Bioorganic & medicinal chemistry letters

Bexarotene prodrugs: Targeting through cleavage by NQO1 (DT-diaphorase)

A Schäfer, ES Burstein, R Olsson

Index: Schaefer, Anja; Burstein, Ethan S.; Olsson, Roger Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 8 p. 1944 - 1947

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Citation Number: 8

Abstract

Abstract Bexarotene, a retinoid X receptor (RXR) agonist, is being tested as a potential disease modifying treatment for neurodegenerative conditions. To limit the peripheral exposure of bexarotene and release it only in the affected areas of the brain, we designed a prodrug strategy based on the enzyme NAD (P) H/quinone oxidoreductase (NQO1) that is elevated in neurodegenerative diseases. A series of indolequinones (known substrates of ...