Presence and inter-individual variability of carboxylesterases (CES1 and CES2) in human lung
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 +5 more
openaire +5 more sources
NOS3 rs3918188C>A is associated with susceptibility to resistant hypertension while CES1 genetic variation was not associated with resistant hypertension among South Africans [PDF]
IntroductionGenetic variation in genes coding for enzymes metabolising antihypertensive drugs, may affect the efficacy of angiotensin converting enzyme (ACE) inhibitors such as enalapril, potentially leading to resistant hypertension (RHTN).
Jonathan N. Katsukunya +17 more
doaj +2 more sources
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 +4 more
doaj +2 more sources
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 +5 more
doaj +2 more sources
Genetic variants of ABCB1 and CES1 genes on dabigatran metabolism in the Kazakh population [PDF]
Background: Allelic variants of genes encoding enzymes of the esterase system (CES1) and P-glycoprotein (ABCB1) can change the metabolism and pharmacokinetics of dabigatran.
Ayan Abdrakhmanov +10 more
doaj +3 more sources
Sacubitril is selectively activated by carboxylesterase 1 (CES1) in the liver and the activation is affected by CES1 genetic variation [PDF]
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 +5 more
+9 more sources
Carboxylesterase 1 family knockout alters drug disposition and lipid metabolism
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 +15 more
doaj +1 more source
Hepatic carboxylesterase 1 is induced by glucose and regulates postprandial glucose levels. [PDF]
Metabolic syndrome, characterized by obesity, hyperglycemia, dyslipidemia and hypertension, increases the risks for cardiovascular disease, diabetes and stroke.
Jiesi Xu +6 more
doaj +1 more source
A recent genome-wide copy number variations (CNVs) scan identified a 16q12.2 deletion that included the carboxylesterase 1 (CES1) gene, which is important in the metabolism of fatty acids and cholesterol.
Bing bing Chen +8 more
doaj +1 more source
Carboxylesterase 1 gene duplication and mRNA expression in adipose tissue are linked to obesity and metabolic function. [PDF]
CONTEXT AND AIMS: Carboxylesterase 1 (CES1) appears to play an important role in the control of the metabolism of triglycerides and cholesterol in adipocytes and other cell types including hepatocytes.
Martin Friedrichsen +5 more
doaj +1 more source

