
Methods, Journal Year: 2025, Volume and Issue: unknown
Published: May 1, 2025
Overexpression of pyruvate kinase (PyK) is linked to many kinds malignant tumors, representing therefore one the most promising therapeutic targets for cancer treatment. Inhibition PyK slows down tumor growth or causes cell death, minimizing proliferation, and understanding inhibitor mechanism action can significantly improve therapy. The present work describes use an amperometric bienzymatic biosensor, based on oxidase (PyOx), in enzyme inhibition studies four inhibitors, CPG77675, Nilotinib, Ruxolitinib, Cerdulatinib. Their studied discussed detail, with a thorough evaluation their enzyme-inhibitor complex binding constants (Ki) concentration required 50% (IC50), employing standard procedure graphical methods. biosensor successfully applied quantification inhibitors by fixed potential amperometry, excellent detection limit values pM range. It first method reported anticancer drugs CPG77675 electrochemical assay brings several advantages over available kits high-throughput screening (HTS) namely: low cost, easy operability robustness demonstrated high reproducibility both operational storage stability, offering opportunity discover new optimize index.
Language: Английский