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Potential applications of BPFP1 in Bcl-2 protein quantification, carcinoma cell visualization, cell sorting and early cancer diagnosis.

Abstract
Overexpression of the Bcl-2 protein has emerged as a hallmark of carcinoma cells and can be employed as a biochemical biomarker of these cells. Therefore, some Bcl-2 protein fluorescence probes (BPFPs) were designed for Bcl-2 protein quantification and carcinoma cells labeling. The high Bcl-2 protein binding affinity (Ki < 1 nM) and selectivity (over 50,000-fold Bcl-2 protein selectivity against Mcl-1 protein) of BPFP1 endow it with the ability to detect trace amounts of Bcl-2 protein. After being incubated with a range of concentrations of Bcl-2 protein, BPFP1 exhibited the desired fluorescence properties and its fluorescence intensity is proportional to Bcl-2 protein concentration. Therefore, BPFP1 provides a convenient approach for Bcl-2 protein quantification and we could determine the concentration of Bcl-2 protein based on the BPFP1's fluorescence intensity. Subsequent studies revealed that BPFP1 can fluorescently label carcinoma cells by binding to overexpressed Bcl-2 protein in living cells, and can distinguish carcinoma cells (HL-60 cells and ACHN cells) from normal-tissue cells (HUVECs) according to the different Bcl-2 protein expression levels between carcinoma cells and normal tissue cells. In the present study, BPFP1 represents a new tool for Bcl-2 protein quantification, carcinoma cell visualization and cell sorting. Moreover, BPFP1 can be used in the future for early cancer diagnosis by detecting carcinoma cells in patient tissues.
AuthorsTao Liang, Jia Li, Yi Zhou, Xuben Hou, Xinying Yang, Hao Fang
JournalEuropean journal of medicinal chemistry (Eur J Med Chem) Vol. 224 Pg. 113725 (Nov 15 2021) ISSN: 1768-3254 [Electronic] France
PMID34375882 (Publication Type: Journal Article)
CopyrightCopyright © 2021 Elsevier Masson SAS. All rights reserved.
Chemical References
  • BCL2 protein, human
  • Proto-Oncogene Proteins c-bcl-2
Topics
  • Carcinoma (genetics)
  • Cell Line, Tumor
  • Early Detection of Cancer (methods)
  • Flow Cytometry (methods)
  • Humans
  • Proto-Oncogene Proteins c-bcl-2 (metabolism)

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