Journal
JOURNAL OF MOLECULAR EVOLUTION
Volume 81, Issue 5-6, Pages 210-217Publisher
SPRINGER
DOI: 10.1007/s00239-015-9710-z
Keywords
In vitro selection; Macrocyclic peptide; EpCAM; Fluorescent imaging probe; Cancer cell imaging
Funding
- Ministry of Health, Labor and Welfare
- Japan Society for the Promotion of Science [24681047, 15K12739]
- [7734]
- Grants-in-Aid for Scientific Research [24681047, 15K12739] Funding Source: KAKEN
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Here, we report a fluorescent probe based on a macrocyclic peptide scaffold that specifically stains EpCAM-expressing MCF7 cells. The 14-mer macrocyclic peptide binding to the extracellular domain of EpCAM with a dissociation constant in the low nM range (1.7 nM) was discovered using the random non-standard peptide-integrated discovery system. Notably, this probe containing a fluorescence tag is less than 3000 Da in total and able to visualize nearly every live cell under high cell-density conditions, which was not achieved by the conventional mAb staining method. This suggests that the molecular probe based on the compact macrocyclic scaffold has great potentials as an imaging tool for the EpCAM biomarker as well as a delivery vehicle for drug conjugates.
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