Title : Substrate-Competitive Activity-Based Profiling of Ester Prodrug Activating Enzymes.

Pub. Date : 2015 Sep 8

PMID : 26262434






4 Functional Relationships(s)
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Compound Name
Protein Name
Organism
1 Substrate-competitive ABPP analysis identified carboxylesterase 1 (CES1) as an oseltamivir-activating enzyme in intestinal cell homogenates. Oseltamivir carboxylesterase 1 Homo sapiens
2 Substrate-competitive ABPP analysis identified carboxylesterase 1 (CES1) as an oseltamivir-activating enzyme in intestinal cell homogenates. Oseltamivir carboxylesterase 1 Homo sapiens
3 Saturating concentrations of oseltamivir lead to a four-fold reduction in the observed rate constant for CES1 inactivation by fluorophosphonates. Oseltamivir carboxylesterase 1 Homo sapiens
4 WWL50, a reported carbamate inhibitor of mouse CES1, blocked oseltamivir hydrolysis activity in human cell homogenates, confirming CES1 is the primary prodrug activating enzyme for oseltamivir in human liver and intestinal cell lines. Oseltamivir carboxylesterase 1 Homo sapiens