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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
1990-12-28
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pubmed:abstractText |
The benzophenanthridine alkaloid chelerythrine is a potent, selective antagonist of the Ca++/phospholopid-dependent protein kinase (Protein kinase C: PKC) from the rat brain. Half-maximal inhibition of the kinase occurs at 0.66 microM. Chelerythrine interacted with the catalytic domain of PKC, was a competitive inhibitor with respect to the phosphate acceptor (histone IIIS) (Ki = 0.7 microM) and a non-competitive inhibitor with respect to ATP. This effect was further evidenced by the fact that chelerythrine inhibited native PKC and its catalytic fragment identically and did not affect [3H]- phorbol 12,13 dibutyrate binding to PKC. Chelerythrine selectively inhibited PKC compared to tyrosine protein kinase, cAMP-dependent protein kinase and calcium/calmodulin-dependent protein kinase. The potent antitumoral activity of celerythrine measured in vitro might be due at least in part to inhibition of PKC and thus suggests that PKC may be a model for rational design of antitumor drugs.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/1-(5-Isoquinolinesulfonyl)-2-Methylp...,
http://linkedlifedata.com/resource/pubmed/chemical/Alkaloids,
http://linkedlifedata.com/resource/pubmed/chemical/Antibiotics, Antineoplastic,
http://linkedlifedata.com/resource/pubmed/chemical/Benzophenanthridines,
http://linkedlifedata.com/resource/pubmed/chemical/Isoquinolines,
http://linkedlifedata.com/resource/pubmed/chemical/Phenanthridines,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase C,
http://linkedlifedata.com/resource/pubmed/chemical/Staurosporine,
http://linkedlifedata.com/resource/pubmed/chemical/chelerythrine
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0006-291X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
172
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
993-9
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:2244923-1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine,
pubmed-meshheading:2244923-Alkaloids,
pubmed-meshheading:2244923-Animals,
pubmed-meshheading:2244923-Antibiotics, Antineoplastic,
pubmed-meshheading:2244923-Benzophenanthridines,
pubmed-meshheading:2244923-Binding, Competitive,
pubmed-meshheading:2244923-Brain,
pubmed-meshheading:2244923-Cell Transformation, Neoplastic,
pubmed-meshheading:2244923-Isoquinolines,
pubmed-meshheading:2244923-Kinetics,
pubmed-meshheading:2244923-Leukemia L1210,
pubmed-meshheading:2244923-Lymphoma,
pubmed-meshheading:2244923-Phenanthridines,
pubmed-meshheading:2244923-Piperazines,
pubmed-meshheading:2244923-Protein Kinase C,
pubmed-meshheading:2244923-Rats,
pubmed-meshheading:2244923-Staurosporine,
pubmed-meshheading:2244923-Tumor Cells, Cultured
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pubmed:year |
1990
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pubmed:articleTitle |
Chelerythrine is a potent and specific inhibitor of protein kinase C.
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pubmed:affiliation |
Sanofi Recherche, Toulouse, France.
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pubmed:publicationType |
Journal Article
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