2h9e
From Proteopedia
(New page: 200px<br /> <applet load="2h9e" size="450" color="white" frame="true" align="right" spinBox="true" caption="2h9e, resolution 2.20Å" /> '''Crystal Structure o...) |
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caption="2h9e, resolution 2.20Å" /> | caption="2h9e, resolution 2.20Å" /> | ||
'''Crystal Structure of FXa/selectide/NAPC2 ternary complex'''<br /> | '''Crystal Structure of FXa/selectide/NAPC2 ternary complex'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2H9E is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Ancylostoma_caninum Ancylostoma caninum] and [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with PO4, ACT and NA as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Coagulation_factor_Xa Coagulation factor Xa], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.6 3.4.21.6] Full crystallographic information is available from [http:// | + | 2H9E is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Ancylostoma_caninum Ancylostoma caninum] and [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=PO4:'>PO4</scene>, <scene name='pdbligand=ACT:'>ACT</scene> and <scene name='pdbligand=NA:'>NA</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Coagulation_factor_Xa Coagulation factor Xa], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.6 3.4.21.6] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2H9E OCA]. |
==Reference== | ==Reference== | ||
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[[Category: selectide]] | [[Category: selectide]] | ||
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Revision as of 15:30, 15 February 2008
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Crystal Structure of FXa/selectide/NAPC2 ternary complex
Contents |
Overview
NAPc2, an anticoagulant protein from the hematophagous nematode, Ancylostoma caninum evaluated in phase-II/IIa clinical trials, inhibits, the extrinsic blood coagulation pathway by a two step mechanism, initially, interacting with the hitherto uncharacterized factor Xa exosite involved, in macromolecular recognition and subsequently inhibiting factor VIIa, (K(i)=8.4 pM) of the factor VIIa/tissue factor complex. NAPc2 is highly, flexible, becoming partially ordered and undergoing significant structural, changes in the C terminus upon binding to the factor Xa exosite. In the, crystal structure of the ternary factor Xa/NAPc2/selectide complex, the, binding interface consists of an intermolecular antiparallel beta-sheet, formed by the segment of the polypeptide chain consisting of residues, 74-80 of NAPc2 with the residues 86-93 of factor Xa that is additional, maintained by contacts between the short helical segment (residues 67-73), and a turn (residues 26-29) of NAPc2 with the short C-terminal helix of, factor Xa (residues 233-243). This exosite is physiologically highly, relevant for the recognition and inhibition of factor X/Xa by, macromolecular substrates and provides a structural motif for the, development of a new class of inhibitors for the treatment of deep vein, thrombosis and angioplasty.
Disease
Known disease associated with this structure: Factor X deficiency OMIM:[227600]
About this Structure
2H9E is a Protein complex structure of sequences from Ancylostoma caninum and Homo sapiens with , and as ligands. Active as Coagulation factor Xa, with EC number 3.4.21.6 Full crystallographic information is available from OCA.
Reference
Intermolecular interactions and characterization of the novel factor Xa exosite involved in macromolecular recognition and inhibition: crystal structure of human Gla-domainless factor Xa complexed with the anticoagulant protein NAPc2 from the hematophagous nematode Ancylostoma caninum., Murakami MT, Rios-Steiner J, Weaver SE, Tulinsky A, Geiger JH, Arni RK, J Mol Biol. 2007 Feb 16;366(2):602-10. Epub 2006 Nov 14. PMID:17173931
Page seeded by OCA on Fri Feb 15 17:30:33 2008
Categories: Ancylostoma caninum | Coagulation factor Xa | Homo sapiens | Protein complex | Arni, R.K. | Geiger, G. | Murakami, M.T. | Tulinsky, A. | ACT | NA | PO4 | Factor xa | Napc2 | Selectide
