Tyrosine407 phosphorylation activates mitochondrial acetyl-CoA acetyltransferase 1 (ACAT1) by stabilizing its tetramer. This is believed to be the mechanisms by which ACAT1 is "hijacked" and contributes to the Warburg effect in cancer. Arecoline is a covalent inhibitor of ACAT1 which binds to and disrupts only ACAT1 tetramers (IC50=11.1 µM). ACAT2 and DLAT are not inhibited. Treatment of xenograft nude mice with Arecoline resulted in a dose-dependent reduction in tumor mass.1 Agonist at muscarinic acetylcholine receptors M1 - M5 (EC50 in the range of 7-410 nM).2 May be effective in dementia.3
