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A Reactivity‐Tunable Self‐Immolative Design Enables Histone Deacetylase‐Targeted Imaging and Prodrug Activation.
- Source :
-
Angewandte Chemie . 11/21/2022, Vol. 134 Issue 47, p1-10. 10p. - Publication Year :
- 2022
-
Abstract
- Histone deacetylase (HDAC)‐targeted probes and prodrugs are crucial for cancer theranostics. We developed a self‐immolative design that enables in vivo activatable near‐infrared fluorescence (NIRF) and photoacoustic (PA) imaging and prodrug release in response to HDAC. This design comprises a phenyl ester linker with tunable reactivity, facilitating efficient release of caged fluorophores/drugs upon deacetylation. We engineered a new fluorophore using a spirocyclic xanthene scaffold with ring‐open property, affording NIRF/PA detection with high contrast. We showed that a nitro‐substituted self‐immolative linker allows sensitive NIRF/PA in vivo imaging of HDAC with minimal interference. A highly efficient prodrug system was further developed for targeted therapy in HDAC‐overexpressed triple negative breast tumors in mice. Our study provides a valuable paradigm for HDAC‐targeted NIRF/PA imaging and prodrug release in vivo, highlighting its potential for bioimaging and drug development. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 00448249
- Volume :
- 134
- Issue :
- 47
- Database :
- Academic Search Index
- Journal :
- Angewandte Chemie
- Publication Type :
- Academic Journal
- Accession number :
- 160200455
- Full Text :
- https://doi.org/10.1002/ange.202203243