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Literature DB >> 2837190

Effects of a protein kinase C inhibitor, K-252a, on human polymorphonuclear neutrophil responsiveness.

Abstract

We investigated the capacity of K-252a, an inhibitor of rat brain protein kinase C (PKC), to influence polymorphonuclear neutrophil (PMN) PKC and PMN activation with chemically and structurally dissimilar agonists. K-252a inhibited PMN PKC (IC50 = 0.58 microM), and caused a concentration-dependent (0.1-10 microM) inhibition of degranulation elicited with the chemotactic peptide, N-formyl-methionyl-leucyl-phenylalanine (FMLP), the lipid agonists, 5(S), 12(R)-dihydroxy-5,14-cis-8,10-trans eicosatetraenoic acid (LTB4) and acetyl-sn-glyceryl-3-phosphorylcholine (AGEPC), and phorbol 12-myristate 13-acetate. Superoxide anion (O2-) production by PMNs exposed to these stimuli as well as sn-1,2-dioctanoylglycerol (diC8) was also suppressed by K-252a. PMN PKC activity was inhibited with concentrations of K-252a which suppressed PMN responsiveness. Therefore, K-252a appears to be a useful probe for examining the role of PKC in the underlying pathway(s) of PMN activation.

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Year: 1988 PMID： 2837190 DOI： 10.1016/s0006-291x(88)80455-8

Source DB: PubMed Journal: Biochem Biophys Res Commun ISSN： 0006-291X Impact factor: 3.575

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Cited

7 in total

1. An apparently novel protein of human leukocytes, reactive with an antibody to protein kinase C-gamma, is rapidly modified upon cell activation: initial characterization in neutrophils and their cytoplasts.

Authors: J I Smallwood; S E Malawista
Journal: Inflammation Date: 1998-02 Impact factor: 4.092

2. Priming effect of fibronectin on respiratory burst of human neutrophils induced by formyl peptides and platelet-activating factor.

Authors: L Stanislawski; T P Huu; A Perianin
Journal: Inflammation Date: 1990-10 Impact factor: 4.092

3. The effect of putative protein kinase C inhibitors, K252a and staurosporine, on the human neutrophil respiratory burst activated by both receptor stimulation and post-receptor mechanisms.

Authors: B Twomey; R E Muid; M M Dale
Journal: Br J Pharmacol Date: 1990-08 Impact factor: 8.739

4. Modification of hepatic protein kinase C with phorbol myristate acetate and staurosporine alters hemodynamics in the perfused rat liver.

Authors: H Inaba; M Araki; T Numai; T Mizuguchi
Journal: J Anesth Date: 1993-01 Impact factor: 2.078

Effects of a protein kinase C inhibitor, K-252a, on human polymorphonuclear neutrophil responsiveness.

1. An apparently novel protein of human leukocytes, reactive with an antibody to protein kinase C-gamma, is rapidly modified upon cell activation: initial characterization in neutrophils and their cytoplasts.

2. Priming effect of fibronectin on respiratory burst of human neutrophils induced by formyl peptides and platelet-activating factor.

3. The effect of putative protein kinase C inhibitors, K252a and staurosporine, on the human neutrophil respiratory burst activated by both receptor stimulation and post-receptor mechanisms.

4. Modification of hepatic protein kinase C with phorbol myristate acetate and staurosporine alters hemodynamics in the perfused rat liver.

Review 5. Aquaporin-4 water channels and synaptic plasticity in the hippocampus.

6. The antipsoriatic drug, anthralin, inhibits protein kinase C--implications for its mechanism of action.

7. Adhesion-dependent protein tyrosine phosphorylation in neutrophils treated with tumor necrosis factor.