人TLR8特异性小分子激动剂的合成
Syntheses of Human TLR8-Specific Small-Molecule Agonists.
作者信息
Beesu Mallesh, Kokatla Hari Prasad, David Sunil A
机构信息
Department of Medicinal Chemistry, University of Minnesota, 2-132, Cancer & Cardiovascular Research Building, 2231 6th Street SE, Minneapolis, MN, 55455, USA.
出版信息
Methods Mol Biol. 2017;1494:29-44. doi: 10.1007/978-1-4939-6445-1_3.
Human toll-like receptor (hTLR)-8 is expressed in myeloid dendritic cells, monocytes, and monocyte-derived dendritic cells. Engagement by TLR8 agonists evokes a distinct cytokine profile which favors the development of type 1 helper T cells. Focused exploration of structure-activity relationships in the imidazoquinolines has led to the identification of several novel human TLR8-specific agonists. The synthetic procedures for best-in-class analogues encompassing four chemotypes are described.
人 toll 样受体（hTLR）-8 在髓样树突状细胞、单核细胞和单核细胞衍生的树突状细胞中表达。TLR8 激动剂与之结合会引发独特的细胞因子谱，有利于 1 型辅助性 T 细胞的发育。对咪唑喹啉类化合物构效关系的深入探索已导致鉴定出几种新型的人 TLR8 特异性激动剂。描述了包含四种化学类型的同类最佳类似物的合成方法。
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