Target Validation Information | |||||
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TTD ID | T70067 | ||||
Target Name | TRAIL receptor 2 (TRAIL-R2) | ||||
Type of Target |
Clinical trial |
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Action against Disease Model | Conatumumab | Drug Info | Conat uM uMab binds to DR5, activating intracellular caspases in vitro in the presence of a cross-linker. Conat uM uMab has activity in vivo and inhibits t uMor growth in colon (Colo205 and HCT-15), lung (H2122) and pancreatic (MiaPaCa2/T2) xenograft models. Conat uM uMab also enhances the antit uMor activity of chemotherapeutics in vivo. Caspase activation in Colo205 t uMors is dose-dependent and correlated with ser uM concentrations of conat uM uMab. Increases in ser uM caspase-3/7 activity and levels of M30 (neoepitope of caspase-cleaved cytokeratin-18) are linked to activation of the extrinsic apoptotic pathway using conat uM uMab in a preclinical model. | [1] | |
References | |||||
REF 1 | Conatumumab, a fully human agonist antibody to death receptor 5, induces apoptosis via caspase activation in multiple tumor types. Cancer Biol Ther. 2010 Apr 15;9(8):618-31. | ||||
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