Inhibition of the all-trans Retinoic Acid (atRA) Hydroxylases CYP26A1 and CYP26B1 Results in Dynamic, Tissue-Specific Changes in Endogenous atRA Signaling

  title={Inhibition of the all-trans Retinoic Acid (atRA) Hydroxylases CYP26A1 and CYP26B1 Results in Dynamic, Tissue-Specific Changes in Endogenous atRA Signaling},
  author={F. Stevison and C. Hogarth and S. Tripathy and Travis M. Kent and N. Isoherranen},
  journal={Drug Metabolism and Disposition},
  pages={846 - 854}
  • F. Stevison, C. Hogarth, +2 authors N. Isoherranen
  • Published 2017
  • Biology, Medicine
  • Drug Metabolism and Disposition
  • All-trans retinoic acid (atRA), the active metabolite of vitamin A, is a ligand for several nuclear receptors and acts as a critical regulator of many physiologic processes. The cytochrome P450 family 26 (CYP26) enzymes are responsible for atRA clearance, and are potential drug targets to increase concentrations of endogenous atRA in a tissue-specific manner. Talarozole is a potent inhibitor of CYP26A1 and CYP26B1, and has shown some success in clinical trials. However, it is not known what… CONTINUE READING
    13 Citations
    The retinoic acid hydroxylase Cyp26a1 has minor effects on postnatal vitamin A homeostasis, but is required for exogenous atRA clearance
    • 7
    • PDF
    Biochemical and physiological importance of the CYP26 retinoic acid hydroxylases.
    • 18
    Knockout of Cyp26a1 and Cyp26b1 during postnatal life causes reduced lifespan, dermatitis, splenomegaly, and systemic inflammation in mice
    • J. Snyder, Guo Zhong, +8 authors N. Isoherranen
    • Biology, Medicine
    • FASEB journal : official publication of the Federation of American Societies for Experimental Biology
    • 2020
    Characterization of Vitamin A Metabolome in Human Livers With and Without Nonalcoholic Fatty Liver Disease
    • 10
    • PDF
    Glycyrrhetinic acid attenuates disturbed vitamin a metabolism in non-alcoholic fatty liver disease through AKR1B10.
    Histamine receptor 1 is expressed in leukaemic cells and affects differentiation sensitivity


    The relative importance of CYP26A1 in hepatic clearance of all-trans retinoic acid.
    • 62
    A Comparison of the Roles of Peroxisome Proliferator-Activated Receptor and Retinoic Acid Receptor on CYP26 Regulation
    • 48
    • PDF
    Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, the Human Liver Retinoic Acid Hydroxylase.
    • 10
    The role of CYP26 enzymes in retinoic acid clearance
    • 148
    Therapeutic potential of the inhibition of the retinoic acid hydroxylases CYP26A1 and CYP26B1 by xenobiotics.
    • 45
    Comparison of the function and expression of CYP26A1 and CYP26B1, the two retinoic acid hydroxylases.
    • 88
    Expression and functional characterization of cytochrome P450 26A1, a retinoic acid hydroxylase.
    • 80