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trans,trans,trans-[pt(py)2(n3)2(biotin)(dca)]
- Development stage
- Preclinical
- Modality
- Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
01
Overview
Trans,trans,trans-[pt(py)2(n3)2(biotin)(dca)] is a novel biotinylated diazido-platinum(IV) complex designed as a photoactive anticancer agent. It exhibits high photocytotoxicity upon visible light irradiation while remaining stable in the dark. The drug is biotinylated to enhance its accumulation and selectivity in cancer cells, which often overexpress biotin transporters. Upon photoactivation, the platinum(IV) complex is reduced to platinum(II) species, which form lesions on DNA, leading to DNA alkylation. Additionally, photoactivation generates reactive oxygen species (ROS) and reactive nitrogen species (RNS), contributing to its cytotoxic effects. The dichloroacetate (DCA) ligand incorporated into the complex is known to inhibit pyruvate dehydrogenase kinase (PDK), further contributing to its anticancer activity. This multi-modal mechanism results in dramatic cellular morphological changes and photocytotoxicity in human ovarian cancer cells.
- Other names
- 2b
02
Targets
PDK (Pyruvate dehydrogenase kinase isoform 1)DNA
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