Proteins > Aldo-keto reductase family 1 member C2
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Aldo-keto reductase family 1 member C2
An aldo-keto reductase family 1 member C2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P52895]
Synonyms
EC 1.-.-.-;
EC 1.1.1.112;
EC 1.1.1.209;
EC 1.1.1.53;
EC 1.1.1.62;
EC 1.3.1.20;
3-alpha-HSD3;
Chlordecone reductase homolog HAKRD;
Dihydrodiol dehydrogenase 2;
DD-2;
DD2;
Dihydrodiol dehydrogenase/bile acid-bind
Research
Bioassay Publications (20)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (10.00) | 29.6817 |
| 2010's | 17 (85.00) | 24.3611 |
| 2020's | 1 (5.00) | 2.80 |
Compounds (21)
Drugs with Inhibition Measurements
Drugs with Other Measurements
Potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the benzoisoxazole moiety: application of a bioisosteric scaffold hopping approach to flufenamic acid.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.European journal of medicinal chemistry, , Volume: 62, 2013
Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17β-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Discovery of substituted 3-(phenylamino)benzoic acids as potent and selective inhibitors of type 5 17β-hydroxysteroid dehydrogenase (AKR1C3).Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
Overview of AKR1C3: Inhibitor Achievements and Disease Insights.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3.ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer.Journal of medicinal chemistry, , Mar-28, Volume: 56, Issue:6, 2013
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Selective inhibition of human type-5 17β-hydroxysteroid dehydrogenase (AKR1C3) by baccharin, a component of Brazilian propolis.Journal of natural products, , Apr-27, Volume: 75, Issue:4, 2012
Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17β-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Discovery of substituted 3-(phenylamino)benzoic acids as potent and selective inhibitors of type 5 17β-hydroxysteroid dehydrogenase (AKR1C3).Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
Structure-based optimization and biological evaluation of human 20α-hydroxysteroid dehydrogenase (AKR1C1) salicylic acid-based inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
Selectivity determinants of inhibitor binding to human 20alpha-hydroxysteroid dehydrogenase: crystal structure of the enzyme in ternary complex with coenzyme and the potent inhibitor 3,5-dichlorosalicylic acid.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Discovery of (R)-2-(6-Methoxynaphthalen-2-yl)butanoic Acid as a Potent and Selective Aldo-keto Reductase 1C3 Inhibitor.Journal of medicinal chemistry, , 08-25, Volume: 59, Issue:16, 2016
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Overview of AKR1C3: Inhibitor Achievements and Disease Insights.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Selective inhibition of human type-5 17β-hydroxysteroid dehydrogenase (AKR1C3) by baccharin, a component of Brazilian propolis.Journal of natural products, , Apr-27, Volume: 75, Issue:4, 2012
Potent and Highly Selective Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors Act as Chemotherapeutic Potentiators in Acute Myeloid Leukemia and T-Cell Acute Lymphoblastic Leukemia.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Selective AKR1C3 Inhibitors Potentiate Chemotherapeutic Activity in Multiple Acute Myeloid Leukemia (AML) Cell Lines.ACS medicinal chemistry letters, , Aug-11, Volume: 7, Issue:8, 2016
Selective inhibition of human type-5 17β-hydroxysteroid dehydrogenase (AKR1C3) by baccharin, a component of Brazilian propolis.Journal of natural products, , Apr-27, Volume: 75, Issue:4, 2012
Enables
This protein enables 11 target(s):
| Target | Category | Definition |
|---|
| aldose reductase (NADPH) activity | molecular function | Catalysis of the reaction: an alditol + NADP+ = an aldose + NADPH + H+. [EC:1.1.1.21] |
| estradiol 17-beta-dehydrogenase [NAD(P)] activity | molecular function | Catalysis of the reaction: estradiol-17-beta + NAD(P)+ = estrone + NAD(P)H + H+. The activity can use NAD+ or NADP+ as the acceptor. [EC:1.1.1.62] |
