of the heat-stable inhibitor proteinJ. Biol. Chem.264(15)8802-8810(1989) 2.Glass, D.B., Lundquist, L.J., Katz, B.M., et al.Protein kinase inhibitor-(6-22)-amide peptide analogs with standard and nonstandard amino acid substitutions for phenylalanine 10. Inhibition of cAMP-dependent protein kinaseJ. Biol. Chem.264(24)14579-14584(1989)