1sr5: Difference between revisions
New page: left|200px<br /> <applet load="1sr5" size="450" color="white" frame="true" align="right" spinBox="true" caption="1sr5, resolution 3.10Å" /> '''ANTITHROMBIN-ANHYDR... |
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[[Image:1sr5. | [[Image:1sr5.jpg|left|200px]]<br /><applet load="1sr5" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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caption="1sr5, resolution 3.10Å" /> | caption="1sr5, resolution 3.10Å" /> | ||
'''ANTITHROMBIN-ANHYDROTHROMBIN-HEPARIN TERNARY COMPLEX STRUCTURE'''<br /> | '''ANTITHROMBIN-ANHYDROTHROMBIN-HEPARIN TERNARY COMPLEX STRUCTURE'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
1SR5 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with NAG, NT1 and NT2 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Thrombin Thrombin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.5 3.4.21.5] Full crystallographic information is available from [http:// | 1SR5 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=NAG:'>NAG</scene>, <scene name='pdbligand=NT1:'>NT1</scene> and <scene name='pdbligand=NT2:'>NT2</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Thrombin Thrombin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.5 3.4.21.5] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SR5 OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: serine proteinase inhibitor]] | [[Category: serine proteinase inhibitor]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:54:33 2008'' |
Revision as of 17:54, 15 February 2008
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ANTITHROMBIN-ANHYDROTHROMBIN-HEPARIN TERNARY COMPLEX STRUCTURE
OverviewOverview
Antithrombin, the principal physiological inhibitor of the blood, coagulation proteinase thrombin, requires heparin as a cofactor. We report, the crystal structure of the rate-determining encounter complex formed, between antithrombin, anhydrothrombin and an optimal synthetic 16-mer, oligosaccharide. The antithrombin reactive center loop projects from the, serpin body and adopts a canonical conformation that makes extensive, backbone and side chain contacts from P5 to P6' with thrombin's, restrictive specificity pockets, including residues in the 60-loop. These, contacts rationalize many earlier mutagenesis studies on thrombin, specificity. The 16-mer oligosaccharide is just long enough to form the, predicted bridge between the high-affinity pentasaccharide-binding site on, antithrombin and the highly basic exosite 2 on thrombin, validating the, design strategy for this synthetic heparin. The protein-protein and, protein-oligosaccharide interactions together explain the basis for, heparin activation of antithrombin as a thrombin inhibitor.
DiseaseDisease
Known diseases associated with this structure: Dysprothrombinemia OMIM:[176930], Hyperprothrombinemia OMIM:[176930], Hypoprothrombinemia OMIM:[176930]
About this StructureAbout this Structure
1SR5 is a Protein complex structure of sequences from Homo sapiens with , and as ligands. Active as Thrombin, with EC number 3.4.21.5 Full crystallographic information is available from OCA.
ReferenceReference
The ternary complex of antithrombin-anhydrothrombin-heparin reveals the basis of inhibitor specificity., Dementiev A, Petitou M, Herbert JM, Gettins PG, Nat Struct Mol Biol. 2004 Sep;11(9):863-7. Epub 2004 Aug 15. PMID:15311268
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