Antiplasmodial Thiostrepton Derivatives: Proteasome Inhibitors with a Dual Mode of Action

被引：71

作者：

Schoof, Sebastian ^{[4
,5
]}

Pradel, Gabriele ^{[1
]}

Aminake, Makoah N. ^{[1
]}

Ellinger, Bernhard ^{[4
,5
]}

Baumann, Sascha ^{[4
,5
]}

Potowski, Marco ^{[4
,5
]}

Najajreh, Yousef ^{[3
,4
,5
]}

Kirschner, Marc ^{[2
]}

Arndt, Hans-Dieter ^{[4
,5
]}

机构：

[1] Univ Wurzburg, Zentrum Infekt Forsch, D-97080 Wurzburg, Germany

[2] Univ Wurzburg, Inst Virol & Immunbiol, D-97078 Wurzburg, Germany

[3] Al Quds Univ, Fac Pharm, IL-20002 Jerusalem, Israel

[4] Tech Univ Dortmund, Fak Chem, D-44221 Dortmund, Germany

[5] Max Planck Inst Mol Physiol, D-44227 Dortmund, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2010年 / 49卷 / 19期

关键词：

antimalarial agents; drug design; natural products; proteasome; thiopeptides; PLASMODIUM-FALCIPARUM; THIOPEPTIDE ANTIBIOTICS; LACTATE-DEHYDROGENASE; IN-VIVO; APICOPLAST; TRANSLATION; BINDING; TARGET; SITES; PROBE;

D O I：

10.1002/anie.200906988

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

(Figure Presented) Two birds, one stone: Semisynthetic derivatives of the ribosomal inhibitor thiostrepton display up to ten times higher antiplasmodial activity than the natural product itself. This activity was correlated with selective functional inhibition of the 20S proteasome. Thiostrepton derivatives are now established as novel antimalarials with a dual mode of action and highly promising scaffolds for proteasome inhibitor development. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：3317 / 3321

页数：5

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