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

Top Publications

  1. ncbi Molecular cloning of multiple cDNAs encoding human enzymes structurally related to 3 alpha-hydroxysteroid dehydrogenase
    K N Qin
    Department of Pediatrics, Cornell University Medical College, New York, NY 10021
    J Steroid Biochem Mol Biol 46:673-9. 1993
  2. ncbi Genomic structure of rat 3alpha-hydroxysteroid/dihydrodiol dehydrogenase (3alpha-HSD/DD, AKR1C9)
    H K Lin
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia 19104 6084, USA
    J Steroid Biochem Mol Biol 71:29-39. 1999
  3. pmc Identification of candidate genes associated with cell wall digestibility and eQTL (expression quantitative trait loci) analysis in a Flint x Flint maize recombinant inbred line population
    Chun Shi
    Technical University of Munich, Am Hochanger 2, 85350 Freising, Germany
    BMC Genomics 8:22. 2007
  4. pmc Dihydrodiol dehydrogenases regulate the generation of reactive oxygen species and the development of cisplatin resistance in human ovarian carcinoma cells
    Jianli Chen
    Department of Pathology and Laboratory Medicine, Temple University School of Medicine, Room 206, OMS, 3400 N Broad Street, Philadelphia, PA 19140, USA
    Cancer Chemother Pharmacol 61:979-87. 2008
  5. pmc Two pathways for prostaglandin F2 alpha synthesis by the primate periovulatory follicle
    Brandy L Dozier
    Department of Physiological Sciences, Eastern Virginia Medical School, 700 Olney Road, Lewis Hall, Norfolk, Virginia 23507, USA
    Reproduction 136:53-63. 2008
  6. doi Interleukin 1β regulates progesterone metabolism in human cervical fibroblasts
    Amy E Roberson
    Department of Cell Biology, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73104, USA
    Reprod Sci 19:271-81. 2012
  7. ncbi cDNA cloning and expression of the human hepatic bile acid-binding protein. A member of the monomeric reductase gene family
    A Stolz
    Division of Gastrointestinal and Liver Diseases, University of Southern California School of Medicine, Los Angeles 90033
    J Biol Chem 268:10448-57. 1993
  8. ncbi Crystal structure of human type III 3alpha-hydroxysteroid dehydrogenase/bile acid binding protein complexed with NADP(+) and ursodeoxycholate
    Y Jin
    Department of Pharmacology, Department of Biochemistry and Biophysics, and The Johnson Research Foundation, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104, USA
    Biochemistry 40:10161-8. 2001
  9. ncbi Structure of the human 3alpha-hydroxysteroid dehydrogenase type 3 in complex with testosterone and NADP at 1.25-A resolution
    V Nahoum
    Oncology and Molecular Endocrinology Research Center, Laval University Medical Center, Quebec, Quebec G1V 4G2, Canada
    J Biol Chem 276:42091-8. 2001
  10. doi The effect of allelic variation in aldo-keto reductase 1C2 on the in vitro metabolism of dihydrotestosterone
    Ryan H Takahashi
    Division of Pharmaceutics and Biopharmaceutics, Faculty of Pharmaceutical Sciences, University of British Columbia, 2146 East Mall, Vancouver, BC, Canada V6T 1Z3
    J Pharmacol Exp Ther 329:1032-9. 2009

Research Grants

  1. Amy E Wright; Fiscal Year: 2014
  2. Development of a Chloroquine Replacement Drug
    MICHAEL KEVIN RISCOE; Fiscal Year: 2010
  3. ANTIMALARIAL ACTION AND RESISTANCE
    Donald Krogstad; Fiscal Year: 1991
  4. INTRACELLULAR TRANSPORT OF AMPHIPATHS
    Bruce Luxon; Fiscal Year: 2000
  5. Dihydrodiol dehydrogenase mediates cisplatin resistance
    Henry Simpkins; Fiscal Year: 2007
  6. Breast cancer and HRT: genetic susceptibility within th*
    Kathleen Malone; Fiscal Year: 2006
  7. Symposium on Aldo-Keto Reductases & Toxicant Metabolism
    TREVOR PENNING; Fiscal Year: 2002
  8. Molecular Mechanisms of Multistage Carcinogenesis
    TREVOR PENNING; Fiscal Year: 2006
  9. Novel Anti-Malarials by Combinatorial Pharmacogenomics
    Joseph DeRisi; Fiscal Year: 2006

Detail Information

Publications231 found, 100 shown here

  1. ncbi Molecular cloning of multiple cDNAs encoding human enzymes structurally related to 3 alpha-hydroxysteroid dehydrogenase
    K N Qin
    Department of Pediatrics, Cornell University Medical College, New York, NY 10021
    J Steroid Biochem Mol Biol 46:673-9. 1993
    ..human chlordecone reductase belong to the aldo-keto reductase superfamily, we named these human clones HAKRa to HAKRd. Northern blot analysis showed that the liver expresses the highest levels of all four clones...
