Science Advances

Supplementary Materials

This PDF file includes:

  • fig. S1. Topology of BRD cavity and binding of chemical scaffolds containing different potential expansion vectors.
  • fig. S2. Structure-activity relationship of the triazolopyridazine class leading to BSP.
  • fig. S3. BSP inhibits growth of cancer cell lines.
  • fig. S4. Effect of BSP and JQ1 on leukemia cell lines.
  • fig. S5. Effect of BSP and JQ1 on leukemia cell lines.
  • fig. S6. Gene expression GO enrichment (biological processes).
  • fig. S7. Gene expression after inhibition of leukemia cell lines with BSP or JQ1.
  • fig. S8. GSEA of K562 and KASUMI-1 cell lines after BSP treatment.
  • fig. S9. GSEA of MV4;11 and OCI-AML3 cell lines after BSP treatment.
  • fig. S10. Effect of BSP on BET-specific genes.
  • fig. S11. Expression of BRD-containing proteins in leukemic cell lines.
  • fig. S12. Effects of the selective inhibition of different BRD subfamilies on transcriptional programs in leukemias.
  • fig. S13. Transcriptional response in leukemia cell lines and inhibitor combination.
  • fig. S14. GSEA comparison of BSP and JQ1 effects on leukemias.
  • fig. S15. BSP profile of cellular receptor activity (ExpresSProfile; CEREP).
  • Legends for tables S1 and S2
  • table S3. BSP profile of cellular receptor activity data (ExpresSProfile; CEREP).
  • table S4. Data collection and refinement statistics for BRD-BSP complexes.
  • table S5. Primers used for qRT-PCR.

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Other Supplementary Material for this manuscript includes the following:

  • table S1 (Microsoft Excel format). Differential scanning fluorimetry profiling of triazolopyridazines against a panel of BRD modules.
  • table S2 (Microsoft Excel format). MetaCore analysis of gene expression data.

Download tables S1 and S2

Files in this Data Supplement: