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Table 1 Activation of human and zebrafish PXRs by androstane and estrane steroids

From: Evolution of pharmacologic specificity in the pregnane X receptor

Cmp. # Compound hPXR Activity hPXR Efficacy zfPXR Activity zfPXR Efficacy Toxicity
  ANDROSTANES      
AN1 5α-Androstan-3α,17β-diol 5.38 0.68 5.19 0.84 None
AN2 5α-Androstan-3,17-dione (androstanedione) 4.90 0.87 5.50 0.86 None
AN3 5α-Androstan-3α-ol (androstanol) 5.20 0.5 5.34 1.00 None
AN4 5α-Androstan-3α-ol-17-one (androsterone) 4.73 0.93 5.60 0.87 None
AN5 5α-Androstan-17β-ol-3-one (dihydrotestosterone) 4.94 0.39 5.21 0.59 None
AN6 5β-Androstan-3α-ol-17-one (etiocholanolone) 5.24 0.54 5.47 0.88 200
AN7 4-Androsten-3,17-dione (androstenedione) 4.69 0.59 5.44 0.14 None
AN8 4-Androsten-17β-ol-3-one (testosterone) 4.14 0.22 5.61 0.12 None
AN9 5-Androsten-3β-ol-17-one (DHEA) 4.49 0.52 4.89 0.35 None
AN10 5α-Androst-16-en-3α-ol (androstenol) 5.26 0.7 5.44 1.02 None
AN11 5β-Androstan-3α,11β-diol-17-one 4.72 0.51 4.52 1.04 None
AN12 5-Androsten-3β-sulfate-17-one (DHEA sulfate) 4.32 0.22 None   None
AN13 5β-Androstan-3α-ol-17-one (epiandrosterone) 5.31 0.7 5.02 0.43 None
AN14 5β-Androstan-3α-ol-11,17-dione 4.39 0.15 5.01 0.49 None
AN15 4-Androsten-17α-ol-3-one (epitestosterone) 4.17 0.9 None   None
AN16 4-Androsten-17α-glucosiduronate-3-one (epitestosterone glucuronide) 4.86 0.69 None   None
AN17 4-Androsten-17α-sulfate-3-one (epitestosterone sulfate) 5.47 0.67 None   None
AN18 5β-Androstan-3α-glucosiduronate-17-one (etiocholanolone glucuronide) None   None   None
AN19 5α-Androstane None   None   100
AN20 5α-Androstan-3β-ol 6.10 0.43 5.57 1.66 50
AN21 5α-Androst-16-en-3β-ol 5.32 1.01 5.48 2.11 50
AN22 5α-Androst-16-en-3-one 5.52 0.96 5.58 0.68 100
AN23 5β-Androstan-3α-ol 5.85 1.12 5.59 0.33 None
AN24 Androst-4,16-dien-3-one 5.15 0.64 5.96 0.17 100
AN25 Androst-5,16-dien-3β-ol None   5.60 1.50 100
  ESTRANES      
ES1 1,3,5(10)-Estratrien-3,17β-diol (estradiol) 4.80 0.34 None   200
ES2 1,3,5(10)-Estratrien-3-ol-17-one (estrone) 4.42 0.47 None   200
ES3 1,3,5(10)-Estratrien-3,16α,17β-triol (estriol) None   None   200
ES4 1,3,5(10)-Estratrien-3,16α-diol-17-one (16α-hydroxyestrone) 5.60 0.42 5.70 0.17 None
ES5 1,3,5(10)-Estratrien-3-ol-4-methoxy-17-one (4-methoxyestrone) 5.40 0.93 5.62 0.19 None
ES6 1,3,5(10)-Estratrien-3,15α,16α,17β-tetrol (estetrol) 5.67 0.29 None   200
ES7 1,3,5(10)-Estratrien-2,3-diol-17-one (2-hydroxyestrone) 5.44 0.93 5.74 0.19 None
ES8 1,3,5(10)-Estratrien-17-one-3-sulfate (estrone sulfate) 5.47 0.43 None   None
ES9 1,3,5(10)-Estratrien-17β-ol-3-glucosiduronate (estradiol glucuronide) None   None   None
ES10 1,3,5(10)-Estratrien-17β-ol-3-sulfate (estradiol sulfate) 6.05 0.6 None   200
ES11 1,3,5(10)-Estratrien-17α-ethinyl-3,17β-diol (ethinyl estradiol) 5.72 0.68 None   200
  1. Activities are in -log(EC50), with EC50 in molar units for the activation of human or zebrafish PXR. Efficacy is relative to 10 μM rifampicin (human PXR) or 20 μM 5α-androstan-3α-ol (zebrafish PXR) which are assigned an efficacy of 1.0. Toxicity is the lowest concentration in micromolar that produced significant toxicity in the HepG2 cells.