AKR1C2

Summary

Gene Symbol: AKR1C2
Description: aldo-keto reductase family 1 member C2
Alias: AKR1C-pseudo, BABP, DD-2, DD/BABP, DD2, DDH2, HAKRD, HBAB, MCDR2, SRXY8, TDD, aldo-keto reductase family 1 member C2, 3-alpha-HSD3, chlordecone reductase homolog HAKRD, dihydrodiol dehydrogenase 2; bile acid binding protein; 3-alpha hydroxysteroid dehydrogenase, type III, pseudo-chlordecone reductase, testicular 17,20-desmolase deficiency, trans-1,2-dihydrobenzene-1,2-diol dehydrogenase, type II dihydrodiol dehydrogenase
Species: human
Products:     AKR1C2

Top Publications

  1. Arthur J, Reichardt J. Modeling single nucleotide polymorphisms in the human AKR1C1 and AKR1C2 genes: implications for functional and genotyping analyses. PLoS ONE. 2010;5:e15604 pubmed publisher
    Enzymes encoded by the AKR1C1 and AKR1C2 genes are responsible for the metabolism of progesterone and 5?-dihydrotestosterone (DHT), respectively...
  2. Hevir N, Vouk K, Sinkovec J, Ribic Pucelj M, Rizner T. Aldo-keto reductases AKR1C1, AKR1C2 and AKR1C3 may enhance progesterone metabolism in ovarian endometriosis. Chem Biol Interact. 2011;191:217-26 pubmed publisher
    ..significantly decreased mRNA levels of PR-AB, HSD17B2 and SRD5A2, significantly increased mRNA levels of AKR1C1, AKR1C2, AKR1C3 and SRD5A1, and negligible mRNA levels of AKR1D1...
  3. Stolz A, Hammond L, Lou H, Takikawa H, Ronk M, Shively J. cDNA cloning and expression of the human hepatic bile acid-binding protein. A member of the monomeric reductase gene family. J Biol Chem. 1993;268:10448-57 pubmed
    ..identified one isoform of dihydrodiol dehydrogenase activity that expresses high affinity bile acid binding (HBAB) with minimal 3 alpha-hydroxysteroid dehydrogenase (3 alpha-HSD) activity for bile acids...
  4. Jin Y, Stayrook S, Albert R, Palackal N, Penning T, Lewis M. Crystal structure of human type III 3alpha-hydroxysteroid dehydrogenase/bile acid binding protein complexed with NADP(+) and ursodeoxycholate. Biochemistry. 2001;40:10161-8 pubmed
    The crystal structure of human type III 3alpha-hydroxysteroid dehydrogenase (HSD)/bile acid binding protein (AKR1C2) complexed with NADP(+) and 3alpha,7beta-dihydroxy-5beta-cholanic acid (ursodeoxycholate) at 3.0 A resolution is presented...
  5. Nahoum V, Gangloff A, Legrand P, Zhu D, Cantin L, Zhorov B, et al. Structure of the human 3alpha-hydroxysteroid dehydrogenase type 3 in complex with testosterone and NADP at 1.25-A resolution. J Biol Chem. 2001;276:42091-8 pubmed
    The first crystallographic structure of human type 3 3alpha-hydroxysteroid dehydrogenase (3alpha-HSD3, AKR1C2), an enzyme playing a critical role in steroid hormone metabolism, has been determined in complex with testosterone and NADP at ..
  6. Takahashi R, Grigliatti T, Reid R, Riggs K. The effect of allelic variation in aldo-keto reductase 1C2 on the in vitro metabolism of dihydrotestosterone. J Pharmacol Exp Ther. 2009;329:1032-9 pubmed publisher
    ..b>AKR1C2 can regulate the extent and duration of activation of the androgen receptor by catalyzing the reduction of DHT to ..
  7. Woo S, Gao H, Henderson D, Zacharias W, Liu G, Tran Q, et al. AKR1C1 as a Biomarker for Differentiating the Biological Effects of Combustible from Non-Combustible Tobacco Products. Genes (Basel). 2017;8: pubmed publisher
    ..Notably, aldo-keto reductase genes, AKR1C1 and AKR1C2, were the core genes in the top enriched pathways and were statistically upregulated more than eight-fold by ..
  8. Andrýs R, Zemanová L, Lenčo J, Bílková Z, Wsól V. Carbonyl-reducing enzymes as targets of a drug-immobilised affinity carrier. Chem Biol Interact. 2015;234:169-77 pubmed publisher
    ..of the presented carrier was demonstrated with pure recombinant enzymes (AKR1A1, AKR1B1, AKR1B10, AKR1C1, AKR1C2, AKR1C3, AKR1C4, CBR1 and CBR3) as well as with two model biological samples (cell extract from genetically ..
  9. Tyagi C, Bathke J, Goyal S, Fischer M, Dahse H, Chacko S, et al. Targeting the intersubunit cavity of Plasmodium falciparum glutathione reductase by a novel natural inhibitor: computational and experimental evidence. Int J Biochem Cell Biol. 2015;61:72-80 pubmed publisher
    ..falciparum strain 3D7 with an IC50 of 3.2±1.9μM and the chloroquine-resistant Dd2 strain with an IC50 of 3.2+1.6μM...

More Information

Publications121 found, 100 shown here

  1. Karstoft K, Clark M, Jakobsen I, Müller I, Pedersen B, Solomon T, et al. The effects of 2 weeks of interval vs continuous walking training on glycaemic control and whole-body oxidative stress in individuals with type 2 diabetes: a controlled, randomised, crossover trial. Diabetologia. 2017;60:508-517 pubmed publisher
    ..CIM/CFAS is a member of the Danish Center for Strategic Research in Type 2 Diabetes (DD2; the Danish Council for Strategic Research, grant no. 09-067009 and 09-075724)...
