Inhibitors of a number of protein–protein interactions (PPIs) have emerged as potential anticancer drug candidates. Now, Nim et al. describe a novel high-throughput method that uses a pooled lentiviral dropout approach to screen a library of human peptide motifs for PPI inhibitors that specifically decreased viability of a pancreatic cancer cell line (RWP1). Target interactions of hits were identified computationally and a subset validated in vitro. Further analysis of the inhibitors in RWP1 cells revealed their mechanisms of action, which included apoptosis and cell-cycle arrest.
References
Nim, S. et al. Pooled screening for antiproliferative inhibitors of protein–protein interactions. Nat. Chem. Bio. http://dx.doi.org/10.1038/nchembio.2026 (2016)
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Crunkhorn, S. Inhibiting protein–protein interactions. Nat Rev Drug Discov 15, 234 (2016). https://doi.org/10.1038/nrd.2016.54
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DOI: https://doi.org/10.1038/nrd.2016.54