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PDBsum entry 4jps
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Transferase/transferase inhibitor
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PDB id
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4jps
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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 nvp-Byl719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.
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Authors
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P.Furet,
V.Guagnano,
R.A.Fairhurst,
P.Imbach-Weese,
I.Bruce,
M.Knapp,
C.Fritsch,
F.Blasco,
J.Blanz,
R.Aichholz,
J.Hamon,
D.Fabbro,
G.Caravatti.
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Ref.
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Bioorg Med Chem Lett, 2013,
23,
3741-3748.
[DOI no: ]
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PubMed id
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Abstract
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Phosphatidylinositol-3-kinase α (PI3Kα) is a therapeutic target of high
interest in anticancer drug research. On the basis of a binding model
rationalizing the high selectivity and potency of a particular series of
2-aminothiazole compounds in inhibiting PI3Kα, a medicinal chemistry program
has led to the discovery of the clinical candidate NVP-BYL719.
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