  2. Cui J, Huang L, Zhao A, Lew J, Yu J, Sahoo S, et al. Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump. J Biol Chem. 2003;278:10214-20 pubmed
    ..7alpha-hydroxylase (Cyp 7a1), sterol 12alpha-hydroxylase (Cyp 8b1), and the intestinal bile acid-binding protein (I-BABP), remained unchanged...
  3. Chen W, Huang Z, Wang W, Mao F, Guan L, Tang Y, et al. Discovery of new antimalarial agents: Second-generation dual inhibitors against FP-2 and PfDHFR via fragments assembely. Bioorg Med Chem. 2017;25:6467-6478 pubmed publisher
    ..Additionally, 24 moderately inhibited the proliferation of chloroquine-resistant P. falciparum Dd2 strain...
  4. Montes R, Perez A, Medeiros C, Araújo M, Lima E, Scotti M, et al. Synthesis, Antifungal Evaluation and In Silico Study of N-(4-Halobenzyl)amides. Molecules. 2016;21: pubmed
    ..3.1.0 and Volsurf v. 1.0.7 softwares were realized, showing that descriptors DRDRDR, DRDRAC, L4LgS, IW4 and DD2 influence the antifungal activity of the haloamides...
  5. Meyers M, Anderson E, McNitt S, Krenning T, Singh M, Xu J, et al. Evaluation of spiropiperidine hydantoins as a novel class of antimalarial agents. Bioorg Med Chem. 2015;23:5144-50 pubmed publisher
    ..310 μM and 0.099 μM, respectively, and the former features equivalent potency on the chloroquine-resistant Dd2 strain...
  6. Harinantenaina Rakotondraibe L, Rasolomampianina R, Park H, Li J, Slebodnik C, Brodie P, et al. Antiproliferative and antiplasmodial compounds from selected Streptomyces species. Bioorg Med Chem Lett. 2015;25:5646-9 pubmed publisher
    ..1, 0.01 and 0.01 μM, respectively), while compounds 4 and 7 exhibited weak antiplasmodial activity against the Dd2 strain of Plasmodium falciparum, with IC50 values of 6.5 and 50 μM, respectively.
  7. Adams M, de Kock C, Smith P, Land K, Liu N, Hopper M, et al. Improved antiparasitic activity by incorporation of organosilane entities into half-sandwich ruthenium(II) and rhodium(III) thiosemicarbazone complexes. Dalton Trans. 2015;44:2456-68 pubmed publisher
    ..for their in vitro antiplasmodial activities against the chloroquine-sensitive (NF54) and chloroquine-resistant (Dd2) Plasmodium falciparum strains, displaying activities in the low micromolar range...
  8. Karstoft K, Clark M, Jakobsen I, Knudsen S, van Hall G, Pedersen B, et al. Glucose effectiveness, but not insulin sensitivity, is improved after short-term interval training in individuals with type 2 diabetes mellitus: a controlled, randomised, crossover trial. Diabetologia. 2017;60:2432-2442 pubmed publisher
    ..CIM/CFAS is a member of DD2-the Danish Center for Strategic Research in Type 2 Diabetes (the Danish Council for Strategic Research, grant no...
  9. Nieves K, Prudhomme J, Le Roch K, Franzblau S, Rodríguez A. Natural product-based synthesis of novel anti-infective isothiocyanate- and isoselenocyanate-functionalized amphilectane diterpenes. Bioorg Med Chem Lett. 2016;26:854-857 pubmed publisher
    ..0066 μM and 0.0025 μM, respectively, against two strains (Dd2 and 3D7) of the malaria parasite...
  10. Dutta P, Bordoloi M, Gogoi K, Roy S, Narzary B, Bhattacharyya D, et al. Antimalarial silver and gold nanoparticles: Green synthesis, characterization and in vitro study. Biomed Pharmacother. 2017;91:567-580 pubmed publisher
    ..methods and were compared for their antiplasmodial potential against chloroquine sensitive (3D7) and resistant (Dd2) strain of Plasmodium falciparum by using 24h schizont maturation assay...
  11. Clave E, Araujo I, Alanio C, Patin E, Bergstedt J, Urrutia A, et al. Human thymopoiesis is influenced by a common genetic variant within the TCRA-TCRD locus. Sci Transl Med. 2018;10: pubmed publisher
    ..study revealed a common variant (rs2204985) within the T cell receptor TCRA-TCRD locus, between the DD2 and DD3 gene segments, which associated with TREC amounts...
  12. Ekengard E, Glans L, Cassells I, Fogeron T, Govender P, Stringer T, et al. Antimalarial activity of ruthenium(II) and osmium(II) arene complexes with mono- and bidentate chloroquine analogue ligands. Dalton Trans. 2015;44:19314-29 pubmed publisher
    ..the new ligands and complexes was evaluated against chloroquine sensitive (NF54 and D10) and chloroquine resistant (Dd2) Plasmodium falciparum malaria parasite strains...
  13. Rasamison V, Brodie P, Merino E, Cassera M, Ratsimbason M, Rakotonandrasana S, et al. Furoquinoline Alkaloids and Methoxyflavones from the Stem Bark of Melicope madagascariensis (Baker) T.G. Hartley. Nat Prod Bioprospect. 2016;6:261-265 pubmed
    ..3) showed weak antimalarial activity (IC50 = 35 µM) against the chloroquine-resistant strain Dd2 of Plasmodium falciparum. Skimmianine (4) displayed moderate cytotoxicity with IC50 value of 1...
  14. Pathak V, Colah R, Ghosh K. Tyrosine kinase inhibitors: New class of antimalarials on the horizon?. Blood Cells Mol Dis. 2015;55:119-26 pubmed publisher
    ..help of modified WHO microtest technique in-vitro for five different Plasmodium falciparum laboratory strains (3D7, Dd2, 7G8, MRC2, PKL9). Imatinib and sorafenib showed a promising antimalarial activity with all the strains...
