Tumor necrosis factor receptor superfamily member 10A (TRAIL-R1)

Tumor necrosis factor receptor superfamily member 10A (TRAIL-R1/DR4) is a type I transmembrane protein that functions as one of the primary receptors for TNF-related apoptosis-inducing ligand (TRAIL). Upon binding trimeric TRAIL ligand, it induces apoptosis via recruitment of FADD adaptor protein and subsequent activation of caspase cascades. It is mainly expressed on damaged, infected, or malignant cells. As an inducer of programmed cell death specifically in cancerous cells while sparing most normal tissues, it has attracted significant interest as an anticancer therapeutic target. However, clinical translation has been hampered by resistance mechanisms within tumors and insufficient efficacy with current agents. The gene encoding this protein is TNFRSF10A; it shares structural features with other members of the TNF-receptor family but uniquely triggers potent apoptotic signaling upon ligand engagement.

Other names

TRAIL receptor-1Death receptor 4DR4TNFRSF10A

Drugs or ligands targeting this molecule typically act by binding to TRAIL-R1, inducing its trimerization and recruitment of adaptor proteins such as FADD. This leads to the formation of the death-inducing signaling complex (DISC), activation of caspase 8/10, and initiation of the extrinsic apoptotic pathway