Synthesis of a BODIPY library and its application to the development of live cell glucagon imaging probe
- Synthesis of a BODIPY library and its application to the development of live cell glucagon imaging probe
- 이준석; 강남영; 김윤경; Samanta Animesh; Feng Suihan; 김형규; Vendrell Marc; 박정환; 장영태
- fluorecence probe; diversity-oriented synthesis; library; glucagon
- Issue Date
- Journal of the American Chemical Society
- VOL 131, NO 29, 10077-10082
- The first BODIPY library (BD) was synthesized, and a highly selective glucagon sensor, Glucagon
Yellow (BD-105), was discovered by fluorescence image-based screening method. BD library was
synthesized via a Knoevenagel-type condensation reaction with 160 benzaldehydes and the 1,3 dimethyl-
BODIPY scaffold. Using BD compounds, a fluorescence image-based screening was performed against
three cell lines including AlphaTC1 and BetaTC6 cells which secret glucagon and insulin, respectively,
and HeLa as control cells. Out of the 160 candidate probes, one compound, Glucagon Yellow, exhibited
selective staining only in AlphaTC1 cells. The selectivity of Glucagon Yellow toward glucagon was confirmed
in vitro by comparison of its fluorescence intensity change against 19 biologically relevant analytes.
Subsequent immunostaining experiments revealed that Glucagon Yellow and the glucagon antibody
colocalized in pancreas tissue, showing a high quantitative correlation analysis by the Pearson’s coefficient
constant (Rr ) 0.950). These results demonstrated the potential application of Glucagon Yellow as a
glucagon imaging agent in live cells and tissues.
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