Discovery of Small-Molecule Inhibitors of the TLR1/TLR2 Complex

被引：130

作者：

Cheng, Kui ^{[1
,2
]}

Wang, Xiaohui ^{[1
,2
]}

Zhang, Shuting ^{[1
,2
]}

Yin, Hang ^{[1
,2
]}

机构：

[1] Univ Colorado, Dept Chem & Biochem, Boulder, CO 80309 USA

[2] Univ Colorado, BioFrontiers Inst, Boulder, CO 80309 USA

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2012年 / 51卷 / 49期

基金：

美国国家卫生研究院;

关键词：

drug discovery; inhibitors; innate immunity; Toll-like receptors; TOLL-LIKE RECEPTORS; STAPHYLOCOCCUS-AUREUS; INNATE IMMUNITY; RECOGNITION; SPECIFICITY; POLYPHENOLS; ANTAGONIST; PROTEINS; BINDING; CANCER;

D O I：

10.1002/anie.201204910

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

An important regulator of innate immunity, the protein complex of Toll-like receptors 1 and 2 (TLR1/TLR2) provides an attractive target for the treatment of various immune disorders. The novel compound CU-CPT22 can compete with the binding of the specific lipoprotein ligand to TLR1/TLR2 (see picture) with high inhibitory activity and specificity. Repression of downstream signaling from TNF-α and IL-1β was also observed. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：12246 / 12249

页数：4

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