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

Gregory J. Aune; Takahisa Furuta; Yves Pommier

doi:10.1097/00001813-200207000-00001

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

Gregory J. Aune, Takahisa Furuta, Yves Pommier

Research output: Contribution to journal › Review article › peer-review

130 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 language	English (US)
Pages (from-to)	545-555
Number of pages	11
Journal	Anti-cancer drugs
Volume	13
Issue number	6
DOIs	https://doi.org/10.1097/00001813-200207000-00001
State	Published - 2002
Externally published	Yes

Keywords

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

ASJC Scopus subject areas

Pharmacology (medical)
Oncology
Cancer Research
Pharmacology

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10.1097/00001813-200207000-00001

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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.",

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AU - Furuta, Takahisa

AU - Pommier, Yves

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N2 - 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.

AB - 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.

KW - Cancer chemotherapy

KW - DNA alkylation

KW - DNA binding

KW - DNA repair

KW - Minor groove binder

KW - Transcription

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

Abstract

Keywords

ASJC Scopus subject areas

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