  15. Abosede O, Vyas N, Singh S, Kumbhar A, Kate A, Kumbhar A, et al. Copper(ii) mixed-ligand polypyridyl complexes with doxycycline - structures and biological evaluation. Dalton Trans. 2016;45:3003-12 pubmed publisher
    ..against the chloroquine-sensitive Plasmodium falciparum NF54 and chloroquine-resistant Plasmodium falciparum Dd2 strains reveal that complex 3 exhibited a higher activity than artesunate drug against the chloroquine-resistant ..
  16. Drinkwater N, Vinh N, Mistry S, Bamert R, Ruggeri C, Holleran J, et al. Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions. Eur J Med Chem. 2016;110:43-64 pubmed publisher
    ..the developed compounds potently inhibit Pf growth in culture, including the multi-drug resistant strain Dd2. The ongoing development of dual PfA-M1/PfA-M17 inhibitors continues to be an attractive strategy for the design of ..
  17. Carrasco M, Machado M, Gonçalves L, Sharma M, Gut J, Lukens A, et al. Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites. ChemMedChem. 2016;11:2194-2204 pubmed publisher
    ..Studies with genetically modified parasites, using a phenotypic assay based on the P. falciparum Dd2-ScDHODH line, which expresses yeast dihydroorotate dehydrogenase (DHODH), showed that one of the azaaurone ..
  18. Baldwin M, Yamodo I, Ranjan R, Li X, Mines G, Marinkovic M, et al. Human erythrocyte band 3 functions as a receptor for the sialic acid-independent invasion of Plasmodium falciparum. Role of the RhopH3-MSP1 complex. Biochim Biophys Acta. 2014;1843:2855-70 pubmed publisher
    ..In contrast, the IgY antibodies had only a marginal inhibitory effect on FCR3 and Dd2 strains (SAD invasion phenotype)...
  19. Gao G, Na W, Wang Y, Zhang H, Li H, Wang Q. Role of a liver fatty acid-binding protein gene in lipid metabolism in chicken hepatocytes. Genet Mol Res. 2015;14:4847-57 pubmed publisher
    ..36, 48, 60, and 72 h after transfection with the interference or overexpression plasmids for L-FABP, PPARα and L-BABP expression levels, and the total amount of cholesterol, were significantly affected by L-FABP expression...
  20. Joshi M, Okombo J, Nsumiwa S, Ndove J, Taylor D, Wiesner L, et al. 4-Aminoquinoline Antimalarials Containing a Benzylmethylpyridylmethylamine Group are Active against Drug Resistant Plasmodium falciparum and Exhibit Oral Activity in Mice. J Med Chem. 2017;: pubmed publisher
    ..improved solubility and decreased lipophilicity and were potent against chloroquine-sensitive (NF54) and resistant (Dd2 and 7G8) P. falciparum strains with 5/6 having IC50s <100 nM against the NF54 strain...
  21. Chakka S, Kalamuddin M, Sundararaman S, Wei L, Mundra S, Mahesh R, et al. Identification of novel class of falcipain-2 inhibitors as potential antimalarial agents. Bioorg Med Chem. 2015;23:2221-40 pubmed publisher
    ..1 ± 0.1 μM. Compounds 62 and 67 inhibited the growth of the drug resistant parasite Dd2 with better efficacy, and compound 74 exhibited a 7- to 12-fold higher potency against Dd2 and MCamp isolates, than ..
  22. Chirawurah J, Ansah F, Nyarko P, Duodu S, Aniweh Y, Awandare G. Antimalarial activity of Malaria Box Compounds against Plasmodium falciparum clinical isolates. Int J Parasitol Drugs Drug Resist. 2017;7:399-406 pubmed publisher
    ..Variations in the potency of the Malaria Box Compounds were observed between P. falciparum clinical isolates and Dd2 strain. We also investigated the sensitivity of the clinical isolates to chloroquine and artesunate...
  23. Hemben A, Ashley J, Tothill I. An immunosensor for parasite lactate dehydrogenase detection as a malaria biomarker - Comparison with commercial test kit. Talanta. 2018;187:321-329 pubmed publisher
    ..The developed sensor was able to detect pLDH in the Dd2luc culture medium supernatant at 0...
  24. Faísca Phillips A, Nogueira F, Murtinheira F, Barros M. Synthesis and antimalarial evaluation of prodrugs of novel fosmidomycin analogues. Bioorg Med Chem Lett. 2015;25:2112-6 pubmed publisher
    ..falciparum Dd2 strain. In addition, it showed very low cytotoxicity against cultured human cells.
  25. Buedenbender L, Robertson L, Lucantoni L, Avery V, Kurtböke D, Carroll A. HSQC-TOCSY Fingerprinting-Directed Discovery of Antiplasmodial Polyketides from the Marine Ascidian-Derived Streptomyces sp. (USC-16018). Mar Drugs. 2018;16: pubmed publisher
    ..activities were tested for the natural products against chloroquine sensitive (3D7) and chloroquine resistant (Dd2) Plasmodium falciparum strains; the two polyketides (1?2) demonstrated an inhibition of >75%..
  26. Edaye S, Tazoo D, Bohle D, Georges E. 3-Iodo-4-aminoquinoline derivative sensitises resistant strains of Plasmodium falciparum to chloroquine. Int J Antimicrob Agents. 2016;47:482-5 pubmed publisher
    ..falciparum CQ resistance transporter (PfCRT) (C2(GC03) or C4(Dd2), respectively)...
  27. Malátková P, Kanavi M, Nobilis M, Wsol V. In vitro metabolism of fenofibric acid by carbonyl reducing enzymes. Chem Biol Interact. 2016;258:153-8 pubmed publisher
    ..AKR1C1, AKR1C2, AKR1C3 and AKR1B1 were also identified as reductases of fenofibric acid but are expected to play only a minor ..
  28. Russo G, Grumetto L, Barbato F, Vistoli G, Pedretti A. Prediction and mechanism elucidation of analyte retention on phospholipid stationary phases (IAM-HPLC) by in silico calculated physico-chemical descriptors. Eur J Pharm Sci. 2017;99:173-184 pubmed publisher
    ..e. IAM.PC.MG and IAM.PC.DD2, with a fairly good degree (r2=0.85) of accuracy...
