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| {{STRUCTURE_2h9e| PDB=2h9e | SCENE= }} | | {{STRUCTURE_2h9e| PDB=2h9e | SCENE= }} |
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| '''Crystal Structure of FXa/selectide/NAPC2 ternary complex'''
| | ===Crystal Structure of FXa/selectide/NAPC2 ternary complex=== |
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| ==Overview==
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| 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.
| | The line below this paragraph, {{ABSTRACT_PUBMED_17173931}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 17173931 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_17173931}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Napc2]] | | [[Category: Napc2]] |
| [[Category: Selectide]] | | [[Category: Selectide]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:01:03 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 19:03:32 2008'' |
