Identification of NQO2 As a Protein Target in Small Molecule Modulation of Hepatocellular Function

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PPublication Type:

Article

Authors:

Arnout G. Schepers, Jing Shan, Andrew G. Cox, Ada Huang, Helen Evans, Chad Walesky, Heather E. Fleming, Wolfram Goessling, and Sangeeta N. Bhatia

Source:

ACS Chemical Biology (2021)

URL:

https://pubs.acs.org/doi/pdf/10.1021/acschembio.1c00503

Abstract:

The utility of in vitro human disease models is mainly dependent on the availability and functional maturity of tissue-specific cell types. We have previously screened for and identified small molecules that can enhance hepatocyte function in vitro. Here, we characterize the functional effects of one of the hits, FH1, on primary human hepatocytes in vitro, and also in vivo on primary hepatocytes in a zebrafish model. Furthermore, we conducted an analogue screen to establish the structure−activity relationship of FH1. We performed affinity-purification proteomics that identified NQO2 to be a potential binding target for this small molecule, revealing a possible link between inflammatory signaling and hepatocellular function in zebrafish and human hepatocyte model systems.


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