  29. Joubert J, Fortuin E, Taylor D, Smith P, Malan S. Pentacycloundecylamines and conjugates thereof as chemosensitizers and reversed chloroquine agents. Bioorg Med Chem Lett. 2014;24:5516-9 pubmed publisher
    ..74-17.6 nM and 27.6-253.5 nM against CQ-sensitive (D10) and CQ-resistant strains (Dd2) of Plasmodium falciparum, respectively...
  30. Zhao X, Chen W, Zhou Z, Wang Q, Liu Z, Moaddel R, et al. Preparation of a biomimetic polyphosphorylcholine monolithic column for immobilized artificial membrane chromatography. J Chromatogr A. 2015;1407:176-83 pubmed publisher
    ..Good correlation was observed between the retention on commercial IAM column (IAM.PC.DD2) and poly(MDPC-co-EDMA) monolith...
  31. Galassi V, Salinas S, Montich G. Conformational changes, from ?-strand to ?-helix, of the fatty acid-binding protein ReP1-NCXSQ in anionic lipid membranes: dependence with the vesicle curvature. Eur Biophys J. 2018;47:165-177 pubmed publisher
    ..Similarly to the observed in L-BABP, another member of the fatty acid binding proteins, a conformational change in ReP1-NCXSQ was coupled to the gel to ..
  32. Grumetto L, Russo G, Barbato F. Polar interactions drug/phospholipids estimated by IAM-HPLC vs cultured cell line passage data: Their relationships and comparison of their effectiveness in predicting drug human intestinal absorption. Int J Pharm. 2016;500:275-90 pubmed publisher
    ..PC.MG (r(2)=0.765) and IAM.PC.DD2 (r(2)=0...
  33. Derikx J, van Waardenburg D, Thuijls G, Willigers H, Koenraads M, van Bijnen A, et al. New Insight in Loss of Gut Barrier during Major Non-Abdominal Surgery. PLoS ONE. 2008;3:e3954 pubmed publisher
    ..Gut mucosal barrier was assessed by plasma markers for enterocyte damage (I-FABP, I-BABP) and urinary presence of tight junction protein claudin-3...
  34. Horváth G, Bencsura Ã, Simon Ã, Tochtrop G, Dekoster G, Covey D, et al. Structural determinants of ligand binding in the ternary complex of human ileal bile acid binding protein with glycocholate and glycochenodeoxycholate obtained from solution NMR. FEBS J. 2016;283:541-55 pubmed publisher
    ..Human ileal bile acid binding protein (I-BABP) is an intracellular carrier of bile salts in the epithelial cells of the distal small intestine and has a key role ..
  35. Popławski P, Wisniewski J, Rijntjes E, Richards K, Rybicka B, Köhrle J, et al. Restoration of type 1 iodothyronine deiodinase expression in renal cancer cells downregulates oncoproteins and affects key metabolic pathways as well as anti-oxidative system. PLoS ONE. 2017;12:e0190179 pubmed publisher
    ..g. TKT, NAMPT, IDH2), sex steroid metabolism and anti-oxidative response (AKR1C2, AKR1B10). DIO1 expression resulted in elevated intracellular concentration of T4...
  36. Pathak V, Colah R, Ghosh K. Plasmodium falciparum malaria skews globin gene expression balance in in-vitro haematopoietic stem cell culture system: Its implications in malaria associated anemia. Exp Parasitol. 2018;185:29-38 pubmed publisher
    ..Upon exposure to the different doses of P. falciparum parasites of strains 3D7, Dd2 and RKL9 (intact and lysed form) at different stages of erythroid development, cells demonstrated suppression in ..
  37. Audere M, Rutka K, Inaskina I, Peculis R, Sepetiene S, Valeina S, et al. Genetic linkage studies of a North Carolina macular dystrophy family. Medicina (Kaunas). 2016;52:180-6 pubmed publisher
    ..Up to date there are three types of NCMD described and consequently named macular dystrophy, retinal: MCDR1, MCDR2 and MCDR3...
  38. Wang W, Li Q, Wei Y, Xue J, Sun X, Yu Y, et al. Novel carbazole aminoalcohols as inhibitors of β-hematin formation: Antiplasmodial and antischistosomal activities. Int J Parasitol Drugs Drug Resist. 2017;7:191-199 pubmed publisher
    ..agents, and several compounds showed potent in vitro activities against Plasmodium falciparum 3D7 and Dd2 strains and adult and juvenile Schistosoma japonicum...
  39. Amaladoss A, Chen Q, Liu M, Dummler S, Dao M, Suresh S, et al. De Novo Generated Human Red Blood Cells in Humanized Mice Support Plasmodium falciparum Infection. PLoS ONE. 2015;10:e0129825 pubmed publisher
    ..falciparum K1 and HB3 strains for 3 cycles, whereas in other strains such as 3D7, DD2, 7G8, FCR3 and W2mef parasites could only be detected for 1 cycle...
  40. Wenners A, Hartmann F, Jochens A, Roemer A, Alkatout I, Klapper W, et al. Stromal markers AKR1C1 and AKR1C2 are prognostic factors in primary human breast cancer. Int J Clin Oncol. 2016;21:548-56 pubmed publisher
    Stromal fibroblasts influence tumor growth and progression. We evaluated two aldo-keto reductases, AKR1C1 and AKR1C2, in stromal fibroblasts and carcinoma cells as prognostic factors in primary human breast cancer...
  41. MacLeod A, McMahon M, Plummer S, Higgins L, Penning T, Igarashi K, et al. Characterization of the cancer chemopreventive NRF2-dependent gene battery in human keratinocytes: demonstration that the KEAP1-NRF2 pathway, and not the BACH1-NRF2 pathway, controls cytoprotection against electrophiles as well as redox-cycling compo. Carcinogenesis. 2009;30:1571-80 pubmed publisher
    ..0-fold. mRNA for aldo-keto reductase (AKR) 1B10, AKR1C1, AKR1C2 and AKR1C3 were induced to the greatest extent, showing increases of between 12- and 16-fold, whereas mRNA for ..
