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Literature summary extracted from

  • Yepuru, M.; Wu, Z.; Kulkarni, A.; Yin, F.; Barrett, C.M.; Kim, J.; Steiner, M.S.; Miller, D.D.; Dalton, J.T.; Narayanan, R.
    Steroidogenic enzyme AKR1C3 is a novel androgen receptor-selective coactivator that promotes prostate cancer growth (2013), Clin. Cancer Res., 19, 5613-5625.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
1.1.1.51 R1881 requires amino acids 1-282 of AKR1C3 to elicit its coactivation, inhibitor GTx-560 requires the full-length AKR1C3 to bind and inhibit R1881-induced activity Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.51 AKR1C3, quantitative enzyme expression analysis by real-time PCR, recombinant expression in HEK-293 cells Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
1.1.1.51 additional information AKR1C3 siRNA reduces androgen receptor signaling in VCaP cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.51 GTx-560 competitively and selectively inhibits AKR1C3-dependent androgen receptor transactivation. GTx-560 completely blocks the formation of testosterone from androstenedione, indicating the ability of AKR1C3 inhibitors, unlike 5alpha-reductase inhibitors, to reduce testosterone levels Homo sapiens
1.1.1.51 additional information small-molecule inhibitors inhibit both the enzymatic and coactivator functions of AKR1C3 resulting in androgen-dependent prostate cancer and CRPC regression. No inhibition by indomethacin Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.51 additional information Homo sapiens AKR1C3 physically interacts with the androgen receptor ?
-
 ?
1.1.1.51 testosterone + NAD(P)+ Homo sapiens
-
 androstenedione + NAD(P)H + H+
-
 r

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.51 Homo sapiens P42330
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.51 LNCaP cell
-
 Homo sapiens
-
1.1.1.51 prostate cancer cell
-
 Homo sapiens
-
1.1.1.51 VCaP cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.51 additional information AKR1C3 physically interacts with the androgen receptor Homo sapiens ?
-
 ?
1.1.1.51 testosterone + NAD(P)+
-
 Homo sapiens androstenedione + NAD(P)H + H+
-
 r

Synonyms

EC Number Synonyms Comment Organism
1.1.1.51 AKR1C3
-
 Homo sapiens
1.1.1.51 aldo keto reductase 1C3
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.51 NAD+
-
 Homo sapiens
1.1.1.51 NADH
-
 Homo sapiens
1.1.1.51 NADP+
-
 Homo sapiens
1.1.1.51 NADPH
-
 Homo sapiens

General Information

EC Number General Information Comment Organism
1.1.1.51 evolution the enzyme belongs to the AKR1C family Homo sapiens
1.1.1.51 malfunction AKR1C3 siRNA reduces androgen receptor signaling in VCaP cells. Small-molecule inhibitors inhibit both the enzymatic and coactivator functions of AKR1C3 resulting in androgen-dependent prostate cancer and CRPC regression Homo sapiens
1.1.1.51 physiological function castration-resistant prostate cancer may occur by several mechanisms including the upregulation of androgen receptor, coactivators, and steroidogenic enzymes, including aldo keto reductase 1C3 (AKR1C3). AKR1C3 converts weaker 17-keto androgenic precursors to more potent 17-hydroxy androgens and is consistently the major upregulated gene in castration-resistant prostate cancer, CRPC. AKR1C3 enhances androgen signaling and prostate cancer xenograft growth. AKR1C3 is a receptor- and tissue-selective pharmacologically targetable coactivator that promotes prostate cancer growth, AKR1C3-dependent R1881-induced androgen receptor transactivation in HEK-293 cells Homo sapiens