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6,6'-Aryl trehalose analogs as potential Mincle ligands.
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2020-05-31 , DOI: 10.1016/j.bmc.2020.115564
Omer K Rasheed 1 , George Ettenger 1 , Cassandra Buhl 2 , Robert Child 2 , Shannon M Miller 2 , Jay T Evans 3 , Kendal T Ryter 4
Affiliation  

6,6-Aryl trehalose derivatives have been synthesized with a view towards identifying novel Th-17-inducing vaccine adjuvants based on the high affinity Mincle ligand Brartemicin. The initial structure-activity relationships of these novel trehalose-based compounds were investigated. All compounds have been evaluated for their ability to engage the Mincle receptor and induce a potential pro-Th17 cytokine profile from human peripheral blood mononuclear cells based on IL-6 production in human peripheral blood mononuclear cells. The preliminary biological characterization of the designed analogs presented in this paper should aid in the future design and testing of more affine ligands that may foster the discovery of novel adjuvants with improved pharmacological properties.



中文翻译:


6,6'-芳基海藻糖类似物作为潜在的 Mincle 配体。



合成了 6,6'-基海藻糖衍生物,旨在鉴定基于高亲和力 Mincle 配体 Bratemicin 的新型 Th-17 诱导疫苗佐剂。研究了这些新型海藻糖化合物的初始结构-活性关系。所有化合物均已评估其与 Mincle 受体结合的能力,并根据人外周血单核细胞中 IL-6 的产生诱导人外周血单核细胞产生潜在的前 Th17 细胞因子谱。本文提出的设计类似物的初步生物学表征应有助于未来设计和测试更多的仿射配体,这可能促进发现具有改进的药理学特性的新型佐剂。

更新日期:2020-05-31
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