  42. Daghir Wojtkowiak E, Wiczling P, Bocian S, Kubik Å, KoÅ›liÅ„ski P, Buszewski B, et al. Least absolute shrinkage and selection operator and dimensionality reduction techniques in quantitative structure retention relationship modeling of retention in hydrophilic interaction liquid chromatography. J Chromatogr A. 2015;1403:54-62 pubmed publisher
    ..Two home-made (Amino-P-C18, Amino-P-C10) and one commercial (IAM.PC.DD2) HILIC stationary phases were considered...
  43. Fallatah O, Georges E. Apigenin-induced ABCC1-mediated efflux of glutathione from mature erythrocytes inhibits the proliferation of Plasmodium falciparum. Int J Antimicrob Agents. 2017;50:673-677 pubmed publisher
    ..that increasing concentrations of API inhibited the proliferation of chloroquine-susceptible (3D7) and -resistant (Dd2) parasites in culture with similar 50% inhibitory concentration (IC50) values (36.02?±?2.4?µM and 34...
  44. Adams M, Barnard L, de Kock C, Smith P, Wiesner L, Chibale K, et al. Cyclopalladated organosilane-tethered thiosemicarbazones: novel strategies for improving antiplasmodial activity. Dalton Trans. 2016;45:5514-20 pubmed publisher
    ..evaluated for in vitro antiplasmodial activity against the chloroquine-sensitive (NF54) and chloroquine-resistant (Dd2) strains of the human malaria parasite Plasmodium falciparum...
  45. Phuangsawai O, Beswick P, Ratanabunyong S, Tabtimmai L, Suphakun P, Obounchoey P, et al. Evaluation of the anti-malarial activity and cytotoxicity of 2,4-diamino-pyrimidine-based kinase inhibitors. Eur J Med Chem. 2016;124:896-905 pubmed publisher
    ..of open access high throughput anti-malarial screening data reported by GlaxoSmithKline at the 3D7 and resistant Dd2 strains. SAR expansion has been performed using structural knowledge of the most plausible parasite target...
  46. Zachmann M, Völlmin J, Hamilton W, Prader A. Steroid 17,20-desmolase deficiency: a new cause of male pseudohermaphroditism. Clin Endocrinol (Oxf). 1972;1:369-85 pubmed
  47. Breton J, Gage M, Hay A, Keen J, Wild C, Donnellan C, et al. Proteomic screening of a cell line model of esophageal carcinogenesis identifies cathepsin D and aldo-keto reductase 1C2 and 1B10 dysregulation in Barrett's esophagus and esophageal adenocarcinoma. J Proteome Res. 2008;7:1953-62 pubmed publisher
    ..05) 3- and 9-fold in erosive and Barrett's epithelium, respectively; and (iii) AKR1C2 levels increased (p<0.05) in erosive and Barrett's epithelium, but were reduced (p<0.05) in EA...
  48. Rossner P, Strapáčová S, Štolcpartová J, Schmuczerova J, Milcova A, Neca J, et al. Toxic Effects of the Major Components of Diesel Exhaust in Human Alveolar Basal Epithelial Cells (A549). Int J Mol Sci. 2016;17: pubmed publisher
    ..Bulky DNA adducts, lipid peroxidation, DNA and protein oxidation and mRNA expression of CYP1A1, CYP1B1, NQO1, POR, AKR1C2 and COX2 were analyzed. Bulky DNA adducts were induced after both treatment periods; the effect of 1-NP was weak...
  49. Brecht A, Oertelt Prigione S, Seeland U, Rücke M, Hättasch R, Wagelöhner T, et al. Left Atrial Function in Preclinical Diastolic Dysfunction: Two-Dimensional Speckle-Tracking Echocardiography-Derived Results from the BEFRI Trial. J Am Soc Echocardiogr. 2016;29:750-758 pubmed publisher
    ..0%) showed an echocardiographically more advanced stage of DD (pseudonormal filling [DD2])...
  50. Davies N, Hayden R, Simpson P, Birtwistle J, Mayer K, Ride J, et al. AKR1C isoforms represent a novel cellular target for jasmonates alongside their mitochondrial-mediated effects. Cancer Res. 2009;69:4769-75 pubmed publisher
    ..In conclusion, we have identified AKR1C isoforms as a novel target of jasmonates in cancer cells and provide further evidence of the promise of these compounds, or derivatives thereof, as adjunctive therapies in the treatment of cancer. ..
  51. Roberts B, Iyamu I, Lee S, Lee E, Ayong L, Kyle D, et al. Spirocyclic chromanes exhibit antiplasmodial activities and inhibit all intraerythrocytic life cycle stages. Int J Parasitol Drugs Drug Resist. 2016;6:85-92 pubmed publisher
    ..compound UCF 201 exhibits a 50% effective concentration (EC50) of 350 nM against the chloroquine-resistant Dd2 strain and a selectivity over 50 using human liver HepG2 cells...
  52. Murray L, Stewart L, Tarr S, Ahouidi A, Diakite M, Amambua Ngwa A, et al. Multiplication rate variation in the human malaria parasite Plasmodium falciparum. Sci Rep. 2017;7:6436 pubmed publisher
    ..6 and 10.5 fold per 48 hours, with clone Dd2 having a higher rate than others (clones 3D7, HB3 and D10)...
  53. Cogliati C, Tomaselli S, Assfalg M, Pedò M, Ferranti P, Zetta L, et al. Disulfide bridge regulates ligand-binding site selectivity in liver bile acid-binding proteins. FEBS J. 2009;276:6011-23 pubmed publisher
    ..Here, the effects of the presence of a naturally occurring disulfide bridge on liver BABP ligand-binding properties and backbone dynamics have been investigated by NMR...
