1RXP

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

Summary for 1RXP

Entry DOI	10.2210/pdb1rxp/pdb
Descriptor	TRYPSIN, CALCIUM ION, SULFATE ION, ... (5 entities in total)
Functional Keywords	tryptase inhibitor; serine protease; azetidinone, hydrolase
Biological source	Bos taurus (cattle)
Cellular location	Secreted, extracellular space: P00760
Total number of polymer chains	1
Total formula weight	23887.93
Authors	Bisacchi, G.S.,Jacobson, B. (deposition date: 2003-12-18, release date: 2004-06-08, Last modification date: 2024-10-16)
Primary citation	Sutton, J.C.,Bolton, S.A.,Davis, M.E.,Hartl, K.S.,Jacobson, B.,Mathur, A.,Ogletree, M.L.,Slusarchyk, W.A.,Zahler, R.,Seiler, S.M.,Bisacchi, G.S. Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors Bioorg.Med.Chem.Lett., 14:2233-2239, 2004 Cited by PubMed Abstract: 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. PubMed: 15081015 DOI: 10.1016/j.bmcl.2004.02.012 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.7 Å)

Structure validation