We thank the U.S. National Institutes of Health (DA026950, DA025740s and NS067425) for financial support of this work. The sTLR2 DNA plasmid was kindly provided by Dr. Chiaki Nishitani and Dr. Yoshio Kuroki.
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Communication
Discovery of Small-Molecule Inhibitors of the TLR1/TLR2 Complex†
Article first published online: 11 SEP 2012
DOI: 10.1002/anie.201204910
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Issue
Angewandte Chemie International Edition
Volume 51, Issue 49, pages 12246–12249, December 3, 2012
Additional Information
How to Cite
Cheng, K., Wang, X., Zhang, S. and Yin, H. (2012), Discovery of Small-Molecule Inhibitors of the TLR1/TLR2 Complex . Angew. Chem. Int. Ed., 51: 12246–12249. doi: 10.1002/anie.201204910
- †
Publication History
- Issue published online: 28 NOV 2012
- Article first published online: 11 SEP 2012
- Manuscript Received: 22 JUN 2012
Funded by
- U.S. National Institutes of Health. Grant Numbers: DA026950, DA025740, NS067425
Keywords:
- drug discovery;
- inhibitors;
- innate immunity;
- Toll-like receptors
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.