Drug name: NP-TRAIL + Bortezomib


Related CSCTT Targets

TRAIL-resistant glioma stem cells [ref.1]

TRAIL, TNFSF10

Cas.no PubChem ID
Known Target
Structure
...
Introduction
TRAIL, PDB ID: P50591. A type-II transmembrane homotrimeric protein that belongs to the TNF gene superfamily, is a promising candidate for cancer therapy because of its selective apoptotic effect in a wide variety of transformed cells without affecting normal cells. NP-TRAIL is covalently conjugating TRAIL to the surface of the iron oxide NP.

Bortezomib

Cas.no PubChem ID
179324-69-7 387447
Known Target
26S proteasome non-ATPase regulatory subunit 2Q13200
Proteasome subunit beta type-1P20618
Proteasome subunit beta type-5P28074
Proteasome subunit beta type-2P49721
26S proteasome non-ATPase regulatory subunit 1Q99460
Structure
...
Introduction
Bortezomib is a reversible inhibitor of the chymotrypsin-like activity of the 26S proteasome in mammalian cells. The 26S proteasome is a large protein complex that degrades ubiquitinated proteins. The active site of the proteasome has chymotrypsin-like, trypsin-like, and postglutamyl peptide hydrolysis activity. The 26S proteasome degrades various proteins critical to cancer cell survival, such as cyclins, tumor suppressors, BCL-2, and cyclin-dependent kinase inhibitors. Inhibition of these degradations sensitizes cells to apoptosis. Bortezomib is a potent inhibitor of 26S proteasome, which sensitizes activity in dividing multiple myeloma and leukemic cells, thus inducing apoptosis. In addition, bortezomib appears to increase the sensitivity of cancer cells to traditional anticancer agents (e.g., gemcitabine, cisplatin, paclitaxel, irinotecan, and radiation).

Reference

  • [1] TRAIL conjugated to nanoparticles exhibits increased anti-tumor activities in glioma cells and glioma stem cells in vitro and in vivo. Perlstein, B., et al. (2013).Neuro Oncol.15(1):29-40.
    23144078. [ 23144078 ]

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