Identification of Small-Molecule Inhibitors of Yersinia pestis Type III Secretion System YscN ATPase

• Published in: PloS one Vol. 6; no. 5; p. e19716
• Main Authors: Swietnicki, Wieslaw, Carmany, Daniel, Retford, Michael, Guelta, Mark, Dorsey, Russell, Bozue, Joel, Lee, Michael S., Olson, Mark A.
• Format: Journal Article
• Language: English
• Published: United States Public Library of Science 18.05.2011; Public Library of Science (PLoS)
• Subjects: Adenosine triphosphatase; Adenosine Triphosphatases - antagonists & inhibitors; Adenosine Triphosphatases - chemistry; Adenosine Triphosphatases - genetics; Adenosine Triphosphatases - secretion; Adenosine Triphosphate - metabolism; Analysis; Animals; Antibiotics; Antigens; ATPases; Bacteria; Bacterial Proteins - antagonists & inhibitors; Bacterial Proteins - chemistry; Bacterial Proteins - genetics; Bacterial Proteins - secretion; Biochemistry; Biology; Bubonic plague; Burkholderia; Burkholderia mallei - drug effects; Burkholderia mallei - enzymology; Carrier Proteins - antagonists & inhibitors; Carrier Proteins - chemistry; Carrier Proteins - genetics; Carrier Proteins - secretion; Catalysis; Catalytic Domain; Cell culture; Cell Death - drug effects; Cells (Biology); Chemistry; Clonal deletion; Disease Models, Animal; E coli; Enzyme Inhibitors - analysis; Enzyme Inhibitors - pharmacology; Enzymes; Escherichia coli; Feasibility studies; Gene Deletion; Genes, Bacterial - genetics; Gram-negative bacteria; Health aspects; HeLa Cells; Homology; Humans; Hydrolysis - drug effects; Identification methods; Infections; Infectious diseases; Inhibitors; Inhibitory Concentration 50; Kinetics; Maltose-Binding Proteins - metabolism; Mammalian cells; Mammals; Medical research; Medicine; Mice; Models, Molecular; Pasteurella; Pathogens; Plague; Plague - microbiology; Protein Multimerization - drug effects; Protein transport; Proteins; Recombinant Fusion Proteins - metabolism; Salmonella; Secretion; Sequence Homology, Amino Acid; Small Molecule Libraries - analysis; Small Molecule Libraries - pharmacology; Therapeutics; Virulence; Virulence (Microbiology); Virulence factors; Yersinia; Yersinia enterocolitica; Yersinia pestis; Yersinia pestis - drug effects; Yersinia pestis - enzymology; Yersinia pestis - genetics; Yersinia pestis - pathogenicity; Zoonoses; United States > US; Maryland

Yersinia pestis is a gram negative zoonotic pathogen responsible for causing bubonic and pneumonic plague in humans. The pathogen uses a type III secretion system (T3SS) to deliver virulence factors directly from bacterium into host mammalian cells. The system contains a single ATPase, YscN, necessa...