BAP1 loss confers sensitivity to bromodomain and extra-terminal inhibitors in renal cell carcinoma

Anticancer Drugs. 2024 Nov 1;35(10):932-942. doi: 10.1097/CAD.0000000000001647. Epub 2024 Jul 23.

Abstract

The tumor suppressor gene BRCA1 associated protein-1 (BAP1) is frequently mutated in renal cell carcinoma (RCC). BAP1 loss-of-function mutations are associated with poor survival outcomes. However, personalized therapy for BAP1-mutated RCC is currently not available. Previously, we found that BAP1 loss renders RCC cells more sensitive to bromodomain and extra-terminal (BET) inhibitors, as demonstrated in both cell culture and xenografted nude mice models. Here, we demonstrate that BAP1 loss in murine RCC cells enhances sensitivity to BET inhibitors in ectopic and orthotopic allograft models. While BAP1 deletion suppresses RCC cell survival in vitro , it does not impede tumor growth in immunocompetent murine models. Thus, the effect of BAP1 loss on the interactions between tumor cells and host microenvironment plays a predominant role in RCC growth, highlighting the importance of utilizing immunocompetent animal models to assess the efficacy of potential anticancer therapies. Mechanistically, BAP1 deletion compromises DNA repair capacity, rendering RCC cells more vulnerable to DNA damage induced by BET inhibitors. Our results indicate that BET inhibitors show promise as targeted therapy for BAP1-deficient RCC.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Bromodomain Containing Proteins
  • Carcinoma, Renal Cell* / drug therapy
  • Carcinoma, Renal Cell* / genetics
  • Carcinoma, Renal Cell* / pathology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • DNA Repair
  • Female
  • Humans
  • Kidney Neoplasms* / drug therapy
  • Kidney Neoplasms* / genetics
  • Kidney Neoplasms* / pathology
  • Mice
  • Mice, Nude
  • Proteins
  • Tumor Suppressor Proteins* / genetics
  • Ubiquitin Thiolesterase* / genetics
  • Xenograft Model Antitumor Assays

Substances

  • Tumor Suppressor Proteins
  • Ubiquitin Thiolesterase
  • BAP1 protein, human
  • BAP1 protein, mouse
  • Antineoplastic Agents
  • bromodomain and extra-terminal domain protein, human
  • Bromodomain Containing Proteins
  • Proteins