Structural insights into drug processing by human carboxylesterase 1: tamoxifen, mevastatin, and inhibition by benzil

CD Fleming, S Bencharit, CC Edwards, JL Hyatt… - Journal of molecular …, 2005 - Elsevier
Human carboxylesterase 1 (hCE1) exhibits broad substrate specificity and is involved in
xenobiotic processing and endobiotic metabolism. We present and analyze crystal …

Modifications of human carboxylesterase for improved prodrug activation

JM Hatfield, M Wierdl, RM Wadkins… - Expert opinion on drug …, 2008 - Taylor & Francis
Background: Carboxylesterases (CEs) are ubiquitous enzymes responsible for the
hydrolysis of numerous clinically useful drugs. As ester moieties are frequently included in …

In silico design and evaluation of carboxylesterase inhibitors

SV Stoddard, X Yu, PM Potter… - Journal of Pesticide …, 2010 - jstage.jst.go.jp
Carboxylesterases (CEs) are important enzymes that catalyze biological detoxification,
hydrolysis of certain pesticides, and metabolism of many esterified drugs. The development …

Examination of the carboxylesterase phenotype in human liver

MK Ross, A Borazjani, R Wang, JA Crow… - Archives of biochemistry …, 2012 - Elsevier
Carboxylesterases (CES) metabolize esters. Two CES isoforms are expressed in human
liver (CES1 and CES2) and liver extracts are used in reaction phenotyping studies to discern …

Different inhibitory effects in rat and human carboxylesterases

S Takahashi, M Katoh, T Saitoh, M Nakajima… - Drug metabolism and …, 2009 - ASPET
In vitro inhibition studies on drug-metabolizing enzyme activity are useful for understanding
drug-drug interactions and for drug development. However, the profile of the inhibitory …

In vitro evaluation of inhibitory effects of antidiabetic and antihyperlipidemic drugs on human carboxylesterase activities

T Fukami, S Takahashi, N Nakagawa, T Maruichi… - Drug metabolism and …, 2010 - ASPET
Human carboxylesterase (CES) 1A is responsible for the biotransformation of angiotensin-
converting enzyme (ACE) inhibitors such as imidapril and temocapril. Because antidiabetic …

Design, synthesis, and structure-activity relationship study of glycyrrhetinic acid derivatives as potent and selective inhibitors against human carboxylesterase 2

LW Zou, YG Li, P Wang, K Zhou, J Hou, Q Jin… - European journal of …, 2016 - Elsevier
Abstract Human carboxylesterase 2 (hCE2), one of the major carboxylesterases in the
human intestine and various tumour tissues, plays important roles in the oral bioavailability …

Identification of di-(2-ethylhexyl) phthalate-induced carboxylesterase 1 in C57BL/6 mouse liver microsomes: purification, cDNA cloning, and baculovirus-mediated …

T Furihata, M Hosokawa, N Koyano, T Nakamura… - Drug metabolism and …, 2004 - ASPET
Several mouse carboxylesterase (CES) isozymes have been identified, but information
about their roles in drug metabolism is limited. In this study, we purified and characterized a …

Inhibitory effects of phthalate esters (PAEs) and phthalate monoesters towards human carboxylesterases (CESs)

J Gong, X Yi, J Liang, Z Liu, Z Du - Toxicology and Applied Pharmacology, 2024 - Elsevier
Phthalate esters (PAEs), accompanied by phthalate monoesters as hydrolysis metabolites in
humans, have been widely used as plasticizers and exhibited disruptive effects on the …

Evaluation of the inhibitory effects of antihypertensive drugs on human carboxylesterase in vitro

X Yanjiao, Z Chengliang, L Xiping, W Tao… - Drug Metabolism and …, 2013 - Elsevier
Human carboxylesterase (CES) 1A and CES2, two major forms of human CES, dominate the
pharmacokinetics of most prodrugs such as imidapril and irinotecan (CPT-11) …