2. Academic Validation
  3. Antibacterial agents that inhibit two-component signal transduction systems

Antibacterial agents that inhibit two-component signal transduction systems

  • Proc Natl Acad Sci U S A. 1998 Apr 28;95(9):5317-22. doi: 10.1073/pnas.95.9.5317.
J F Barrett 1,  R M Goldschmidt,  L E Lawrence,  B Foleno,  R Chen,  J P Demers,  S Johnson,  R Kanojia,  J Fernandez,  J Bernstein,  L Licata,  A Donetz,  S Huang,  D J Hlasta,  M J Macielag,  K Ohemeng,  R Frechette,  M B Frosco,  D H Klaubert,  J M Whiteley,  L Wang,  J A Hoch
Affiliations

Affiliation

  • 1 The R. W. Johnson Pharmaceutical Research Institute, Route 202, P.O. Box 300, Raritan, NJ 08869, USA.
PMID: 9560273 DOI: 10.1073/pnas.95.9.5317
Abstract

A class of antibacterials has been discovered that inhibits the growth of Gram-positive pathogenic bacteria. RWJ-49815, a representative of a family of hydrophobic tyramines, in addition to being a potent bactericidal Gram-positive Antibacterial, inhibits the autophosphorylation of kinase A of the KinA::Spo0F two-component signal transduction system in vitro. Analogs of RWJ-49815 vary greatly in their ability to inhibit growth of bacteria and this ability correlates directly with their activity as kinase A inhibitors. Compared with the potent Quinolone, ciprofloxacin, RWJ-49815 exhibits reduced resistance emergence in a laboratory passage experiment. Inhibition of the histidine protein kinase::response regulator two-component signal transduction pathways may present an opportunity to depress chromosomal resistance emergence by targeting multiple proteins with a single inhibitor in a single bacterium. Such inhibitors may represent a class of antibacterials that potentially may represent a breakthrough in Antibacterial therapy.

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