Ecteinascidin 743: A novel anticancer drug with a unique mechanism of action

Gregory J. Aune, Takahisa Furuta, Yves Pommier

Research output: Contribution to journalReview article

114 Scopus citations

Abstract

Ecteinascidin 743 (Et743) is an interesting compound in phase II/III clinical trials. Its chemistry is complex, its mechanism of action is original and it is active in human cancers, such as sarcomas refractory to conventional chemotherapy. The present review describes the discovery of the drug, its specific interactions with DNA and its reversible alkylation mechanism with guanine N2 in the DNA minor groove. Et743 is a selective transcription inhibitor, which has the unique characteristic of poisoning transcription-coupled nucleotide excision repair. Understanding the molecular pharmacology of Et743 should help in deciding which patients should receive Et743 treatments and which agents should be most useful in association.

Original languageEnglish (US)
Pages (from-to)545-555
Number of pages11
JournalAnti-cancer drugs
Volume13
Issue number6
DOIs
StatePublished - Aug 7 2002
Externally publishedYes

Keywords

  • Cancer chemotherapy
  • DNA alkylation
  • DNA binding
  • DNA repair
  • Minor groove binder
  • Transcription

ASJC Scopus subject areas

  • Oncology
  • Pharmacology
  • Pharmacology (medical)
  • Cancer Research

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