  2. ncbi Genomic structure of rat 3alpha-hydroxysteroid/dihydrodiol dehydrogenase (3alpha-HSD/DD, AKR1C9)
    H K Lin
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia 19104 6084, USA
    J Steroid Biochem Mol Biol 71:29-39. 1999
    ..chlordecone reductase/DD4, AKR1C4), type 2 3alpha-HSD (AKR1C3) and type 3 3alpha-HSD (bile-acid binding protein, AKR1C2) genes...
  3. pmc Identification of candidate genes associated with cell wall digestibility and eQTL (expression quantitative trait loci) analysis in a Flint x Flint maize recombinant inbred line population
    Chun Shi
    Technical University of Munich, Am Hochanger 2, 85350 Freising, Germany
    BMC Genomics 8:22. 2007
    ..Cell-wall digestibility is the major target for improving the feeding value of forage maize. An understanding of the molecular basis for cell-wall digestibility is crucial towards breeding of highly digestible maize...
  4. pmc Dihydrodiol dehydrogenases regulate the generation of reactive oxygen species and the development of cisplatin resistance in human ovarian carcinoma cells
    Jianli Chen
    Department of Pathology and Laboratory Medicine, Temple University School of Medicine, Room 206, OMS, 3400 N Broad Street, Philadelphia, PA 19140, USA
    Cancer Chemother Pharmacol 61:979-87. 2008
    We have previously demonstrated that overexpression of dihydrodiol dehydrogenase isoform 1 (DDH1) or DDH2 leads to the induction of drug resistance to platinum based drugs in human ovarian, lung, cervical and germ cell tumor cell lines...
  5. pmc Two pathways for prostaglandin F2 alpha synthesis by the primate periovulatory follicle
    Brandy L Dozier
    Department of Physiological Sciences, Eastern Virginia Medical School, 700 Olney Road, Lewis Hall, Norfolk, Virginia 23507, USA
    Reproduction 136:53-63. 2008
    ..PGF2 alpha can also be synthesized from PGE2 via the enzymes AKR1C1 and AKR1C2. Monkey granulosa cell levels of AKR1C1/AKR1C2 mRNA was low 0-12 h, peaked at 24 h, and returned to low levels by ..
  6. doi Interleukin 1β regulates progesterone metabolism in human cervical fibroblasts
    Amy E Roberson
    Department of Cell Biology, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73104, USA
    Reprod Sci 19:271-81. 2012
    ..through the regulation of the expression of 20α-hydroxysteroid dehydrogenases (aldo-keto reductase [AKR]1C1, AKR1C2, or AKR1C3), 5α-reductase type 1 (5α-RDT1), and/or 17β-hydroxysteroid dehyrogenases (17β-HSD) type 1 and 2...
  7. ncbi cDNA cloning and expression of the human hepatic bile acid-binding protein. A member of the monomeric reductase gene family
    A Stolz
    Division of Gastrointestinal and Liver Diseases, University of Southern California School of Medicine, Los Angeles 90033
    J Biol Chem 268:10448-57. 1993
    ..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...
  8. ncbi Crystal structure of human type III 3alpha-hydroxysteroid dehydrogenase/bile acid binding protein complexed with NADP(+) and ursodeoxycholate
    Y Jin
    Department of Pharmacology, Department of Biochemistry and Biophysics, and The Johnson Research Foundation, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104, USA
    Biochemistry 40:10161-8. 2001
    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...
