Target intelligence / Profile preview

Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand Receptor 2 (DR5)

Target
DR5
Molecular classification
TNF Receptor Superfamily, Receptor
01

Overview

Tumor necrosis factor-related apoptosis-inducing ligand receptor 2 (DR5) is a key mediator of programmed cell death via interaction with its cognate ligand TRAIL. Its selective pro-apoptotic activity against tumor cells makes it an attractive target for anticancer therapies—though challenges remain regarding resistance mechanisms within certain malignancies.

Other names
TRAILR2TNFRSF10BKILLER/DR5
02

Mechanism of action

DR5 agonists induce apoptosis by binding to DR5, leading to receptor oligomerization, recruitment of FADD and caspase-8/10, and activation of the caspase cascade.

03

Biological functions

ApoptosisSignal transductionImmune responseCell deathNF-kappaB signaling
04

Disease associations

Cancer
05

Safety considerations

Resistance mechanisms within tumorsPotential off-target effectsSystemic toxicityLimited clinical efficacy
06

Interacting drugs

Recombinant human TRAIL variants

1 more in the full profile.

07

Biomarkers

DR5 expression levels in tumor tissue

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