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Discovery of small molecule inhibitors for the C. elegans caspase CED-3 by high-throughput screening

Author:
Brantley, Scott, Cotten, Steven W., Lamson, David R., Smith, Ginger R., Liu, Rihe, Williams, Kevin P.
Source:
Biochemical and biophysical research communications 2017
ISSN:
0006-291X
Subject:
apoptosis, caspases, chemotypes, inhibitory concentration 50, models, screening
Abstract:
C.elegans has been widely used as a model organism for programmed cell death and apoptosis. Although, the CED-3 caspase is the primary effector of cell death in C. elegans, no selective inhibitors have been identified. Utilizing high-throughput screening with recombinant C. elegans CED-3 protein, we have discovered and confirmed 21 novel small molecule inhibitors. Six compounds had IC50 values < 10 μM. From these, four distinct chemotypes were identified. The inhibitor scaffolds described here could lead to the development of selective molecular probes to facilitate our understanding of programmed cell death in this model organism.
Agid:
5762178