  54. Kim L, Kim M, Kim J, Cho H. Aldo-keto reductase activity after diethylhexyl phthalate exposure in eutopic and ectopic endometrial cells. Eur J Obstet Gynecol Reprod Biol. 2017;215:215-219 pubmed publisher
    ..DEHP upregulated AKR1C1, AKR1C2, AKR1C3, and AKR1B10 expression in EE, while EC showed continuously increased AKR1C3 expression before and after ..
  55. Chopra R, Chibale K, Singh K. Pyrimidine-chloroquinoline hybrids: Synthesis and antiplasmodial activity. Eur J Med Chem. 2018;148:39-53 pubmed publisher
    ..The most active hybrids of the series were further screened against the chloroquine resistant (CQR) Dd2 strain of the parasite and for in vitro cytotoxicity against mammalian Vero cell lines...
  56. Kaur H, Balzarini J, de Kock C, Smith P, Chibale K, Singh K. Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. Eur J Med Chem. 2015;101:52-62 pubmed publisher
    ..and quinoline moiety were synthesized and tested for in vitro antiplasmodial activity against NF54 and Dd2 strains of Plasmodium falciparum...
  57. Nondo R, Moshi M, Erasto P, Masimba P, Machumi F, Kidukuli A, et al. Anti-plasmodial activity of Norcaesalpin D and extracts of four medicinal plants used traditionally for treatment of malaria. BMC Complement Altern Med. 2017;17:167 pubmed publisher
    ..falciparum (3D7), chloroquine-resistant P. falciparum (Dd2, K1) and artemisinin-resistant P...
  58. Dhingra S, Redhi D, Combrinck J, Yeo T, Okombo J, Henrich P, et al. A Variant PfCRT Isoform Can Contribute to Plasmodium falciparum Resistance to the First-Line Partner Drug Piperaquine. MBio. 2017;8: pubmed publisher
    ..gene editing, we report that addition of the C101F mutation to the chloroquine (CQ) resistance-conferring PfCRT Dd2 isoform common to Asia can confer PPQ resistance to cultured parasites...
  59. van Rooyen D, Gent R, Barnard L, Swart A. The in vitro metabolism of 11β-hydroxyprogesterone and 11-ketoprogesterone to 11-ketodihydrotestosterone in the backdoor pathway. J Steroid Biochem Mol Biol. 2018;178:203-212 pubmed publisher
    ..by steroidogenic enzymes in the backdoor pathway-5α-reductase (SRD5A) and 3α-hydroxysteroid type 3 (AKR1C2) converted 11OHP4 to 5α-pregnan-11β-ol,3,20-dione and 5α-pregnan-3α,11β-diol-20-one, while 11KP4 ..
  60. Nishizawa M, Nakajima T, Yasuda K, Kanzaki H, Sasaguri Y, Watanabe K, et al. Close kinship of human 20alpha-hydroxysteroid dehydrogenase gene with three aldo-keto reductase genes. Genes Cells. 2000;5:111-25 pubmed
    ..PCR) with gene-specific primers, we were able to isolate the human 20alpha-HSD, bile acid-binding protein (BABP) [AKR 1C2], prostaglandin F synthase (PGFS) [AKR 1C3], and dihydrodiol dehydrogenase (DD) 4 [AKR 1C4] genes...
  61. Tochtrop G, Richter K, Tang C, Toner J, Covey D, Cistola D. Energetics by NMR: site-specific binding in a positively cooperative system. Proc Natl Acad Sci U S A. 2002;99:1847-52 pubmed
    ..With ongoing improvements in sensitivity and resolution, NMR methods are becoming more amenable to dissecting the complex binding energetics of multisite systems. ..
  62. Trauger J, Jiang A, Stearns B, LoGrasso P. Kinetics of allopregnanolone formation catalyzed by human 3 alpha-hydroxysteroid dehydrogenase type III (AKR1C2). Biochemistry. 2002;41:13451-9 pubmed
    ..These results characterize the role of 3alpha-HSD type III in allopregnanolone formation and suggest that activation of this enzyme by fluoxetine is likely not the mechanism by which fluoxetine increases allopregnanolone concentrations. ..
  63. Lu D. AKR1C2 small interfering RNA (siRNA) inhibited beta-catenin expression and transcriptional activation in human liver cancer cell line QGY7701. Hepatogastroenterology. 2007;54:2088-91 pubmed
    It has been proved that changes in the Wnt/beta-catenin pathway lead to hepatocarcinogenesis and the AKR1C2 gene may contribute to the occurrence, advancement and invasiveness of liver cancer...
  64. Setlur S, Chen C, Hossain R, Ha J, Van Doren V, Stenzel B, et al. Genetic variation of genes involved in dihydrotestosterone metabolism and the risk of prostate cancer. Cancer Epidemiol Biomarkers Prev. 2010;19:229-39 pubmed publisher
    ..We also investigated associations between SNPs in genes (HSD3B1, SRD5A1/2, and AKR1C2) involved in the conversion of testosterone to DHT, and in DHT metabolism and PCA risk...
  65. Jin Y, Mesaros A, Blair I, Penning T. Stereospecific reduction of 5?-reduced steroids by human ketosteroid reductases of the AKR (aldo-keto reductase) superfamily: role of AKR1C1-AKR1C4 in the metabolism of testosterone and progesterone via the 5?-reductase pathway. Biochem J. 2011;437:53-61 pubmed publisher
  66. Jernberg E, Thysell E, Bovinder Ylitalo E, Rudolfsson S, Crnalic S, Widmark A, et al. Characterization of prostate cancer bone metastases according to expression levels of steroidogenic enzymes and androgen receptor splice variants. PLoS ONE. 2013;8:e77407 pubmed publisher
    ..Significantly higher levels of SRD5A1, AKR1C2, AKR1C3, and HSD17B10 mRNA were however found in bone metastases than in non-malignant and/or malignant prostate ..
  67. Manandhar M, Lowery M, Boulware K, Lin K, Lu Y, Wood R. Transcriptional consequences of XPA disruption in human cell lines. DNA Repair (Amst). 2017;57:76-90 pubmed publisher
    ..Only 27 common genes were different by more than 1.5-fold. The most significant hits were AKR1C1 and AKR1C2, involved in steroid hormone metabolism. AKR1C2 protein was lower in all of the immortalized XPA-deficient cells...
