Results 21 to 30 of about 3,685 (179)

Carboxylesterase 1 is a core metabolic vulnerability of platinum-resistant high-grade serous ovarian carcinoma [PDF]

Journal of Experimental & Clinical Cancer Research
Background Platinum-resistant high-grade serous ovarian carcinoma (HGSOC) is a major clinical challenge, with high mortality rates and no effective therapeutic options. Metabolic adaptations—including enhanced lipid catabolism, oxidative phosphorylation (
Irene Flati, Davide Vecchiotti, Fiorenza Di Giovanni, Daniela Verzella, Francesca Dall’Aglio, Angelo Sarra, Chiara Battistini, Melissa Zambuto, Giuseppe Frisullo, Jessica Cornice, Ilaria Nunzi, Mauro Di Vito Nolfi, Harry J. Whitwell, Francesca Veglianti, Hafiz Nadeem Khan, Saverio Marchi, Guido Franzoso, Ugo Cavallaro, Daniel D’Andrea, Edoardo Alesse, Francesca Zazzeroni, Daria Capece   +21 more
doaj   +2 more sources

The role of ABCB1 and CES1 genotypes on the efficacy and safety of dabigatran: a systematic review and meta-analysis [PDF]

Human Genomics
Introduction : Dabigatran is a direct oral anticoagulant associated with a high incidence of gastrointestinal bleeding, which presents a significant clinical concern.
Weam Aldiban, Nada G. Hamam, Nereen A. Almosilhy, Kholoud Elsamman, Mohamed Wagdy, Doaa Mashaly, Suhel F. Batarseh, Youssef El-Sherif, Basma Badrawy Khalefa, Zina Otmani   +9 more
doaj   +2 more sources

Associations Between CES1 Variants and Dosing and Adverse Effects in Children Taking Methylphenidate

Frontiers in Pediatrics, 2023
BackgroundMethylphenidate is the most prescribed stimulant to treat attention deficit-hyperactivity disorder (ADHD). Despite its widespread usage, a fair proportion of children are classified as non-responders to the medication. Variability in response and occurrence of adverse events with methylphenidate use may be due to several factors, including ...
Jacob T Brown, Catherine A. McCarty
exaly   +4 more sources

Melatonin Inhibits Lipid Accumulation to Repress Prostate Cancer Progression by Mediating the Epigenetic Modification of CES1

Clinical and Translational Medicine, 2021
Background Androgen deprivation therapy (ADT) is the main clinical treatment for patients with advanced prostate cancer (PCa). However, PCa eventually progresses to castration‐resistant prostate cancer (CRPC), largely because of androgen receptor ...
Haruhiko Sugimura, Xiong Yang
exaly   +2 more sources

Effects of exercise and walnut oil on CES1 and inflammatory factors in the liver of type 2 diabetic rats

European Journal of Medical Research
Carboxylesterase 1 (CES1) and inflammatory factors play important roles in regulating lipid metabolism and maintaining glucose homeostasis. Exercise and walnut oil have anti-inflammatory effects, but the effects of exercise and walnut oil on CES1 and ...
Shujuan Hu, Xuan Liu, Yiting Ding, Jun Chen, Xianwang Wang   +4 more
doaj   +2 more sources

Presence and inter-individual variability of carboxylesterases (CES1 and CES2) in human lung

Biochemical Pharmacology, 2018
Lungs are pharmacologically active organs and the pulmonary drug metabolism is of interest for inhaled drugs design. Carboxylesterases (CESs) are enzymes catalyzing the hydrolysis of many structurally different ester, amide and carbamate chemicals, including prodrugs.
Gabriele Morena, Puccini Paola, Lucchi Marco, Vizziello Anna, Gervasi Pier Giovanni, Longo Vincenzo   +5 more
openaire   +5 more sources

Simultaneously Predicting the Pharmacokinetics of CES1-Metabolized Drugs and Their Metabolites Using Physiologically Based Pharmacokinetic Model in Cirrhosis Subjects

Pharmaceutics
Hepatic carboxylesterase 1 (CES1) metabolizes numerous prodrugs into active ingredients or direct-acting drugs into inactive metabolites. We aimed to develop a semi-physiologically based pharmacokinetic (semi-PBPK) model to simultaneously predict the ...
Xin Luo, Zexin Zhang, Ruijing Mu, Guangyu Hu, Li Liu, Xiaodong Liu   +5 more
doaj   +2 more sources

Unraveling the Link Between Azathioprine and Acute Pancreatitis: Integrating Network Toxicology, Machine Learning, and Mendelian Randomization [PDF]

CPT: Pharmacometrics & Systems Pharmacology
Azathioprine (AZA), a widely used immunosuppressant, can induce acute pancreatitis (AP), yet the underlying molecular mechanisms remain unclear. This study employed an integrative multiomics strategy—combining network toxicology, machine learning ...
Zhijun Xie, Hang Lei, Pengcheng Zhang, Zhi Li, Wenfu Tang   +4 more
doaj   +2 more sources

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

The FASEB Journal, 2016
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 ejection fraction. As a prodrug, sacubitril must be metabolized (hydrolyzed) to its active metabolite sacubitrilat (LBQ657) to exert its intended therapeutic effects.
Jian, Shi, Xinwen, Wang, Jenny, Nguyen, Audrey H, Wu, Barry E, Bleske, Hao-Jie, Zhu   +5 more
openaire   +5 more sources

Carboxylesterase 1 family knockout alters drug disposition and lipid metabolism

Acta 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, Jing Wang, Alejandra Martínez-Chávez, Michel Hillebrand, Niels de Vries, Joke Beukers, Els Wagenaar, Yaogeng Wang, Maria C. Lebre, Hilde Rosing, Sjoerd Klarenbeek, Rahmen Bin Ali, Colin Pritchard, Ivo Huijbers, Jos H. Beijnen, Alfred H. Schinkel   +15 more
doaj   +1 more source