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 language | English |
|---|---|
| Pages (from-to) | 5345-5357 |
| Number of pages | 13 |
| Journal | International Journal of Nanomedicine |
| Volume | 12 |
| DOIs | |
| Publication status | Published - 2017 Jul 26 |
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Keywords
- AZD4547
- Fibroblast growth factor 3
- In situ imaging
- Inhibitor
- Kinase
- Quantum dot
ASJC Scopus subject areas
- Bioengineering
- Biophysics
- Biomaterials
- Drug Discovery
- Organic Chemistry
Cite this
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; Sim, Taebo; Lee, Jiyeon.
In: International Journal of Nanomedicine, Vol. 12, 26.07.2017, p. 5345-5357.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - In situ imaging of quantum dot-AZD4547 conjugates for tracking the dynamic behavior of fibroblast growth factor receptor 3
AU - Hwang, Gyoyeon
AU - Kim, Hyeonhye
AU - Yoon, Hojong
AU - Song, Chiman
AU - Lim, Dong-Kwon
AU - Sim, Taebo
AU - Lee, Jiyeon
PY - 2017/7/26
Y1 - 2017/7/26
N2 - 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.
AB - 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.
KW - AZD4547
KW - Fibroblast growth factor 3
KW - In situ imaging
KW - Inhibitor
KW - Kinase
KW - Quantum dot
UR - http://www.scopus.com/inward/record.url?scp=85026478143&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85026478143&partnerID=8YFLogxK
U2 - 10.2147/IJN.S141595
DO - 10.2147/IJN.S141595
M3 - Article
C2 - 28794627
AN - SCOPUS:85026478143
VL - 12
SP - 5345
EP - 5357
JO - International Journal of Nanomedicine
JF - International Journal of Nanomedicine
SN - 1176-9114
ER -