Science Advances

Supplementary Materials

This PDF file includes:

  • Supplementary Materials and Methods
  • fig. S1. Cellular characterization of LSD1 reversible inhibitors.
  • fig. S2. Comparison of polymyxin B and polymyxin E conformations from multiple data sets.
  • fig. S3. Characterization of the binding of E11 to LSD1-CoREST in solution by isothermal titration calorimetry.
  • fig. S4. Noncovalent quinazoline-derived compound MC3767 binds the LSD1 active site in a multiple stacking assembly as E11.
  • fig. S5. Workflow of the PDB search for multicopy stacking small-molecule inhibitors.
  • fig. S6. Comparison of histone methyltransferase G9a-like protein (GLP) and histone demethylase LSD1 in complex with compound E11.
  • fig. S7. LSD1 druggable space is expanded by the binding of noncovalent compounds.
  • table S1. Diffraction, data collection, and refinement statistics.
  • table S2. Diffraction, data collection, and refinement statistics for all data sets of polymyxins B and E.
  • table S3. List of protein inhibitor structures displaying multiple stacking conformation identified from PDB search.
  • table S4. List of published LSD1 PDB structures in complex with ligands.
  • References (3755)

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