Cancers | |
The Flavin Reductase MsuE Is a Novel Nitroreductase that Can Efficiently Activate Two Promising Next-Generation Prodrugs for Gene-Directed Enzyme Prodrug Therapy | |
Laura K. Green1  Mathew A. Storey1  Elsie M. Williams1  Adam V. Patterson2  Jeff B. Smaill2  Janine N. Copp1  | |
[1] School of Biological Sciences, Victoria University of Wellington, Kelburn Parade, Wellington 6140, New Zealand;Maurice Wilkins Centre for Molecular Biodiscovery, School of Biological Sciences, University of Auckland, Auckland 1142, New Zealand | |
关键词: gene therapy; GDEPT; nitroaromatic prodrug; nitroreductase; CB1954; PR-104A; Nitro-CBI-DEI; SOS chromotest; | |
DOI : 10.3390/cancers5030985 | |
来源: mdpi | |
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【 摘 要 】
Bacterial nitroreductase enzymes that can efficiently catalyse the oxygen-independent reduction of prodrugs originally developed to target tumour hypoxia offer great potential for expanding the therapeutic range of these molecules to aerobic tumour regions, via the emerging cancer strategy of gene-directed enzyme prodrug therapy (GDEPT). Two promising hypoxia prodrugs for GDEPT are the dinitrobenzamide mustard PR-104A, and the nitrochloromethylbenzindoline prodrug nitro-CBI-DEI. We describe here use of a nitro-quenched fluorogenic probe to identify MsuE from
【 授权许可】
CC BY
© 2013 by the authors; licensee MDPI, Basel, Switzerland.
【 预 览 】
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