Results 31 to 40 of about 6,033 (189)

Cannabinoid Inhibition of Carboxylesterase 1 (CES1)

The FASEB Journal, 2019
The increasing use of cannabis for both medical indications and on a recreational basis poses a potential for drug interactions between cannabis or one or more of its constituents and conventional therapeutic agents. Although significant efforts have been made to assess the in vitro and
Yuli Qian, John S. Markowitz
openaire   +1 more source

Accurate Assessment and Tracking the Process of Liver-Specific Injury by the Residual Tissue Activity of Carboxylesterase 1 and Dipeptidyl Peptidase 4

Engineering, 2022
Accurately assessing and tracking the progression of liver-specific injury remains a major challenge in the field of biomarker research. Here, we took a retrospective validation approach built on the mutuality between serum and tissue biomarkers to ...
Qiusha Pan, Peifang Song, Zhenhua Ni, Xingkai Qian, Anqi Wang, Liwei Zou, Yong Liu, Ping Wang, Weidong Zhang, Hong Ma, Ling Yang   +10 more
doaj   +1 more source

Global inactivation of carboxylesterase 1 (Ces1/Ces1g) protects against atherosclerosis in Ldlr −/− mice [PDF]

Scientific Reports, 2017
AbstractAtherosclerotic cardiovascular disease is a leading cause of death in the western world. Increased plasma triglyceride and cholesterol levels are major risk factors for this disease. Carboxylesterase 1 (Ces1/Ces1g) has been shown to play a role in metabolic control.
Jiesi Xu, Yang Xu, Yanyong Xu, Liya Yin, Yanqiao Zhang   +4 more
openaire   +2 more sources

Metabolism of remimazolam in primary human hepatocytes during continuous long-term infusion in a 3-D bioreactor system [PDF]

, 2019
Background: Remimazolam is an ultra-short acting benzodiazepine under development for procedural sedation and general anesthesia. It is hydrolyzed by CES1 to an inactive metabolite (CNS7054).
Damm, Georg, Freyer, Nora, Greuel, Selina, Knöspel, Fanny, Petersen, Karl-Uwe, Schneider, Christin, Seehofer, Daniel, Stöhr, Thomas, Zeilinger, Katrin   +8 more
core   +1 more source

Combined Ensemble Docking and Machine Learning in Identification of Therapeutic Agents with Potential Inhibitory Effect on Human CES1

Molecules, 2019
The human carboxylesterase 1 (CES1), responsible for the biotransformation of many diverse therapeutic agents, may contribute to the occurrence of adverse drug reactions and therapeutic failure through drug interactions.
Eliane Briand, Ragnar Thomsen, Kristian Linnet, Henrik Berg Rasmussen, Søren Brunak, Olivier Taboureau   +5 more
doaj   +1 more source

Fluorogenic chemical tools to shed light on CES1-mediated adverse drug interactions. [PDF]

Chem Commun (Camb)
Studying factors that cause interindividual variability of carboxylesterase 1 (CES1) activity is currently difficult due to limited methods. To address this, fluorogenic chemical tools that can monitor CES1 activity in live cells were developed.
Karns CJ, Spidle TP, Adusah E, Gao M, Nehls JE, Beck MW.   +5 more
europepmc   +4 more sources

Regulation of carboxylesterase 1 (CES1) in human adipose tissue

Biochemical and Biophysical Research Communications, 2009
Carboxylesterase 1 (CES1) has recently been suggested to play a role in lipolysis. Our aim was to study the regulation of CES1 expression in human adipose tissue. In the SOS Sib Pair Study, CES1 expression was higher in obese compared with lean sisters (n=78 pairs, P=8.7x10(-18)) and brothers (n=12 pairs, P=0.048).
Jernås, Margareta, Olsson, Bob, Arner, Peter, Jacobson, Peter, Sjöström, Lars, Walley, Andrew, Froguel, Philippe, McTernan, Philip G., Hoffstedt, Johan, Carlsson, Lena M.S.   +9 more
openaire   +2 more sources

Comparison of the structure and activity of glycosylated and asglycosylated human carboxylesterase 1 [PDF]

, 2015
Human Carboxylesterase 1 (hCES1) is the key liver microsomal enzyme responsible for detoxification and metabolism of a variety of clinical drugs. To analyse the role of the single N-linked glycan on the structure and activity of the enzyme, authentically
AC Hemmert, AJ McCoy, Andreas Hofmann, AR Aricescu, CD Fleming, CD Fleming, CL Morton, David J. Scott, DI Stuart, DL Kroetz, DL Kroetz, DL Ollis, EI Parkinson, F Gorrec, G Koshland DN, GN Murshudov, HM Greenblatt, HM Greenblatt, J Monod, J Newman, JA Crow, JE Nettleship, JE Nettleship, JL Vaughn, Joanne E. Nettleship, K Nishi, LA Needham, M Alam, M Husokawa, M Suzuki-Kurasaki, Martin A. Walsh, Michael H. Charlton, MJ Hatfield, Nahid Rahman, NS Berrow, P Emsley, PA Karplus, PJ Reeves, PM Potter, PM Potter, Raymond J. Owens, RM Wadkins, RM Wadkins, RS Holmes, S Bencharit, S Bencharit, S Bencharit, S Bencharit, S Bencharit, S Takahashi, SN Ho, T Satoh, T Satoh, TS Walter, U Boonyuen, Victoria Arena de Souza, VT Chang   +56 more
core   +6 more sources

The novel carboxylesterase 1 variant c.662A>G may decrease the bioactivation of oseltamivir in humans. [PDF]

PLoS ONE, 2017
Human carboxylesterase 1 (CES1) is a serine esterase that hydrolyses various exogenous and endogenous compounds including oseltamivir, a prodrug used to treat influenza. A novel CES1 c.662A>G single nucleotide polymorphism (SNP) was predicted to decrease
Jaeseong Oh, SeungHwan Lee, Howard Lee, Joo-Youn Cho, Seo Hyun Yoon, In-Jin Jang, Kyung-Sang Yu, Kyoung Soo Lim   +7 more
doaj   +1 more source

Permeability of 16 Straight- and Branched-Chain Parabens Using the Caco-2 Assay. [PDF]

J Appl Toxicol
ABSTRACT The in vitro intestinal permeability of straight‐ and branched‐chain parabens has not been extensively investigated. Sixteen parabens were tested in the Caco‐2 assay. Passive diffusion was measured using PAMPA. The transport of the MCT1 substrate, p‐coumaric acid, as well as propylparaben and isopropylparaben, was investigated.
Hewitt NJ, Mayer M, Schepky A, Ellison C.   +3 more
europepmc   +2 more sources