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Blood clotting,hydrolase
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PDB id
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1x7a
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Contents |
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* Residue conservation analysis
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PDB id:
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| Name: |
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Blood clotting,hydrolase
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Title:
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Porcine factor ixa complexed to 1-{3-[amino(imino) methyl]phenyl}-n-[4-(1h-benzimidazol-1-yl)-2-fluorophenyl]- 3-(trifluoromethyl)-1h-pyrazole-5-carboxamide
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Structure:
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Coagulation factor ixa. Chain: c. Fragment: heavy chain, proteinase. Synonym: christmas factor. Coagulation factor ix, light chain. Chain: l. Fragment: light chain. Synonym: mature porcine factor ix
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Source:
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Sus scrofa. Pig. Organism_taxid: 9823. Organism_taxid: 9823
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Biol. unit:
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Tetramer (from
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Resolution:
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Authors:
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R.S.Alexander,A.M.Smallwood,J.M.Smallheer,J.Wang,S.Wang, S.Nakajima,K.A.Rossi,F.Barbera,D.Burdick,J.M.Luettgen
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Key ref:
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J.M.Smallheer
et al.
(2004).
SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.
Bioorg Med Chem Lett,
14,
5263-5267.
PubMed id:
DOI:
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Date:
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13-Aug-04
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Release date:
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16-Aug-05
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PROCHECK
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Headers
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References
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Enzyme class:
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Chains C, L:
E.C.3.4.21.22
- Coagulation factor IXa.
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Reaction:
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Hydrolyzes one Arg-|-Ile bond in factor X to form factor Xa.
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Gene Ontology (GO) functional annotation
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Cellular component
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extracellular region
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1 term
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Biological process
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proteolysis
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1 term
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Biochemical function
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catalytic activity
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4 terms
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DOI no:
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Bioorg Med Chem Lett
14:5263-5267
(2004)
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PubMed id:
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SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.
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J.M.Smallheer,
R.S.Alexander,
J.Wang,
S.Wang,
S.Nakajima,
K.A.Rossi,
A.Smallwood,
F.Barbera,
D.Burdick,
J.M.Luettgen,
R.M.Knabb,
R.R.Wexler,
P.K.Jadhav.
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ABSTRACT
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Modifications to the P4 moiety and pyrazole C3 substituent of factor Xa
inhibitor SN-429 provided several new compounds, which are 5-10nM inhibitors of
factor IXa. An X-ray crystal structure of one example complexed to factor IXa
shows that these compounds adopt a similar binding mode to that previously
observed with pyrazole inhibitors in the factor Xa active site both with regard
to how the inhibitor binds and the position of Tyr99.
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Literature references that cite this PDB file's key reference
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PubMed id
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Reference
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D.J.Johnson,
J.Langdown,
and
J.A.Huntington
(2010).
Molecular basis of factor IXa recognition by heparin-activated antithrombin revealed by a 1.7-A structure of the ternary complex.
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Proc Natl Acad Sci U S A, 107,
645-650.
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PDB code:
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A.Sun,
J.J.Yoon,
Y.Yin,
A.Prussia,
Y.Yang,
J.Min,
R.K.Plemper,
and
J.P.Snyder
(2008).
Potent non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complex.
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J Med Chem, 51,
3731-3741.
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A.Savarino
(2007).
In-Silico docking of HIV-1 integrase inhibitors reveals a novel drug type acting on an enzyme/DNA reaction intermediate.
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Retrovirology, 4,
21.
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The most recent references are shown first.
Citation data come partly from CiteXplore and partly
from an automated harvesting procedure. Note that this is likely to be
only a partial list as not all journals are covered by
either method. However, we are continually building up the citation data
so more and more references will be included with time.
Where a reference describes a PDB structure, the PDB
code is
shown on the right.
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Links
