Small-molecule SUMO inhibition for biomarker-informed B-cell lymphoma therapy

Haematologica. 2023 Feb 1;108(2):555-567. doi: 10.3324/haematol.2022.280995.

Abstract

Aberrant activity of the SUMOylation pathway has been associated with MYC overexpression and poor prognosis in aggressive B-cell lymphoma (BCL) and other malignancies. Recently developed small-molecule inhibitors of SUMOylation (SUMOi) target the heterodimeric E1 SUMO activation complex (SAE1/UBA2). Here, we report that activated MYC signaling is an actionable molecular vulnerability in vitro and in a preclinical murine in vivo model of MYC-driven BCL. While SUMOi conferred direct effects on MYC-driven lymphoma cells, SUMO inhibition also resulted in substantial remodeling of various subsets of the innate and specific immunity in vivo. Specifically, SUMOi increased the number of memory B cells as well as cytotoxic and memory T cells, subsets that are attributed a key role within a coordinated anti-tumor immune response. In summary, our data constitute pharmacologic SUMOi as a powerful therapy in a subset of BCL causing massive remodeling of the normal B-cell and T-cell compartment.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biomarkers
  • Humans
  • Lymphoma* / drug therapy
  • Lymphoma, B-Cell* / drug therapy
  • Mice
  • Proto-Oncogene Proteins c-myc / metabolism
  • Signal Transduction
  • Ubiquitin-Activating Enzymes / metabolism

Substances

  • Proto-Oncogene Proteins c-myc
  • Biomarkers
  • UBA2 protein, human
  • Ubiquitin-Activating Enzymes

Grants and funding

Funding: This work was supported by Deutsche Forschungsgemeinschaft (DFG, SFB824/C3 and SFB1335/P3 to UK; grant KE 222/10-1 to UK and SM, DFG grants MU 1764/7-1 (#494535244) and MU 1764/7-1 to to SM), Deutsche Krebshilfe (grants 70114425 and 70114724 to UK, grant 70114823 to SM), Stiftung Charité (to UK), and Wilhelm-Sander Foundation (2017.048.2 to UK). UD is a participant in the BIH-Charité Junior Clinician Scientist program funded by the Charité - Universitätsmedizin Berlin and the Berlin Institute of Health.