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 …

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 …

Dabigatran etexilate activation is affected by the CES1 genetic polymorphism G143E (rs71647871) and gender

J Shi, X Wang, JH Nguyen, BE Bleske, Y Liang… - Biochemical …, 2016 - Elsevier
The oral anticoagulant prodrug dabigatran etexilate (DABE) is sequentially metabolized by
intestinal carboxylesterase 2 (CES2) and hepatic carboxylesterase 1 (CES1) to form its …

Carboxylesterase 1 and precision pharmacotherapy: pharmacogenetics and nongenetic regulators

L Her, HJ Zhu - Drug Metabolism and Disposition, 2020 - Elsevier
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 …

Regulation of carboxylesterases and its impact on pharmacokinetics and pharmacodynamics: an up-to-date review

Y Liu, J Li, HJ Zhu - Expert Opinion on Drug Metabolism & …, 2024 - Taylor & Francis
ABSTRACT Introduction Carboxylesterase 1 (CES1) and carboxylesterase 2 (CES2) are
among the most abundant hydrolases in humans, catalyzing the metabolism of numerous …

Human carboxylesterases and fluorescent probes to image their activity in live cells

A Singh, M Gao, MW Beck - RSC Medicinal Chemistry, 2021 - pubs.rsc.org
Human carboxylesterases (CESs) are serine hydrolases that are responsible for the phase I
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 …

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 …

Comparative proteomics analysis of human liver microsomes and S9 fractions

X Wang, B He, J Shi, Q Li, HJ Zhu - Drug metabolism and disposition, 2020 - Elsevier
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 …

Sacubitril is selectively activated by carboxylesterase 1 (CES1) in the liver and the activation is affected by CES1 genetic variation

J Shi, X Wang, J Nguyen, AH Wu, BE Bleske… - Drug Metabolism and …, 2016 - Elsevier
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 …