Journal
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 133, Issue 11, Pages 3764-3767Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ja111312h
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Funding
- National Institutes of Health [DA026950, DA025740, NS067425, RR025780, DA029119]
- China Scholarship Council [2009619072]
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The protein-RNA interface has been regarded as undruggable despite its importance in many biological processes. The toll-like receptor 3 (TLR3)/double-stranded RNA (dsRNA) complex provides an exciting target for a number of infectious diseases and cancers. We describe the development of a series of small-molecule probes that were shown to be competitive inhibitors of dsRNA binding to TLR3 with high affinity and specificity. In a multitude of assays, compound 4a was profiled as a potent antagonist to TLR3 signaling and also repressed the expression of downstream signaling pathways mediated by the TLR3/dsRNA complex, including TNF-alpha and IL-1 beta.
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