BioCentury
ARTICLE | Distillery Therapeutics

Cancer

November 26, 2018 8:11 PM UTC

Cell culture studies identified a nicotonic acetylcholine receptor α7 (CHRNA7) antagonist that could help treat glioblastoma, lung adenocarcinoma and neuroblastoma. Chemical synthesis and cell-based testing of structural hybrids of a stilbene-based nAchR inhibitor tool compound and a previously reported resveratrol-based mitochondrial-targeted compound yielded a compound that bound human CHRNA7 with a Ki of 164 nM and inhibited growth in human glioblastoma, lung adenocarcinoma and neuroblastoma cell lines with IC50 values of 0.11, 0.49 and 10 μM, respectively. Next steps could include testing the compound in animal models of those cancers...