Aglow: A Fluorescence Assay and Machine Learning Model to Identify Inhibitors of Intracellular Infection.

Journal: ACS infectious diseases
PMID:

Abstract

is a genus of Gram-negative bacteria that has for centuries caused large-scale morbidity and mortality. In recent years, the resurgence of rickettsial diseases as a major cause of pyrexias of unknown origin, bioterrorism concerns, vector movement, and concerns over drug resistance is driving a need to identify novel treatments for these obligate intracellular bacteria. Utilizing an uvGFP plasmid reporter, we developed a screen for identifying anti-rickettsial small molecule inhibitors using as a model organism. The screening data were utilized to train a Bayesian model to predict growth inhibition in this assay. This two-pronged methodology identified anti-rickettsial compounds, including duartin and JSF-3204 as highly specific, efficacious, and noncytotoxic compounds. Both molecules exhibited growth inhibition of , the causative agent of epidemic typhus. These small molecules and the workflow, featuring a high-throughput phenotypic screen for growth inhibitors of intracellular spp. and machine learning models for the prediction of growth inhibition of an obligate intracellular Gram-negative bacterium, should prove useful in the search for new therapeutic strategies to treat infections from spp. and other obligate intracellular bacteria.

Authors

  • Alexander Lemenze
    Department of Medicine, and the Ruy V. Lourenco Center for the Study of Emerging and Reemerging Pathogens, Rutgers University - New Jersey Medical School, Medical Sciences Building, 185 South Orange Avenue, Newark, New Jersey 07103, United States.
  • Nisha Mittal
    Department of Pharmacology, Physiology, and Neuroscience, Rutgers University - New Jersey Medical School, Medical Sciences Building, 185 South Orange Avenue, Newark, New Jersey 07103, United States.
  • Alexander L Perryman
    Division of Infectious Disease, Department of Medicine, and the Ruy V. Lourenço Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University-New Jersey Medical School, Newark, New Jersey, 07103, USA.
  • Samer S Daher
    Department of Pharmacology, Physiology, and Neuroscience, Rutgers University New Jersey Medical School, I-503 185 South Orange Avenue, Newark, NJ, 07103, USA.
  • Sean Ekins
    Collaborations in Chemistry, 5616 Hilltop Needmore Road, Fuquay-Varina, NC 27526, USA; Collaborative Drug Discovery, 1633 Bayshore Highway, Suite 342, Burlingame, CA 94010, USA; Collaborations Pharmaceuticals, Inc., 5616 Hilltop Needmore Road, Fuquay-Varina, NC 27526, USA; Phoenix Nest, Inc., P.O. Box 150057, Brooklyn, NY 11215, USA; Hereditary Neuropathy Foundation, 401 Park Avenue South, 10th Floor, New York, NY 10016, USA. Electronic address: ekinssean@yahoo.com.
  • James Occi
    Department of Medicine, and the Ruy V. Lourenco Center for the Study of Emerging and Reemerging Pathogens, Rutgers University - New Jersey Medical School, Medical Sciences Building, 185 South Orange Avenue, Newark, New Jersey 07103, United States.
  • Yong-Mo Ahn
    Department of Pharmacology, Physiology, and Neuroscience, Rutgers University - New Jersey Medical School, Medical Sciences Building, 185 South Orange Avenue, Newark, New Jersey 07103, United States.
  • Xin Wang
    Key Laboratory of Bio-based Material Science & Technology (Northeast Forestry University), Ministry of Education, Harbin 150040, China.
  • Riccardo Russo
    Department of Medicine, Center for Emerging and Re-emerging Pathogens, Rutgers University Newark New Jersey 07103 USA.
  • Jimmy S Patel
    Department of Pharmacology, Physiology, and Neuroscience, Rutgers University - New Jersey Medical School, Medical Sciences Building, 185 South Orange Avenue, Newark, New Jersey 07103, United States.
  • Robin M Daugherty
    Department of Microbiology and Immunology, University of South Alabama, 5851 USA Drive North, Mobile, Alabama 36688, United States.
  • David O Wood
    Department of Microbiology and Immunology, University of South Alabama, 5851 USA Drive North, Mobile, Alabama 36688, United States.
  • Nancy Connell
    Department of Medicine, Center for Emerging and Re-emerging Pathogens, Rutgers University Newark New Jersey 07103 USA.
  • Joel S Freundlich
    Division of Infectious Disease, Department of Medicine, and the Ruy V. Lourenço Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University-New Jersey Medical School, Newark, New Jersey, 07103, USA. freundjs@rutgers.edu.