Results 51 to 60 of about 15,347 (200)

Pharmacogenomic assessment of carboxylesterases 1 and 2

Genomics, 2004
Human carboxylesterases 1 and 2 (CES1 and CES2) catalyze the hydrolysis of many exogenous compounds. Alterations in carboxylesterase sequences could lead to variability in both the inactivation of drugs and the activation of prodrugs. We resequenced CES1 and CES2 in multiple populations (n = 120) to identify single-nucleotide polymorphisms and ...
Sharon, Marsh, Ming, Xiao, Jinsheng, Yu, Ranjeet, Ahluwalia, Matthew, Minton, Robert R, Freimuth, Pui-Yan, Kwok, Howard L, McLeod   +7 more
openaire   +2 more sources

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

Acute Toxicity of Insecticide Thiamethoxam to Crayfish (Astacus leptodactylus): Alterations in Oxidative Stress Markers, ATPases and Cholinesterase

Acta Chimica Slovenica, 2021
Thiamethoxam (Thmx) is a globally used neonicotinoid pesticide contaminated in freshwater ecosystems with residues detected in fishery products. Astacus leptodactylus is a popular freshwater crustacean  that is cultivated and exported in many countries ...
Miraç Uçkun, Ertan Yoloğlu, Aysel Alkan Uçkun, Özden Barım Öz   +3 more
doaj   +1 more source

Confounding Effect of Hepatic Carboxylesterase 1 (CES1) Variability on Clopidogrel Oxidation. [PDF]

Mol Pharm
Clopidogrel, a frequently used prodrug, is converted to its active metabolite through the intermediate 2-oxo-clopidogrel by cytochrome P450 (CYP) enzymes, which accounts for only 5%-15% of its metabolism. Majority of the clopidogrel dose (85%-90%) is extensively hydrolyzed to its inactive metabolite, clopidogrel carboxylic acid by carboxylesterase 1 ...
Subash S, Singh DK, Khojasteh SC, Murray BP, Zientek MA, Jones RS, Kulkarni P, Smith BJ, Prasad B.   +8 more
europepmc   +3 more sources

Carboxylesterase 1 genes:systematic review and evaluation of existing genotyping procedures [PDF]

, 2018
The carboxylesterase 1 gene (CES1) encodes a hydrolase that metabolizes commonly used drugs. The CES1-related pseudogene, carboxylesterase 1 pseudogene 1 (CES1P1), has been implicated in gene exchange with CES1 and in the formation of hybrid genes ...
Henrik Berg Rasmussen, Majbritt Busk Madsen, Madsen, Majbritt Busk, Rasmussen, Henrik Berg   +3 more
core   +1 more source

Dual-Purpose Inoculants and Their Effects on Corn Silage

Microorganisms, 2020
This study was conducted to screen dual-purpose lactic acid bacteria (LAB) from uncontrolled farm-scale silage, and then we confirmed their effects on corn silage.
Dimas Hand Vidya Paradhipta, Seong Shin Lee, Byeongsam Kang, Young Ho Joo, Hyuk Jun Lee, Yeyeong Lee, Jinwoo Kim, Sam Churl Kim   +7 more
doaj   +1 more source

Inhibition of carboxylesterase activity of THP1 monocytes/macrophages and recombinant human carboxylesterase 1 by oxysterols and fatty acids [PDF]

Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids, 2010
Two major isoforms of human carboxylesterases (CEs) are found in metabolically active tissues, CES1 and CES2. These hydrolytic enzymes are involved in xenobiotic and endobiotic metabolism. CES1 is abundantly expressed in human liver and monocytes/macrophages, including the THP1 cell line; CES2 is expressed in liver but not in monocytes/macrophages. The
J Allen, Crow, Katye L, Herring, Shuqi, Xie, Abdolsamad, Borazjani, Philip M, Potter, Matthew K, Ross   +5 more
openaire   +2 more sources

Trypanosoma cruzi: Carboxylesterase activity in intact epimastigotes [PDF]

, 1983
1. 1. Carboxylesterase activity corresponding to types A and B has been demonstrated in intact T. cruzi epimastigotes as shown by the hydrolysis of several esters of p-nitrophenol and the effect of suitable inhibitors. 2. 2.
Repetto Scaramelli, Yolanda, Morello Casté, Antonio, Aldunate,   +2 more
core   +1 more source

Reaction mechanism of the pNPA hydrolysis by the human carboxylesterase-1: geometry configurations at PES stationary points

, 2021
Reaction mechanism of the pNPA (p-nitrophenyl acetate) hydrolysis by the human carboxylesterase-1.
Nemukhin Alexander V., Kulakova Anna M., Khrenova Maria G.   +2 more
core   +1 more source

Chemically Regulated STING‐Activating Prodrugs of Deoxyribose Cyclic Dinucleotides Elicit Robust Immune Activation and Durable Antitumor Immunity

Angewandte Chemie, EarlyView.
All three diastereoisomers of an esterase‐sensitive phosphotriester dCDN prodrug demonstrate improved activity. The (Rp,Rp) diastereoisomer shows the highest activity with an EC50 of 1.7 nM in STING activation and displays the most pronounced antitumor activity via intravenous administration, significantly suppressing tumor proliferation, extending the
Zhiqiang Xie, Huimin Liu, Yuchen Yang, Xiaohan Sun, Jingwen Wang, Tianxiang Liu, Baifan Wang, Wenrui Qiu, Yiwen Sun, Yuting Bai, Yao Zhang, Dejun Ma, Rong Xiang, Shibo Li, Zhen Xi   +14 more
wiley   +2 more sources