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.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Biflavonoids / chemistry*
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Biflavonoids / pharmacology*
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Catechin / analogs & derivatives*
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Catechin / chemistry
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Catechin / pharmacology
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Drug Discovery
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Macrophages / drug effects
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Macrophages / metabolism
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Mice
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Nitric Oxide / antagonists & inhibitors
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Nitric Oxide / biosynthesis
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Structure-Activity Relationship
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Toll-Like Receptor 1 / antagonists & inhibitors*
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Toll-Like Receptor 1 / chemistry*
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Toll-Like Receptor 2 / antagonists & inhibitors*
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Toll-Like Receptor 2 / chemistry*
Substances
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Biflavonoids
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Toll-Like Receptor 1
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Toll-Like Receptor 2
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benzotropolone
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Nitric Oxide
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Catechin