  68. Kumar R, Duffy S, Avery V, Davis R. Synthesis of antimalarial amide analogues based on the plant serrulatane diterpenoid 3,7,8-trihydroxyserrulat-14-en-19-oic acid. Bioorg Med Chem Lett. 2017;27:4091-4095 pubmed publisher
    ..acid (16-18) were evaluated for their antimalarial activity against 3D7 (chloroquine sensitive) and Dd2 (chloroquine resistant) Plasmodium falciparum strains, and preliminary cytotoxicity data were also acquired using ..
  69. Horváth G, Biczók L, Majer Z, Kovacs M, Micsonai A, Kardos J, et al. Structural insight into a partially unfolded state preceding aggregation in an intracellular lipid-binding protein. FEBS J. 2017;284:3637-3661 pubmed publisher
    Human ileal bile acid-binding protein (I-BABP) has a key role in the intracellular transport and metabolic targeting of bile salts...
  70. Bo A, Thomsen R, Nielsen J, Nicolaisen S, Beck Nielsen H, Rungby J, et al. Early onset type 2 diabetes: Age gradient in Clinical and Behavioural Risk Factors in 5115 Persons with Newly Diagnosed Type 2 Diabetes - Results from the DD2 study. Diabetes Metab Res Rev. 2017;: pubmed publisher
    ..To examine the association between early onset of type 2 diabetes (DM) and clinical and behavioural risk factors for later diabetes complications...
  71. Ciaccio P, Tew K. cDNA and deduced amino acid sequences of a human colon dihydrodiol dehydrogenase. Biochim Biophys Acta. 1994;1186:129-32 pubmed
    ..Northern blots revealed that dihydrodiol dehydrogenase(s) were markedly induced in HT29 colon cells by treatment with the Michael acceptor agent ethacrynic acid. ..
  72. Adagu I, Warhurst D. Association of cg2 and pfmdr1 genotype with chloroquine resistance in field samples of Plasmodium falciparum from Nigeria. Parasitology. 1999;119 ( Pt 4):343-8 pubmed
    ..Among field samples from children in Zaria, northern Nigeria, the Tyr-86 polymorphism in pfmdr1 and Ala-281 and the Dd2 kappa repeat of cg2, were significantly associated...
  73. Kazemi Noureini S, Colonna Romano S, Ziaee A, Malboobi M, Yazdanbod M, Setayeshgar P, et al. Differential gene expression between squamous cell carcinoma of esophageus and its normal epithelium; altered pattern of mal, akr1c2, and rab11a expression. World J Gastroenterol. 2004;10:1716-21 pubmed
    ..The expression of mal gene was remarkably down regulated in all 10 surveyed tumor tissues. Akr1c2, a member of the aldo-keto reductase 1C family, which is involved in metabolism of sex hormones and xenobiotics, ..
  74. Lewis M, Wiebe J, Heathcote J. Expression of progesterone metabolizing enzyme genes (AKR1C1, AKR1C2, AKR1C3, SRD5A1, SRD5A2) is altered in human breast carcinoma. BMC Cancer. 2004;4:27 pubmed
    ..of 18S rRNA) of 5alphaR type 1 (SRD5A1), 5alphaR type 2 (SRD5A2), 3alpha-HSO type 2 (AKR1C3), 3alpha-HSO type 3 (AKR1C2) and 20alpha-HSO (AKR1C1) mRNAs in paired (tumorous and nontumorous) breast tissues from 11 patients, and unpaired ..
  75. Toke O, Monsey J, Dekoster G, Tochtrop G, Tang C, Cistola D. Determinants of cooperativity and site selectivity in human ileal bile acid binding protein. Biochemistry. 2006;45:727-37 pubmed
    Human ileal bile acid binding protein (I-BABP) is a member of the family of intracellular lipid-binding proteins and is thought to play a role in the enterohepatic circulation of bile salts...
  76. Wang S, Yang Q, Fung K, Lin H. AKR1C2 and AKR1C3 mediated prostaglandin D2 metabolism augments the PI3K/Akt proliferative signaling pathway in human prostate cancer cells. Mol Cell Endocrinol. 2008;289:60-6 pubmed publisher
    ..11-ketoprostaglandin reductase activity and is capable of converting PGD2 to 9alpha, 11beta-PGF2alpha, whereas AKR1C2-mediated PG metabolism remains unclear...
  77. Li W, Hou G, Zhou D, Lou X, Xu Y, Liu S, et al. The roles of AKR1C1 and AKR1C2 in ethyl-3,4-dihydroxybenzoate induced esophageal squamous cell carcinoma cell death. Oncotarget. 2016;7:21542-55 pubmed publisher
  78. Vihma V, Naukkarinen J, Turpeinen U, Hamalainen E, Kaprio J, Rissanen A, et al. Metabolism of sex steroids is influenced by acquired adiposity-A study of young adult male monozygotic twin pairs. J Steroid Biochem Mol Biol. 2017;172:98-105 pubmed publisher
    ..9 (SD 0.7) vs. 2.4 (1.0) nmol/l, P=0.040] and mRNA expressions of DHT-inactivating AKR1C2 (P=0.021) and cortisol-producing HSD11B1 (P=0.008) higher in the heavier compared to the leaner co-twins...
  79. Badiee M, Tochtrop G. Bile Acid Recognition by Mouse Ileal Bile Acid Binding Protein. ACS Chem Biol. 2017;: pubmed publisher
    Ileal bile acid binding protein (I-BABP, gene name FABP6) is a component of the bile acid recycling system, expressed in the ileal enterocyte...
  80. Robertson L, Duffy S, Wang Y, Wang D, Avery V, Carroll A. Pimentelamines A-C, Indole Alkaloids Isolated from the Leaves of the Australian Tree Flindersia pimenteliana. J Nat Prod. 2017;: pubmed publisher
    ..Antiplasmodial activity was also reported for the natural products against chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) Plasmodium falciparum with IC50 values ranging from 0.19 to 3.6 ?M.
