Correlation Engine 2.0
Clear Search sequence regions


  • aldehyde (1)
  • cellular (1)
  • factor (4)
  • Hep (1)
  • humans (1)
  • leupeptins (2)
  • libraries (2)
  • NRF1 (8)
  • protein human (1)
  • ubiquitin (5)
  • Sizes of these terms reflect their relevance to your search.

    The transcription factor nuclear factor erythroid 2-related factor 1 (NRF1) maintains proteostasis and promotes cellular resilience by stimulating the transcription of proteasomal subunits and a host of protective enzymes. Although NRF1 activation would likely be beneficial in a number of disease states, information regarding its ligandability and upstream regulation are lacking. Herein we report a high-throughput chemical screen that identified selective stimulators of NRF1-driven transcription, including unannotated inhibitors of the ubiquitin proteasome system (UPS) as well as two non-UPS-targeted compounds that synergistically activate NRF1 in the context of submaximal UPS inhibition. This work introduces a suite of tool molecules to study the NRF1 transcriptional response and to uncover the druggable components governing NRF1 activity in cells. © 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

    Citation

    Jonathan Iaconelli, Lara Ibrahim, Emily Chen, Mitchell Hull, Peter G Schultz, Michael J Bollong. Small-Molecule Stimulators of NRF1 Transcriptional Activity. Chembiochem : a European journal of chemical biology. 2020 Jul 01;21(13):1816-1819

    Expand section icon Mesh Tags

    Expand section icon Substances


    PMID: 31596542

    View Full Text