Eltrombopag promotes DNA repair in human hematopoietic stem and progenitor cells

Exp Hematol. 2019 May:73:1-6.e6. doi: 10.1016/j.exphem.2019.03.002. Epub 2019 Apr 13.

Abstract

A causal link between hematopoietic stem/progenitor cell (HSPC) dysfunction and DNA damage accrual has been proposed. Clinically relevant strategies to maintain genome integrity in these cells are needed. Here we report that eltrombopag, a small molecule agonist of the thrombopoietin (TPO) receptor used in the clinic, promotes DNA double-strand break (DSB) repair in human HSPCs. We found that eltrombopag specifically activates the classic nonhomologous end-joining (C-NHEJ) DNA repair mechanism, a pathway known to support genome integrity. Eltrombopag-mediated DNA repair results in enhanced genome stability, survival, and function of primary human HSPCs, as demonstrated in karyotyping analyses, colony-forming unit assays and after transplantation in immunodeficient NSG mice. Eltrombopag may offer a new therapeutic modality to protect human HSPCs against genome insults.

Publication types

  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzoates / pharmacology*
  • Cells, Cultured
  • DNA Breaks, Double-Stranded*
  • DNA End-Joining Repair / drug effects*
  • Hematopoietic Stem Cells / metabolism*
  • Humans
  • Hydrazines / pharmacology*
  • Pyrazoles / pharmacology*
  • Receptors, Thrombopoietin / metabolism

Substances

  • Benzoates
  • Hydrazines
  • Pyrazoles
  • Receptors, Thrombopoietin
  • MPL protein, human
  • eltrombopag