TNF-related apoptosis-inducing ligand (TRAIL, APO2L) is a member of the TNF cytokine superfamily，and is involved in pathogenesis of and/or possible treatment approaches for a variety of diseases including but not limited to cancer, obesity, diabetes, rheumatoid arthritis, and neurodegenerative diseases[2]. TRAIL secreted from natural killer (NK) cells binds to death receptors (DR4 or DR5). Bioymifi is an activator of the TRAIL receptor DR5 for cancer therapy. Bioymifi bound the extracellular domain (ECD) of DR5 with a Kd of 1.2 μM[3]. Human glioblastoma cells T98G cells, lung cancer cell lines H460 and H1155, the cervical cancer cell line HeLa, the osteosarcoma cell line U2OS, the pancreatic carcinoma cell line Miapaca and the colon cancer cell line HT29 showed single-agent sensitivity to bioymifi which is dependent on caspase-8[3]. Caspase-3 was rapidly activated as early as 2 h after bioymifi treatment (5 μM) of T98G cells and its activity was markedly increased after 8 h of treatment[3].
作用机制
Bioymifi bound the extracellular domain (ECD) of DR5.
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