THDP17 decreases ammonia production through glutaminase inhibition. A new drug for hepatic encephalopathy therapy.

ABSTRACT: Ammonia production is implicated in the pathogenesis of hepatic encephalopathy (HE), being intestinal glutaminase activity the main source for ammonia. Management of ammonia formation can be effective in HE treatment by lowering intestinal ammonia production. The use of glutaminase inhibitors represents one way to achieve this goal. In this work, we have performed a search for specific inhibitors that could decrease glutaminase activity by screening two different groups of compounds: i) a group integrated by a diverse, highly pure small molecule compounds derived from thiourea ranging from 200 to 800 Daltons; and ii) a group integrated by commonly use compounds in the treatment of HE. Results shown that THDP-17 (10 µM), a thiourea derivate product, could inhibit the intestinal glutaminase

SUBMITTER: Diaz-Herrero MM 

PROVIDER: S-EPMC4201470 | biostudies-literature | 2014

REPOSITORIES: biostudies-literature