Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:2.7.11.13 (
protein kinase C
)
49,245
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Retroviral infection
is associated with immunosuppression, which has been shown to be due, in part, to the action of the envelope protein p15E. We studied a synthetic peptide (CKS-17) homologous to a highly conserved domain of the retroviral envelope protein p15E, which, when conjugated to BSA (CKS-17-BSA), can inhibit IL-1- and phorbol ester-mediated responses in cultured murine thymoma cells, and Ca2(+)- and phosphatidylserine-dependent
protein kinase C
(
PKC
) activity of cell homogenates. We characterized the mechanism of inhibition of
PKC
by the peptide. Using
PKC
purified from rat brain we found that CKS-17-BSA inhibited
PKC
-catalyzed Ca2(+)- and phosphatidylserine-dependent histone phosphorylation with an estimated ID50 of 4 microM. CKS-17-BSA did not inhibit the catalytic subunit of cAMP-dependent protein kinase. CKS-17-BSA also inhibited the Ca2(+)- and PS-independent activity of a catalytic fragment of
PKC
that was generated by limited trypsin treatment. However, CKS-17-BSA did not act as a competitive inhibitor of
PKC
with respect to ATP or phosphoacceptor substrate, despite the similarity between the CKS-17 sequence and substrates and pseudosubstrates of
PKC
. We conclude that this peptide homologue of a retroviral envelope protein has a novel mechanism of inhibition of
PKC
.
...
PMID:Inhibition of protein kinase C by a peptide conjugate homologous to a domain of the retroviral protein p15E. 221 53
