Regulation of volume-regulated anion channels alters sensitivity to platinum chemotherapy

Sci Adv. 2024 Dec 13;10(50):eadr9364. doi: 10.1126/sciadv.adr9364. Epub 2024 Dec 13.

Abstract

Cisplatin-based chemotherapy is used across many common tumor types, but resistance reduces the likelihood of long-term survival. We previously found the puromycin-sensitive aminopeptidase, NPEPPS, as a druggable driver of cisplatin resistance in vitro and in vivo and in patient-derived organoids. Here, we present a general mechanism where NPEPPS interacts with the volume-regulated anion channels (VRACs) to control cisplatin import into cells and thus regulate cisplatin response across a range of cancer types. We also find the NPEPPS/VRAC gene expression ratio is a predictive measure of cisplatin response in multiple cancer cohorts, showing the broad applicability of this mechanism. Our work describes a specific mechanism of cisplatin resistance, which, given the characteristics of NPEPPS as a drug target, has the potential to improve cancer patient outcomes. In addition, we describe an intracellular mechanism regulating VRAC activity, which is critical for volume regulation in normal cells - a finding with functional implications beyond cancer.

MeSH terms

  • Aminopeptidases / genetics
  • Aminopeptidases / metabolism
  • Animals
  • Antineoplastic Agents* / pharmacology
  • Cell Line, Tumor
  • Cisplatin* / pharmacology
  • Drug Resistance, Neoplasm* / genetics
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Neoplasms / drug therapy
  • Neoplasms / genetics
  • Neoplasms / metabolism
  • Neoplasms / pathology

Substances

  • Cisplatin
  • Antineoplastic Agents
  • Aminopeptidases