Alkaline phosphatase (ALP) activatable small molecule-based prodrugs for cancer theranostics.
Kartikay TyagiReena KumariV VenkateshPublished in: Organic & biomolecular chemistry (2023)
Highly water-soluble small molecule-based prodrugs (5-FUPD and SAHAPD) are formulated. They comprise a phosphate group to lock the active drug payload (5-fluorouracil and SAHA) along with a turn-on fluorophore consisting of a glutathione (GSH) depletory feature. Installation of the phosphate group along with purification of final product has been accomplished in an operationally facile manner. Activation of the prodrugs is facilitated by alkaline phosphatase (ALP)-mediated hydrolysis of the phosphate group followed by 1,8-elimination. The prodrugs were found to be highly effective against ALP flared human cervical cancer (HeLa) and liver cancer (HepG2) cell lines. Most notably, they were found to be innocuous to normal liver cells (WRL-68).
Keyphrases
- small molecule
- fluorescent probe
- water soluble
- cell cycle arrest
- living cells
- protein protein
- induced apoptosis
- endothelial cells
- papillary thyroid
- machine learning
- cell death
- quantum dots
- deep learning
- squamous cell
- sensitive detection
- single molecule
- electronic health record
- anaerobic digestion
- young adults
- neural network