Chandramohan A
A high-throughput microfluidic mechanoporation platform to enable intracellular delivery of cyclic peptides in cell-based assays
Cyclic peptides are poised to target historically difficult to drug intracellular protein–protein interactions, however, their general cell impermeability poses a challenge for characterizing function.
ReadDe-risking drug discovery of intracellular targeting peptides: screening strategies to eliminate false-positive hits
Non-specific promiscuous compounds can mislead researchers and waste significant resources. This phenomenon, though well-documented for small molecules, has not been widely explored for the peptide modality. Here, we demonstrate that two purported peptide-based KRas inhibitors, SAH-SOS1A and cyclorasin 9A5, exemplify false-positive molecules – both in terms of their binding affinities and cellular activities.
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