ReviewCurrent drug metabolism2019
The Impact of Carboxylesterases in Drug Metabolism and Pharmacokinetics.
Review in Current drug metabolism, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 75 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
75 citing papers in PubMed, 191 citations in OpenAlex.
- Pharmacokinetic Properties and Therapeutic Effectiveness of Remimazolam in ICU Patients With Mechanical Ventilation: A Preliminary Study.Pharmacology research & perspectives · 2025Trial
- Soft drugs: design principles and topical applications.Nature reviews. Drug discovery · 2026Review
- StagX1, an isoquinolinone compound, selectively targets CES1-positive Ewing sarcoma cells as a potential therapeutic agent.Molecular therapy. Oncology · 2026Article
- Impact of cannabis, benzodiazepines, and methamphetamine use on inflammatory and hepatic biomarkers in Benin City, Nigeria: a case-control study.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Genetic architecture of the murine serum metabolome reveals carboxyl esterases as master regulators of circulating fatty acid metabolism.bioRxiv : the preprint server for biology · 2026Article
- An Approach Toward Radioiodination and Radiopharmacological Evaluation of a Carborane-Containing Analog of Indomethacin.Molecules (Basel, Switzerland) · 2026Article
- Oridonin exerts dual therapeutic effects in MASLD mice by integrating lipid homeostasis and drug bioactivation via the LXRα-CES1/CES2 pathway.Acta pharmacologica Sinica · 2026Article
- Ester Prodrug NLRP3 Inflammasome Inhibitor NT-0796 is Brain Active due to Activation by Local Expression of Carboxylesterase-1.ACS chemical neuroscience · 2026Article
- Stereoselective design of amino acid bioconjugates: targeting strategies and physicochemical optimization.RSC medicinal chemistry · 2026Review
- Experimental and In Silico Approaches to Study Carboxylesterase Substrate Specificity.Journal of xenobiotics · 2026Review
- ModularFrontiers in toxicology · 2026Article
- Computational proteome-wide screening reveals potential targets of astragaloside IV inFrontiers in veterinary science · 2026Article
- Flumazenil reversal of remimazolam-induced sedation: a narrative review of safety, pharmacokinetics, and clinical considerations.Frontiers in medicine · 2026Review
- Biotin methyl ester enhances cargo release in RUSH system and enables rapid biotinylation with TurboID.Communications biology · 2025Article
- Confounding Effect of Hepatic Carboxylesterase 1 (CES1) Variability on Clopidogrel Oxidation.Molecular pharmaceutics · 2025Article
- Discovery of orally active and serine-targeting covalent inhibitors against hCES2A for ameliorating irinotecan-triggered gut toxicity.Acta pharmaceutica Sinica. B · 2025Article
- Characterization of hydrolase activity in ocular tissues of humans and preclinical species.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Peptide-Drug Conjugates: A New Hope for Cancer.Journal of peptide science : an official publication of the European Peptide Society · 2025Review
- Comparative transcriptomic profiling of drug-metabolizing enzymes and drug transporters in rabbit ocular subtissues, liver, and duodenum.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Discovery of BAY 3389934 Hydrochloride: A Potent and Selective Small-Molecule Dual Factor IIa/Xa Inhibitor with Short Half-Life for the Acute Treatment of Sepsis-Induced Coagulopathy.Journal of medicinal chemistry · 2025Article
15 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
1 author at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundCarboxylesterases (CES) play a critical role in catalyzing hydrolysis of esters, amides, carbamates and thioesters, as well as bioconverting prodrugs and soft drugs. The unique tissue distribution of CES enzymes provides great opportunities to design prodrugs or soft drugs for tissue targeting. Marked species differences in CES tissue distribution and catalytic activity are particularly challenging in human translation.
methodsReview and summarization of CES fundamentals and applications in drug discovery and development.
resultsHuman CES1 is one of the most highly expressed drug metabolizing enzymes in the liver, while human intestine only expresses CES2. CES enzymes have moderate to high inter-individual variability and exhibit low to no expression in the fetus, but increase substantially during the first few months of life. The CES genes are highly polymorphic and some CES genetic variants show significant influence on metabolism and clinical outcome of certain drugs. Monkeys appear to be more predictive of human pharmacokinetics for CES substrates than other species. Low risk of clinical drug-drug interaction is anticipated for CES, although they should not be overlooked, particularly interaction with alcohols. CES enzymes are moderately inducible through a number of transcription factors and can be repressed by inflammatory cytokines.
conclusionAlthough significant advances have been made in our understanding of CESs, in vitro - in vivo extrapolation of clearance is still in its infancy and further exploration is needed. In vitro and in vivo tools are continuously being developed to characterize CES substrates and inhibitors.
Indexed as
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What Socratic holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.