MicroRNAs as regulators, biomarkers and therapeutic targets in liver diseases
- Xiaolin Wang, Yong He, B. Mackowiak, B. Gao
- Biology, MedicineGut
- 30 October 2020
The roles of miRNAs in intercellular communication between hepatocytes and other types of cells via extracellular vesicles in the pathogenesis of liver diseases and the challenges in miRNA-based therapy for liver diseases are discussed.
Genome-wide analysis of human constitutive androstane receptor (CAR) transcriptome in wild-type and CAR-knockout HepaRG cells.
- Daochuan Li, B. Mackowiak, Hongbing Wang
- BiologyBiochemical Pharmacology
- 1 November 2015
Mechanisms of xenobiotic receptor activation: Direct vs. indirect.
- B. Mackowiak, Hongbing Wang
- BiologyBiochimica et Biophysica Acta
- 1 September 2016
Mechanistic Insights of Phenobarbital-Mediated Activation of Human but Not Mouse Pregnane X Receptor
- Linhao Li, Matthew A. Welch, Hongbing Wang
- Biology, ChemistryMolecular Pharmacology
- 10 July 2019
It is shown that in a human CAR (hCAR)-knockout (KO) HepaRG cell line, PB significantly induces the expression of CYP2B6 and CYP3A4, two shared target genes of hCAR and human PXR (hPXR), and structure-activity analysis revealed that the amino acid tryptophan-299 within the ligand binding pocket of hP XR plays a key role in the agonistic binding of PB.
The Roles of Xenobiotic Receptors: Beyond Chemical Disposition
- B. Mackowiak, J. Hodge, S. Stern, Hongbing Wang
- BiologyDrug Metabolism And Disposition
- 1 September 2018
Recent advances in studying the noncanonical functions of xenobiotic receptors are highlighted with a particular focus placed on the roles of CAR and PXR in energy homeostasis and cancer development.
Identification of Modulators That Activate the Constitutive Androstane Receptor From the Tox21 10K Compound Library
- Caitlin Lynch, B. Mackowiak, M. Xia
- Biology, ChemistryToxicological Sciences
- 22 September 2018
Four compounds, neticonazole, diphenamid, phenothrin, and rimcazoles, have been identified as novel hCAR activators, one of which shows potential selectivity toward hCAR over its sister receptor, the pregnane X receptor (PXR).
E-Selectin-Dependent Inflammation and Lipolysis in Adipose Tissue Exacerbate Steatosis-to-NASH Progression via S100A8/9
- R. Rodrigues, Yong He, Bin Gao
- Medicine, BiologyCellular and Molecular Gastroenterology and…
- 1 August 2021
High-content Analysis of Constitutive Androstane Receptor (CAR) Translocation Identifies Mosapride Citrate as a CAR Agonist that Represses Gluconeogenesis.
- B. Mackowiak, Linhao Li, Hongbing Wang
- BiologyBiochemical Pharmacology
- 12 July 2019
Human constitutive androstane receptor agonist DL5016: A novel sensitizer for cyclophosphamide-based chemotherapies.
- Dongdong Liang, Linhao Li, F. Xue
- Biology, ChemistryEuropean journal of medicinal chemistry
- 1 October 2019
Molecular Basis of Metabolism-Mediated Conversion of PK11195 from an Antagonist to an Agonist of the Constitutive Androstane Receptor
- B. Mackowiak, Linhao Li, Hongbing Wang
- Biology, ChemistryMolecular Pharmacology
- 1 July 2017
Results indicate that removal of a methyl group switches PK11195 from a potent antagonist of hCAR to an agonist in HPH and highlights the importance of physiologically relevant metabolism when attempting to define the biologic action of small molecules.
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