A novel caspase 8 selective small molecule potentiates TRAIL-induced cell death.

ABSTRACT: Recombinant soluble TRAIL and agonistic antibodies against TRAIL receptors (DR4 and DR5) are currently being created for clinical cancer therapy, due to their selective killing of cancer cells and high safety characteristics. However, resistance to TRAIL and other targeted therapies is an important issue facing current cancer research field. An attractive strategy to sensitize resistant malignancies to TRAIL-induced cell death is the design of small molecules that target and promote caspase 8 activation. For the first time, we describe the discovery and characterization of a small molecule that directly binds caspase 8 and enhances its activation when combined with TRAIL, but not alone. The molecule was identified through an in silico chemical screen for compounds with affinity for the cas

SUBMITTER: Bucur O 

PROVIDER: S-EPMC4426715 | biostudies-literature | 2015 May

REPOSITORIES: biostudies-literature