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| {{STRUCTURE_1bth| PDB=1bth | SCENE= }} | | {{STRUCTURE_1bth| PDB=1bth | SCENE= }} |
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| '''STRUCTURE OF THROMBIN COMPLEXED WITH BOVINE PANCREATIC TRYPSIN INHIBITOR'''
| | ===STRUCTURE OF THROMBIN COMPLEXED WITH BOVINE PANCREATIC TRYPSIN INHIBITOR=== |
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| ==Overview==
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| Previous crystal structures of thrombin indicate that the 60-insertion loop is a rigid moiety that partially occludes the active site, suggesting that this structural feature plays a decisive role in restricting thrombin's specificity. This restricted specificity is typified by the experimental observation that thrombin is not inhibited by micromolar concentrations of basic pancreatic trypsin inhibitor (BPTI). Surprisingly, a single atom mutation in thrombin (E192Q) results in a 10(-8) M affinity for BPTI. The crystal structure of human thrombin mutant E192Q has been solved in complex with BPTI at 2.3 A resolution. Binding of the Kunitz inhibitor is accompanied by gross structural rearrangements in thrombin. In particular, thrombin's 60-loop is found in a significantly different conformation. Concomitant reorganization of other surface loops that surround the active site, i.e. the 37-loop, the 148-loop and the 99-loop, is observed. Thrombin can therefore undergo major structural reorganization upon strong ligand binding. Implications for the interaction of thrombin with antithrombin and thrombomodulin are discussed.
| | The line below this paragraph, {{ABSTRACT_PUBMED_9214615}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 9214615 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_9214615}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Serine proteinase kunitz-like inhibitor]] | | [[Category: Serine proteinase kunitz-like inhibitor]] |
| [[Category: Thrombin inhibitor]] | | [[Category: Thrombin inhibitor]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 11:56:11 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 19:41:53 2008'' |
