Characterization of novel small-molecule NRF2 activators: Structural and biochemical validation of stereospecific KEAP1 binding.

@article{Huerta2016CharacterizationON,
  title={Characterization of novel small-molecule NRF2 activators: Structural and biochemical validation of stereospecific KEAP1 binding.},
  author={Carlos Huerta and Xin Jiang and Isaac Trevi{\~n}o and Christopher F. Bender and Deborah A. Ferguson and Brandon L. Probst and Kerren Kalai Swinger and Vincent S. Stoll and Philip J. Thomas and Irina Dulubova and Melean Visnick and William Christian Wigley},
  journal={Biochimica et biophysica acta},
  year={2016},
  volume={1860 11 Pt A},
  pages={
          2537-2552
        }
}
BACKGROUND Semi-synthetic oleanane triterpenoid antioxidant inflammation modulators (tpAIMs) are small molecules that interact with KEAP1 cysteine residue 151 (C151) and activate NRF2. Exploration of the structure-activity relationship between the tpAIMs and KEAP1 is limited by the predominantly hydrocarbon nature of the oleanane triterpenoid pentacyclic ring structure. Therefore, we used novel, chemically-tractable, synthetic antioxidant inflammation modulators (sAIMs) to probe the… Expand
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