1dwb

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[[Image:1dwb.gif|left|200px]]
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{{Seed}}
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[[Image:1dwb.png|left|200px]]
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{{STRUCTURE_1dwb| PDB=1dwb | SCENE= }}
{{STRUCTURE_1dwb| PDB=1dwb | SCENE= }}
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'''CRYSTALLOGRAPHIC ANALYSIS AT 3.0-ANGSTROMS RESOLUTION OF THE BINDING TO HUMAN THROMBIN OF FOUR ACTIVE SITE-DIRECTED INHIBITORS'''
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===CRYSTALLOGRAPHIC ANALYSIS AT 3.0-ANGSTROMS RESOLUTION OF THE BINDING TO HUMAN THROMBIN OF FOUR ACTIVE SITE-DIRECTED INHIBITORS===
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==Overview==
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The mode of binding of four active-site directed inhibitors to human thrombin has been determined by x-ray crystallographic analysis. The inhibitors studied are benzamidine, PPACK, NAPAP, and MD-805, of which the last three are compounds evolved specifically to inhibit thrombin. Crystal structures were determined in the presence of both the inhibitor and the undecapeptide [des-amino Asp55]hirudin(55-65) which binds distant from the active site. Despite having significantly different chemical structures, NAPAP and MD-805 bind to thrombin in a very similar "inhibitor binding mode" which is not that expected by direct analogy with the binding of substrate. Both inhibitors bind to thrombin in a similar way as to trypsin, but thrombin has an extra loop, the "Tyr-Pro-Pro-Trp loop," not present in trypsin, which gives further binding interactions and is seen to move somewhat to accommodate binding of the different inhibitors. The fact that NAPAP and MD-805 require different stereochemistry for potent inhibition is demonstrated, and its structural basis clarified. The wealth of data on analogs and variants of these lead compounds is shown to be compatible with this inhibitor binding mode.
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(as it appears on PubMed at http://www.pubmed.gov), where 1939071 is the PubMed ID number.
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{{ABSTRACT_PUBMED_1939071}}
==About this Structure==
==About this Structure==
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[[Category: Banner, D W.]]
[[Category: Banner, D W.]]
[[Category: Hadvary, P.]]
[[Category: Hadvary, P.]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 14:21:25 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 23:42:53 2008''

Revision as of 20:42, 30 June 2008

Image:1dwb.png

Template:STRUCTURE 1dwb

CRYSTALLOGRAPHIC ANALYSIS AT 3.0-ANGSTROMS RESOLUTION OF THE BINDING TO HUMAN THROMBIN OF FOUR ACTIVE SITE-DIRECTED INHIBITORS

Template:ABSTRACT PUBMED 1939071

About this Structure

1DWB is a Protein complex structure of sequences from Hirudo medicinalis and Homo sapiens. Full crystallographic information is available from OCA.

Reference

Crystallographic analysis at 3.0-A resolution of the binding to human thrombin of four active site-directed inhibitors., Banner DW, Hadvary P, J Biol Chem. 1991 Oct 25;266(30):20085-93. PMID:1939071

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