ArticleNature chemical biology2014
Integrated phenotypic and activity-based profiling links Ces3 to obesity and diabetes.
Article in Nature chemical biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers.
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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.
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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.
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Who cites it
59 citing papers in PubMed.
- Inhibiting menin attenuates high-fat diet-induced weight gain by limiting intestinal lipid absorption in mice.The Journal of clinical investigation · 2026Article
- The Pyrazolone Scaffold: A Privileged Motif for Molecular Hybridization in Drug Discovery.ChemMedChem · 2026Review
- CES3 promotes NSCLC progression via lipid metabolic reprogramming regulated by TFAP2A.Journal of Cancer · 2026Article
- Discovery of lignans as the effective inhibitors of CES1A alleviate lipid droplets formation.Journal of enzyme inhibition and medicinal chemistry · 2025Article
- Effects of exercise and walnut oil on CES1 and inflammatory factors in the liver of type 2 diabetic rats.European journal of medical research · 2025Article
- A fluorescent probe with a vanillin-pyridine-imidazole core structure for carboxylesterase detection in macrophage polarization during bone homeostasis.Frontiers in chemistry · 2025Article
- Increased serum carboxylesterase-1 levels are associated with metabolic dysfunction associated steatotic liver disease and metabolic syndrome in children with obesity.Italian journal of pediatrics · 2024Article
- Thermogenic Fat as a New Obesity Management Tool: From Pharmaceutical Reagents to Cell Therapies.Biomedicines · 2024Review
- Gehua Jiejiu Dizhi decoction ameliorates alcoholic fatty liver in mice by regulating lipid and bile acid metabolism and with exertion of antioxidant stress based on 4DLabel-free quantitative proteomic study.Journal of traditional Chinese medicine = Chung i tsa chih ying wen pan · 2024Article
- Localization of Sites of Osimertinib Action in Rat Intestine, Skin, and Lung by Immunohistochemistry.Acta histochemica et cytochemica · 2023Article
- CES1 Releases Oxylipins from Oxidized Triacylglycerol (oxTAG) and Regulates Macrophage oxTAG/TAG Accumulation and PGEACS chemical biology · 2023Article
- Firefly luciferin methyl ester illuminates the activity of multiple serine hydrolases.Chemical communications (Cambridge, England) · 2023Article
- MFGE8 links absorption of dietary fatty acids with catabolism of enterocyte lipid stores through HNF4γ-dependent transcription of CES enzymes.Cell reports · 2023Article
- Prenylcysteine Oxidase 1 Is a Key Regulator of Adipogenesis.Antioxidants (Basel, Switzerland) · 2023Article
- Organ and cell-specific biomarkers of Long-COVID identified with targeted proteomics and machine learning.Molecular medicine (Cambridge, Mass.) · 2023Article
- Interfering with lipid metabolism through targeting CES1 sensitizes hepatocellular carcinoma for chemotherapy.JCI insight · 2023Article
- Discovery of triterpenoids as potent dual inhibitors of pancreatic lipase and human carboxylesterase 1.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Carboxylesterase 1d Inactivation Augments Lung Inflammation in Mice.ACS pharmacology & translational science · 2022Article
- Adipose tissue-specific ablation of Ces1d causes metabolic dysregulation in mice.Life science alliance · 2022Article
- A clickable photoaffinity probe of betulinic acid identifies tropomyosin as a target.Acta pharmaceutica Sinica. B · 2022Article
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16 authors.
Funding
Abstract
Phenotypic screening is making a comeback in drug discovery as the maturation of chemical proteomics methods has facilitated target identification for bioactive small molecules. A limitation of these approaches is that time-consuming genetic methods or other means are often required to determine the biologically relevant target (or targets) from among multiple protein-compound interactions that are typically detected. Here, we have combined phenotypic screening of a directed small-molecule library with competitive activity-based protein profiling to map and functionally characterize the targets of screening hits. Using this approach, we identify carboxylesterase 3 (Ces3, also known as Ces1d) as a primary molecular target of bioactive compounds that promote lipid storage in adipocytes. We further show that Ces3 activity is markedly elevated during adipocyte differentiation. Treatment of two mouse models of obesity-diabetes with a Ces3 inhibitor ameliorates multiple features of metabolic syndrome, illustrating the power of the described strategy to accelerate the identification and pharmacologic validation of new therapeutic targets.
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