Ferroptosis-centered Drug Response Information
General Information of the Drug (ID: ferrodrug0405)
| Name |
ALZ003
|
||||
|---|---|---|---|---|---|
| Drug Type |
Small molecule
|
||||
Full List of Ferroptosis Target Related to This Drug
Phospholipid hydroperoxide glutathione peroxidase (GPX4)
| In total 1 item(s) under this Target | |||||
| Experiment 1 Reporting the Ferroptosis-centered Drug Act on This Target | [1] | ||||
| Target for Ferroptosis | Suppressor | ||||
| Responsed Disease | Glioblastoma | ICD-11: 2A00 | |||
| Responsed Regulator | Androgen receptor (AR) | Suppressor | |||
| Pathway Response | Fatty acid metabolism | hsa01212 | |||
| Apoptosis | hsa04210 | ||||
| Ubiquitin mediated proteolysis | hsa04120 | ||||
| Cell Process | Cell ferroptosis | ||||
| Cell apoptosis | |||||
| Cell proliferation | |||||
| In Vitro Model | U-87MG cells | Glioblastoma | Homo sapiens | CVCL_GP63 | |
| A-172 cells | Glioblastoma | Homo sapiens | CVCL_0131 | ||
| In Vivo Model |
NOD-SCID male mice (8-week-old) were purchased from BioLASCO Taiwan Co., Ltd. (Taipei, Taiwan). For glioblastoma and TMZ-resistant glioblastoma transplantation, luciferase-expressed U87MG cells (2 x 105) and U87MG-R cells (2 x 105) were injected into the cortex, respectively, at the depth of 3 mm using stereotactic guidance and microprocessor single syringe (Harvard Apparatus, Holliston, MA, USA). After 10 days of transplantation, TMZ (15 mg/kg) and ALZ003 were orally and intravenously administrated three times per week, respectively.
Click to Show/Hide
|
||||
| Response regulation | ALZ003 targeting AR for degradation strongly exhibits the therapeutic effect on glioblastoma, including TMZ-resistant tumor,in vitroandin vivo. Particularly, GPX4 was positively regulated by AR, and overexpression of AR also prevented lipid peroxidation. | ||||