Supplementary Materials

Supplementary Material for:

Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy

William C. Stafford, Xiaoxiao Peng, Maria Hägg Olofsson, Xiaonan Zhang, Diane K. Luci, Li Lu, Qing Cheng, Lionel Trésaugues, Thomas S. Dexheimer, Nathan P. Coussens, Martin Augsten, Hanna-Stina Martinsson Ahlzén, Owe Orwar, Arne Östman, Sharon Stone-Elander, David J. Maloney, Ajit Jadhav, Anton Simeonov, Stig Linder, Elias S. J. Arnér*

*Corresponding author. Email: elias.arner{at}ki.se

Published 14 February 2018, Sci. Transl. Med. 10, eaaf7444 (2018)
DOI: 10.1126/scitranslmed.aaf7444

This PDF file includes:

  • Materials and Methods
  • Fig. S1. Structures and activities of TRi-1, TRi-2, and analogs.
  • Fig. S2. Compound reactivity with reduced GSH.
  • Fig. S3. Inhibition of human TXNRD1 and TXNRD2 by TRi-1 or auranofin.
  • Fig. S4. Inhibition of cellular TXNRD in HCT116 cells after 3 hours of treatment.
  • Fig. S5. TXNRD1 thermostabilization with inhibitors.
  • Fig. S6. Comparison of cytotoxicity profiles of TXNRD1 inhibitory small molecules within the NCI-60 cancer cell panel.
  • Fig. S7. FaDu cell colony formation assay.
  • Fig. S8. GSH depletion in FaDu cells using preincubation with BSO.
  • Fig. S9. Average mouse weights during repeated-dose toxicity study.
  • Fig. S10. Average mouse weights during MDA-MB-231 xenograft study in athymic mice.
  • Table S1. Top 53 compounds from the TXN reductase inhibitor high-throughput screen.
  • Table S2. SMILES of TRi-1, TRi-2, and analogs.
  • Table S3. Mouse liver microsome stability of TRi-1, TRi-2, and auranofin.
  • Table S4. Growth inhibition for TRi-1, TRi-2, and auranofin tested with the NCI-60 cancer cell panel.
  • Table S5. Death of mice treated with the combination of auranofin and BSO.
  • Table S6. Comparisons of effects between TRi-1 and auranofin.
  • References (5762)

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