DL5050, a Selective Agonist for the Human Constitutive Androstane Receptor [PDF]
ACS Medicinal Chemistry Letters, 2019 The constitutive androstane receptor (CAR) is a xenobiotic sensor governing the transcription of genes involved in drug disposition, energy homeostasis, and cell proliferation. However, currently available human CAR (hCAR) agonists are nonselective, which commonly activate hCAR along with other nuclear receptors, especially the closely related human ...
Dongdong Liang +6 more
europepmc +5 more sources
Searching for Constitutive Androstane Receptor Modulators [PDF]
Drug Metabolism and Disposition, 2022 The constitutive androstane receptor (CAR; NR1I3) has been established as one of the main drug- and xenobiotic-responsive transcriptional regulators, collectively called xenosensors. CAR activates the expression of several oxidative, hydrolytic, and conjugative drug-metabolizing enzymes and drug transporters, and therefore, it contributes to drug and ...
P. Honkakoski
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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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Dimorphic metabolic and endocrine disorders in mice lacking the constitutive androstane receptor [PDF]
Scientific Reports, 2019 AbstractMetabolic diseases such as obesity, type II diabetes and hepatic steatosis are a public health concern in developed countries. The metabolic risk is gender‐dependent. The constitutive androstane receptor (CAR), which is at the crossroads between energy metabolism and endocrinology, has recently emerged as a promising therapeutic agent for the ...
Lukowicz, Céline +24 more
europepmc +8 more sources
Transcriptomic analysis across liver diseases reveals disease-modulating activation of constitutive androstane receptor in cholestasis [PDF]
JHEP Reports, 2020 Background & Aims: Liver diseases are caused by many factors, such as genetics, nutrition, and viruses. Therefore, it is important to delineate transcriptomic changes that occur in various liver diseases.
Bhoomika Mathur +10 more
doaj +3 more sources
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.
europepmc +2 more sources
Induction of bilirubin clearance by the constitutive androstane receptor (CAR) [PDF]
Proceedings of the National Academy of Sciences, 2003 Bilirubin clearance is one of the numerous important functions of the liver. Defects in this process result in jaundice, which is particularly common in neonates. Elevated bilirubin levels can be decreased by treatment with phenobarbital. Because the nuclear hormone receptor constitutive androstane receptor (CAR) mediates hepatic effects of this ...
W. HUANG +6 more
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Yes-Associated Protein Is Crucial for Constitutive Androstane Receptor-Driven Hepatocyte Proliferation But Not for Induction of Drug Metabolism Genes in Mice. [PDF]
Hepatology, 2021 Constitutive androstane receptor (CAR) agonists, such as 1,4‐bis [2‐(3,5‐dichloropyridyloxy)] benzene (TCPOBOP), are known to cause robust hepatocyte proliferation and hepatomegaly in mice along with induction of drug metabolism genes without any ...
Bhushan B +10 more
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Drug Metabolism and Pharmacokinetics, 2023 The mouse cytochrome P450 1A2 (Cyp1a2) gene is one of the constitutive androstane receptor (CAR, NR1I3) activator-inducible genes, and the regions involved in induction were examined herein. A reporter gene assay indicated the involvement of the -0.2-kb region in the induction of transcriptional activation by the mouse CAR agonist ligand 1,4-bis-[2-(3 ...
Yuki, Kawasaki +2 more
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Metamizole is a Moderate Cytochrome P450 Inducer Via the Constitutive Androstane Receptor and a Weak Inhibitor of CYP1A2. [PDF]
Clin Pharmacol Ther, 2021 Metamizole is an analgesic and antipyretic drug used intensively in certain countries. Previous studies have shown that metamizole induces cytochrome (CYP) 2B6 and possibly CYP3A4.
Bachmann F +6 more
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