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PDBsum entry 3cd8
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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 and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.
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Authors
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B.K.Albrecht,
J.C.Harmange,
D.Bauer,
L.Berry,
C.Bode,
A.A.Boezio,
A.Chen,
D.Choquette,
I.Dussault,
C.Fridrich,
S.Hirai,
D.Hoffman,
J.F.Larrow,
P.Kaplan-Lefko,
J.Lin,
J.Lohman,
A.M.Long,
J.Moriguchi,
A.O'Connor,
M.H.Potashman,
M.Reese,
K.Rex,
A.Siegmund,
K.Shah,
R.Shimanovich,
S.K.Springer,
Y.Teffera,
Y.Yang,
Y.Zhang,
S.F.Bellon.
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Ref.
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J Med Chem, 2008,
51,
2879-2882.
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PubMed id
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Abstract
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Tumorigenesis is a multistep process in which oncogenes play a key role in tumor
formation, growth, and maintenance. MET was discovered as an oncogene that is
activated by its ligand, hepatocyte growth factor. Deregulated signaling in the
c-Met pathway has been observed in multiple tumor types. Herein we report the
discovery of potent and selective triazolopyridazine small molecules that
inhibit c-Met activity.
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