TRAIL   Click here for help

GtoPdb Ligand ID: 5065

Synonyms: Apo-2 ligand (Apo-2L)
Compound class: Endogenous peptide in human, mouse or rat
Comment: TRAIL is a cytokine of the tumor necrosis factor (TNF) ligand family. TRAIL binds to several TNF family receptors, activating MAPK8/JNK, caspase 8, and caspase 3. Its interaction with death receptors on tumor cells triggers apoptosis. Binding to decoy receptors may neutralise TRAIL activity. Because TRAIL exhibits much stronger apoptotic activity than other TNF family members, kills tumor cells more effectively than normal cells, and presents less risk of inducing an inflammatory repsonse following systemic administration, use of TRAIL as an anti-cancer therapeutic has been widely examined. Huang et al. (2017) [2] describe the development and potent anti-tumor activity of a TRAIL fusion protein nanoparticle formulation in a xenograft model [1]. To date, no pharmaceutical agents targeting TRAIL or its receptors in cancer have been approved.
Species: Human
Click here for help

Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

✖

View interactive charts of activity data across species
Natural/Endogenous Targets
Target
death receptor 4
death receptor 5
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
death receptor 5 Ligand is endogenous in the given species Hs Agonist Agonist 7.2 pKd - 3
⤷ pKd 7.2 (Kd 5.9x10-8 M) [3]
death receptor 4 Ligand is endogenous in the given species Hs None - - - -
⤷
Targets where the ligand is described in the comment field
Target Comment
decoy receptor 2 Decoy receptor for TRAIL (TNFSF10, P50591).
decoy receptor 1 Decoy receptor for TRAIL (TNFSF10, P50591).
osteoprotegerin Acts as a decoy receptor for RANK ligand (TNFSF11, O14788) and possibly for TRAIL (TNFSF10, P50591).