1btw

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{{STRUCTURE_1btw| PDB=1btw | SCENE= }}
{{STRUCTURE_1btw| PDB=1btw | SCENE= }}
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'''EPISELECTION: NOVEL KI ~NANOMOLAR INHIBITORS OF SERINE PROTEASES SELECTED BY BINDING OR CHEMISTRY ON AN ENZYME SURFACE'''
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===EPISELECTION: NOVEL KI ~NANOMOLAR INHIBITORS OF SERINE PROTEASES SELECTED BY BINDING OR CHEMISTRY ON AN ENZYME SURFACE===
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==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.
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(as it appears on PubMed at http://www.pubmed.gov), where 7599119 is the PubMed ID number.
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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: Tripeptideboronate 1,3-propanediol monoester-inhibited]]
[[Category: Tripeptideboronate 1,3-propanediol monoester-inhibited]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 11:57:06 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 19:42:57 2008''

Revision as of 16:42, 30 June 2008

Template:STRUCTURE 1btw

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

Template:ABSTRACT PUBMED 7599119

About this Structure

1BTW 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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