1dit

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{{STRUCTURE_1dit| PDB=1dit | SCENE= }}
{{STRUCTURE_1dit| PDB=1dit | SCENE= }}
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'''COMPLEX OF A DIVALENT INHIBITOR WITH THROMBIN'''
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===COMPLEX OF A DIVALENT INHIBITOR WITH THROMBIN===
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==Overview==
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A new class of divalent thrombin inhibitors is described that contains an alpha-keto-amide transition-state mimetic linking an active site binding group and a group that binds to the fibrinogen-binding exosite. The X-ray crystallographic structure of the most potent member of this new class, CVS995, shows many features in common with other divalent thrombin inhibitors and clearly defines the transition-state-like binding of the alpha-keto-amide group. The structure of the active site part of the inhibitor shows a network of water molecules connecting both the side-chain and backbone atoms of thrombin and the inhibitor. Direct peptide analogues of the new transition-state-containing divalent thrombin inhibitors were compared using in vitro assays of thrombin inhibition. There was no direct correlation between the binding constants of the peptides and their alpha-keto-amide counterparts. The most potent alpha-keto-amide inhibitor, CVS995, with a Ki = 1 pM, did not correspond to the most potent divalent peptide and contained a single amino acid deletion in the exosite binding region with respect to the equivalent region of the natural thrombin inhibitor hirudin. The interaction energies of the active site, transition state, and exosite binding regions of these new divalent thrombin inhibitors are not additive.
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The line below this paragraph, {{ABSTRACT_PUBMED_8868478}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 8868478 is the PubMed ID number.
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{{ABSTRACT_PUBMED_8868478}}
==About this Structure==
==About this Structure==
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[[Category: Hydrolase]]
[[Category: Hydrolase]]
[[Category: Inhibitor]]
[[Category: Inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 13:53:45 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 23:07:47 2008''

Revision as of 20:07, 30 June 2008

Image:1dit.png

Template:STRUCTURE 1dit

COMPLEX OF A DIVALENT INHIBITOR WITH THROMBIN

Template:ABSTRACT PUBMED 8868478

About this Structure

1DIT is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Synthesis, structure, and structure-activity relationships of divalent thrombin inhibitors containing an alpha-keto-amide transition-state mimetic., Krishnan R, Tulinsky A, Vlasuk GP, Pearson D, Vallar P, Bergum P, Brunck TK, Ripka WC, Protein Sci. 1996 Mar;5(3):422-33. PMID:8868478

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