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Discovery of Small‐Molecule Inhibitors of the TLR1/TLR2 Complex
Author(s) -
Cheng Kui,
Wang Xiaohui,
Zhang Shuting,
Yin Hang
Publication year - 2012
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201204910
Subject(s) - tlr2 , regulator , innate immune system , ligand (biochemistry) , psychological repression , computational biology , receptor , small molecule , chemistry , computer science , microbiology and biotechnology , biology , biochemistry , gene , gene expression
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.