1rxp

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Image:1rxp.gif

1rxp, resolution 1.70Å

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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

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 with CA, SO4 and 169 as ligands. Active as Trypsin, with EC number 3.4.21.4 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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