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PDBsum entry 2f9b
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Hydrolase/blood clotting
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PDB id
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2f9b
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Contents |
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94 a.a.
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254 a.a.
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149 a.a.
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* Residue conservation analysis
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PDB id:
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Hydrolase/blood clotting
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Title:
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Discovery of novel heterocyclic factor viia inhibitors
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Structure:
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Coagulation factor vii. Chain: l. Fragment: light chain, residues 61-212. Engineered: yes. Coagulation factor vii. Chain: h. Fragment: heavy chain, residues 213-466. Engineered: yes. Tissue factor.
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Gene: f7. Expressed in: homo sapiens. Expression_system_taxid: 9606. Expression_system_cell_line: embryonic kidney cell line 293. Gene: f3. Expressed in: escherichia coli.
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Biol. unit:
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Trimer (from
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Resolution:
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2.54Å
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R-factor:
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0.226
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R-free:
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0.286
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Authors:
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R.Rai,A.Kolesnikov,P.A.Sprengeler,S.Torkelson,T.Ton,B.A.Katz,C.Yu, J.Hendrix,W.D.Shrader,R.Stephens,R.Cabuslay,E.Sanford,W.B.Young
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Key ref:
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R.Rai
et al.
(2006).
Discovery of novel heterocyclic factor VIIa inhibitors.
Bioorg Med Chem Lett,
16,
2270-2273.
PubMed id:
DOI:
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Date:
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05-Dec-05
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Release date:
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28-Feb-06
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PROCHECK
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Headers
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References
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P08709
(FA7_HUMAN) -
Coagulation factor VII from Homo sapiens
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Seq:
Struc:
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466 a.a.
94 a.a.
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Enzyme class:
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Chains L, H:
E.C.3.4.21.21
- coagulation factor VIIa.
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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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DOI no:
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Bioorg Med Chem Lett
16:2270-2273
(2006)
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PubMed id:
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Discovery of novel heterocyclic factor VIIa inhibitors.
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R.Rai,
A.Kolesnikov,
P.A.Sprengeler,
S.Torkelson,
T.Ton,
B.A.Katz,
C.Yu,
J.Hendrix,
W.D.Shrader,
R.Stephens,
R.Cabuslay,
E.Sanford,
W.B.Young.
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ABSTRACT
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Structure-activity relationships and binding mode of novel heterocyclic factor
VIIa inhibitors will be described. In these inhibitors, a highly basic
5-amidinoindole moiety has been successfully replaced with a less basic
5-aminopyrrolo[3,2-b]pyridine scaffold.
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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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T.Shiraishi,
S.Kadono,
M.Haramura,
H.Kodama,
Y.Ono,
H.Iikura,
T.Esaki,
T.Koga,
K.Hattori,
Y.Watanabe,
A.Sakamoto,
K.Yoshihashi,
T.Kitazawa,
K.Esaki,
M.Ohta,
H.Sato,
and
T.Kozono
(2010).
Design and synthesis of peptidomimetic factor VIIa inhibitors.
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Chem Pharm Bull (Tokyo),
58,
38-44.
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PDB code:
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E.Persson,
and
O.H.Olsen
(2009).
Activation loop 3 and the 170 loop interact in the active conformation of coagulation factor VIIa.
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FEBS J,
276,
3099-3109.
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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
