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In Vitro and In Vivo Metabolism Studies
Drug metabolism studies play a critical role in the discovery and development of new chemical entities. These studies provide in-depth understanding...
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In vitro screening of understudied PFAS with a focus on lipid metabolism disruption
Per- and polyfluoroalkyl substances (PFAS) are man-made chemicals used in many industrial applications. Exposure to PFAS is associated with several...
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In silico and in vitro metabolism studies of the new synthetic opiate AP-237 (bucinnazine) using bioinformatics tools
The recent emergence of new synthetic opioids (NSOs) compounds in the illicit market is increasingly related to fatal cases. Identification and...
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In vitro to in vivo extrapolation to derive a metabolism factor for estimating the aggregate exposure to salicylic acid after dermal exposure of its esters
As part of the safety assessment of salicylate esters in cosmetics, we developed a metabolism factor based on in vitro to in vivo extrapolation...
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In Vitro and In Silico ADME Prediction
Pharmacokinetic issues have been identified as a major cause for the attrition of new chemical entities in drug discovery. High development costs and...
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Preclinical Pharmacokinetics and in vitro Metabolism of FHND5071, a Novel Selective RET Kinase Inhibitor
Background and ObjectivesRearranged during transfection (RET) is a transmembrane receptor tyrosine kinase that plays a crucial role in tumorigenesis....
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Metabolism of alcohol ethoxylates (AEs) in rat, hamster, and human hepatocytes and liver S9: a pilot study for metabolic stability, metabolic pathway, and metabolites identification in vitro and in silico
Alcohol ethoxylates (AEs) are a well-known class of non-ionic surfactants widely used by the personal care market. The aim of this study was to...
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Combined contributions of cytochrome P450s (CYPs) and non-enzymatic metabolism in the in vitro biotransformation of anaprazole, a novel proton pump inhibitor
Anaprazole, a new proton pump inhibitor (PPI), is designed for the treatment of acid-related diseases, such as gastric ulcers and gastroesophageal...
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Cardiac Metabolism
The heart is composed of a heterogeneous mixture of cellular components perfectly intermingled and able to integrate common environmental signals to...
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Use of innovative, cross-disciplinary in vitro, in silico and in vivo approaches to characterize the metabolism of chloro-alpha-pyrrolidinovalerophenone (4-Cl-PVP)
Synthetic cathinones constitute a family of new psychoactive substances, the consumption of which is increasingly worldwide. A lack of metabolic...
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Drug Metabolism
Living systems have developed elimination mechanisms to dispose of waste products and protect themselves from exposure to potentially harmful...
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Metabolism Pharmacology
Safety pharmacology defines studies that investigate the potential undesirable pharmacodynamic effects of a substance on physiological functions in...
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Evaluation of Metabolism-Dependent Drug Toxicity
Drug metabolism is well-established to play key roles in drug toxicity. Drug toxicity can be enhanced via biotransformation of a parent drug to...
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Perspectives on Retinal Dolichol Metabolism, and Visual Deficits in Dolichol Metabolism-Associated Inherited Disorders
De novo synthesis of dolichol (Dol) and dolichyl phosphate (Dol-P) is essential for protein glycosylation. Herein, we provide a brief overview of Dol...
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In vitro metabolism of helenalin and its inhibitory effect on human cytochrome P450 activity
Sesquiterpene lactone helenalin is used as an antiphlogistic in European and Chinese folk medicine. The pharmacological activities of helenalin have...
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Metabolism in Hematopoiesis and Its Malignancy
Hematopoietic stem cells (HSCs) are multipotent stem cells that can self-renew and generate all blood cells of different lineages. The system is...
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Serine metabolism in macrophage polarization
ObjectiveEmerging studies have revealed that macrophages possess different dependences on the uptake, synthesis, and metabolism of serine for their...
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Metabolism of Cancer Stem Cell
Nowadays, cancer is considered as a stem cell disease of altered metabolism. The metabolism of cancer stem cells (CSCs) is less well characterized...
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Lactate as a major epigenetic carbon source for histone acetylation via nuclear LDH metabolism
Histone acetylation involves the transfer of two-carbon units to the nucleus that are embedded in low-concentration metabolites. We found that...
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HERC5 downregulation in non-small cell lung cancer is associated with altered energy metabolism and metastasis
BackgroundMetastasis is the leading cause of cancer-related death in non-small cell lung cancer (NSCLC) patients. We previously showed that low HERC5...
