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

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.

journal_name

Anticancer Drugs

journal_title

Anti-cancer drugs

authors

Aune GJ,Furuta T,Pommier Y

doi

10.1097/00001813-200207000-00001

subject

Has Abstract

pub_date

2002-07-01 00:00:00

pages

545-55

issue

6

eissn

0959-4973

issn

1473-5741

journal_volume

13

pub_type

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