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PDBsum entry 1w2k
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Contents |
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251 a.a.
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142 a.a.
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188 a.a.
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References listed in PDB file
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Key reference
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Title
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Design of selective phenylglycine amide tissue factor/factor viia inhibitors.
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Authors
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K.Groebke zbinden,
D.W.Banner,
J.Ackermann,
A.D'Arcy,
D.Kirchhofer,
Y.H.Ji,
T.B.Tschopp,
S.Wallbaum,
L.Weber.
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Ref.
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Bioorg Med Chem Lett, 2005,
15,
817-822.
[DOI no: ]
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PubMed id
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Abstract
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Proof of concept experiments have shown that tissue factor/factor VIIa
inhibitors have antithrombotic activity without enhancing bleeding propensity.
Starting from lead compounds generated by a biased combinatorial approach,
phenylglycine amide tissue factor/factor VIIa inhibitors with low nanomolar
affinity and good selectivity against other serine proteases of the coagulation
cascade were designed, using the guidance of X-ray structural analysis and
molecular modelling.
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