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FtsZ is an essential bacterial guanosine triphosphatase and homolog of mammalian beta-tubulin that polymerizes and assembles into a ring to initiate cell division. We have created a class of small synthetic antibacterials, exemplified by PC190723, which inhibits FtsZ and prevents cell division. PC190723 has potent and selective in vitro bactericidal activity against staphylococci, including methicillin- and multi-drug-resistant Staphylococcus aureus. The putative inhibitor-binding site of PC190723 was mapped to a region of FtsZ that is analogous to the Taxol-binding site of tubulin. PC190723 was efficacious in an in vivo model of infection, curing mice infected with a lethal dose of S. aureus. The data validate FtsZ as a target for antibacterial intervention and identify PC190723 as suitable for optimization into a new anti-staphylococcal therapy.

Titel:	An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
Autor/in / Beteiligte Person:	Haydon, DJ ; Stokes, NR ; Ure, R ; Galbraith, G ; Bennett, JM ; Brown, DR ; Baker, PJ ; Barynin, VV ; Rice, DW ; Sedelnikova, SE ; Heal, JR ; Sheridan, JM ; Aiwale, ST ; Chauhan, PK ; Srivastava, A ; Taneja, A ; Collins, I ; Errington, J ; Czaplewski, LG
Link:	Volltext (PDF)
Zeitschrift:	Science (New York, N.Y.), Jg. 321 (2008-09-19), Heft 5896, S. 1673-5
Veröffentlichung:	<Oct. 4, 1991- > : Washington, DC : American Association for the Advancement of Science ; <i>Original Publication</i>: New York, N.Y. : [s.n.] 1880-, 2008
Medientyp:	academicJournal
ISSN:	1095-9203 (electronic)
DOI:	10.1126/science.1159961
Schlagwort:	Amino Acid Sequence Animals Anti-Bacterial Agents therapeutic use Bacillus subtilis chemistry Bacillus subtilis genetics Bacterial Proteins chemistry Bacterial Proteins genetics Bacterial Proteins metabolism Binding Sites Cell Division drug effects Crystallography, X-Ray Cytoskeletal Proteins chemistry Cytoskeletal Proteins genetics Cytoskeletal Proteins metabolism Drug Resistance, Bacterial genetics Drug Resistance, Multiple, Bacterial Ligands Methicillin Resistance Mice Microbial Sensitivity Tests Models, Molecular Molecular Sequence Data Mutation Protein Conformation Pyridines chemistry Pyridines metabolism Pyridines therapeutic use Staphylococcus aureus chemistry Thiazoles chemistry Thiazoles metabolism Thiazoles therapeutic use Tubulin chemistry Tubulin metabolism Anti-Bacterial Agents pharmacology Bacillus subtilis drug effects Bacterial Proteins antagonists & inhibitors Cytoskeletal Proteins antagonists & inhibitors Pyridines pharmacology Staphylococcal Infections drug therapy Staphylococcus aureus drug effects Thiazoles pharmacology
Sonstiges:	Nachgewiesen in: MEDLINE Sprachen: English Publication Type: Journal Article; Research Support, Non-U.S. Gov't Language: English [Science] 2008 Sep 19; Vol. 321 (5896), pp. 1673-5. MeSH Terms: Anti-Bacterial Agents / pharmacology ; Bacillus subtilis / drug effects ; Bacterial Proteins / antagonists & inhibitors ; Cytoskeletal Proteins / antagonists & inhibitors ; Pyridines / pharmacology ; Staphylococcal Infections / drug therapy ; Staphylococcus aureus / drug effects ; Thiazoles / pharmacology ; Amino Acid Sequence ; Animals ; Anti-Bacterial Agents / therapeutic use ; Bacillus subtilis / chemistry ; Bacillus subtilis / genetics ; Bacterial Proteins / chemistry ; Bacterial Proteins / genetics ; Bacterial Proteins / metabolism ; Binding Sites ; Cell Division / drug effects ; Crystallography, X-Ray ; Cytoskeletal Proteins / chemistry ; Cytoskeletal Proteins / genetics ; Cytoskeletal Proteins / metabolism ; Drug Resistance, Bacterial / genetics ; Drug Resistance, Multiple, Bacterial ; Ligands ; Methicillin Resistance ; Mice ; Microbial Sensitivity Tests ; Models, Molecular ; Molecular Sequence Data ; Mutation ; Protein Conformation ; Pyridines / chemistry ; Pyridines / metabolism ; Pyridines / therapeutic use ; Staphylococcus aureus / chemistry ; Thiazoles / chemistry ; Thiazoles / metabolism ; Thiazoles / therapeutic use ; Tubulin / chemistry ; Tubulin / metabolism Comments: Comment in: Science. 2008 Sep 19;321(5896):1644-5. (PMID: 18801989) Grant Information: United Kingdom Biotechnology and Biological Sciences Research Council; United Kingdom Wellcome Trust Molecular Sequence: GENBANK EU914258; EU914259; EU914260; EU914261; EU914262; EU914263; EU914264 ; PDB 2VXY; R2VXYSF Substance Nomenclature: 0 (Anti-Bacterial Agents) ; 0 (Bacterial Proteins) ; 0 (Cytoskeletal Proteins) ; 0 (FtsZ protein, Bacteria) ; 0 (Ligands) ; 0 (PC190723) ; 0 (Pyridines) ; 0 (Thiazoles) ; 0 (Tubulin) Entry Date(s): Date Created: 20080920 Date Completed: 20081002 Latest Revision: 20220409 Update Code: 20240513

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An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.