Discovery of small-molecule fluorescent probes for C-Met

Eur J Med Chem. 2022 Feb 15:230:114114. doi: 10.1016/j.ejmech.2022.114114. Epub 2022 Jan 12.

Abstract

C-mesenchymal-epithelia transition factor (c-Met) is highly expressed in various solid tumors such as gastric cancer, liver cancer, and lung cancer, playing a pivotal role in the growth, maintenance, and development of different tumor cells. In this study, three small-molecule fluorescent probes (5, 11, 16) targeting c-Met were developed, and their design strategies were also initially explored. In general, the fluorescence properties of the probes themselves could meet the imaging requirements, and they have shown sufficient inhibitory activities against c-Met, especially probe 16, reflecting the targeting and acceptance. Also, fluorescence polarization assays and flow cytometry analysis verified the binding between the probes and c-Met. Cell imaging confirmed that these probes could be used to label c-Met on living cells. It is of positive significance for the development of c-Met kinase inhibitors and tumor pathology research.

Keywords: C-Met; Cancers; Cell imaging; Fluorescent inhibitors; Fluorescent probes.

MeSH terms

  • Cell Line, Tumor
  • Fluorescent Dyes*
  • Humans
  • Neoplasms
  • Proto-Oncogene Proteins c-met / analysis*

Substances

  • Fluorescent Dyes
  • Proto-Oncogene Proteins c-met