1bty: Difference between revisions

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[[Image:1bty.gif|left|200px]]
{{Seed}}
[[Image:1bty.png|left|200px]]


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{{STRUCTURE_1bty|  PDB=1bty  |  SCENE=  }}  
{{STRUCTURE_1bty|  PDB=1bty  |  SCENE=  }}  


'''EPISELECTION: NOVEL KI ~NANOMOLAR INHIBITORS OF SERINE PROTEASES SELECTED BY BINDING OR CHEMISTRY ON AN ENZYME SURFACE'''
===EPISELECTION: NOVEL KI ~NANOMOLAR INHIBITORS OF SERINE PROTEASES SELECTED BY BINDING OR CHEMISTRY ON AN ENZYME SURFACE===




==Overview==
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A novel class of mechanism-based inhibitors of the serine proteases is developed using epitaxial selection. Tripeptide boronates esterified by an alcohol or alcohols at the boron retain the tight binding to trypsin-like enzymes associated with transition-state analogs and incorporate additional groups that can be utilized for selectivity between proteases. Formed by reaction of a series of alcohols with the inhibitor boronate oxygen(s), the most structurally compatible alcohol-derivatized inhibitors are either selected by binding to the enzyme (epitaxial selection) or assembled by epitaxial reaction on the enzyme surface. Mass spectrometry of the derivatized boronates and X-ray crystallography of the complexes identify the chemical structures and the three-dimensional interactions of inhibitors generated. This scheme also engineers novel, potent (Ki approximately 7 nM), and more specific inhibitors of individual serine proteases, by derivitizations of compounds obtained by epitaxial selection.
The line below this paragraph, {{ABSTRACT_PUBMED_7599119}}, adds the Publication Abstract to the page
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{{ABSTRACT_PUBMED_7599119}}


==About this Structure==
==About this Structure==
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[[Category: Stroud, R M.]]
[[Category: Stroud, R M.]]
[[Category: Benzamidine inhibited]]
[[Category: Benzamidine inhibited]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May  2 11:57:10 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 19:43:02 2008''

Revision as of 16:43, 30 June 2008

File:1bty.png

Template:STRUCTURE 1bty

EPISELECTION: NOVEL KI ~NANOMOLAR INHIBITORS OF SERINE PROTEASES SELECTED BY BINDING OR CHEMISTRY ON AN ENZYME SURFACE

Template:ABSTRACT PUBMED 7599119

About this Structure

1BTY is a Single protein structure of sequence from Bos taurus. Full crystallographic information is available from OCA.

Reference

Episelection: novel Ki approximately nanomolar inhibitors of serine proteases selected by binding or chemistry on an enzyme surface., Katz BA, Finer-Moore J, Mortezaei R, Rich DH, Stroud RM, Biochemistry. 1995 Jul 4;34(26):8264-80. PMID:7599119

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