  9. ncbi Structure of the human 3alpha-hydroxysteroid dehydrogenase type 3 in complex with testosterone and NADP at 1.25-A resolution
    V Nahoum
    Oncology and Molecular Endocrinology Research Center, Laval University Medical Center, Quebec, Quebec G1V 4G2, Canada
    J Biol Chem 276:42091-8. 2001
    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 ..
  10. doi The effect of allelic variation in aldo-keto reductase 1C2 on the in vitro metabolism of dihydrotestosterone
    Ryan H Takahashi
    Division of Pharmaceutics and Biopharmaceutics, Faculty of Pharmaceutical Sciences, University of British Columbia, 2146 East Mall, Vancouver, BC, Canada V6T 1Z3
    J Pharmacol Exp Ther 329:1032-9. 2009
    ..b>AKR1C2 can regulate the extent and duration of activation of the androgen receptor by catalyzing the reduction of DHT to ..
  11. doi Aldo-keto reductases AKR1C1, AKR1C2 and AKR1C3 may enhance progesterone metabolism in ovarian endometriosis
    N Hevir
    Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia
    Chem Biol Interact 191:217-26. 2011
    ..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...
  12. pmc Human cytosolic hydroxysteroid dehydrogenases of the aldo-ketoreductase superfamily catalyze reduction of conjugated steroids: implications for phase I and phase II steroid hormone metabolism
    Yi Jin
    Centers of Excellence in Environmental Toxicology and Cancer Pharmacology, Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6084, USA
    J Biol Chem 284:10013-22. 2009
    ..AKR1C isoform was similar to that of the corresponding free steroid except for the reduction of DhtG catalyzed by AKR1C2, where a complete inversion in stereochemical preference to 3beta-reduction (with DhtG) from 3alpha-reduction (..
  13. ncbi Selective and potent inhibitors of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) that metabolizes neurosteroids derived from progesterone
    Yu Higaki
    Laboratory of Biochemistry, Gifu Pharmaceutical University, 5 6 1 Mitahora Higashi, 502 8585, Gifu, Japan
    Chem Biol Interact 143:503-13. 2003
    ..precursors among four human 3(20)alpha-hydroxysteroid dehydrogenases (AKR1C1-AKR1C4) suggests that AKR1C1 and AKR1C2 are involved in the catabolism and synthesis, respectively, of the neuroactive steroids in the human brain...
  14. doi In vitro antimalarial activity of medicinal plant extracts against Plasmodium falciparum
    Asokan Bagavan
    Unit of Nanotechnology and Bioactive Natural Products, Post Graduate and Research Department of Zoology, C Abdul Hakeem College, Melvisharam 632 509, Vellore District, Tamil Nadu, India
    Parasitol Res 108:15-22. 2011
    ..and methanol and tested for their antimalarial activity against chloroquine (CQ)-sensitive (3D7) and CQ-resistant (Dd2 and INDO) strains of Plasmodium falciparum in culture using the fluorescence-based SYBR Green assay...
  15. pmc Characterization of the aldo-keto reductase 1C gene cluster on pig chromosome 10: possible associations with reproductive traits
    Dan J Nonneman
    USDA ARS, US Meat Animal Research Center, Clay Center, Nebraska, 68933, USA
    BMC Vet Res 2:28. 2006
    ..Because of their location in the swine genome and their implication in reproductive physiology, this gene cluster was characterized and evaluated for effects on reproductive traits in swine...
  16. ncbi The nuclear receptors FXR and LXRalpha: potential targets for the development of drugs affecting lipid metabolism and neoplastic diseases
    E J Niesor
    Symphar, Innovative Pharmaceutical Research, 1290 Versoix, Geneva, Switzerland
    Curr Pharm Des 7:231-59. 2001
    ..1,1-bisphosphonate esters, has been discovered which up regulate the Intestinal Bile Acid Binding Protein gene (I-BABP) as demonstrated for chenodeoxycholic acid, however there are no known synthetic activators yet identified for ..
