Arylacetamide Deacetylase Is Responsible for Activation of Prasugrel in Human and Dog.
Kanazawa, Japan. In Drug Metab Dispos, 30 Jan 2016
It is efficiently hydrolyzed in the intestine after oral administration, and the enzyme responsible for the hydrolysis in human was demonstrated to be carboxylesterase (CES) 2. Prasugrel hydrolase activity is detected in dog intestine where CES enzymes are absent, so this prompted us to investigate the involvement of enzyme(s) other than CES.
Notum deacylates Wnt proteins to suppress signalling activity.
Potters Bar, United Kingdom. In Nature, Apr 2015
Kinetic and mass spectrometric analyses of human proteins show that Notum is a carboxylesterase that removes an essential palmitoleate moiety from Wnt proteins and thus constitutes the first known extracellular protein deacylase.
Enzyme-catalyzed activation of anticancer prodrugs.
Amsterdam, Netherlands. In Pharmacol Rev, 2004
The following endogenous enzymes are discussed: aldehyde oxidase, amino acid oxidase, cytochrome P450 reductase, DT-diaphorase, cytochrome P450, tyrosinase, thymidylate synthase, thymidine phosphorylase, glutathione S-transferase, deoxycytidine kinase, carboxylesterase, alkaline phosphatase, beta-glucuronidase and cysteine conjugate beta-lyase.
Modulation of irinotecan metabolism by ketoconazole.
Rotterdam, Netherlands. In J Clin Oncol, 2002
RESULTS: With ketoconazole coadministration, the relative formation of APC was reduced by 87% (P =.002), whereas the relative exposure to the carboxylesterase-mediated SN-38 as expected on the basis of dose (area under the plasma concentration-time curve normalized to dose) was increased by 109% (P =.004).