Journal
JOURNAL OF NATURAL PRODUCTS
Volume 79, Issue 4, Pages 1193-1197Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.5b01091
Keywords
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Funding
- University of Oklahoma Junior Faculty Fellowship
- Oklahoma Center for the Advancement of Science and Technology (OCAST) [HR15-161]
- University of Oklahoma start-up funding
- Undergraduate Research Opportunity Program (UROP) Award
- Institutional Development Award (IDeA) from National Institute of General Medical Sciences of the National Institutes of Health [P20GM103640]
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Caseinolytic protease P (ClpP) maintains essential roles in bacterial homeostasis. As such, both the inhibition and activation of this enzyme result in bactericidal activity, making ClpP a promising target for antibacterial drug development. Herein, we report the results of a fluorescence-based screen of similar to 450 structurally diverse fungal and bacterial secondary metabolites. Sclerotiamide (1), a paraherquamide-related indolinone, was identified as the first non-peptide-based natural product activator of ClpP. Structure-activity relationships arising from the initial screen, preliminary biochemical evaluation of 1, and rationale for the exploitation of this chemotype to develop novel ClpP activators are presented.
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