Title : Human Intestinal Raf Kinase Inhibitor Protein (RKIP) Catalyzes Prasugrel as a Bioactivation Hydrolase.

Pub. Date : 2016 Jan

PMID : 26558823






4 Functional Relationships(s)
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Compound Name
Protein Name
Organism
1 Prasugrel is a thienopyridine antiplatelet prodrug that undergoes rapid hydrolysis in vivo to a thiolactone metabolite by human carboxylesterase-2 (hCE2) during gastrointestinal absorption. Prasugrel Hydrochloride carboxylesterase 2 Homo sapiens
2 Prasugrel is a thienopyridine antiplatelet prodrug that undergoes rapid hydrolysis in vivo to a thiolactone metabolite by human carboxylesterase-2 (hCE2) during gastrointestinal absorption. Prasugrel Hydrochloride carboxylesterase 2 Homo sapiens
3 Using size-exclusion column chromatography of a human small intestinal S9 fraction, another peak besides the hCE2 peak was observed to have prasugrel hydrolyzing activity, and this protein was found to have a molecular weight of about 20 kDa. Prasugrel Hydrochloride carboxylesterase 2 Homo sapiens
4 Second, we evaluated the enzymatic kinetic parameters for prasugrel hydrolysis using recombinant human RKIP and hCE2 and estimated the contributions of these two hydrolyzing enzymes to the prasugrel hydrolysis reaction in human intestine, which were approximately 40% for hRKIP and 60% for hCE2. Prasugrel Hydrochloride carboxylesterase 2 Homo sapiens