In situ imaging of quantum dot-AZD4547 conjugates for tracking the dynamic behavior of fibroblast growth factor receptor 3

Gyoyeon Hwang,1,2,* Hyeonhye Kim,1,* Hojong Yoon,1 Chiman Song,1 Dong-Kwon Lim,3 Taebo Sim,1,3 Jiyeon Lee1,2 1Chemical Kinomics Research Center, Materials and Life Science Research Division, Korea Institute of Science and Technology, Seoul, 2Bio-Med, Korea University of Science and Technology, Daej...

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Autores principales: Hwang G, Kim H, Yoon H, Song C, Lim D, Sim T, Lee J
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Publicado: Dove Medical Press 2017
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spelling oai:doaj.org-article:f3ac4e4e397b47b2abdbc655996253c02021-12-02T02:10:26ZIn situ imaging of quantum dot-AZD4547 conjugates for tracking the dynamic behavior of fibroblast growth factor receptor 31178-2013https://doaj.org/article/f3ac4e4e397b47b2abdbc655996253c02017-07-01T00:00:00Zhttps://www.dovepress.com/in-situ-imaging-of-quantum-dot-azd4547-conjugates-for-tracking-the-dyn-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Gyoyeon Hwang,1,2,* Hyeonhye Kim,1,* Hojong Yoon,1 Chiman Song,1 Dong-Kwon Lim,3 Taebo Sim,1,3 Jiyeon Lee1,2 1Chemical Kinomics Research Center, Materials and Life Science Research Division, Korea Institute of Science and Technology, Seoul, 2Bio-Med, Korea University of Science and Technology, Daejeon, 3KU-KIST Graduate School of Converging Science and Technology, Korea University, Seoul, Republic of Korea *These authors contributed equally to this work Abstract: Fibroblast growth factor receptors (FGFRs) play an important role in determining cell proliferation, differentiation, migration, and survival. Although a variety of small-molecule FGFR inhibitors have been developed for cancer therapeutics, the interaction between FGFRs and FGFR inhibitors has not been well characterized. The FGFR–inhibitor interaction can be characterized using a new imaging probe that has strong, stable signal properties for in situ cellular imaging of the interaction without quenching. We developed a kinase–inhibitor-modified quantum dot (QD) probe to investigate the interaction between FGFR and potential inhibitors. Especially, turbo-green fluorescent protein-FGFR3s were overexpressed in HeLa cells to investigate the colocalization of FGFR3 and AZD4547 using the QD-AZD4547 probe. The result indicates that this probe is useful for investigating the binding behaviors of FGFR3 with the FGFR inhibitor. Thus, this new inhibitor-modified QD probe is a promising tool for understanding the interaction between FGFR and inhibitors and for creating future high-content, cell-based drug screening strategies. Keywords: quantum dot, fibroblast growth factor 3, AZD4547, kinase–inhibitor, in situ imagingHwang GKim HYoon HSong CLim DSim TLee JDove Medical PressarticleQuantum dotFibroblast growth factor 3AZD4547kinase-inhibitorIn situ imagingMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 5345-5357 (2017)
institution DOAJ
collection DOAJ
language EN
topic Quantum dot
Fibroblast growth factor 3
AZD4547
kinase-inhibitor
In situ imaging
Medicine (General)
R5-920
spellingShingle Quantum dot
Fibroblast growth factor 3
AZD4547
kinase-inhibitor
In situ imaging
Medicine (General)
R5-920
Hwang G
Kim H
Yoon H
Song C
Lim D
Sim T
Lee J
In situ imaging of quantum dot-AZD4547 conjugates for tracking the dynamic behavior of fibroblast growth factor receptor 3
description Gyoyeon Hwang,1,2,* Hyeonhye Kim,1,* Hojong Yoon,1 Chiman Song,1 Dong-Kwon Lim,3 Taebo Sim,1,3 Jiyeon Lee1,2 1Chemical Kinomics Research Center, Materials and Life Science Research Division, Korea Institute of Science and Technology, Seoul, 2Bio-Med, Korea University of Science and Technology, Daejeon, 3KU-KIST Graduate School of Converging Science and Technology, Korea University, Seoul, Republic of Korea *These authors contributed equally to this work Abstract: Fibroblast growth factor receptors (FGFRs) play an important role in determining cell proliferation, differentiation, migration, and survival. Although a variety of small-molecule FGFR inhibitors have been developed for cancer therapeutics, the interaction between FGFRs and FGFR inhibitors has not been well characterized. The FGFR–inhibitor interaction can be characterized using a new imaging probe that has strong, stable signal properties for in situ cellular imaging of the interaction without quenching. We developed a kinase–inhibitor-modified quantum dot (QD) probe to investigate the interaction between FGFR and potential inhibitors. Especially, turbo-green fluorescent protein-FGFR3s were overexpressed in HeLa cells to investigate the colocalization of FGFR3 and AZD4547 using the QD-AZD4547 probe. The result indicates that this probe is useful for investigating the binding behaviors of FGFR3 with the FGFR inhibitor. Thus, this new inhibitor-modified QD probe is a promising tool for understanding the interaction between FGFR and inhibitors and for creating future high-content, cell-based drug screening strategies. Keywords: quantum dot, fibroblast growth factor 3, AZD4547, kinase–inhibitor, in situ imaging
format article
author Hwang G
Kim H
Yoon H
Song C
Lim D
Sim T
Lee J
author_facet Hwang G
Kim H
Yoon H
Song C
Lim D
Sim T
Lee J
author_sort Hwang G
title In situ imaging of quantum dot-AZD4547 conjugates for tracking the dynamic behavior of fibroblast growth factor receptor 3
title_short In situ imaging of quantum dot-AZD4547 conjugates for tracking the dynamic behavior of fibroblast growth factor receptor 3
title_full In situ imaging of quantum dot-AZD4547 conjugates for tracking the dynamic behavior of fibroblast growth factor receptor 3
title_fullStr In situ imaging of quantum dot-AZD4547 conjugates for tracking the dynamic behavior of fibroblast growth factor receptor 3
title_full_unstemmed In situ imaging of quantum dot-AZD4547 conjugates for tracking the dynamic behavior of fibroblast growth factor receptor 3
title_sort in situ imaging of quantum dot-azd4547 conjugates for tracking the dynamic behavior of fibroblast growth factor receptor 3
publisher Dove Medical Press
publishDate 2017
url https://doaj.org/article/f3ac4e4e397b47b2abdbc655996253c0
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