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

Gyoyeon Hwang, Hyeonhye Kim, Hojong Yoon, Chiman Song, Dong-Kwon Lim, Taebo Sim, Jiyeon Lee

Research output: Contribution to journalArticle

2 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)5345-5357
Number of pages13
JournalInternational Journal of Nanomedicine
Volume12
DOIs
Publication statusPublished - 2017 Jul 26

Keywords

  • AZD4547
  • Fibroblast growth factor 3
  • In situ imaging
  • Inhibitor
  • Kinase
  • Quantum dot

ASJC Scopus subject areas

  • Bioengineering
  • Biophysics
  • Biomaterials
  • Drug Discovery
  • Organic Chemistry

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