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Issue 9, 2020
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Optimized HSP90 mediated fluorescent probes for cancer-specific bioimaging

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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

06 Nov 2019
14 Jan 2020
First published
16 Jan 2020

J. Mater. Chem. B, 2020,8, 1878-1896
Article type

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, 8, 1878
DOI: 10.1039/C9TB02505G

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