Synthetic lethality by lentiviral short hairpin RNA silencing of thymidylate kinase and doxorubicin in colon cancer cells regardless of the p53 status

Cancer Res. 2008 Apr 15;68(8):2831-40. doi: 10.1158/0008-5472.CAN-07-3069.

Abstract

Intracellular supply of dTTP is a highly regulated process and has been a key target for chemotherapeutic drug development. Thymidylate kinase (TMPK) is the key enzyme for dTTP formation in both de novo and salvage pathways. In this study, we used lentiviral-based small hairpin RNA to silence TMPK expression in p53(+/+) and p53(-/-) HCT-116 colon cancer cells. This approach was sufficient to decrease the dTTP pool gradually without affecting p53 expression and generating cytotoxicity. TMPK knockdown significantly increased doxorubicin sensitivity dramatically in p53-proficient, p53-null HCT-116, and LoVo colon cancer cells. The decrease in the dTTP pool using this approach augmented the DNA damage response and enhanced apoptotic induction after exposure to low-dose doxorubicin, leading to cell death. In contrast, silencing of thymidylate synthase which blocks the de novo pathway was incapable of sensitizing p53-null HCT-116 cells to doxorubicin-induced apoptosis because of the compensation by the salvage pathway. Our results suggest the lentiviral delivery of small hairpin RNA targeting TMPK in combination with a low dose of doxorubicin as a new approach to kill colon cancer cells regardless of p53 status.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibodies, Monoclonal
  • Cell Line, Tumor
  • Colonic Neoplasms
  • DNA Damage
  • Doxorubicin / toxicity*
  • Gene Silencing*
  • Genetic Vectors
  • Humans
  • Lentivirus / genetics*
  • Nucleoside-Phosphate Kinase / genetics*
  • RNA, Catalytic / genetics*
  • RNA, Small Interfering / genetics*
  • RNA, Viral / genetics*
  • Tumor Suppressor Protein p53 / antagonists & inhibitors*
  • Tumor Suppressor Protein p53 / deficiency
  • Tumor Suppressor Protein p53 / genetics*

Substances

  • Antibodies, Monoclonal
  • RNA, Catalytic
  • RNA, Small Interfering
  • RNA, Viral
  • Tumor Suppressor Protein p53
  • Doxorubicin
  • Nucleoside-Phosphate Kinase
  • dTMP kinase