Literature DB >> 32571022

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

Gaopan Dong1, Long Chen2, Jing Zhang3, Tingting Liu1,4, Lupei Du1, Chunquan Sheng2, Minyong Li1.   

Abstract

The first small-molecule fluorescent turn-on probes for detecting PDEδ protein were rationally designed, showing reasonable fluorescent properties and the fluorescent ability has been applied for visualization of the PDEδ protein in living cells and at tissue levels. The qPCR results showed that the mRNA expression of KRAS, PDEδ, 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 PDEδ protein, as well as in obtaining a better understanding of the pathological and physiological roles of PDEδ protein.

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Year:  2020        PMID: 32571022     DOI: 10.1021/acs.analchem.0c00335

Source DB:  PubMed          Journal:  Anal Chem        ISSN: 0003-2700            Impact factor:   6.986


  3 in total

1.  Discovery of novel KRAS‒PDEδ inhibitors with potent activity in patient-derived human pancreatic tumor xenograft models.

Authors:  Long Chen; Jing Zhang; Xinjing Wang; Yu Li; Lu Zhou; Xiongxiong Lu; Guoqiang Dong; Chunquan Sheng
Journal:  Acta Pharm Sin B       Date:  2021-07-19       Impact factor: 11.413

2.  Development of PD3 and PD3-B for PDEδ inhibition to modulate KRAS activity.

Authors:  Jungeun Lee; Ho Jin Lee; Yeongcheol Lee; Bumhee Lim; Jongsik Gam; Dong-Chan Oh; Jeeyeon Lee
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

Review 3.  NBD-based synthetic probes for sensing small molecules and proteins: design, sensing mechanisms and biological applications.

Authors:  Chenyang Jiang; Haojie Huang; Xueying Kang; Liu Yang; Zhen Xi; Hongyan Sun; Michael D Pluth; Long Yi
Journal:  Chem Soc Rev       Date:  2021-07-05       Impact factor: 60.615

  3 in total

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