Reference: Venturi V, et al. (2012) The protein synthesis inhibitors mycalamides A and E have limited susceptibility toward the drug efflux network. J Biochem Mol Toxicol 26(3):94-100

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Abstract

The mycalamides belong to a family of protein synthesis inhibitors noted for antifungal, antitumour, antiviral, immunosuppressive, and nematocidal activities. Here we report a systematic analysis of the role of drug efflux pumps in mycalamide resistance and the first isolation of mycalamide E. In human cell lines, neither P-glycoprotein overexpression nor the use of efflux pump inhibitors significantly modulated mycalamide A toxicity in the systems tested. In Saccharomyces cerevisiae, it appears that mycalamide A is subject to efflux by the principle mediator of xenobiotic efflux, Pdr5p along with the major facilitator superfamily pump Tpo1p. Mycalamide E showed a similar efflux profile. These results suggest that future drugs based on the mycalamides are likely to be valuable in situations where efflux pump-based resistance leads to failure of other chemotherapeutic approaches, although efflux may be a mediator of resistance in antifungal applications.

Reference Type
Journal Article
Authors
Venturi V, Davies C, Singh AJ, Matthews JH, Bellows DS, Northcote PT, Keyzers RA, Teesdale-Spittle PH
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