Identification of NQO2 As a Protein Target in Small Molecule Modulation of Hepatocellular Function
Name
Schepers+-+2021+-+Main+.pdf
Description
Accepted version
Size
1.24 MB
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Unknown
Checksum (MD5)
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Author(s)
Schepers, Arnout G
Shan, Jing
Cox, Andrew G
Huang, Ada
Evans, Helen
Walesky, Chad
Fleming, Heather E
Goessling, Wolfram
Bhatia, Sangeeta N
Date Issued
August 2021
Journal
ACS Chemical Biology
Publisher
American Chemical Society (ACS)
Citation
Schepers, Arnout G, Shan, Jing, Cox, Andrew G, Huang, Ada, Evans, Helen et al. 2021. "Identification of NQO2 As a Protein Target in Small Molecule Modulation of Hepatocellular Function." ACS Chemical Biology, 16 (9).
Version
Author's final manuscript
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.
MIT Department
Koch Institute for Integrative Cancer Research at MIT
Harvard University--MIT Division of Health Sciences and Technology
Massachusetts Institute of Technology. Institute for Medical Engineering & Science
Massachusetts Institute of Technology. Department of Electrical Engineering and Computer Science
Howard Hughes Medical Institute
Terms of Use
Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International
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DOI of Published Version
https://doi.org/10.1021/ACSCHEMBIO.1C00503
