Results 171 to 180 of about 10,733 (194)
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Structural Insights into Drug Processing by Human Carboxylesterase 1: Tamoxifen, Mevastatin, and Inhibition by Benzil

Journal of Molecular Biology, 2005
Human carboxylesterase 1 (hCE1) exhibits broad substrate specificity and is involved in xenobiotic processing and endobiotic metabolism. We present and analyze crystal structures of hCE1 in complexes with the cholesterol-lowering drug mevastatin, the breast cancer drug tamoxifen, the fatty acyl ethyl ester (FAEE) analogue ethyl acetate, and the novel ...
Christopher D, Fleming   +10 more
openaire   +2 more sources

Selective and sensitive detection and quantification of human carboxylesterase 1 by a ratiometric fluorescence probe

Dyes and Pigments, 2019
Abstract A novel ratiometric fluorescent probe derived from 2-(2′-hydroxy-3′-methoxyphenyl) benzothiazole (HMBT) for human carboxylesterase 1 (hCES1) has been synthesized and well characterized. The probe was designed by modulating the excited state intramolecular proton transfer (ESIPT) emission of HMBT via introducing of an octanoyl group.
Zhao-ming Liu   +6 more
openaire   +1 more source

Selective Near-Infrared Fluorescent Chemosensors for Human Carboxylesterase 1 Activity

Analytical Chemistry
Carboxylesterase 1 (CES1) is an enzyme that is crucial for drug metabolism by hydrolyzing a range of ester- and amide-containing drugs, which, in turn, influences drug efficacy and safety. Accurate monitoring of CES1 activity bears importance for the clinical setting, providing invaluable guidance in the utilization of numerous drugs that undergo ...
Seylan Ayan   +4 more
openaire   +2 more sources

Exploring human carboxylesterases 1 and 2 selectivity of two families of substrates at an atomistic level

Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics
Human carboxylesterases (CES) are enzymes that play an important role in the metabolism and biotransformation of diverse substances. The two more relevant isoforms, CES1A1 and CES2A1, catalyze the hydrolysis of numerous approved drugs and prodrugs. The elucidation of CES isoform substrates specificity constitutes a very relevant medicinal chemistry ...
Ribone, Sergio Roman   +2 more
openaire   +3 more sources

P.1.b.007 Developmental expression and activity of carboxylesterase 1 and carboxylesterase 2 in mouse and human

European Neuropsychopharmacology, 2009
H.J. Zhu   +4 more
openaire   +1 more source

New bysspectin A derivatives as potent inhibitors of human carboxylesterase 2A

European Journal of Medicinal Chemistry, 2023
Xinyong Liu, Yunqing Song
exaly  

Discovery of a highly specific and efficacious inhibitor of human carboxylesterase 2 by large-scale screening

International Journal of Biological Macromolecules, 2019
Yun-Qing Song   +2 more
exaly  

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