Identification and characterization of novel benzil (diphenylethane-1, 2-dione) analogues as inhibitors of mammalian carboxylesterases

RM Wadkins, JL Hyatt, X Wei, KJP Yoon… - Journal of medicinal …, 2005 - ACS Publications
Carboxylesterases (CE) are ubiquitous enzymes responsible for the metabolism of xenobiotics.
Because the structural and amino acid homology among esterases of different classes, …

Inhibition of carboxylesterases by benzil (diphenylethane-1, 2-dione) and heterocyclic analogues is dependent upon the aromaticity of the ring and the flexibility of the …

JL Hyatt, V Stacy, RM Wadkins, KJP Yoon… - Journal of medicinal …, 2005 - ACS Publications
… i values for the compounds toward three mammalian CEs when using o-nitrophenyl acetate
… inhibitor of mammalian CEs. This was demonstrated to be correct with a K i value of 1 nM …

Requirements for mammalian carboxylesterase inhibition by substituted ethane-1, 2-diones

EI Parkinson, MJ Hatfield, L Tsurkan, JL Hyatt… - Bioorganic & medicinal …, 2011 - Elsevier
Carboxylesterases (CE) are ubiquitous enzymes found in both human and animal tissues …
We have recently identified benzil is a potent inhibitor of mammalian CEs, and in this study, we …

Hydrolytic metabolism of pyrethroids by human and other mammalian carboxylesterases

MK Ross, A Borazjani, CC Edwards… - Biochemical pharmacology, 2006 - Elsevier
… The primary aim of this study was to examine whether the human carboxylesterases hCE-1
metabolism using CEs from other mammalian species. The expression of hCE-1 and hCE-2 …

Carboxylesterases: dual roles in lipid and pesticide metabolism

MK Ross, TM Streit, KL Herring, S Xie - Journal of pesticide science, 2010 - jstage.jst.go.jp
… are widely expressed in multiple mammalian tissues.Carboxylesterases (CES) are multifunctional
… They have shown that the diphenylethane-1,2dione chemotype (benzil) is an excellent …

Carboxylesterases: a multifunctional enzyme involved in pesticide and lipid metabolism

MK Ross, MJ Edelmann - … for pesticide QSAR and PBPK/PD …, 2012 - ACS Publications
… (1). CES catalyze the hydrolysis of several pesticides within mammalian species. CES are
… obtained with pyrethroids and recombinant carboxylesterase isoforms, examine interactions …

Human carboxylesterases and their role in xenobiotic and endobiotic metabolism

MK Ross, JA Crow - Journal of biochemical and molecular …, 2007 - Wiley Online Library
… Several phase I enzymes are expressed in mammalian liver … composed of both paraoxonases
and carboxylesterases (CEs). … human and other mammalian carboxylesterases. Biochem …

Carboxylesterases: General detoxifying enzymes

MJ Hatfield, RA Umans, JL Hyatt, CC Edwards… - Chemico-biological …, 2016 - Elsevier
… Humans and small mammals demonstrate different levels of carboxylesterase expression. …
it appears as though through evolution, higher mammals (primates) have lost expression of …

Selective inhibition of carboxylesterases by isatins, indole-2, 3-diones

JL Hyatt, T Moak, MJ Hatfield, L Tsurkan… - Journal of medicinal …, 2007 - ACS Publications
… (diphenylethane-1,2-dione) as a potent selective inhibitor of CEs, we sought to evaluate the
inhibitory activity of related 1,2-… In mammals, they tend to be expressed in tissues likely to be …

Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils

LD Hicks, JL Hyatt, T Moak, CC Edwards… - Bioorganic & medicinal …, 2007 - Elsevier
… We have synthesized and assessed the ability of symmetrical fluorobenzoins and fluorobenzils
to inhibit mammalian carboxylesterases (CE). The majority of the latter were excellent …