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The expanding role of prodrugs in contemporary drug design and development
J Rautio, NA Meanwell, L Di… - Nature reviews drug …, 2018 - nature.com
Prodrugs are molecules with little or no pharmacological activity that are converted to the
active parent drug in vivo by enzymatic or chemical reactions or by a combination of the two …
active parent drug in vivo by enzymatic or chemical reactions or by a combination of the two …
Role of carboxylesterase and arylacetamide deacetylase in drug metabolism, physiology, and pathology
M Nagaoka, Y Sakai, M Nakajima, T Fukami - Biochemical Pharmacology, 2024 - Elsevier
Abstract Carboxylesterases (CES1 and CES2) and arylacetamide deacetylase (AADAC),
which are expressed primarily in the liver and/or gastrointestinal tract, hydrolyze drugs …
which are expressed primarily in the liver and/or gastrointestinal tract, hydrolyze drugs …
Dabigatran etexilate activation is affected by the CES1 genetic polymorphism G143E (rs71647871) and gender
The oral anticoagulant prodrug dabigatran etexilate (DABE) is sequentially metabolized by
intestinal carboxylesterase 2 (CES2) and hepatic carboxylesterase 1 (CES1) to form its …
intestinal carboxylesterase 2 (CES2) and hepatic carboxylesterase 1 (CES1) to form its …
Carboxylesterase 1 and precision pharmacotherapy: pharmacogenetics and nongenetic regulators
Carboxylesterase (CES) 1 is the most abundant drug-metabolizing enzyme in human livers,
comprising approximately 1% of the entire liver proteome. CES1 is responsible for 80 …
comprising approximately 1% of the entire liver proteome. CES1 is responsible for 80 …
Regulation of carboxylesterases and its impact on pharmacokinetics and pharmacodynamics: an up-to-date review
ABSTRACT Introduction Carboxylesterase 1 (CES1) and carboxylesterase 2 (CES2) are
among the most abundant hydrolases in humans, catalyzing the metabolism of numerous …
among the most abundant hydrolases in humans, catalyzing the metabolism of numerous …
Human carboxylesterases and fluorescent probes to image their activity in live cells
Human carboxylesterases (CESs) are serine hydrolases that are responsible for the phase I
metabolism of an assortment of ester, amide, thioester, carbonate, and carbamate …
metabolism of an assortment of ester, amide, thioester, carbonate, and carbamate …
Pharmacogenetics of angiotensin-converting enzyme inhibitors (ACEI) and angiotensin II receptor blockers (ARB) in cardiovascular diseases
L da Cunha Agostini, NNT Silva… - European Journal of …, 2024 - Elsevier
Cardiovascular diseases (CVDs) have a high mortality rate, and despite the several
available therapeutic targets, non-response to antihypertensives remains a common …
available therapeutic targets, non-response to antihypertensives remains a common …
Cholinesterase and carboxylesterase inhibitors as pharmacological agents
GF Makhaeva, EV Rudakova, NV Kovaleva… - Russian Chemical …, 2019 - Springer
Literature data and authors' own results on the role of serine hydrolases,
acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), as drug targets for treatment …
acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), as drug targets for treatment …
Comparative proteomics analysis of human liver microsomes and S9 fractions
Human liver microsomes (HLM) and human liver S9 fractions (HLS9) are commonly used to
study drug metabolism in vitro. However, a quantitative comparison of HLM and HLS9 …
study drug metabolism in vitro. However, a quantitative comparison of HLM and HLS9 …
Sacubitril is selectively activated by carboxylesterase 1 (CES1) in the liver and the activation is affected by CES1 genetic variation
Sacubitril was recently approved by the Food and Drug Administration for use in
combination with valsartan for the treatment of patients with heart failure with reduced …
combination with valsartan for the treatment of patients with heart failure with reduced …