Identifying drug-target selectivity of small-molecule CRM1/XPO1 inhibitors by CRISPR/Cas9 genome editing.

@article{Neggers2015IdentifyingDS,
  title={Identifying drug-target selectivity of small-molecule CRM1/XPO1 inhibitors by CRISPR/Cas9 genome editing.},
  author={Jasper Edgar Neggers and Thomas Vercruysse and Maarten Jacquemyn and Elisabeth Vanstreels and Erkan Baloglu and Sharon Shacham and Marsha L. Crochiere and Yosef Landesman and Dirk Daelemans},
  journal={Chemistry & biology},
  year={2015},
  volume={22 1},
  pages={
          107-16
        }
}
Validation of drug-target interaction is essential in drug discovery and development. The ultimate proof for drug-target validation requires the introduction of mutations that confer resistance in cells, an approach that is not straightforward in mammalian cells. Using CRISPR/Cas9 genome editing, we show that a homozygous genomic C528S mutation in the XPO1 gene confers cells with resistance to selinexor (KPT-330). Selinexor is an orally bioavailable inhibitor of exportin-1 (CRM1/XPO1) with… CONTINUE READING
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