LIPID MAPS

all-trans Retinoic acid is a metabolite of vitamin A and a ligand for retinoic acid receptors (RARs) with IC50 values of 9, 3, and 10 nM for RARα, RARβ, and RARγ, respectively, in radioligand binding assays.¹ It induces expression of a luciferase reporter in COS-7 cells expressing RARα, RARβ, or RARγ (EC50s = 169, 9, and 2 nM, respectively). all-trans Retinoic acid (17 nmol) reduces papilloma formation induced by phorbol 12-myristate 13-acetate (TPA) in mice.² It reduces bile duct proliferation, hydroxyproline levels, and liver inflammation in a rat model of α-naphthylisothiocyanate-induced chronic cholestasis and reduces plasma levels of alkaline phosphatase and bile salts in the Mdr2-/- mouse model of cholestasis.³ all-trans Retinoic acid also reduces hepatic fat accumulation, triglycerides, body weight, and serum glucose levels in mice with Western diet-induced obesity.⁴

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References

1. Kim, S.C., Kim, C.K., Axe, D., et al. All-trans-retinoic acid ameliorates hepatic steatosis in mice by a novel transcriptional cascade. Hepatology 59(5), 1750-1760 (2014).

2. Cai, S.Y., Mennone, A., Soroka, C.J., et al. All-trans-retinoic acid improves cholestasis in α-naphthylisothiocyanate-treated rats and Mdr2-/- mice. J. Pharmacol. Exp. Ther. 349(1), 94-98 (2014).

3. Verma, A.K., Slaga, T.J., Wertz, P.W., et al. Inhibition of skin tumor promotion by retinoic acid and its metabolite 5,6-epoxyretinoic acid. Cancer Res. 40(7), 2367-2371 (1980).

4. Idrest, N., Marill, J., Flexor, M.A., et al. Activation of retinoic acid receptor-dependent transcription by all-trans-retinoic acid metabolites and isomers. J. Biol. Chem. 277(25), 31491-31498 (2002).