| oxidoreductase activity, acting on NAD(P)H, quinone or similar compound as acceptor | molecular function | Catalysis of an oxidation-reduction (redox) reaction in which NADH or NADPH acts as a hydrogen or electron donor and reduces a quinone or a similar acceptor molecule. [GOC:ai] |
| phenanthrene 9,10-monooxygenase activity | molecular function | Catalysis of the reaction: phenanthrene + O2 + NADH + H+ = H2O + NAD+ + phenanthrene-9,10-oxide. [UM-BBD_reactionID:r0495] |
| carboxylic acid binding | molecular function | Binding to a carboxylic acid, an organic acid containing one or more carboxyl (COOH) groups or anions (COO-). [GOC:mah, ISBN:0198506732] |
| bile acid binding | molecular function | Binding to a bile acid, a steroid carboxylic acids occurring in bile. [GOC:rph] |
| androstan-3-alpha,17-beta-diol dehydrogenase activity | molecular function | Catalysis of the reaction: NAD+ + androstan-3-alpha,17-beta-diol = 17-beta-hydroxyandrostan-3-one + NADH + H+. [EC:1.1.1.53, MetaCyc:1.1.1.53-RXN] |
| ketosteroid monooxygenase activity | molecular function | Catalysis of the reaction: O2 + NADPH + progesterone = H2O + NADP+ + testosterone acetate. [EC:1.14.13.54, MetaCyc:1.14.13.54-RXN] |
| trans-1,2-dihydrobenzene-1,2-diol dehydrogenase activity | molecular function | Catalysis of the reaction: NADP+ + trans-1,2-dihydrobenzene-1,2-diol = NADPH + catechol. [EC:1.3.1.20, MetaCyc:1.3.1.20-RXN] |
| indanol dehydrogenase activity | molecular function | Catalysis of the reaction: indan-1-ol + NAD(P)+ = indanone + NAD(P)H + H+. [EC:1.1.1.112, MetaCyc:INDANOL-DEHYDROGENASE-RXN] |
| androsterone dehydrogenase activity | molecular function | Catalysis of the reaction: NAD(P)+ + androsterone = NAD(P)H + H+ + 5-alpha-androstane-3,17-dione. [EC:1.1.1.209, MetaCyc:1.1.1.209-RXN] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Involved In
This protein is involved in 12 target(s):
| Target | Category | Definition |
|---|
| prostaglandin metabolic process | biological process | The chemical reactions and pathways involving prostaglandins, any of a group of biologically active metabolites which contain a cyclopentane ring due to the formation of a bond between two carbons of a fatty acid. They have a wide range of biological activities. [ISBN:0198506732] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| digestion | biological process | The whole of the physical, chemical, and biochemical processes carried out by multicellular organisms to break down ingested nutrients into components that may be easily absorbed and directed into metabolism. [GOC:isa_complete, ISBN:0198506732] |
| steroid metabolic process | biological process | The chemical reactions and pathways involving steroids, compounds with a 1,2,cyclopentanoperhydrophenanthrene nucleus. [ISBN:0198547684] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| epithelial cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of an epithelial cell, any of the cells making up an epithelium. [GOC:ecd, PMID:11839751] |
| progesterone metabolic process | biological process | The chemical reactions and pathways involving progesterone, a steroid hormone produced in the ovary which prepares and maintains the uterus for pregnancy. Also found in plants. [GOC:jl, http://www.cogsci.princeton.edu/] |
| daunorubicin metabolic process | biological process | The chemical reactions and pathways involving daunorubicin, a chemotherapeutic of the anthracycline family that is given as a treatment for some types of cancer. [PMID:20837989] |
| doxorubicin metabolic process | biological process | The chemical reactions and pathways involving doxorubicin, an anthracycline antibiotic, used in cancer chemotherapy. [PMID:10200167] |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| cellular response to jasmonic acid stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a jasmonic acid stimulus. [GOC:mah] |
| cellular response to prostaglandin D stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a prostagladin D stimulus. [GOC:sl] |