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. 1993 Sep 1;294(Pt 2):335–337. doi: 10.1042/bj2940335

Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C.

S E Wilkinson 1, P J Parker 1, J S Nixon 1
PMCID: PMC1134458  PMID: 8373348

Abstract

The protein kinase C (PKC) family of isoenzymes is believed to mediate a wide range of signal-transduction pathways in many different cell types. A series of bisindolylmaleimides have been evaluated as inhibitors of members of the conventional PKC family (PKCs-alpha, -beta, -gamma) and of a representative of the new, Ca(2+)-independent, PKC family, PKC-epsilon. In contrast with the indolocarbazole staurosporine, all the bisindolylmaleimides investigated showed slight selectivity for PKC-alpha over the other isoenzymes examined. In addition, bisindolylmaleimides bearing a conformationally restricted side-chain were less active as inhibitors of PKC-epsilon. Most noticeable of these was Ro 32-0432, which showed a 10-fold selectivity for PKC-alpha and a 4-fold selectivity for PKC-beta I over PKC-epsilon.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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