📜3-溴-2-氟苯胺置于磺酰氯体系中,用 二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 4.0H,反应生成7-溴-2-氯苯并噻唑
参考文献:Small Molecules Enhance Functional O-Mannosylation Of Alpha-Dystroglycan
标题:Small Molecules Enhance Functional O-Mannosylation Of Alpha-Dystroglycan
摘要:Alpha-Dystroglycan (Alpha-Dg),A Highly Glycosylated Receptor For Extracellular Matrix Proteins,Plays A Critical Role In Many Biological Processes. Hypoglycosylation Of Alpha-Dg Results In Various Types Of Muscular Dystrophies And Is Also Highly Associated With Progression Of Majority Of Cancers. Currently,There Are No Effective Treatments For Those Devastating Diseases. Enhancing Functional O-Mannosyl Glycans (Fog) Of Alpha-Dg On The Cell Surfaces Is A Potential Approach To Address This Unmet Challenge. Based On The Hypothesis That The Cells Can Up-Regulate Fog Of Alpha-Dg In Response To Certain Chemical Stimuli,We Developed A Cell-Based High-Throughput Screening (Hts) Platform For Searching Chemical Enhancers Of Fog Of Alpha-Dg From A Large Chemical Library With 364,168 Compounds. Sequential Validation Of The Hits From A Primary Screening Campaign And Chemical Works Led To Identification Of A Cluster Of Compounds That Positively Modulate Fog Of Alpha-Dg On Various Cell Surfaces Including Patient-Derived Myoblasts. These Compounds Enhance Fog Of Alpha-Dg By Almost Ten Folds,Which Provide Us Powerful Tools For O-Mannosylation Studies And Potential Starting Points For The Development Of Drug To Treat Dystroglycanopathy. (C) 2015 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2015.11.011