Interrogation of the Structure-Activity Relationship of a Lipophilic Nitroaromatic Prodrug Series Designed for Cancer Gene Therapy Applications

• Main Authors: Amir Ashoorzadeh (Author), Alexandra M. Mowday (Author), Christopher P. Guise (Author), Shevan Silva (Author), Matthew R. Bull (Author), Maria R. Abbattista (Author), Janine N. Copp (Author), Elsie M. Williams (Author), David F. Ackerley (Author), Adam V. Patterson (Author), Jeff B. Smaill (Author)
• Format: Book
• Published: MDPI AG, 2022-02-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

PR-104A is a dual hypoxia/nitroreductase gene therapy prodrug by virtue of its ability to undergo either one- or two-electron reduction to its cytotoxic species. It has been evaluated extensively in pre-clinical GDEPT studies, yet off-target human aldo-keto reductase AKR1C3-mediated activation has l...