From natural product to marketed drug: the tiacumicin odyssey

被引：66

作者：

Erb, William ^{[1
]}

Zhu, Jieping ^{[2
]}

机构：

[1] ESPCI, Chim Organ Lab, F-75231 Paris 05, France

[2] Ecole Polytech Fed Lausanne, EPFL SB ISIC LSPN, Inst Chem Sci & Engn, CH-1015 Lausanne, Switzerland

来源：

NATURAL PRODUCT REPORTS | 2013年 / 30卷 / 01期

关键词：

CLOSTRIDIUM-DIFFICILE INFECTION; IN-VITRO ACTIVITIES; RNA-POLYMERASE HOLOENZYME; FIDAXOMICIN OPT-80; BACILLUS-SUBTILIS; STRUCTURAL BASIS; TRANSCRIPTION INITIATION; BACTERIAL TRANSCRIPTION; MAJOR METABOLITE; ORAL VANCOMYCIN;

D O I：

10.1039/c2np20080e

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The first members of the tiacumicin family of antibiotics, encompassing more than 40 compounds, were isolated in 1975. Structurally, the core aglycon is an 18-membered macrolactone having two conjugated diene units, one isolated double bond, 5 stereogenic centers and most often, at least one glycosidic linkage. Tiacumicin B, a RNA synthesis inhibitor, is a narrow-spectrum antibiotic against clostridia. For the treatment of Clostridium difficile infection (CDI), it has the same cure rate as vancomycin but with lower relapse rate and was approved by the FDA in May 2011. The aim of this review is to present an overview of the chemistry and biology of tiacumicins since their discovery.

引用

页码：161 / 174

页数：14

共 120 条

[1] In vitro activity of OPT-80 against clostridium difcile [J].