Environmentally sensitive fluorescent probes with improved properties for detecting and imaging PDEδ in live cells and tumor slices  

作　　者：Keliang Li Shanchao Wu Gaopan Dong Yu Li Wei Wang Guoqiang Dong Zhanying Hong Minyong Li Chunquan Sheng 

机构地区：[1]School of Pharmacy,Second Military Medical University,Shanghai 200433,China [2]Department of Medicinal Chemistry,Key Laboratory of Chemical Biology(MOE),School of Pharmaceutical Sciences,Cheeloo College of Medicine,Shandong University,Ji’nan 250012,China

出　　处：《Chinese Chemical Letters》2023年第11期214-219,共6页中国化学快报（英文版）

基　　金：supported by the National Key Research and Development Program of China(No.2020YFA0509200 to C.Sheng);National Natural Science Foundation of China(Nos.81903436 to Y.Li,82204211 to W.Wang and 22077138 to S.Wu);Shanghai Rising-Star Program(No.22QA1411300 to S.Wu).

摘　　要：Kirsten rat sarcoma viral oncogene homolog(KRAS)-phosphodiesterase-delta(PDEδ)is a promising target for antitumor drug discovery.Herein,highly efficient and environmentally sensitive fluorescent probes of PDEδ(DS-Probes)were rationally designed.As compared with the reported PDEδprobes,DS-Probes showed higher binding affinity and selectivity,which were able to conveniently and efficiently label PDEδin live cells as well as tumor tissues.Therefore,these fluorescent probes are expected to facilitate PDEδ-based mechanism elucidation,drug discovery and pathologic diagnosis.

关 键 词：ANTITUMOR PDEδ Fluorescent probes Environmentally sensitive Binding affinity 

分 类 号：R73[医药卫生—肿瘤]