ARTICLE | Distillery Techniques


October 27, 2016 7:00 AM UTC

A phenoxybenzamide analog that inhibits PARP-10 could be useful for investigating the role of the enzyme in cancer. In vitro assay screening of a small molecule library yielded a compound that inhibited PARP-10 activity with an IC50 of 329 nM and more than 100 times greater selectivity for PARP-10 over 14 other PARP enzymes, including PARP-1, PARP-2 and PARP-3. In HeLa cells, the compound increased sensitivity to the anti-neoplastic agent Droxia hydroxyurea compared with vehicle. Next steps could include using the compound to probe the role of PARP-10 in tumor models...