This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.

Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.


1btz

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
(New page: 200px<br /><applet load="1btz" size="450" color="white" frame="true" align="right" spinBox="true" caption="1btz, resolution 2.0&Aring;" /> '''EPISELECTION: NOVEL K...)
Current revision (15:36, 13 March 2024) (edit) (undo)
 
(16 intermediate revisions not shown.)
Line 1: Line 1:
-
[[Image:1btz.gif|left|200px]]<br /><applet load="1btz" size="450" color="white" frame="true" align="right" spinBox="true"
 
-
caption="1btz, resolution 2.0&Aring;" />
 
-
'''EPISELECTION: NOVEL KI ~NANOMOLAR INHIBITORS OF SERINE PROTEASES SELECTED BY BINDING OR CHEMISTRY ON AN ENZYME SURFACE'''<br />
 
-
==Overview==
+
==Episelection: novel KI ~nanomolar inhibitors of serine proteases selected by binding or chemistry on an enzyme surface==
-
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.
+
<StructureSection load='1btz' size='340' side='right'caption='[[1btz]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
 +
== Structural highlights ==
 +
<table><tr><td colspan='2'>[[1btz]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1BTZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1BTZ FirstGlance]. <br>
 +
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2&#8491;</td></tr>
 +
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0ZY:N-(TERT-BUTOXYCARBONYL)-L-ALANYL-N-{(1R)-5-AMMONIO-1-[HYDROXY(METHOXY)BORANYL]PENTYL}-L-VALINAMIDE'>0ZY</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene></td></tr>
 +
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1btz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1btz OCA], [https://pdbe.org/1btz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1btz RCSB], [https://www.ebi.ac.uk/pdbsum/1btz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1btz ProSAT]</span></td></tr>
 +
</table>
 +
== Function ==
 +
[https://www.uniprot.org/uniprot/TRY1_BOVIN TRY1_BOVIN]
 +
== Evolutionary Conservation ==
 +
[[Image:Consurf_key_small.gif|200px|right]]
 +
Check<jmol>
 +
<jmolCheckbox>
 +
<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/bt/1btz_consurf.spt"</scriptWhenChecked>
 +
<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
 +
<text>to colour the structure by Evolutionary Conservation</text>
 +
</jmolCheckbox>
 +
</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1btz ConSurf].
 +
<div style="clear:both"></div>
-
==About this Structure==
+
==See Also==
-
1BTZ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] with CA and CH3 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1BTZ OCA].
+
*[[Trypsin 3D structures|Trypsin 3D structures]]
-
 
+
__TOC__
-
==Reference==
+
</StructureSection>
-
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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=7599119 7599119]
+
[[Category: Bos taurus]]
[[Category: Bos taurus]]
-
[[Category: Single protein]]
+
[[Category: Large Structures]]
-
[[Category: Trypsin]]
+
[[Category: Finer-Moore J]]
-
[[Category: Finer-Moore, J.]]
+
[[Category: Katz BA]]
-
[[Category: Katz, B.A.]]
+
[[Category: Stroud RM]]
-
[[Category: Stroud, R.M.]]
+
-
[[Category: CA]]
+
-
[[Category: CH3]]
+
-
[[Category: tripeptideboronate methyl ester inhibited]]
+
-
 
+
-
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Nov 20 11:55:11 2007''
+

Current revision

Episelection: novel KI ~nanomolar inhibitors of serine proteases selected by binding or chemistry on an enzyme surface

PDB ID 1btz

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1btz"
Personal tools