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.
Bioymifi 细胞实验
Cell Line
Concentration
Treated Time
Description
References
293T cells
2 μM
24 h
To detect the effect of Bioymifi on AGE-induced β-catenin/TCF transcriptional activity, KDR and HDAC9 promoter activity. The results showed that Bioymifi significantly reduced these activities
Cell Commun Signal. 2024 Mar 15;22(1):182.
HUVECs
2 μM
24 h
To detect the effect of Bioymifi on AGE-induced β-catenin Y142 phosphorylation. The results showed that Bioymifi significantly reduced the phosphorylation level of β-catenin Y142
Cell Commun Signal. 2024 Mar 15;22(1):182.
intestinal organoids
100 nM
72 h
promoted organoid growth and the expression of ISC and intestinal epithelial cell marker genes
Cell Death Dis. 2024 Jan 10;15(1):27.
Adult mouse cardiac fibroblasts (AMCFs)
1 µM
24 h
Bioymifi increased BrdU incorporation in WT AMCFs but not in DR5KO AMCFs, indicating enhanced fibroblast proliferation via DR5-mediated mechanisms.
Front Cardiovasc Med. 2021 Aug 30;8:699102.
Neonatal rat ventricular fibroblasts (NRVFs)
1 µM
24 h
Bioymifi activation of DR5 did not induce apoptosis but increased proliferation via ERK1/2 signaling.
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