1btw

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[[Image:1btw.gif|left|200px]]
[[Image:1btw.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1btw |SIZE=350|CAPTION= <scene name='initialview01'>1btw</scene>, resolution 1.7&Aring;
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The line below this paragraph, containing "STRUCTURE_1btw", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=BLY:LYSINE+BORONIC+ACID'>BLY</scene>, <scene name='pdbligand=BOC:TERT-BUTYL+HYDROGEN+CARBONATE'>BOC</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=HPG:HYDROXYPROPYLOXY+GROUP'>HPG</scene>, <scene name='pdbligand=PDO:1,3-PROPANDIOL'>PDO</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Trypsin Trypsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.4 3.4.21.4] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1btw| PDB=1btw | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1btw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1btw OCA], [http://www.ebi.ac.uk/pdbsum/1btw PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1btw RCSB]</span>
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}}
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'''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'''
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[[Category: Katz, B A.]]
[[Category: Katz, B A.]]
[[Category: Stroud, R M.]]
[[Category: Stroud, R M.]]
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[[Category: tripeptideboronate 1,3-propanediol monoester-inhibited]]
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[[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 Sun Mar 30 19:08:10 2008''
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Revision as of 08:57, 2 May 2008

Image:1btw.gif

Template:STRUCTURE 1btw

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


Overview

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.

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 Page seeded by OCA on Fri May 2 11:57:06 2008

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