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. 2018 Aug 20;40(2):447–475. doi: 10.1210/er.2018-00089

Table 3.

Steady-State Kinetic Parameters for Human AKRs

Substrate
Product
Cofactor
Reduction
K m (μM)
k cat (min−1)
k cat/Km (min−1 mM−1)
AKR1C1
 ProgesteroneR 20α-HydroxyP NADPH 20-Ketosteroid 5.7 0.93 210a
 Androsterone 5α-Androstane-3α,17β-diol NADPH 17-Ketosteroid 21 0.18 9b
 5α-DHTR 5α-Androstane-3α,17β-diol NADPH 3-Ketosteroid 81 0.66 8b
AKR1C2
 5α-DHTR 5α-Androstane-3α,17β-diol NADPH 3-Ketosteroid 4.6 3.8 820a
 5α-DHTS 5α-Androstane-3α,17β-diol NADPH 3-Ketosteroid 2.9 1.8 620c
 5α-DHP 3α-Hydroxy-5α-pregnane-20-one NADPH 3-Ketosteroid 1.8 0.18 100d
 5β-DHP 3α-Hydroxy-5β-pregnane-20-one NADPH 3-Ketosteroid 0.6 0.5 1200e
 4-Androstene-3,17-dioneR Testosterone NADPH 17-Ketosteroid ND ND ND
AKR1C3
 5α-DHTR 5α-Androstane-3α,17β-diol NADPH 3-Ketosteroid 19.8 0.26 6a
 5α-Androstane-3,17-dioneS Androsterone; NADPH 3-Ketosteroid 5.0 7.63 56a
5α-DHT 17-Ketosteroid
 4-Androstene-3,17-dioneR Testosterone NADPH 17-Ketosteroid 13.4 0.87 65f
 AndrosteroneS 5α-Androstane-3α,17β-diol NADPH 17-Ketosteroid 8.9 10.2 42a
 EstroneR 17β-Estradiol NADPH 17-Ketosteroid 9.0 0.068 7.5g
 Progesterone 20α-HydroxyP NADPH 20-Ketosteroid 2.8 1.0 370f
AKR1C4
 5α-DHTR 5α-Androstane-3α,17β-diol NADPH 3-Ketosteroid 8.3 1.92 231a
 5β-DHT 5β-Androstane-3α,17β-diol NADPH 3-Ketosteroid 0.2 4.7 23,500e
 5β-DHP 3α-Hydroxy-5β-pregnane-20-one; NADPH 3-Ketosteroid 0.3 4.9 16,300e
5β-Pregnane-3α,20α-diol 20-Ketosteroid
 20α-Hydroxy-5β-pregnane-3-one 5β-Pregnane-3α,20α-diol NADPH 3-Ketosteroid 0.3 4.3 14,300e
 3α-Hydroxy-5β-pregnane-20-one 5β-Pregnane-3α,20α-diol NADPH 20-Ketosteroid 0.4 1.5 3800e
AKR1D1
 Testosterone 5β-Dihydrotestosterone NADPH 5β-Reduction 2.7 8.4 3120h
 Cortisol 5β-Dihydrocortisol NADPH 5β-Reduction 13.1 2.7 210h
 Cortisone 5β-Dihydrocortisone NADPH 5β-Reduction 15.1 11.7 780h
 4-Cholesten-7α-ol-3-one 7α-Hydroxy-5β-dihydrocholestan-3-one NADPH 5β-Reduction 0.8 2.0 2530h
 Cholestenone 5β−dihydrochlestenone NADPH 5β-Reduction 0.3 0.60 1980d

Abbreviation: ND, not determined.

a

Byrns et al., 2008, Biochem Pharmacol (56).

b

Penning et al., 2000, Biochem J (24).

c

Jin and Penning, 2006, Biochemistry (54).

d

Trauger et al., 2002, Biochemistry (55).

e

Jin et al., 2011, Biochem J (34).

f

Sharma et al., 2006, Mol Cell Endocrinol (36).

g

Byrns et al., 2010, J Steroid Biochem Mol Biol (26).

h

Chen et al., 2011, Steroids (37).