Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase
- PMID: 3457562
- DOI: 10.1016/0006-291x(86)90008-2
Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase
Abstract
Staurosporine, microbial alkaloid which has been known to have antifungal activity was found to inhibit markedly phospholipid/Ca++dependent protein kinase (protein kinase C) from rat brain, with an IC50 value of 2.7 nM. However, it had little effect on the binding of 3H-phorbol-12, 13-dibutyrate (PDBu) to protein kinase C. The inhibition of protein kinase C was not competitive with phospholipid. This compound also showed the strong cytotoxic effect on the growth of HeLa S3 cells, with an IC50 value of 4 X 10(-12)M under the condition of 72 hr-exposure.
Similar articles
-
A protein kinase inhibitor, staurosporine, enhances the expression of phorbol dibutyrate binding sites in human polymorphonuclear leucocytes.Biochem J. 1993 Feb 1;289 ( Pt 3)(Pt 3):695-701. doi: 10.1042/bj2890695. Biochem J. 1993. PMID: 8435068 Free PMC article.
-
Staurosporine up-regulates the expression of phorbol dibutyrate binding sites in human platelets.Biochem Pharmacol. 1994 May 18;47(10):1797-804. doi: 10.1016/0006-2952(94)90308-5. Biochem Pharmacol. 1994. PMID: 8204096
-
Tumor-promoting phorbol esters stimulate bovine cerebral cortex capillary endothelial cell growth in vitro.Biochem Biophys Res Commun. 1989 Jan 31;158(2):584-9. doi: 10.1016/s0006-291x(89)80089-0. Biochem Biophys Res Commun. 1989. PMID: 2917003
-
Protein kinase C translocation in rat stomach fundus: effects of serotonin, carbamylcholine and phorbol dibutyrate.J Pharmacol Exp Ther. 1991 Jan;256(1):103-9. J Pharmacol Exp Ther. 1991. PMID: 1988650
-
Specific binding of phorbol ester tumor promoters to mouse tissues and cultured cells.Carcinog Compr Surv. 1982;7:519-35. Carcinog Compr Surv. 1982. PMID: 7039833 Review.
Cited by
-
Caspase-3 Activation Correlates With the Initial Mitochondrial Membrane Depolarization in Neonatal Cerebellar Granule Neurons.Front Cell Dev Biol. 2020 Jul 2;8:544. doi: 10.3389/fcell.2020.00544. eCollection 2020. Front Cell Dev Biol. 2020. PMID: 32714930 Free PMC article.
-
The calcium channel agonist Bay K 8644 promotes the growth of human liver cancer HepG2 cells in vitro: suppression with overexpressed regucalcin.Mol Cell Biochem. 2020 Sep;472(1-2):173-185. doi: 10.1007/s11010-020-03795-7. Epub 2020 Jun 26. Mol Cell Biochem. 2020. PMID: 32591915
-
Properties of 5-hydroxytryptamine3 receptor-gated currents in adult rat dorsal root ganglion neurones.Br J Pharmacol. 1991 Jan;102(1):272-6. doi: 10.1111/j.1476-5381.1991.tb12165.x. Br J Pharmacol. 1991. PMID: 2043929 Free PMC article.
-
Towards selective pharmacological modulation of protein kinase C--opportunities for the development of novel antineoplastic agents.Br J Cancer. 1992 Jul;66(1):10-9. doi: 10.1038/bjc.1992.209. Br J Cancer. 1992. PMID: 1637658 Free PMC article. Review. No abstract available.
-
Modulation of 1,25-dihydroxyvitamin D3-dependent Ca2+ uptake in skeletal muscle by protein kinase C.Biochem J. 1992 Jan 15;281 ( Pt 2)(Pt 2):349-52. doi: 10.1042/bj2810349. Biochem J. 1992. PMID: 1310592 Free PMC article.
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources