PMID- 15600237 OWN - NLM STAT- MEDLINE DCOM- 20050304 LR - 20061115 IS - 1472-4472 (Print) IS - 1472-4472 (Linking) VI - 5 IP - 8 DP - 2004 Aug TI - Structure-activity relationship analysis and therapeutic potential of peptide deformylase inhibitors. PG - 809-22 AB - Peptide deformylase inhibitors (PDFIs) appear to be one of the most exciting classes of antibacterial agents discovered to date. Rapid progress in the development of PDFIs has been possible because peptide deformylase is a metalloprotease, and this class of enzymes shows a high degree of structure-function conservation, and because the most potent PDFIs are hydroxamate derivatives, a well known category of pharmacophores. The current challenge in structure-activity relationship analysis is obtaining molecules with potent in vivo antibacterial activity against a range of drug-resistant pathogens. The PDFIs currently in clinical trials target community-based bacterial infections, with a potential major pharmaceutical market. FAU - Boularot, Adrien AU - Boularot A AD - Centre National de la Recherche Scientifique, Protein Maturation Group, Institut des Sciences du Vegetal, UPR2355, Batiment 23, 1 avenue de la Terrasse, F-91198 Gif-sur-Yvette, France. FAU - Giglione, Carmela AU - Giglione C FAU - Artaud, Isabelle AU - Artaud I FAU - Meinnel, Thierry AU - Meinnel T LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Review PL - England TA - Curr Opin Investig Drugs JT - Current opinion in investigational drugs (London, England : 2000) JID - 100965718 RN - 0 (Anti-Bacterial Agents) RN - 0 (Chelating Agents) RN - 0 (Enzyme Inhibitors) RN - EC 3.5.- (Amidohydrolases) RN - EC 3.5.1.88 (peptide deformylase) SB - IM MH - Amidohydrolases/*antagonists & inhibitors/metabolism MH - Animals MH - Anti-Bacterial Agents/*pharmacology MH - Chelating Agents/pharmacology MH - Drug Resistance, Bacterial MH - Enzyme Inhibitors/chemistry/*pharmacology MH - Humans MH - Molecular Conformation MH - Structure-Activity Relationship RF - 126 EDAT- 2004/12/17 09:00 MHDA- 2005/03/05 09:00 CRDT- 2004/12/17 09:00 PHST- 2004/12/17 09:00 [pubmed] PHST- 2005/03/05 09:00 [medline] PHST- 2004/12/17 09:00 [entrez] PST - ppublish SO - Curr Opin Investig Drugs. 2004 Aug;5(8):809-22.