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Synthetic myelin basic protein peptide analogs are specific inhibitors of phospholipid/calcium-dependent protein kinase (protein kinase C).
- Source :
-
Biochemical and biophysical research communications [Biochem Biophys Res Commun] 1986 Jan 14; Vol. 134 (1), pp. 78-84. - Publication Year :
- 1986
-
Abstract
- Synthetic peptide analogs of the bovine myelin basic protein (MBP) corresponding to residues 104-118 were found to specifically inhibit phospholipid/ Ca2+-dependent protein kinase (protein kinase C). The peptides [Ala107]MBP (104-118) and [Ala113]MBP (104-118) inhibited protein phosphorylation of intact MBP, histone H1 and peptide phosphorylation with MBP(104-123), MBP(104-118) or [Ala105]MBP (104-118) as substrates. The inhibitor peptides [Ala107]MBP(104-118) and [Ala113]MBP (104-118), containing alanine in place of the arginine recognition sites, apparently inhibited the enzyme noncompetitively with respect to substrates, with IC50 values ranging from 46-145 and 28-62 microM, respectively. These peptide analogs did not inhibit cyclic AMP-dependent protein kinase or myosin light chain kinase but inhibited phospholipid/Ca2+-dependent phosphorylation of endogenous proteins in the total, solubilized fraction of rat brain.
- Subjects :
- Amino Acid Sequence
Animals
Brain enzymology
Cattle
Kinetics
Myelin Basic Protein pharmacology
Myosin-Light-Chain Kinase
Peptide Fragments chemical synthesis
Peptide Fragments pharmacology
Protein Kinase Inhibitors
Rats
Myelin Basic Protein chemical synthesis
Protein Kinase C antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 0006-291X
- Volume :
- 134
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Biochemical and biophysical research communications
- Publication Type :
- Academic Journal
- Accession number :
- 2418828
- Full Text :
- https://doi.org/10.1016/0006-291x(86)90529-2