  81. Winters C, Molowa D, Guzelian P. Isolation and characterization of cloned cDNAs encoding human liver chlordecone reductase. Biochemistry. 1990;29:1080-7 pubmed
    ..Northern blot analysis of RNA from human, gerbil, rabbit, hamster, mouse, and rat livers disclosed hybridization with CDR cDNA only for the first three species.(ABSTRACT TRUNCATED AT 250 WORDS) ..
  82. Qin K, Khanna M, Cheng K. Structure of a gene coding for human dihydrodiol dehydrogenase/bile acid-binding protein. Gene. 1994;149:357-61 pubmed
    The structure and sequence of the gene (DD/BABP) encoding a human dihydrodiol dehydrogenase/bile acid-binding protein (DD/BABP) were determined by analysis of genomic clones...
  83. Dufort I, Soucy P, Labrie F, Luu The V. Molecular cloning of human type 3 3 alpha-hydroxysteroid dehydrogenase that differs from 20 alpha-hydroxysteroid dehydrogenase by seven amino acids. Biochem Biophys Res Commun. 1996;228:474-9 pubmed
    ..1, 78.3, and 67.4% identity with rat 3 alpha-HSD and rabbit and rat 20 alpha-HSD, respectively. 3 alpha-HSD3 belongs to the aldo-keto reductase family and like almost all the members of this family preferred NADPH as cofactor. ..
  84. Rizner T, Lin H, Peehl D, Steckelbroeck S, Bauman D, Penning T. Human type 3 3alpha-hydroxysteroid dehydrogenase (aldo-keto reductase 1C2) and androgen metabolism in prostate cells. Endocrinology. 2003;144:2922-32 pubmed
    ..By controlling local ligand concentration AKRs may regulate steroid hormone action at the prereceptor level. AKR1C2 is expressed in prostate, and in vitro it will catalyze the nicotinamide adenine dinucleotide (NAD(+))-dependent ..
  85. Ji Q, Aoyama C, Nien Y, Liu P, Chen P, Chang L, et al. Selective loss of AKR1C1 and AKR1C2 in breast cancer and their potential effect on progesterone signaling. Cancer Res. 2004;64:7610-7 pubmed
    ..Selective loss of AKR1C1, which encodes a 20alpha-hydroxysteroid dehydrogenase [20alpha-HSD (EC 1.1.1.149)], and AKR1C2, which encodes a 3alpha-hydroxysteroid dehydrogenase [3alpha-HSD (EC 1.1.1...
  86. Mindnich R, Haller F, Halbach F, Moeller G, Hrabe de Angelis M, Adamski J. Androgen metabolism via 17beta-hydroxysteroid dehydrogenase type 3 in mammalian and non-mammalian vertebrates: comparison of the human and the zebrafish enzyme. J Mol Endocrinol. 2005;35:305-16 pubmed
    ..Our results suggest that 17beta-HSD type 3 might play slightly different roles in zebrafish compared with human although testosterone itself is likely to have similar functions in both organisms. ..
  87. Toke O, Monsey J, Cistola D. Kinetic mechanism of ligand binding in human ileal bile acid binding protein as determined by stopped-flow fluorescence analysis. Biochemistry. 2007;46:5427-36 pubmed
    Cooperative ligand binding to human ileal bile acid binding protein (I-BABP) was studied using the stopped-flow fluorescence technique...
  88. MARIN Y, Seiberg M, Lin C. Aldo-keto reductase 1C subfamily genes in skin are UV-inducible: possible role in keratinocytes survival. Exp Dermatol. 2009;18:611-8 pubmed publisher
    ..AKR1C1 and AKR1C2 inactivate progesterone and 5alpha-dihydrotestosterone, respectively, whereas AKR1C3 activates oestradiol and ..
  89. Roberson A, Hyatt K, Kenkel C, Hanson K, Myers D. Interleukin 1? regulates progesterone metabolism in human cervical fibroblasts. Reprod Sci. 2012;19:271-81 pubmed publisher
    ..through the regulation of the expression of 20?-hydroxysteroid dehydrogenases (aldo-keto reductase [AKR]1C1, AKR1C2, or AKR1C3), 5?-reductase type 1 (5?-RDT1), and/or 17?-hydroxysteroid dehyrogenases (17?-HSD) type 1 and 2...
  90. Emter R, Natsch A. Dual regulation of skin sensitizer-induced HMOX1 expression by Bach1 and Nrf2: Comparison to regulation of the AKR1C2-ARE element in the KeratinoSens cell line. Toxicol Appl Pharmacol. 2015;288:281-8 pubmed publisher
    ..based on luciferase expression regulated by the antioxidant response element (ARE) of the aldoketoreductase 1C2 (AKR1C2) gene. Luciferase upregulation is dependent on Nrf2, while HMOX1 upregulation is only partially Nrf2-dependent...
  91. Stapelfeld C, Maser E. Sex hormones reduce NNK detoxification through inhibition of short-chain dehydrogenases/reductases and aldo-keto reductases in vitro. Chem Biol Interact. 2017;276:167-173 pubmed publisher
    ..carbonyl reduction is catalyzed by members of the AKR- and the SDR-superfamilies which include AKR1B10, AKR1C1, AKR1C2, AKR1C4, 11?-HSD1 and CBR1...
  92. Gedebjerg A, Almdal T, Berencsi K, Rungby J, Nielsen J, Witte D, et al. Prevalence of micro- and macrovascular diabetes complications at time of type 2 diabetes diagnosis and associated clinical characteristics: A cross-sectional baseline study of 6958 patients in the Danish DD2 cohort. J Diabetes Complications. 2018;32:34-40 pubmed publisher
    ..One-third of patients with T2D had diabetes complications around time of diagnosis. Our findings suggest different pathophysiological mechanisms behind micro- and macrovascular complications. ..