Phosphorylation of BlaR1 in Manifestation of Antibiotic Resistance in Methicillin-Resistant Staphylococcus aureus and Its Abrogation by Small Molecules.

Academic Article


  • Methicillin-resistant Staphylococcus aureus (MRSA), an important human pathogen, has evolved an inducible mechanism for resistance to β-lactam antibiotics. We report herein that the integral membrane protein BlaR1, the β-lactam sensor/signal transducer protein, is phosphorylated on exposure to β-lactam antibiotics. This event is critical to the onset of the induction of antibiotic resistance. Furthermore, we document that BlaR1 phosphorylation and the antibiotic-resistance phenotype are both reversed in the presence of synthetic protein kinase inhibitors of our design, restoring susceptibility of the organism to a penicillin, resurrecting it from obsolescence in treatment of these intransigent bacteria.
  • Authors

  • Boudreau, Marc
  • Fishovitz, Jennifer
  • Llarrull, Leticia I
  • Xiao, Qiaobin
  • Mobashery, Shahriar
  • Status

    Publication Date

  • October 9, 2015
  • Published In


  • BlaR1
  • MRSA
  • Stk1
  • kinase inhibitor
  • phosphorylation
  • Digital Object Identifier (doi)

    Start Page

  • 454
  • End Page

  • 459
  • Volume

  • 1
  • Issue

  • 10