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

  • Hwang, Gyoyeon; 
  • Kim, Hyeonhye; 
  • Yoon, Hojong; 
  • Song, Chiman; 
  • Lim, Dong-Kwon; 
  • 외 2명
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4
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5

초록

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.

키워드

quantum dot; fibroblast growth factor 3; AZD4547; kinase-inhibitor; in situ imaging; SURFACE MODIFICATION; TYROSINE KINASES; DRUG DISCOVERY; CANCER; DOTS; AZD4547; INHIBITOR; IDENTIFICATION; NANOPARTICLES; ANGIOGENESIS
제목
In situ imaging of quantum dot-AZD4547 conjugates for tracking the dynamic behavior of fibroblast growth factor receptor 3
저자
Hwang, Gyoyeon; Kim, Hyeonhye; Yoon, Hojong; Song, Chiman; Lim, Dong-Kwon; Sim, Taebo; Lee, Jiyeon
DOI
10.2147/IJN.S141595
발행일
2017
유형
Article
저널명
International Journal of Nanomedicine
권
12
페이지
5345 ~ 5357