Introduction: The ability of most laboratories to easily access CRISPR/Cas9 engineering
tools has caused a revolution in biology. One of the areas that will continue to be impacted by genome
editing is the drug discovery process.
Objective: CRISPR/Cas9 will not only serve to accelerate the drug discovery pipeline, but also
streamline line it by identifying high-value targets, facilitating the validation of drug: target interactions
and mechanisms of action, and stimulating the development of phenotype-based high throughput
screens as alternatives to target-based assays.
Conclusion: We review the literature and hurdles that have been overcome to develop the current
generation of tools being used to enrich the drug discovery paradigm.