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Optimized HSP90 mediated fluorescent probes for cancer-specific bioimaging

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Abstract

Cancer-specific bioimaging has been correlated with fluorescence-guided tumor therapy, garnering extensive interest from researchers. Herein, a highly efficient tumor-targeting fluorescent probe (NP-001), which is integrated with 4-hydroxy-1,8-naphthalimide and NVP-AUY922, for tumor imaging has been established. 4-Hydroxy-1,8-naphthalimide is a fluorescent molecule with remarkable imaging compatibility. NVP-AUY922 is a heat shock protein 90 (HSP90) inhibitor with preferential tumor selectivity that is conjugated to 4-hydroxy-1,8-naphthalimide as a tumor-targeting ligand. NP-002, a resorcinol-blocked probe which prevented binding with an amino acid residue of the HSP90 ATP binding pocket, was also synthesized as a control. In vitro and ex vivo assays showed that NP-001 could arrest cell proliferation, induce apoptosis and accumulate to inhibit HSP90. Confocal laser scanning microscopy (CLSM) also confirmed that NP-001 could be selectively internalized by tumor cells for cancer-specific bioimaging. Moreover, pharmacokinetic studies and histological analysis also indicated that NP-001 had a relatively longer retention time and showed no major organ-related toxicities. Overall, these encouraging data suggest that NP-001 is a promising new candidate for the early diagnosis of metastatic disease as well as targeted tumor imaging.

Graphical abstract: Optimized HSP90 mediated fluorescent probes for cancer-specific bioimaging

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Supplementary files

Article information


Submitted
06 Nov 2019
Accepted
14 Jan 2020
First published
16 Jan 2020

J. Mater. Chem. B, 2020, Advance Article
Article type
Paper

Optimized HSP90 mediated fluorescent probes for cancer-specific bioimaging

S. Zhu, Y. Li, Y. Huang, M. Zhang, X. Gu, Y. He, H. Liu, M. Ma and W. Lu, J. Mater. Chem. B, 2020, Advance Article , DOI: 10.1039/C9TB02505G

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