Ecteinascidin 743: a novel anticancer drug with a unique mechanism of action
作者:
Gregory Aune,
Takahisa Furuta,
Yves Pommier,
期刊:
Anti-Cancer Drugs
(OVID Available online 2002)
卷期:
Volume 13,
issue 6
页码: 545-555
ISSN:0959-4973
年代: 2002
出版商: OVID
关键词: Cancer chemotherapy;DNA alkylation;DNA binding;DNA repair;minor groove binder;transcription
数据来源: OVID
摘要:
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 guanineN2in 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.
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