Description:
Project ID: D2014-29
Novelty: A microplate-based, dual-assay approach using a single reagent to evaluate antibiotic activity of drug molecules during early stage development.
Background: The rise in organisms resistant to existing drugs has added urgency to the search for new antimicrobial agents. This has led the scientific community to research extensively to identify unique microbial targets for validation and new drug development to combat this growing threat of microbial resistance. In this process of new drug development it is always desirable to adopt an appropriate, convenient and affordable route to identify new drug molecules. This is particularly true for the early stage screening of novel classes of compounds, where a large number of analogues must be evaluated for antibiotic activity. Novel in vitro assays for efficacy against related nonpathogenic microbes can provide a readily obtainable and cost-effective means of establishing structure-activity relationships (SAR), designing improved analogues, and selecting promising agents for more rigorous testing.
Invention description: Researchers at the University of Toledo have established a microplate-based, dual-assay approach using a single reagent to evaluate antibiotic activity of drug candidates1. The bacterial assay uses nonpathogenic bacteria to allow efficacy testing without a dedicated microbial laboratory. This assay can be adapted to target other microbial systems, such as fungi and biofilms, as well. Application of this screening approach to antibiotic standards demonstrates the ability of this assay to identify bacterial selectivity and efficacy. When tested with selected agents, this assay shows compounds with antibiotic activity and identifies EC50 and EC90 values.
Applications: To identify new class of antibiotics via simple efficacy screening approach.
Publications:
1. Sarver JG, Trendel JA, Bearss NR, Wang L, Luniwal A, Erhardt PW, Viola RE. Early stage efficacy and toxicology screening for antibiotics and enzyme inhibitors. J Biomol Screen. 2012 Jun; 17(5):673-82. [Link]