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New strategies to inhibit KEAP1 and the Cul3-based E3 ubiquitin ligases by Peter Canning, and Alex N. Bullock Biochm. Soc. Trans. Volume 42(1):103-107 February 1, 2014 ©2014 by Portland Press Ltd
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Regulation of Nrf2Under basal conditions, Nrf2 is polyubiquitylated by the KEAP1–Cul3 E3 ligase and subsequently degraded by the proteasome. Peter Canning, and Alex N. Bullock Biochm. Soc. Trans. 2014;42:103-107 ©2014 by Portland Press Ltd
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Model of the KEAP1 CRL3 structure and potential sites for small-molecule inhibitorsThe KEAP1– Nrf2 crystal structure (PDB code 2FLU) [45] is shown alongside an early inhibitor of this interaction [46]. Peter Canning, and Alex N. Bullock Biochm. Soc. Trans. 2014;42:103-107 ©2014 by Portland Press Ltd
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