2. Academic Validation
  3. Development of coumarin and procaine linked hybrid molecules as a novel class of SHP1 fluorescent activators

Development of coumarin and procaine linked hybrid molecules as a novel class of SHP1 fluorescent activators

  • Eur J Med Chem. 2025 Apr 15:288:117394. doi: 10.1016/j.ejmech.2025.117394.
Xu-Yang Mu 1,  Li-Xin Gao 2,  Zhen-Xuan Zhang 3,  Zi-Tong Cao 4,  Qing Cao 5,  Chun Zhang 5,  Jia Li 6,  Da-Jun Xiang 7,  Yu-Bo Zhou 8,  Wen-Long Wang 9
Affiliations

Affiliations

  • 1 School of Life Sciences and Health Engineering, Jiangnan University, Wuxi, 214122, China; School of Chemical and Material Engineering, Jiangnan University, Wuxi, 214122, China.
  • 2 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
  • 3 School of Life Sciences and Health Engineering, Jiangnan University, Wuxi, 214122, China; Zhongshan Institute for Drug Discovery, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Zhongshan Tsuihang New District, Guangdong, 528400, China.
  • 4 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; Institute of Pharmaceutical Science, China Pharmaceutical University, Nanjing, Jiangsu, 210009, China.
  • 5 School of Life Sciences and Health Engineering, Jiangnan University, Wuxi, 214122, China.
  • 6 Zhongshan Institute for Drug Discovery, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Zhongshan Tsuihang New District, Guangdong, 528400, China.
  • 7 Xishan People's Hospital of Wuxi City, Wuxi, Jiangsu, 214105, China. Electronic address: xiangdjxshospital@yeah.net.
  • 8 Zhongshan Institute for Drug Discovery, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Zhongshan Tsuihang New District, Guangdong, 528400, China. Electronic address: ybzhou@simm.ac.cn.
  • 9 School of Life Sciences and Health Engineering, Jiangnan University, Wuxi, 214122, China; School of Chemical and Material Engineering, Jiangnan University, Wuxi, 214122, China. Electronic address: wenlongwang@jiangnan.edu.cn.
PMID: 39987836 DOI: 10.1016/j.ejmech.2025.117394
Abstract

The development of small fluorescent organic molecules used in bioimaging experiment has boomed the progress of molecular and cellular biology, providing new and efficient tools to elucidate a myriad of cellular and multicellular processes. In this work, a class of fluorescent activators against SHP1 was designed and synthesized for the first time. The representative compound 3n showed activating effect against SHP1 with EC50 of 17.66 ± 1.48 μM and a fluorescence quantum yield of 0.521 in DMSO. Meanwhile, 3n showed good selectivity for SHP1, inhibited the proliferation of SU-DHL-2 cells and OCI-Ly10 cells with IC50 of 8.66 ± 1.26 μM and 9.16 ± 0.53 μM and exhibited potential for cellular imaging on human breast Cancer cells.

Keywords

Cellular imaging; Coumarin-procaine hybrid molecules; Fluorescent organic molecules; SHP1; Selectivity for SHP1 homologous proteins.

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