Metabolism-Disrupting Chemicals and the Constitutive Androstane Receptor CAR [PDF]
Cells, 2020 During the last two decades, the constitutive androstane receptor (CAR; NR1I3) has emerged as a master activator of drug- and xenobiotic-metabolizing enzymes and transporters that govern the clearance of both exogenous and endogenous small molecules ...
Jenni Küblbeck +2 more
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Clinical Relevance of the Constitutive Androstane Receptor. [PDF]
Drug Metab Dispos, 2022 Constitutive androstane receptor (CAR) (NR1I3), a xenobiotic receptor, has long been considered a master mediator of drug disposition and detoxification.
Stern S, Kurian R, Wang H.
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Constitutive androstane receptor, liver pathophysiology and chemical contaminants: current evidence and perspectives [PDF]
Frontiers in EndocrinologyIntroductionThe Constitutive Androstane Receptor (CAR) (NR1I3), a pivotal member of the xenosensor family, plays a key role in the hepatic detoxification of xenobiotic and endobiotic chemicals through the induction of the expression of drug-metabolizing ...
Francesca De Battistis +4 more
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Transporter Gene Regulation in Sandwich Cultured Human Hepatocytes Through the Activation of Constitutive Androstane Receptor (CAR) or Aryl Hydrocarbon Receptor (AhR) [PDF]
Frontiers in Pharmacology, 2021 The induction potentials of ligand-activated nuclear receptors on metabolizing enzyme genes are routinely tested for new chemical entities. However, regulations of drug transporter genes by the nuclear receptor ligands are underappreciated, especially in
Congrong Niu, Bill Smith, Yurong Lai
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Constitutive Androstane Receptor-Mediated Inhibition of Metformin on Phase II Metabolic Enzyme SULT2A1 [PDF]
International Journal of Endocrinology, 2021 Background. Metformin, as a first-line treatment for diabetes, interacts with many protein kinases and transcription factors which affect the expression of downstream target genes governing drug metabolism.
Xiaowen Hu +3 more
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Constitutive Androstane Receptor: A Peripheral and a Neurovascular Stress or Environmental Sensor [PDF]
Cells, 2020 Xenobiotic nuclear receptors (NR) are intracellular players involved in an increasing number of physiological processes. Examined and characterized in peripheral organs where they govern metabolic, transport and detoxification mechanisms, accumulating ...
Fabiana Oliviero +6 more
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Constitutive androstane receptor induced-hepatomegaly and liver regeneration is partially via yes-associated protein activation [PDF]
Acta Pharmaceutica Sinica B, 2021 The constitutive androstane receptor (CAR, NR3I1) belongs to nuclear receptor superfamily. It was reported that CAR agonist TCPOBOP induces hepatomegaly but the underlying mechanism remains largely unknown.
Yue Gao +11 more
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Gadd45b is required in part for the anti-obesity effect of constitutive androstane receptor (CAR) [PDF]
Acta Pharmaceutica Sinica B, 2021 Crosstalk between xenobiotic metabolism and energy metabolism in the liver has provided a potential opportunity to target xenobiotic receptors to treat metabolic diseases. Activation of constitutive androstane receptor (CAR), a xenobiotic-sensing nuclear
Xinran Cai +4 more
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Discovery of Novel Human Constitutive Androstane Receptor Agonists with the Imidazo[1,2-a]pyridine Structure. [PDF]
J Med Chem, 2023 The nuclear constitutive androstane receptor (CAR, NR1I3) plays significant roles in many hepatic functions, such as fatty acid oxidation, biotransformation, liver regeneration, as well as clearance of steroid hormones, cholesterol, and bilirubin.
Mejdrová I +14 more
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Deletion of Constitutive Androstane Receptor Led to Intestinal Alterations and Increased Imidacloprid in Murine Liver. [PDF]
J Endocr Soc, 2022 Imidacloprid (IMI) is the most frequently detected neonicotinoid pesticide in the environment. Despite typically low toxicity in vertebrates, IMI exposure is associated with liver and gastrointestinal toxicity.
Sen A, Goforth M, Cooper KK, Anakk S.
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