Targeting nuclear import and export in hematological malignancies

Leukemia. 2020 Nov;34(11):2875-2886. doi: 10.1038/s41375-020-0958-y. Epub 2020 Jul 5.

Abstract

The transport of proteins across the nuclear membrane is a highly regulated process, essential for the cell function. This transport is actively mediated by members of the karyopherin family, termed importins, or exportins, depending on the direction of transport. These proteins play an active part in tumorigenesis, through aberrant localization of their cargoes, which include oncogenes, tumor-suppressor genes and mediators of key signal transduction pathways. Overexpression of importins and exportins is reported in many malignancies, with implications in cell growth and viability, differentiation, drug resistance, and tumor microenvironment. Given their broad significance across tumors and pathways, much effort is being put to develop specific inhibitors as a novel anticancer therapeutics. Already, selinexor, a specific inhibitor of exportin-1 (XPO1), is approved for clinical use. This review will focus on the role of importins and exportins in hematological malignancies. We will discuss current preclinical and clinical data on importins and exportins, and demonstrate how our growing understanding of their functions has identified new therapeutic targets.

Publication types

  • Review

MeSH terms

  • Active Transport, Cell Nucleus / drug effects*
  • Animals
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Biomarkers, Tumor
  • Cell Transformation, Neoplastic / drug effects
  • Cell Transformation, Neoplastic / metabolism
  • Clinical Trials as Topic
  • Drug Development
  • Gene Expression Regulation, Neoplastic / drug effects
  • Hematologic Neoplasms / drug therapy
  • Hematologic Neoplasms / etiology*
  • Hematologic Neoplasms / metabolism*
  • Hematologic Neoplasms / pathology
  • Humans
  • Karyopherins / antagonists & inhibitors
  • Karyopherins / metabolism
  • Molecular Targeted Therapy*
  • Signal Transduction / drug effects*

Substances

  • Antineoplastic Agents
  • Biomarkers, Tumor
  • Karyopherins