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PDBsum entry 3ffg
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References listed in PDB file
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Key reference
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Title
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Phenyltriazolinones as potent factor xa inhibitors.
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Authors
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M.L.Quan,
D.J.Pinto,
K.A.Rossi,
S.Sheriff,
R.S.Alexander,
E.Amparo,
K.Kish,
R.M.Knabb,
J.M.Luettgen,
P.Morin,
A.Smallwood,
F.J.Woerner,
R.R.Wexler.
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Ref.
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Bioorg Med Chem Lett, 2010,
20,
1373-1377.
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PubMed id
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Abstract
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We have discovered that phenyltriazolinone is a novel and potent P1 moiety for
coagulation factor Xa. X-ray structures of the inhibitors with a
phenyltriazolinone in the P1 position revealed that the side chain of Asp189 has
reoriented resulting in a novel S1 binding pocket which is larger in size to
accommodate the phenyltriazolinone P1 substrate.
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