TLR1/TLR2 复合物小分子抑制剂的发现。
Discovery of small-molecule inhibitors of the TLR1/TLR2 complex.
机构信息
Department of Chemistry and Biochemistry and the BioFrontiers Institute, University of Colorado at Boulder, Boulder, CO 80309, USA.
出版信息
Angew Chem Int Ed Engl. 2012 Dec 3;51(49):12246-9. doi: 10.1002/anie.201204910. Epub 2012 Sep 11.
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 () that can compete with the synthetic triacylated lipoprotein (PamCSK) binding to TLR1/2 with high inhibitory activity and specificity. Repression of downstream signaling from TNF-α and IL-1β has also been observed.
摘要
Toll 样受体 1 和 2（TLR1/2）的蛋白复合物是先天免疫的重要调节剂，因此为治疗各种免疫紊乱提供了有吸引力的靶标。在这里，我们报告了一种新型化合物（），它可以与合成的三酰化脂蛋白（PamCSK）竞争结合 TLR1/2，具有高抑制活性和特异性。还观察到对 TNF-α 和 IL-1β 的下游信号转导的抑制。
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