  17. pmc Yeast dihydroorotate dehydrogenase as a new selectable marker for Plasmodium falciparum transfection
    Suresh M Ganesan
    Center for Molecular Parasitology, Department of Microbiology and Immunology, Drexel University College of Medicine, 2900 W Queen Lane, Philadelphia, PA 19129, USA
    Mol Biochem Parasitol 177:29-34. 2011
    ..Atovaquone, however, could not be used for such selection with the Dd2 strain of P. falciparum...
  18. ncbi Rab coupling protein (RCP): a novel target of progesterone action in primate endometrium
    V S Patil
    Primate Biology Department, National Institute for Research in Reproductive Health, Indian Council of Medical Research, Parel, Mumbai 400 012, India
    J Mol Endocrinol 35:357-72. 2005
    ..b>DD2, one of the differentially expressed cDNA fragments, showed higher representation in nonreceptive endometria than ..
  19. pmc Plasmodium falciparum is able to invade erythrocytes through a trypsin-resistant pathway independent of glycophorin B
    Deepak Gaur
    Laboratory of Malaria and Vector Research, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA
    Infect Immun 71:6742-6. 2003
    ..through the trypsin-resistant pathway, we have studied the invasion phenotypes of five parasite strains, 3D7, HB3, Dd2, 7G8, and Indochina I, on trypsin-treated normal and glycophorin B-deficient erythrocytes...
  20. doi Progesterone is extensively metabolized in osteoblasts: implications for progesterone action on bone
    M Quinkler
    Clinical Endocrinology, Internal Medicine, Center for Gastroenterology, Hepatology and Endocrinology, Charite Campus Mitte, Charite University Medicine Berlin, Chariteplatz 1, Berlin, Germany
    Horm Metab Res 40:679-84. 2008
    ..This activity was concomitant with expression of mRNAs for the enzymes AKR1C1, 5 alpha-reductase type 1 and AKR1C2, and 3 beta-HSD type 1 and 3-hydroxysteroid epimerase...
  21. ncbi Impaired dihydrotestosterone catabolism in human prostate cancer: critical role of AKR1C2 as a pre-receptor regulator of androgen receptor signaling
    Qing Ji
    Department of Medicine, Keck School of Medicine, University of Southern California, 2011 Zonal Avenue, Los Angeles, CA 90033, USA
    Cancer Res 67:1361-9. 2007
    We previously reported the selective loss of AKR1C2 and AKR1C1 in prostate cancers compared with their expression in paired benign tissues...
  22. doi Characterization of human liver enzymes involved in the biotransformation of boceprevir, a hepatitis C virus protease inhibitor
    Anima Ghosal
    Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, 2015 Galloping Hill Road, K 15 1945, Kenilworth, NJ 07033, USA
    Drug Metab Dispos 39:510-21. 2011
    ..Screening of boceprevir with recombinant human aldo-keto reductases (AKRs) revealed that AKR1C2 and AKR1C3 exhibited catalytic activity with respect to the formation of M+2 metabolites (M28 and M31)...
  23. ncbi NMR-based modeling and binding studies of a ternary complex between chicken liver bile acid binding protein and bile acids
    Simona Tomaselli
    Laboratorio NMR, ISMAC, CNR, via Bassini 15, 20133, Milano, Italy
    Proteins 69:177-91. 2007
    Chicken liver bile acid binding protein (cL-BABP) is involved in bile acid transport in the liver cytosol...
  24. pmc Revisiting the Plasmodium falciparum RIFIN family: from comparative genomics to 3D-model prediction
    Emanuele Bultrini
    Dipartimento di Malattie Infettive, Parassitarie ed Immunomediate, Istituto Superiore di Sanita, Viale Regina Elena, 299, 00161 Roma, Italy
    BMC Genomics 10:445. 2009
    ..Despite recent advances, our knowledge of the regulation of RIFIN gene expression is still poor and the biological role of the protein products remain obscure...
