1s17 | pdb_00001s17
Identification of Novel Potent Bicyclic Peptide Deformylase Inhibitors
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Overview
Screening of our compound collection using Staphylococcus aureus, Ni-Peptide deformylase (PDF) afforded a very potent PDF inhibitor with an, IC(50) in the low nanomolar range but with poor antibacterial activity, (MIC). Three-dimensional structural information obtained from Pseudomonas, aeruginosa Ni-PDF complexed with the inhibitor suggested the synthesis of, a variety of analogues that would maintain high binding affinity while, attempting to improve antibacterial activity. Many of the compounds, synthesized proved to be excellent PDF-Ni inhibitors and some showed, increased antibacterial activity in selected strains.
About this Structure
1S17 is a Single protein structure of sequence from Pseudomonas aeruginosa with NI, GNR and GOL as ligands. Active as Peptide deformylase, with EC number 3.5.1.88 Full crystallographic information is available from OCA.
Reference
Identification of novel potent bicyclic peptide deformylase inhibitors., Molteni V, He X, Nabakka J, Yang K, Kreusch A, Gordon P, Bursulaya B, Warner I, Shin T, Biorac T, Ryder NS, Goldberg R, Doughty J, He Y, Bioorg Med Chem Lett. 2004 Mar 22;14(6):1477-81. PMID:15006385
Page seeded by OCA on Wed Nov 21 02:01:41 2007
