Deformylase

The natural role of peptide deformylases (EC 3.5.1.31) is the hydrolysis of the N-terminal formyl group from nascent peptides. This enzyme combines a good... 

Figure 6.37 Peptide deformylase-catalyzed hydrolysis of N-formyl amino acids.

PROTEIN STRUCTURE OF PEPTIDE DEFORMYLASES Three-dimensional Structure Metal-binding Site... 

DESIGN AND SAR OF PEPTIDE DEFORMYLASE INHIBITORS Early Substrate-based Inhibitors... 

This article summarises the general characteristics of a novel antibacterial target, peptide deformylase (PDF) and reviews the design, structure-activity relationships (SAR) and properties of known PDF inhibitors, including pre-clinical and clinical data for the most advanced members of this class. 

Peptide deformylase inhibitors, 44 (2006) 109 Peroxisome proliferator-acrtvated receptor gamma (PPARy) ligands, 42 (2004) 1 Pharmacology of Alzheimer s disease,... 

The major successes in treating bacterial infections that were achieved by the antibiotics discovered in the middle part of the last century are now under severe threat from the emergence of resistant strains. Very few new classes of antibacterial have been created in the past 20 years. Peptide deformylase represents a new biochemical target and clinical candidates are beginning to emerge. Chapter 3 reviews progress to date. 

Some of the above mentioned studies also use two-layer ONIOM QM MM approaches to include the full protein in an MM description. Other examples of QM MM calculations of metal enzymes include heme oxygenase [89], nitrate reductase [90] and peptide deformylase [91]. Finally, we note that the ONIOM (I IF Amber) potential energy surface has been directly used in a molecular dynamics study (ONIOM/MD) of cytidine deaminase [92],... 

Methyl- l-[methyl-(2-pyridin-2-yl-ethyl)amino]propane-2-thiol (108) is a tridentate N2S ligand with an aliphatic thiolate ligand. The single-crystal X-ray structures demonstrate that the zinc complexes are close structural analogs of the His2Cys site found in peptide deformylase.873... 

An enzymatic pathway for indole degradation was found in A. niger, inducible by the substrate within a 5-h period during growth. Among the enzymes found, anthranilate hydroxylase, N-formylanthranilate deformylase, 2,3-dihydroxybenzoate decarboxylase, and catechol dioxygenase were isolated, and their activities were demonstrated in a cell-free system [342],... 

Peptide Deformylase Inhibitors as Novel Antibacterial Agents. 183... 

This macrocyclic peptidomimetic compound exhibits potent inhibitory activity against Escherichia coli deformylase as well as strong antibacterial activity against both Gram-positive and Gram-negative bacteria. 

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