1rxp | pdb_00001rxp
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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| 1rxp, resolution 1.70Å | |||||||||||||
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| Ligands: | CA, SO4 and 169 | ||||||||||||
| Activity: | Trypsin, with EC number 3.4.21.4 | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
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
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