  25. ncbi Crystal structure of human prostaglandin F synthase (AKR1C3)
    Junichi Komoto
    Department of Molecular Biosciences, University of Kansas, 1200 Sunnyside Avenue, Lawrence, Kansas 66045 7534, USA
    Biochemistry 43:2188-98. 2004
    ..Since the substrate binding cavity of PGFS is relatively large in comparison with those of AKR1C1 and AKR1C2, PGFS (AKR1C3) could catalyze the reduction and/or oxidation reactions of various compounds over a relatively wide ..
  26. ncbi Comparison between immobilized artificial membrane (IAM) HPLC data and lipophilicity in n-octanol for quinolone antibacterial agents
    Francesco Barbato
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita degli Studi di Napoli Federico II, via D Montesano, 49, I 80131 Naples, Italy
    Eur J Pharm Sci 31:288-97. 2007
    ..PC.MG and IAM.PC.DD2; it is expressed as the logarithm of the retention factor measured with (or extrapolated to) 100% aqueous eluent at ..
  27. ncbi cDNA cloning, expression, and mutagenesis study of liver-type prostaglandin F synthase
    T Suzuki
    Second Department, Osaka Bioscience Institute, 6 2 4 Furuedai, Suita, Osaka 565 0874, Japan
    J Biol Chem 274:241-8. 1999
    ..77, and 76% identity with the bovine lung PGF synthase and human liver dihydrodiol dehydrogenase (DD) isozymes DD1, DD2, and DD4, respectively...
  28. doi Differentiation associated changes in gene expression profiles of interstitial cystitis and control urothelial cells
    Deborah R Erickson
    Department of Surgery, Division of Urology, College of Medicine, University of Kentucky, Lexington, Kentucky 40536 0298, USA
    J Urol 180:2681-7. 2008
    ..We evaluated gene expression profiles after inducing differentiation in cultured interstitial cystitis and control urothelial cells...
  29. doi Androgen metabolism in adipose tissue: recent advances
    Karine Blouin
    Molecular Endocrinology and Oncology Research Center, Laval University Medical Research Center, Canada Department of Nutrition, Laval University, Canada
    Mol Cell Endocrinol 301:97-103. 2009
    ..Aldo-keto reductase 1C (AKR1C) enzymes, especially AKR1C2 and AKR1C3, through local synthesis and inactivation of androgens, may be involved in the fine regulation of ..
  30. ncbi Microparticles in deep venous thrombosis, antiphospholipid syndrome and Factor V Leiden
    M C Flores-Nascimento
    Hematology Hemotherapy Center, State University of Campinas, Campinas, SP, Brazil
    Platelets 20:367-75. 2009
    ..The MPs procoagulant activity was analyzed by D-dimer (DD2) and Thrombin Generation Test (TGT) on a healthy pool of plasmas adjusted or not by their number (10,000 MPs)...
  31. doi Loss of enterocyte mass is accompanied by diminished turnover of enterocytes after myeloablative therapy in haematopoietic stem-cell transplant recipients
    J P M Derikx
    Department of Surgery, University Hospital Maastricht and Nutrition and Toxicology Research Institute NUTRIM, Maastricht University, The Netherlands
    Ann Oncol 20:337-42. 2009
    ..and enterocyte loss was explored by examining citrulline serum levels and by assessing circulating intestinal fatty acid-binding protein (I-FABP) and ileal bile acid-binding protein (I-BABP), proteins released by dying mature enterocytes.
  32. doi Synthesis and antimalarial activity of ethylene glycol oligomeric ethers of artemisinin
    Minette Steyn
    Pharmaceutical Chemistry, North West University, Potchefstroom, South Africa
    J Pharm Pharmacol 63:278-86. 2011
    ....
  33. ncbi Identification of a bile acid-responsive element in the human ileal bile acid-binding protein gene. Involvement of the farnesoid X receptor/9-cis-retinoic acid receptor heterodimer
    J Grober
    Physiologie de la Nutrition, Ecole Nationale Supérieure de Biologie Appliquée à la Nutrition et à l Alimentation, EP 1777 CNRS CESG, F 21000, Dijon, France
    J Biol Chem 274:29749-54. 1999
    Intestinal bile acid-binding protein (I-BABP) is a cytosolic protein that binds bile acids (BAs) with a high affinity...
