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rdf:type |
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lifeskim:mentions |
umls-concept:C0006826,
umls-concept:C0087111,
umls-concept:C0164786,
umls-concept:C0205314,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0243077,
umls-concept:C0285558,
umls-concept:C0679622,
umls-concept:C0812228,
umls-concept:C1705328,
umls-concept:C1705341,
umls-concept:C1880355,
umls-concept:C1883254
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pubmed:issue |
6
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|
pubmed:dateCreated |
2006-2-7
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|
pubmed:abstractText |
A novel series of Akt/PKB inhibitors derived from a screening lead (1) has been prepared. The novel trans-3,4'-bispyridinylethylenes described herein are potent inhibitors of Akt/PKB with IC(50) values in the low double-digit nanomolar range against Akt1. Compound 2q shows excellent selectivity against distinct families of kinases such as tyrosine kinases and CAMK, and displays poor to modest selectivity against closely related kinases in the AGC and CMGC families. The cellular activities including inhibition of cell growth and phosphorylation of downstream target GSK3 are also described. The X-ray structure of compound 2q complexed with PKA in the ATP binding site was determined.
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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 |
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:ArriesShannonS,
pubmed-author:BauchJoy LJL,
pubmed-author:BouskaJennifer JJJ,
pubmed-author:ChuI YIY,
pubmed-author:ClaiboneAkiyoA,
pubmed-author:DaltonChrisC,
pubmed-author:De JongRonR,
pubmed-author:GirandaVincent LVL,
pubmed-author:GongJianchunJ,
pubmed-author:JakobClarissa GCG,
pubmed-author:JohnsonEric FEF,
pubmed-author:KlinghoferVeredV,
pubmed-author:LiQunQ,
pubmed-author:LiTongmeiT,
pubmed-author:LiuXuesongX,
pubmed-author:LuoYanY,
pubmed-author:MarshKennan CKC,
pubmed-author:OltersdorfTilmanT,
pubmed-author:RosenbergSaul HSH,
pubmed-author:StollVincent SVS,
pubmed-author:ZhuGui-DongGD
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|
pubmed:issnType |
Print
|
|
pubmed:day |
15
|
|
pubmed:volume |
16
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
1679-85
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:16403626-Adenosine Triphosphate,
pubmed-meshheading:16403626-Antineoplastic Agents,
pubmed-meshheading:16403626-Binding Sites,
pubmed-meshheading:16403626-Calcium-Calmodulin-Dependent Protein Kinases,
pubmed-meshheading:16403626-Cell Proliferation,
pubmed-meshheading:16403626-Enzyme Inhibitors,
pubmed-meshheading:16403626-Ethylenes,
pubmed-meshheading:16403626-Glycogen Synthase Kinase 3,
pubmed-meshheading:16403626-Humans,
pubmed-meshheading:16403626-Neoplasms,
pubmed-meshheading:16403626-Phosphorylation,
pubmed-meshheading:16403626-Protein-Serine-Threonine Kinases,
pubmed-meshheading:16403626-Protein-Tyrosine Kinases,
pubmed-meshheading:16403626-Proto-Oncogene Proteins c-akt,
pubmed-meshheading:16403626-Structure-Activity Relationship
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pubmed:year |
2006
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pubmed:articleTitle |
Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.
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|
pubmed:affiliation |
Cancer Research, GPRD, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. qun.li@abbott.com
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pubmed:publicationType |
Journal Article,
Evaluation Studies
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