Discovery of small-molecule inhibitors of the TLR1/TLR2 complex

  • Angew Chem Int Ed Engl. 2012 Dec 3;51(49):12246-9. doi: 10.1002/anie.201204910.
Kui Cheng  1 ,  Xiaohui Wang ,  Shuting Zhang ,  Hang Yin
Affiliations
  • 1. Department of Chemistry and Biochemistry and the BioFrontiers Institute, University of Colorado at Boulder, Boulder, CO 80309, USA.
PMID: 22969053 DOI: 10.1002/anie.201204910
Abstract

The protein complex of Toll-like Receptor 1 and 2 (TLR1/2) is an important regulator of innate immunity, and therefore provides an attractive target for the treatment of various immune disordres. Here we report a novel compound (CU-CPT22) that can compete with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with high inhibitory activity and specificity. Repression of downstream signaling from TNF-α and IL-1β has also been observed.

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