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. 2019 Oct 18;9(6):1113–1144. doi: 10.1016/j.apsb.2019.10.001

Table 2.

Endogenous and exogenous substrates of UGTs and ligands of transcription factors.

Family Enzyme Endogenous substrate Xenobiotic substrate Transcription factor
UGT1A UGT1A1 Bilirubin, estradiol, fatty acids SN-38, leonurine, bergenin, axitinib CAR, PXR, PPARα, AhR43, NRF2
UGT1A3 Bile acid, arachidonic Polyaromatic amines, non-steroidal anti-inflammatory drugs, statins, ahydroxygenkwanin, genkwanin, ursolic acid44, fimasartan45, alpinetin23 PPARα, HNF1, AhR, LXR, PXR
UGT1A4 Eicosanoids Imipramine, lamotrigine, clonazolam, deschloroetizolam, etizolam, flubromazolammetizolam HNF1, PPARα, PXR, CAR, AhR, HNF1α
UGT1A6 Serotonin 1-Naphthol 4-nitrophenol AhR, CAR, PXR, PPARα
UGT1A7 Unknown Icaritin, carcinogens AhR, HNF1, HNF4α, NRF2
UGT1A8 Fatty acids Retinoids, catechol estrogens, opioids, coumarins, flavonoids, anthraquinones, phenols, raloxifene HNF1, HNF4α, AhR, NRF2
UGT1A9 Steroids, fatty acids Bulky phenols, propofol, mycophenolic acid, niflumic acid, psoralidin CAR, HNF1, HNF4α, PPARα, AhR, NRF2
UGT1A10 Estrogens Nitrosamine, flavonoids, polycyclic aromatic hydrocarbons, raloxifene, dopamine HNF1α, HNF4α, AhR, NRF2
UGT2A UGT2A2/3 Hyodeoxycholic acid Tobacco carcinogen HNF1, LXR
UGT2B UGT2B4 Arachidonic acid Naftopidil, deoxynivalenol PPARα, AhR, FXR
UGT2B7 Sex-steroid hormones, glucocorticoids, mineralocorticoid, bile acids Naftopidil, deoxynivalenol, mirabegron, efavirenz, zidovudine, codeine, morphine HNF1α46, CAR, PXR, FXR, PPAR, NRF2
UGT2B10 Eicosanoids Amitriptyline, imipramine, clomipramine, trimipramine CAR, FXR, AR
UGT2B11 Unknown 3a-Hydroxyandrogens, 3a-pregnanes, Hydroxylestrogens ER, AR
UGT2B15 Sex-steroid hormones Oxazepam, lorazepam, sipoglitazar, bisphenol-A AR, ER, HNF3α, FXR
UGT2B17 Sex-steroid hormones Coumarins, anthraquinones flavonoids, chlorantraniliprole HNF1α, HNF4α, HNF3α, AR, ER
UGT2B28 Sex-steroid hormones Unknown ER, AR
UGT3 UGT3 Unknown N-Acetylglucosamine Unknown
UGT8 UGT8A1 Bile acids Unknown LXR