rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
1999-8-19
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pubmed:abstractText |
Balanol is a potent inhibitor of cyclic AMP-dependent protein kinase and protein kinase C, acting competitively with ATP with an affinity 3000 times that of ATP. We tested the capacity of balanol to inhibit representative serine- and threonine-specific protein kinases from the protein kinase subfamily that shares a common conserved catalytic core with cyclic AMP-dependent protein kinase. Balanol's pattern of interactions indicates considerable diversity of the ATP/balanol-binding sites of protein kinases within familial groups and even among isoforms of the same kinase. We propose that balanol is a protean structure that may be modified to produce selective, high-affinity inhibitors and probes of the ATP-binding sites of serine/threonine protein kinases.
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pubmed:grant |
|
pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
|
pubmed:status |
MEDLINE
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pubmed:month |
Aug
|
pubmed:issn |
0026-895X
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pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:volume |
56
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
370-6
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:10419556-Adenosine Triphosphate,
pubmed-meshheading:10419556-Adenylate Cyclase,
pubmed-meshheading:10419556-Azepines,
pubmed-meshheading:10419556-Calcium-Calmodulin-Dependent Protein Kinases,
pubmed-meshheading:10419556-Catalytic Domain,
pubmed-meshheading:10419556-Cells, Cultured,
pubmed-meshheading:10419556-Enzyme Inhibitors,
pubmed-meshheading:10419556-GTP-Binding Protein alpha Subunits, Gs,
pubmed-meshheading:10419556-HeLa Cells,
pubmed-meshheading:10419556-Humans,
pubmed-meshheading:10419556-Hydroxybenzoic Acids,
pubmed-meshheading:10419556-Isoenzymes,
pubmed-meshheading:10419556-Protein-Serine-Threonine Kinases
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pubmed:year |
1999
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pubmed:articleTitle |
Inhibition of protein kinases by balanol: specificity within the serine/threonine protein kinase subfamily.
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pubmed:affiliation |
Department of Pharmacology and Medicine, University of California at San Diego, La Jolla, California, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, Non-U.S. Gov't
|