Photosensitization of Bacterial Pathogens through Small Molecule Activators of Heme Biosynthesis

Abstract

Gram-positive bacteria cause the majority of skin and soft tissue infections (SSTIs), resulting in the most common reason for clinic visits in the United States. Recently, it was discovered that Gram-positive pathogens utilize a unique heme biosynthesis pathway, which implicates this pathway as a novel target for development of antibacterial therapies. We report here the identification of a small molecule activator of coproporphyrinogen oxidase (HemY) from Gram-positive bacteria, an enzyme essential for heme biosynthesis. Activation of HemY induces accumulation of coproporphyrin III and leads to photosensitization of Gram-positive pathogens. In combination with light, HemY activation reduces bacterial burden and tissue ulceration in murine models of SSTI. Thus, small molecule activation of HemY represents an effective strategy for the development of light-bases antimicrobial therapies.

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Document Details

Document Type
Technical Report
Publication Date
Dec 01, 2017
Accession Number
AD1059208

Entities

People

  • Duco Jansen
  • Eric P. Skaar
  • Gary Sulikowski

Organizations

  • Vanderbilt University

Tags

Communities of Interest

  • Advanced Electronics
  • Energy and Power Technologies

DTIC Thesaurus Topics

  • Amino Acids
  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Bacteria
  • Bacterial Infections
  • Biomedical Research
  • Chemical Synthesis
  • Chemistry
  • Dermatologic Agents
  • Gram-Positive Bacteria
  • Health Services
  • Infection
  • Infectious Diseases
  • Light Sources
  • Medical Personnel
  • Microbiology
  • Organic Chemistry
  • Skin Diseases
  • Soft Tissues
  • Therapy
  • Tissues
  • United States

Readers

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