Synthesis of a substrate of protein kinase C and its corresponding phosphopeptide.
The syntheses of a protein kinase C (PKC) peptide substrate, H-Lys-Arg-Thr-Leu-Arg-OH, and a phosphopeptide analog of the synthetic substrate, H-Lys-Arg-Thr(P)-Leu-Arg-OH, are reported. PKC phosphorylates the peptide with an apparent KM of 0.30 +/- 0.04 mM and an apparent Vmax equal to one-tenth that of histone III-S. The synthesis of the phosphopeptide features a recently developed convenient phosphorylation procedure for serine and threonine using N,N-diethylamino-dibenzylphosphoramidite. A complete characterization of the PKC substrate and its corresponding phosphopeptide by C-H COSY 2D n.m.r. is included.
de Bont
H B
HB
Dept. of Organic Chemistry, Gorlaeus Laboratories, University of Leiden, The Netherlands.
Liskamp
R M
RM
O'Brian
C A
CA
Erkelens
C
C
Veeneman
G H
GH
van Boom
J H
JH
D055598:Chemical Phenomena; D002621:Chemistry; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D010748:Phosphopeptides / Q000138:chemical synthesis; D011493:Protein Kinase C; D013379:Substrate Specificity
D010748:Phosphopeptides; D011493:Protein Kinase C