1rxp
From Proteopedia
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| - | [[Image:1rxp.gif|left|200px]] | + | [[Image:1rxp.gif|left|200px]] |
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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 |
| + | |PDB= 1rxp |SIZE=350|CAPTION= <scene name='initialview01'>1rxp</scene>, resolution 1.70Å | ||
| + | |SITE= | ||
| + | |LIGAND= <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene> and <scene name='pdbligand=169:1-(4-TERT-BUTYLCARBAMOYL-PIPERAZINE-1-CARBONYL)-3-(3-GUANIDINO-PROPYL)-4-OXO-AZETIDINE-2-CARBOXYLIC ACID'>169</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] | ||
| + | |GENE= | ||
| + | }} | ||
| + | |||
| + | '''STRUCTURE OF TRYPSIN (ORTHORHOMBIC) WITH 1-(4-TERT-BUTYLCARBAMOYL- PIPERAZINE-1-CARBONYL)-3-(3-GUANIDINO-PROPYL)-4-OXO-AZETIDINE-2-CARBOXYLIC ACID''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1RXP is a [ | + | 1RXP is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1RXP OCA]. |
==Reference== | ==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:[http:// | + | 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:[http://www.ncbi.nlm.nih.gov/pubmed/15081015 15081015] |
[[Category: Bos taurus]] | [[Category: Bos taurus]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
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[[Category: tryptase inhibitor; serine protease; azetidinone]] | [[Category: tryptase inhibitor; serine protease; azetidinone]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 13:57:37 2008'' |
Revision as of 11:57, 20 March 2008
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| , resolution 1.70Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , and | ||||||
| Activity: | Trypsin, with EC number 3.4.21.4 | ||||||
| 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 Thu Mar 20 13:57:37 2008
