Lysosomal P-gp targeted agent 1

Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp) . Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume[1].