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TOP3
- Development stage
- Preclinical
- Modality
- Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Recombinant Proteins and Enzymes
01
Overview
TOP3 (TAT-ODD-procaspase-3) is a protein prodrug designed to target hypoxia-inducible factor (HIF)-active cancer cells. It is specifically processed and activated in these hypoxic cells, leading to cell death. This mechanism allows for targeted delivery and activation within the tumor microenvironment, which is often characterized by hypoxia. TOP3 has shown promise in improving survival in orthotopic pancreatic cancer models, particularly when combined with standard chemotherapeutic drugs like gemcitabine or TS-1.
02
Targets
CASP3 (Caspase-3)EGLN1 (Prolyl hydroxylase domain-containing protein 2)HIF3A (Hypoxia-inducible factor 3-alpha)
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