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Tumor necrosis factor-related apoptosis-inducing ligand death receptor
- Molecular classification
- TNF receptor superfamily, Receptor
01
Overview
The tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) death receptors are cell surface receptors that mediate apoptosis upon binding to TRAIL. These receptors, primarily DR4 and DR5, are part of the TNF receptor superfamily and selectively induce apoptosis in cancer cells, making them attractive targets for anticancer therapies. Decoy receptors like DcR1 and DcR2 can inhibit apoptosis. Clinical trials have shown limited success due to resistance mechanisms, prompting research into combination therapies.
- Other names
- TRAIL receptorDR4TRAIL-R1TNFRSF10ADR5TRAIL-R2TNFRSF10B
02
Mechanism of action
Upon binding of TRAIL, the receptor trimerizes and recruits FADD, activating caspase 8 and triggering downstream effector caspases leading to apoptosis.
03
Biological functions
Induction of extrinsic apoptotic pathwayApoptosisSignal transductionImmune regulation
04
Disease associations
Cancer
05
Safety considerations
Acquired resistance mechanisms within tumorsPotential toxicity to normal tissuesLimited survival benefit in clinical trials
06
Interacting drugs
Soluble recombinant human TRAIL
1 more in the full profile.
07
Biomarkers
Expression levels of DR4/DR5Expression levels of decoy receptors (DcR1, DcR2)Activation of non-apoptotic pathways (e.g., NF-kappa B)
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