Literature DB >> 8365480

Staurosporine-related compounds, K252a and UCN-01, inhibit both cPKC and nPKC.

K Mizuno1, T C Saido, S Ohno, T Tamaoki, K Suzuki.   

Abstract

The potent inhibitors of protein kinase C (PKC), H7, staurosporine, and staurosporine derivatives, were examined for their inhibitory effects on novel PKC (nPKC) isozymes delta and epsilon. H7 and staurosporine, usually used as selective inhibitors of PKC, showed similar inhibitory effects on cPKC (a mixture of cPKC alpha, beta, and gamma) and nPKC delta and epsilon. The inhibitory effects of K252a, a non-selective protein kinase inhibitor, on cPKC was 3.2- and 22-fold higher than those on nPKC epsilon and delta, respectively. The staurosporine derivatives UCN-01 and UCN-01-Me also showed selective inhibition of cPKC.

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Year:  1993        PMID: 8365480     DOI: 10.1016/0014-5793(93)80254-r

Source DB:  PubMed          Journal:  FEBS Lett        ISSN: 0014-5793            Impact factor:   4.124


  7 in total

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6.  Abrogation of the radiation-induced G2 checkpoint by the staurosporine derivative UCN-01 is associated with radiosensitisation in a subset of colorectal tumour cell lines.

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  7 in total

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