TNF-related apoptosis-inducing ligand receptor 2 (TRAIL-R2)

TNF-related apoptosis-inducing ligand receptor 2 (TRAIL-R2), also known as Death Receptor 5 (DR5) and TNFRSF10B, is a cell surface receptor belonging to the TNF receptor superfamily. It contains extracellular cysteine-rich repeats and an intracellular death domain. TRAIL-R2 binds to TRAIL and mediates apoptosis by engaging a caspase-dependent pathway, involving the adaptor protein FADD to form the death-inducing signaling complex (DISC). The gene is located on human chromosome 8p22-21, and its mRNA is widely expressed. TRAIL-R2 is an important therapeutic target, particularly in cancer therapy. Various agents, including monoclonal antibodies (like Tigatuzumab), agonist antibodies, luminescent iridium complex-peptide hybrids, and bispecific antibodies, have been developed to target TRAIL-R2 to induce apoptosis in cancer cells. Its existence alongside TRAIL-R1/DR4 suggests a complex regulatory system for apoptotic signaling. Recent research also explores its links to cellular stress pathways like GCN2 regulation.

Other names

Death Receptor 5DR5tumor necrosis factor receptor superfamily member 10BTNFRSF10B

Activation of TRAIL-R2 to induce apoptosis in target cells, often mediated via the formation of the death-inducing signaling complex (DISC) involving FADD and caspases.