Discovery of Turn-On Fluorescent Probes for Detecting PDEδ Protein in Living Cells and Tumor Slices

被引：9

作者：

Dong, Gaopan ^{[1
]}

Chen, Long ^{[2
]}

Zhang, Jing ^{[3
]}

Liu, Tingting ^{[1
,4
]}

Du, Lupei ^{[1
]}

Sheng, Chunquan ^{[2
]}

Li, Minyong ^{[1
]}

机构：

[1] Shandong Univ, Dept Med Chem, Key Lab Chem Biol MOE, Sch Pharmaceut Sci,Cheeloo Coll Med, Jinan 250012, Shandong, Peoples R China

[2] Second Mil Med Univ, Sch Pharm, Dept Med Chem, Shanghai 200433, Peoples R China

[3] Second Mil Med Univ, Dept Pathol, Changhai Hosp, Shanghai 200433, Peoples R China

[4] Shandong First Med Univ & Shandong Acad Med Sci, Inst Pharmacol, Sch Pharmaceut Sci, Tai An 271000, Shandong, Peoples R China

来源：

ANALYTICAL CHEMISTRY | 2020年 / 92卷 / 14期

基金：

中国国家自然科学基金;

关键词：

CANCER; KRAS; INHIBITION; PATHWAYS;

D O I：

10.1021/acs.analchem.0c00335

中图分类号：

O65 [分析化学];

学科分类号：

070302 ; 081704 ;

摘要：

The first small-molecule fluorescent turn-on probes for detecting PDE delta protein were rationally designed, showing reasonable fluorescent properties and the fluorescent ability has been applied for visualization of the PDE delta protein in living cells and at tissue levels. The qPCR results showed that the mRNA expression of KRAS, PDE delta, AKT1, MAPK1, MEK7, RAF1, and mTOR were downregulated by probes 1-3 through PI3K/AKT/mTOR and MAPK signal pathways. The probes also can downregulate the protein level of pErk and tErk. Therefore, these small-molecule fluorescent probes are expected to be used in the screening of antipancreatic cancer drugs targeting the PDE delta protein, as well as in obtaining a better understanding of the pathological and physiological roles of PDE delta protein.

引用

页码：9516 / 9522

页数：7

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