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1bth

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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'''
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===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.
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The line below this paragraph, {{ABSTRACT_PUBMED_9214615}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 9214615 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9214615}}
==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]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 11:56:11 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 19:41:53 2008''

Revision as of 16:41, 30 June 2008

Image:1bth.png

Template:STRUCTURE 1bth

STRUCTURE OF THROMBIN COMPLEXED WITH BOVINE PANCREATIC TRYPSIN INHIBITOR

Template:ABSTRACT PUBMED 9214615

About this Structure

1BTH is a Protein complex structure of sequences from Bos taurus. Full crystallographic information is available from OCA.

Reference

The thrombin E192Q-BPTI complex reveals gross structural rearrangements: implications for the interaction with antithrombin and thrombomodulin., van de Locht A, Bode W, Huber R, Le Bonniec BF, Stone SR, Esmon CT, Stubbs MT, EMBO J. 1997 Jun 2;16(11):2977-84. PMID:9214615

Page seeded by OCA on Mon Jun 30 19:41:53 2008

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