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Compound NSC84167 selectively targets NRF2-activated pancreatic cancer by inhibiting asparagine synthesis pathway by Dai, Bingbing (author);Augustine, Jithesh J. (author);Kang, Ya’an (author);Roife, David (author);Li, Xinqun (author);Deng, Jenying (author);Tan, Lin (author);Rusling, Leona A. (author);Weinstein, John N. (author);Lorenzi, Philip L. (author);Kim, Michael P. (author);Fleming, Jason B. (author) is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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Nuclear factor erythroid 2-related factor 2 (NRF2) is aberrantly activated in about 93% of pancreatic cancers. Activated NRF2 regulates multiple downstream molecules involved in cancer cell metabolic reprogramming, translational control, and treatment resistance; however, targeting NRF2 for pancreatic cancer therapy remains largely unexplored. In this study, we used the online computational tool CellMiner^TM^ to explore the NCI-60 drug databases for compounds with anticancer activities correlating most closely with the mRNA expression of NQO1, a marker for NRF2 pathway activity. Among the >100,000 compounds analyzed, NSC84167, termed herein as NRF2 synthetic lethality compound-01 (NSLC01), was one of the top hits (__r__ = 0.71, __P__ < 0.001) and selected for functional characterization. NSLC01 selectively inhibited the viabilities of four out of seven conventional pancreatic cancer cell lines and induced dramatic apoptosis in the cells with high NRF2 activation. The selective anticancer activity of NSLC01 was further validated with a panel of nine low-passage pancreatic patient-derived cell lines, and a significant reverse correlation between log(IC~50~) of NSLC01 and NQO1 express

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Author

Dai, Bingbing (author);Augustine, Jithesh J. (author);Kang, Ya’an (author);Roife, David (author);Li, Xinqun (author);Deng, Jenying (author);Tan, Lin (author);Rusling, Leona A. (author);Weinstein, John N. (author);Lorenzi, Philip L. (author);Kim, Michael P. (author);Fleming, Jason B. (author)

Publisher

Springer Science and Business Media LLC

Published

2021

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)