1rxp

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[[Image:1rxp.gif|left|200px]]
[[Image:1rxp.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1rxp |SIZE=350|CAPTION= <scene name='initialview01'>1rxp</scene>, resolution 1.70&Aring;
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The line below this paragraph, containing "STRUCTURE_1rxp", 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=169:1-(4-TERT-BUTYLCARBAMOYL-PIPERAZINE-1-CARBONYL)-3-(3-GUANIDINO-PROPYL)-4-OXO-AZETIDINE-2-CARBOXYLIC+ACID'>169</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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_1rxp| PDB=1rxp | 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=1rxp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1rxp OCA], [http://www.ebi.ac.uk/pdbsum/1rxp PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1rxp RCSB]</span>
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}}
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'''STRUCTURE OF TRYPSIN (ORTHORHOMBIC) WITH 1-(4-TERT-BUTYLCARBAMOYL- PIPERAZINE-1-CARBONYL)-3-(3-GUANIDINO-PROPYL)-4-OXO-AZETIDINE-2-CARBOXYLIC ACID'''
'''STRUCTURE OF TRYPSIN (ORTHORHOMBIC) WITH 1-(4-TERT-BUTYLCARBAMOYL- PIPERAZINE-1-CARBONYL)-3-(3-GUANIDINO-PROPYL)-4-OXO-AZETIDINE-2-CARBOXYLIC ACID'''
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[[Category: Bisacchi, G S.]]
[[Category: Bisacchi, G S.]]
[[Category: Jacobson, B.]]
[[Category: Jacobson, B.]]
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[[Category: azetidinone]]
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[[Category: Azetidinone]]
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[[Category: serine protease]]
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[[Category: Serine protease]]
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[[Category: tryptase inhibitor]]
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[[Category: Tryptase inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 08:02:00 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:34:25 2008''
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Revision as of 05:02, 3 May 2008

Image:1rxp.gif

Template:STRUCTURE 1rxp

STRUCTURE OF TRYPSIN (ORTHORHOMBIC) WITH 1-(4-TERT-BUTYLCARBAMOYL- PIPERAZINE-1-CARBONYL)-3-(3-GUANIDINO-PROPYL)-4-OXO-AZETIDINE-2-CARBOXYLIC ACID


Overview

A series of nonguanidine N1-activated C4-carboxy azetidinone tryptase inhibitors was prepared by solid-phase methodology to quickly assess the SAR associated with distal functionality on the N1-activating group. From these studies, potent inhibitors with improved specificity were discovered.

About this Structure

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

Reference

Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors., Sutton JC, Bolton SA, Davis ME, Hartl KS, Jacobson B, Mathur A, Ogletree ML, Slusarchyk WA, Zahler R, Seiler SM, Bisacchi GS, Bioorg Med Chem Lett. 2004 May 3;14(9):2233-9. PMID:15081015 Page seeded by OCA on Sat May 3 08:02:00 2008

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OCA

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