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Staurosporine‐related compounds, K252a and UCN‐01, inhibit both cPKC and nPKC
Author(s) -
Mizuno Keiko,
Saido Takaomi C.,
Ohno Shigeo,
Tamaoki Tatsuya,
Suzuki Koichi
Publication year - 1993
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(93)80254-r
Subject(s) - staurosporine , protein kinase c , inhibitory postsynaptic potential , chemistry , alpha (finance) , pharmacology , protein kinase a , isozyme , enzyme , biochemistry , biology , medicine , endocrinology , construct validity , nursing , patient satisfaction
The potent inhibitors of protein kinase C (PKC), H7, staurosporine, and staurosporine derivatives, were examined for their inhibitory effects on novel PKC (nPKC) isozymes δ and ε. H7 and staurosporine, usually used as selective inhibitors of PKC, showed similar inhibitory effects on cPKC (a mixture of cPKCα,β, and γ) and nPKCδ and ε. The inhibitory effects of K252a, a non‐selective protein kinase inhibitor, on cPKC was 3.2‐ and 22‐fold higher than those on nPKCε and δ, respectively. The staurosporine derivatives UCN‐01 and UCN‐01‐Me also showed selective inhibition of cPKC.