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TPE-1(Hyd-DOX)-DEVD
- Development stage
- Preclinical
- Lead developer
- Soochow University
- Modality
- Small Molecules, Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
**TPE-1(Hyd-DOX)-DEVD** is a preclinical self-reporting theranostic nanoprobe developed at Soochow University for activatable cancer chemotherapy and noninvasive monitoring of treatment response. The construct combines a tetraphenylethylene aggregation-induced-emission fluorogen, a DEVD caspase-3-responsive peptide sequence, and doxorubicin attached through an acid-labile hydrazone linker. In the acidic tumor microenvironment, doxorubicin is released and induces cytotoxicity primarily through DNA intercalation and topoisomerase II inhibition. Apoptosis-associated caspase-3 subsequently cleaves the DEVD motif, promoting aggregation and enhanced tetraphenylethylene fluorescence; the TPE-to-doxorubicin fluorescence ratio is intended to report drug activation and therapeutic response in real time. Preclinical in vitro and in vivo studies reported tumor-growth suppression and biocompatibility.
- Other names
- TPE-1 (Hyd-DOX)-DEVD
02
Targets
TOP2A (DNA topoisomerase II)CASP3 (Caspase-3)DNA
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