叔丁氧甲酰基-N-ε-二甲基-L-赖氨酸置于sodium Carbonate,N,N-二异丙基乙胺,Sodium Hydroxide体系中,用 1,4-二氧六环,甲醇,二氯甲烷,水,乙腈 用作溶剂,化学反应 13.0H,反应生成Fmoc-N',N',N'-三甲基-L-赖氨酸氯化物
参考文献:Development Of A Fluorogenic Probe With A Transesterification Switch For Detection Of Histone Deacetylase Activity
标题:Development Of A Fluorogenic Probe With A Transesterification Switch For Detection Of Histone Deacetylase Activity
摘要:Histone Deacetylases (Hdacs) Are Key Enzymatic Regulators Of Many Cellular Processes Such As Gene Expression,Cell Cycle,And Tumorigenesis. These Enzymes Are Attractive Targets For Drug Development. However,Very Few Simple Methods For Monitoring Hdac Activity Have Been Reported. Here,We Have Developed A Fluorogenic Probe,K4(Ac)-Ccb,Which Consists Of The Histone H3 Peptide Containing Acetyl-Lys And A Coumarin Fluorophore With A Carbonate Ester. By The Simple Addition Of The Probe To A Hdac Solution,Enzyme Activity Was Clearly Detected Through Spontaneous Intramolecular Transesterification,Which Renders The Probe Fluorescent. In Addition,K4(Ac)-Ccb Can Be Applied To The Evaluation Of Hdac Inhibitor Activity. This Is The First Report To Demonstrate The Monitoring Of Hdac Activity By Using A One-Step Procedure. Thus,Our Novel Fluorogenic Probe Will Provide A Powerful Tool For Epigenetic Research And The Discovery Of Hdac-Targeted Drugs.
Doi:10.1021/ja306045J