Enzymatic properties of a member (AKR1C20) of the aldo-keto reductase family

Biol Pharm Bull. 2006 Mar;29(3):539-42. doi: 10.1248/bpb.29.539.

Abstract

AKR1C20, a member of the aldo-keto reductase (AKR) superfamily, found by mouse genomic analysis, exhibits the highest sequence identity (89%) with mouse liver 17beta-hydroxysteroid dehydrogenase (HSD) type 5, but its function remains unknown. In this report, we have expressed the recombinant AKR1C20 from its cDNA, and examined its properties. The purified enzyme was a 36-kDa monomer, and showed both 17beta-HSD and 3alpha-HSD activities in the presence of NADP(H) as the coenzymes. While the Km values for testosterone and 5alpha-dihydrotestosterone were high (>0.2 mM), those for 3alpha-hydroxy- and 3-keto-steroids were low (0.3-5 microM), resulting in high catalytic efficiency for the substrates. Although no significant dehydrogenase activity towards non-steroidal alcohols was observed, the enzyme highly reduced alpha-dicarbonyl compounds such as 16-ketoestrone, 9,10-phenanthrenequinone, acenaphthenequinone, 1-phenylisatin and camphorquinone. The pH optima of the dehydrogenase and reductase activities were 10.5 and 6.5-7.5, respectively. The enzyme was inhibited by sulfobromophthalein, hexestrol, indomethacin and flufenamic acid. The properties of AKR1C20 are distinct from those of previously known mouse 17beta-HSD type 5 (AKR1C6), 3alpha-HSD (AKR1C14) and other members of the AKR1C subfamily. Thus, AKR1C20 is a novel 3alpha(17beta)-HSD, which may also function as a reductase for xenobiotic alpha-dicarbonyl compounds.

MeSH terms

  • 17-Hydroxysteroid Dehydrogenases / genetics
  • 17-Hydroxysteroid Dehydrogenases / isolation & purification
  • 17-Hydroxysteroid Dehydrogenases / metabolism
  • 3-alpha-Hydroxysteroid Dehydrogenase (B-Specific) / genetics
  • 3-alpha-Hydroxysteroid Dehydrogenase (B-Specific) / metabolism
  • Alcohol Oxidoreductases / genetics*
  • Alcohol Oxidoreductases / metabolism*
  • Aldehyde Reductase
  • Aldo-Keto Reductases
  • Animals
  • DNA, Complementary / biosynthesis
  • DNA, Complementary / genetics
  • Electrophoresis, Polyacrylamide Gel
  • Hydroxysteroids / metabolism
  • Ketosteroids / metabolism
  • Kinetics
  • Liver / enzymology
  • Mice
  • RNA, Messenger / biosynthesis
  • RNA, Messenger / genetics
  • Recombinant Proteins / genetics
  • Recombinant Proteins / isolation & purification
  • Recombinant Proteins / metabolism
  • Substrate Specificity

Substances

  • DNA, Complementary
  • Hydroxysteroids
  • Ketosteroids
  • RNA, Messenger
  • Recombinant Proteins
  • 17-Hydroxysteroid Dehydrogenases
  • Alcohol Oxidoreductases
  • Aldo-Keto Reductases
  • Aldehyde Reductase
  • 3-alpha-Hydroxysteroid Dehydrogenase (B-Specific)
  • AKR7A5 protein, mouse