rdf:type |
|
lifeskim:mentions |
umls-concept:C0026837,
umls-concept:C0034328,
umls-concept:C0035647,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0231517,
umls-concept:C0243071,
umls-concept:C0243077,
umls-concept:C0376358,
umls-concept:C1516170,
umls-concept:C1707689,
umls-concept:C1883254
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pubmed:issue |
8
|
pubmed:dateCreated |
2001-4-30
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pubmed:abstractText |
In view of its role in tumor promotion and signal transduction, protein kinase C (PKC) has proven to be an exciting target for cancer therapy. With the aid of molecular modeling, we rationally designed and stereoselectively synthesized a new class of rigidified pyrrolidone-based PKC activators. Pyrrolidone 15 was found to exhibit reasonable affinity for PKCdelta, with lower affinity for the other isozymes tested. Pyrrolidone 2 causes the dose-dependent induction of apoptosis in LNCaP prostate cancer cells. This apoptotic effect could be markedly potentiated by the use of LNCaP cells overexpressing the PKCalpha or delta isozymes.
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pubmed:grant |
|
pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Activators,
http://linkedlifedata.com/resource/pubmed/chemical/Isoenzymes,
http://linkedlifedata.com/resource/pubmed/chemical/PRKCA protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/PRKCD protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase C,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase C-alpha,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase C-delta,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrrolidinones
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
|
pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:Flippen-AndersonJJ,
pubmed-author:FujiiTT,
pubmed-author:KazanietzM GMG,
pubmed-author:KozikowskiA PAP,
pubmed-author:RauserLL,
pubmed-author:RongS BSB,
pubmed-author:RothB LBL,
pubmed-author:SavageJJ,
pubmed-author:SenMM,
pubmed-author:ShawM TMT,
pubmed-author:WangSS,
pubmed-author:ZhaoL YLY
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pubmed:issnType |
Print
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pubmed:day |
23
|
pubmed:volume |
11
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
955-9
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:11327599-Antineoplastic Agents,
pubmed-meshheading:11327599-Apoptosis,
pubmed-meshheading:11327599-Dose-Response Relationship, Drug,
pubmed-meshheading:11327599-Drug Design,
pubmed-meshheading:11327599-Enzyme Activators,
pubmed-meshheading:11327599-Humans,
pubmed-meshheading:11327599-Isoenzymes,
pubmed-meshheading:11327599-Male,
pubmed-meshheading:11327599-Prostate,
pubmed-meshheading:11327599-Prostatic Neoplasms,
pubmed-meshheading:11327599-Protein Kinase C,
pubmed-meshheading:11327599-Protein Kinase C-alpha,
pubmed-meshheading:11327599-Protein Kinase C-delta,
pubmed-meshheading:11327599-Pyrrolidinones,
pubmed-meshheading:11327599-Stereoisomerism,
pubmed-meshheading:11327599-Tumor Cells, Cultured
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pubmed:year |
2001
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pubmed:articleTitle |
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.
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pubmed:affiliation |
Department of Neurology, Georgetotwn University, Medical Center, Washington, DC 20007, 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.
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