Inhibition of PKC and PKA by chemopreventive organoselenium compounds

P. G. Foiles, H. Fujiki, M. Suganuma, S. Okabe, J. Yatsunami, L. M. Miglietta, P. Upadhyaya, K. El-Bayoumy, Z. Ronai

Research output: Contribution to journalArticlepeer-review

26 Scopus citations


Numerous efficacy studies in rodents revealed that 1,4-phenylenebis(methylene)-selenocyanate (p-XSC) is a more effective chemopreventive organoselenium compound and less toxic than benzyl selenocyanate (BSC) or the inorganic compound Na2SeO3. To explore mechanisms which mediate chemopreventive activities of p-XSC we have tested its effect on protein kinase A and C using in vitro and cell culture systems. While p-XSC did completely inhibit and PKA activity, BSC was less active and Na2SeO3 had no effect. Comparative EC50 revealed values of 0.1, 1 and >10 μM for p-XSC, BSC and Na2SeO3, respectively. p-XSC was also capable of inhibiting protein phosphorylation in cultures of primary human fibroblasts and altered morphology of rat fibroblast (R6) cells. When combined, sub-optimal doses of p-XSC and staurosporine yielded an additive effect on cell morphology. The ability of p-XSC and BSC to inhibit protein kinase A and C activities may in part account for the mechanism(s) by which these agents mediate their chemopreventive effects.

Original languageEnglish (US)
Pages (from-to)685-690
Number of pages6
JournalInternational journal of oncology
Issue number3
StatePublished - 1995

All Science Journal Classification (ASJC) codes

  • Oncology
  • Cancer Research


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