Congratulations to NU scientists Richard B. Silverman and Neil L. Kelleher on their recent publication in the Journal of the American Chemical Society, titled
“Mechanism of Inactivation of Ornithine Aminotransferase by (1 S,3 S)-3-Amino-4-(hexafluoropropan-2-ylidenyl)cyclopentane-1-carboxylic Acid.”
The paper addresses new efforts towards developing drugs for hepatocellular carcinoma (HCC) — the most common form of liver cancer for which there is currently no effective treatment. The inhibition / inactivation of an enzyme called ornithine aminotransferase (OAT) has been implicated as a potential therapeutic pathway for HCC and the authors of the current study have previously identified several inhibitors of OAT. Here, they proceed to characterize the mechanism(s) of OAT inactivation and report that a two-step modification resulting in an addition of a trifluoromethyl group appears to be key to the process.
Original story posted by Chemistry of Life Processes Institute on July 9, 2019.