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.
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Penning et al., 2000, Biochem J (24).
Jin and Penning, 2006, Biochemistry (54).
Trauger et al., 2002, Biochemistry (55).
Jin et al., 2011, Biochem J (34).
Sharma et al., 2006, Mol Cell Endocrinol (36).
Byrns et al., 2010, J Steroid Biochem Mol Biol (26).
Chen et al., 2011, Steroids (37).