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3-hydroxy-1-alkyl-2-methylpyridine-4(1H)-thiones: inhibition of the Pseudomonas aeruginosa virulence factor LasB

Academic Article
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Overview

related to degree

  • Moreno, Amira, Ph.D. in Chemistry, Scripps Research 2006 - 2012

authors

  • Garner, A. L.
  • Struss, A. K.
  • Fullagar, J. L.
  • Agrawal, A.
  • Moreno, Amira
  • Cohen, S. M.
  • Janda, Kim

publication date

  • August 2012

journal

  • ACS Medicinal Chemistry Letters  Journal

abstract

  • Bacterial resistance coupled to our current arsenal of antibiotics presents us with a growing threat to public health, thus warranting the exploration of alternative antibacterial strategies. In particular, the targeting of virulence factors has been regarded as a "second generation" antibiotic approach. In Pseudomonas aeruginosa, a Zn(2+) metalloprotease virulence factor, LasB or P. aeruginosa elastase, has been implicated in the development of P. aeruginosa-related keratitis, pneumonia and burn infection. Moreover, the enzyme also plays a critical role in swarming and biofilm formation, both of which are processes that have been linked to antibiotic resistance. To further validate the importance of LasB in P. aeruginosa infection, we describe our efforts toward the discovery of non-peptidic small molecule inhibitors of LasB. Using identified compounds, we have confirmed the role that LasB plays in P. aeruginosa swarming and demonstrate the potential for LasB-targeted small molecules in studying antimicrobial resistant P. aeruginosa phenotypes.
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Research

keywords

  • antibiotics
  • hydroxypyridinthiones
  • metalloprotease inhibitors
  • virulence factors
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Identity

PubMed Central ID

  • PMC3501683

International Standard Serial Number (ISSN)

  • 1948-5875

Digital Object Identifier (DOI)

  • 10.1021/ml300128f

PubMed ID

  • 23181168
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Additional Document Info

start page

  • 668

end page

  • 672

volume

  • 3

issue

  • 8

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