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. Author manuscript; available in PMC: 2019 Aug 1.
Published in final edited form as: Drug Metab Rev. 2018 Aug;50(3):256–342. doi: 10.1080/03602532.2018.1483401

Table 4.

P450 7B1

Properties References
Physiological substrates: 25- and 27-Hydroxycholesterol, pregnenolone, dehydroepiandrosterone (DHEA), epiandrosterone, 5α-androstane-3β,17β-diol, estrone (Rose et al. 1997; Steckelbroeck et al. 2002; Kim SB et al. 2004; Stiles et al. 2009; Yantsevich et al. 2014; Pan et al. 2016)

Function: 25-Hydroxycholesterol 7α-hydroxylase, oxysterol and steroid 6α- or 7α-hydroxylase (Fig. 6); involved in metabolism of neurosteroids (brain), bile acid synthesis (liver), and metabolism of estrogen receptor ligands (in prostate)

Inhibition: Possible liver failure and progressive neuropathy

Inhibitors:

Drugs:

Imidazole and triazole drugs (ketoconazole, bifoconazole, miconazole, clotrimazole, econazole, fluconazole, tioconazole, voriconazole) a (Kim SB et al. 2004; Yantsevich et al. 2014)
Metyrapone a (Yantsevich et al. 2014)

Physiological compounds:

5α-Androstane-3β,17β-diol, estrone, testosterone, 17β-estradiol b (Kim SB et al. 2004; Tang et al. 2006; Pettersson et al. 2008)
5α-Dihydrotestosterone b (at high concentrations) (Pettersson et al. 2008)
Estrogens (estrone, 17β-estradiol–in the absence of estrogen receptor α) b (Tang et al. 2006)
Triiodothyronine c (T3) (Ellis 2006)
β-Amyloid peptide (non-competitive inhibition) (Kim SB et al. 2004)

Physiological condition and illnesses:

Breast cancer d (Wu et al. 2013)
Prostatic cancer d (in type 2 diabetes) (Lutz et al. 2018)

Other compounds:

Pesticides a (tebuconazole, propiconazole) (Yantsevich et al. 2014)


Induction: Immunostimulatory effect of 7α-hydroxydehydroepiandosterone (used in rheumatoid artritis)

Inducers:

Drugs:

Rifampicin (Kim B et al. 2013)

Physiological compounds:

17β-Estradiol e (in human embryonic kidney (HEK293) cells transfected with estrogen receptor α) (Dulos, van der Vleuten, et al. 2005; Tang et al. 2006)
Interleukin-1 β interleukin-1α, interleukin-7, interleukin-17, activator protein-1, nuclear factor–κΒ, tumor necrosis factor-α e (Dulos, Kaptein, et al. 2005; Dulos, van der Vleuten, et al. 2005; Dulos and Boots 2006)

Physiological condition and illnesses:

Prostatic cancer f (Olsson et al. 2007)
Psoriasis f (Sumantran et al. 2016)

Other compounds:

Oleic acid anilide e (An et al. 2008)

Footnotes:

a

Competitive inhibition, ligand binding

b

Decreased/suppressed/inhibited activity/product formation

c

Reduced/suppressed mRNA and/or protein level/expression and activity

d

Gene downregulated/suppressed

e

Increased transcription/mRNA/protein expression/levels /and/or catalytic activity

f

Up-regulation of biosynthesis, increased expression of protein