Results 31 to 40 of about 10,733 (194)

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

open access: yes, 2021
Reaction mechanism of the pNPA (p-nitrophenyl acetate) hydrolysis by the human carboxylesterase-1.
Nemukhin Alexander V.   +2 more
core   +1 more source

Structural insights into catalytical capability for CPT11 hydrolysis and substrate specificity of a novel marine microbial carboxylesterase, E93

open access: yesFrontiers in Microbiology, 2023
IntroductionCPT11 (Irinotecan; 7-ethyl-10-[4-(1-piperidino)-1-piperidino] carbonyloxycamptothecin) is an important camptothecin-based broad-spectrum anticancer prodrug.
Yang Li   +6 more
doaj   +1 more source

Carboxylesterase 1 family knockout alters drug disposition and lipid metabolism

open access: yesActa Pharmaceutica Sinica B, 2023
The mammalian carboxylesterase 1 (Ces1/CES1) family comprises several enzymes that hydrolyze many xenobiotic chemicals and endogenous lipids. To investigate the pharmacological and physiological roles of Ces1/CES1, we generated Ces1 cluster knockout ...
Changpei Gan   +15 more
doaj   +1 more source

Age-Dependent Human Hepatic Carboxylesterase 1 (CES1) and Carboxylesterase 2 (CES2) Postnatal Ontogeny [PDF]

open access: yesDrug Metabolism and Disposition, 2016
Human hepatic carboxylesterase 1 and 2 (CES1 and CES2) are important for the disposition of ester- and amide-bond-containing pharmaceuticals and environmental chemicals. CES1 and CES2 ontogeny has not been well characterized, causing difficulty in addressing concerns regarding juvenile sensitivity to adverse outcomes associated with exposure to certain
Ronald N Hines   +2 more
openaire   +2 more sources

Baboon carboxylesterases 1 and 2: sequences, structures and phylogenetic relationships with human and other primate carboxylesterases [PDF]

open access: yesJournal of Medical Primatology, 2009
AbstractBackground  Carboxylesterase (CES) is predominantly responsible for the detoxification of a wide range of drugs and narcotics, and catalyze several reactions in cholesterol and fatty acid metabolism. Studies of the genetic and biochemical properties of primate CES may contribute to an improved understanding of human disease, including ...
Holmes, Roger S   +3 more
openaire   +3 more sources

Treatment of cholinergic‐induced status epilepticus with polytherapy targeting GABA and glutamate receptors

open access: yesEpilepsia Open, 2023
Despite new antiseizure medications, the development of cholinergic‐induced refractory status epilepticus (RSE) continues to be a therapeutic challenge as pharmacoresistance to benzodiazepines and other antiseizure medications quickly develops.
Jerome Niquet   +3 more
doaj   +1 more source

Metabolism and Interspecies Variation of IMMH-010, a Programmed Cell Death Ligand 1 Inhibitor Prodrug

open access: yesPharmaceutics, 2021
IMMH-010 is an ester prodrug of YPD-29B, a potent programmed cell death ligand 1 (PD-L1) inhibitor. The metabolism of IMMH-010 was investigated and compared in various species.
Yuchen Wang   +10 more
doaj   +1 more source

Impact of carboxylesterase 1 genetic polymorphism on trandolapril activation in human liver and the pharmacokinetics and pharmacodynamics in healthy volunteers

open access: yesClinical and Translational Science, 2021
Trandolapril, an angiotensin‐converting enzyme inhibitor prodrug, needs to be activated by carboxylesterase 1 (CES1) in the liver to exert its intended therapeutic effect.
Xinwen Wang   +6 more
doaj   +1 more source

Mouse Pharmacokinetics and In Vitro Metabolism of SH-11037 and SH-11008, Synthetic Homoisoflavonoids for Retinal Neovascularization

open access: yesPharmaceutics, 2022
Cremastranone is a member of the homoisoflavanone family with anti-angiogenic activity in the eyes. SH-11037, a potent and selective synthetic homoisoflavonoid derived from cremastranone, was studied here for pharmacokinetics and metabolism ...
Eun-yeong Kim   +5 more
doaj   +1 more source

Stability of Methylphenidate under Various pH Conditions in the Presence or Absence of Gut Microbiota

open access: yesPharmaceuticals, 2021
Methylphenidate is one of the most widely used oral treatments for attention-deficit/hyperactivity disorder (ADHD). The drug is mainly absorbed in the small intestine and has low bioavailability.
Julia Aresti-Sanz   +4 more
doaj   +1 more source

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