基于表面等离子体共振技术筛选与转录因子AP-2γ具有高亲和力的小分子化合物  

Screening of Small Molecular Compounds Interacting with Transcription Factor AP-2γby Surface Plasmon Resonance from a Library of FDA Approved Drugs

作　　者：赖丹宁 张逸菲 王培鑫 林少玲[2] 胡嘉淼 LAI Dan-ning;ZHANG Yi-fei;WANG Pei-xin;LIN Shao-ling;HU Jia-miao(Engineering Research Centre of Fujian-Taiwan Special Marine Food Processing and Nutrition,Ministry of Education,Fuzhou 350002,China;College of Food Science,Fujian Agriculture and Forestry University,Fuzhou 350002,China)

机构地区：[1]闽台特色海洋食品加工及营养健康教育部工程研究中心,福建福州350002 [2]福建农林大学食品科学学院,福建福州350002

出　　处：《食品与药品》2021年第4期289-295,共7页Food and Drug

基　　金：国家自然科学基金(编号:81703065)。

摘　　要：目的从FDA批准的1018种小分子化合物中筛选与AP-2γ蛋白具有高亲和力的小分子化合物。方法采用表面等离子体共振技术,以FDA分子库的1018种小分子作为固定相,AP-2γ蛋白溶液作为流通相,筛选能高度亲和AP-2γ蛋白的小分子化合物,测定相互作用的动力学常数。结果该研究成功筛选出了80种能与目标AP-2γ蛋白特异性结合的药物分子。同时,通过结合能力动力学分布图可知这80种小分子与AP-2γ蛋白的特异性结合都是稳定的。结论筛选出与AP-2γ蛋白具有高亲和力的小分子化合物,以期为新型抗肿瘤药物的开发提供依据。Objective To screen small molecular compounds with high affinity to AP-2γprotein from 1018 small molecular compounds approved by FDA.Methods Using surface plasmon resonance(SPR)technique,1018 kinds of small molecules from FDA molecular library were used as stationary phase,and AP-2γprotein solution was used as the flow phase.The small molecule compounds with high affinity to AP-2γprotein were screened,and the kinetic constants of the interaction were determined.Results 80 drug molecules that can specifically bind to the target AP-2γprotein were successfully screened.The dynamic distribution diagram of binding ability showed that the specific binding was stable.Conclusion Small molecular compounds with high affinity to AP-2γprotein are screened in order to provide basis for the development of new antitumor drugs.

关 键 词：AP-2γ蛋白 表面等离子体共振 亲和力 抗肿瘤药物 

分 类 号：Q6-33[生物学—生物物理学] R91[医药卫生—药学]