University of Cincinnati

University of Delaware

Cincinnati Children's Hospital Medical Center

Guorui Li

Edward J Merino

James Mulloy

Zhihao Zhuang

Tiffany Bell-Horwath

James C Mulloy

Deubiquitinating enzyme (DUB) probes are provided that resemble native diubiquitin (diUB) with a similar linkage size and that may contain a Michael acceptor for trapping the DUB active-site cysteine. For example, both K63- and K48-linked diubiquitin probes are generated using a facile chemical ligation method, utilizing the linker compound 3-(2-(bromomethyl)-1,3-dioxolan-2-yl)prop-2-en-1-amine. The diUb probes are capable of labelling DUBs from different families and may be employed to reveal intrinsic linkage specificities of DUBs.

Method of generating linkage-specific di-and polyprotein probes

Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of reactive oxygen species (ROS) and are therefore selective anti-cancer therapeutics for cancers associated with elevated ROS. Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.

ROS-activated compounds as selective anti-cancer therapeutics

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Baltimore, MD, United States of America

Guorui Li