CUR5g is a potent autophagy inhibitor. CUR5g selectively inhibits autophagosome degradation in cancer cells by blocking autophagosome-lysosome fusion. CUR5g blocks the recruitment of STX17 to autophagosomes via a UVRAG-dependent mechanism, resulting in the inability of autophagosomes to fuse with lysosomes. CUR5g improves the anticancer effect of Cisplatin against A549 cells both in vitro and in vivo.
CUR5g (0-40 μM, 0-24 h) selectively induces autophagosome accumulation in cancer cells[1].CUR5g (0-40 μM, 0-24 h) up-regulates LC3B-II and sequestosome 1 (SQSTM1) levels[1].CUR5g (0-40 μM, 24 h) inhibits proliferation and migration of A549 cells, but dose not induce apoptosis or necrosis[1].
CUR5g (40 mg/kg, Injected via caudal vein, once every 2 days for up to 15 days) exhibits synergistic anticancer effects with Cisplatin (1 mg/kg) and inhibits autophagic flux in vivo[1].
References:
[1]. Chen J, et al. CUR5g, a novel autophagy inhibitor, exhibits potent synergistic anticancer effects with cisplatin against non-small-cell lung cancer. Cell Death Discov. 2022 Oct 31;8(1):435.