DrugTargetSeqR: a genomics- and CRISPR-Cas9–based method to analyze drug targets

June 15th, 2014 by Corynn Kasap

Nature Chemical Biology 10, 626 (2014). doi:10.1038/nchembio.1551

Authors: Corynn Kasap, Olivier Elemento & Tarun M Kapoor

To identify physiological targets of drugs and bioactive small molecules, we developed an approach, named DrugTargetSeqR, which combines high-throughput sequencing, computational mutation discovery and clustered regularly interspaced short palindromic repeats (CRISPR)-Cas9–based genome editing. We applied this approach to ispinesib and YM155, drugs that have undergone clinical trials as anticancer agents, and uncovered mechanisms of action and identified genetic and epigenetic mechanisms likely to cause drug resistance in human cancer cells.

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