1rxp
From Proteopedia
| Line 4: | Line 4: | ||
|PDB= 1rxp |SIZE=350|CAPTION= <scene name='initialview01'>1rxp</scene>, resolution 1.70Å | |PDB= 1rxp |SIZE=350|CAPTION= <scene name='initialview01'>1rxp</scene>, resolution 1.70Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= | + | |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> |
| - | |ACTIVITY= [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] | + | |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> |
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |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> | ||
}} | }} | ||
| Line 25: | Line 28: | ||
[[Category: Bisacchi, G S.]] | [[Category: Bisacchi, G S.]] | ||
[[Category: Jacobson, B.]] | [[Category: Jacobson, B.]] | ||
| - | [[Category: | + | [[Category: azetidinone]] |
| - | [[Category: | + | [[Category: serine protease]] |
| - | + | [[Category: tryptase inhibitor]] | |
| - | [[Category: tryptase inhibitor | + | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:34:25 2008'' |
Revision as of 20:34, 30 March 2008
| |||||||
| , resolution 1.70Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , , | ||||||
| Activity: | Trypsin, with EC number 3.4.21.4 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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 Sun Mar 30 23:34:25 2008
