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PDBsum entry 2f7x
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References listed in PDB file
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Key reference
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Title
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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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Authors
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Q.Li,
T.Li,
G.D.Zhu,
J.Gong,
A.Claibone,
C.Dalton,
Y.Luo,
E.F.Johnson,
Y.Shi,
X.Liu,
V.Klinghofer,
J.L.Bauch,
K.C.Marsh,
J.J.Bouska,
S.Arries,
R.De jong,
T.Oltersdorf,
V.S.Stoll,
C.G.Jakob,
S.H.Rosenberg,
V.L.Giranda.
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Ref.
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Bioorg Med Chem Lett, 2006,
16,
1679-1685.
[DOI no: ]
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PubMed id
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Note In the PDB file this reference is
annotated as "TO BE PUBLISHED".
The citation details given above were identified by an automated
search of PubMed on title and author
names, giving a
perfect match.
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Abstract
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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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