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PDBsum entry 1rxp
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Hydrolase PDB id
1rxp

 

 

 

 

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Contents
Protein chain
223 a.a. *
Ligands
SO4
169
Metals
_CA
Waters ×226
* Residue conservation analysis
PDB id:
1rxp
Name: Hydrolase
Title: Structure of trypsin (orthorhombic) with 1-(4-tert-butylcarbamoyl- piperazine-1-carbonyl)-3-(3-guanidino-propyl)-4-oxo-azetidine-2- carboxylic acid
Structure: Trypsin. Chain: a. Ec: 3.4.21.4
Source: Bos taurus. Cattle. Organism_taxid: 9913. Organ: pancreas
Resolution:
1.70Å     R-factor:   0.195     R-free:   0.222
Authors: G.S.Bisacchi,B.Jacobson
Key ref: J.C.Sutton et al. (2004). Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. Bioorg Med Chem Lett, 14, 2233-2239. PubMed id: 15081015 DOI: 10.1016/j.bmcl.2004.02.012
Date:
18-Dec-03     Release date:   08-Jun-04    
PROCHECK
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 Headers
 References

Protein chain
Pfam   ArchSchema ?
P00760  (TRY1_BOVIN) -  Serine protease 1 from Bos taurus
Seq:
Struc: 		246 a.a.
223 a.a.
Key:    PfamA domain  Secondary structure  CATH domain

 Enzyme reactions 
   Enzyme class: E.C.3.4.21.4  - trypsin.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
      Reaction: Preferential cleavage: Arg-|-Xaa, Lys-|-Xaa.

 

 
DOI no: 10.1016/j.bmcl.2004.02.012 Bioorg Med Chem Lett 14:2233-2239 (2004)
PubMed id: 15081015  
 
 
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
J.C.Sutton, S.A.Bolton, M.E.Davis, K.S.Hartl, B.Jacobson, A.Mathur, M.L.Ogletree, W.A.Slusarchyk, R.Zahler, S.M.Seiler, G.S.Bisacchi.
 
  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.
 

Literature references that cite this PDB file's key reference

  PubMed id Reference
17894328 P.Singh, S.A.Williams, M.H.Shah, T.Lectka, G.J.Pritchard, J.T.Isaacs, and S.R.Denmeade (2008).
Mechanistic insights into the inhibition of prostate specific antigen by beta-lactam class compounds.
  Proteins, 70, 1416-1428.  
The most recent references are shown first. Citation data come partly from CiteXplore and partly from an automated harvesting procedure. Note that this is likely to be only a partial list as not all journals are covered by either method. However, we are continually building up the citation data so more and more references will be included with time.

 

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