  34. pmc Effect of treating Schistosoma haematobium infection on Plasmodium falciparum-specific antibody responses
    L Reilly
    Institute for Immunology and Infection Research, School of Biological Sciences, Ashworth Laboratories, University of Edinburgh, Edinburgh, UK
    BMC Infect Dis 8:158. 2008
    ..responses directed against plasmodia merozoite surface proteins MSP-1 (DPKMWR, MSP1(19)), and MSP-2 (CH150 and Dd2) which are potential vaccine candidates as well as crude malaria (schizont) and schistosome (whole worm homogenate) ..
  35. pmc Molecular cloning of two human liver 3 alpha-hydroxysteroid/dihydrodiol dehydrogenase isoenzymes that are identical with chlordecone reductase and bile-acid binder
    Y Deyashiki
    Biochemistry Laboratory, Gifu Pharmaceutical University, Japan
    Biochem J 299:545-52. 1994
    Human liver contains two dihydrodiol dehydrogenases, DD2 and DD4, associated with 3 alpha-hydroxysteroid dehydrogenase activity. We have raised polyclonal antibodies that cross-reacted with the two enzymes and isolated two 1...
  36. doi Comparisons of (+/-)-benzo[a]pyrene-trans-7,8-dihydrodiol activation by human cytochrome P450 and aldo-keto reductase enzymes: effect of redox state and expression levels
    Amy M Quinn
    Center of Excellence in Environmental Toxicology, Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6084, USA
    Chem Res Toxicol 21:1086-94. 2008
    ..Initial rates of (+/-)-B[ a]P-7,8-diol oxidation were measured for AKR1A1, AKR1C2, P450 1A1, and P450 1B1 as the ratio of NADPH/NAD (+) cofactors was varied to determine the redox state necessary ..
  37. doi Reinvestigation of structure-activity relationship of methoxylated chalcones as antimalarials: synthesis and evaluation of 2,4,5-trimethoxy substituted patterns as lead candidates derived from abundantly available natural β-asarone
    Rakesh Kumar
    Natural Plant Products Division, Institute of Himalayan Bioresource Technology C S I R, Palampur 176061, H P, India
    Eur J Med Chem 45:5292-301. 2010
    ..8 μM) and 26 (IC(50): 2 μM) were also relatively non-toxic. Furthermore, compound 12 showed excellent resistance index of 1.1 against chloroquine resistant Dd2 strain of P. falciparum.
  38. ncbi Structure-function aspects and inhibitor design of type 5 17beta-hydroxysteroid dehydrogenase (AKR1C3)
    T M Penning
    Department of Pharmacology, University of Pennsylvania School of Medicine, 3620 Hamilton Walk, Philadelphia, PA 19104 6084, USA
    Mol Cell Endocrinol 171:137-49. 2001
    ..Many of these properties are shared by the related AKR1C1, AKR1C2 and AKR1C4 isoforms. RT-PCR shows that AKR1C3 is dominantly expressed in the human prostate and mammary gland...
  39. ncbi Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump
    Jisong Cui
    Department of Atherosclerosis and Endocrinology, Merck Research Laboratories, Rahway, New Jersey 07065, USA
    J Biol Chem 278:10214-20. 2003
    ..7alpha-hydroxylase (Cyp 7a1), sterol 12alpha-hydroxylase (Cyp 8b1), and the intestinal bile acid-binding protein (I-BABP), remained unchanged...
  40. pmc Existence and significance of hepatitis B virus DNA in kidneys of IgA nephropathy
    Nian song Wang
    Department of Nephrology, The Sixth Affiliated Hospital of Shanghai Jiaotong University, 600 Yushan Road, Shanghai 200233, China
    World J Gastroenterol 11:712-6. 2005
    ..To investigate the existence and significance of hepatitis B virus (HBV) DNA in the pathogenesis of IgA nephropathy (IgAN)...
  41. ncbi Proteomic characterization of the site-dependent functional difference in the rat small intestine
    Gotaro Iiizumi
    Laboratory for Nutritional Biochemistry, School of Agriculture, Meiji University, 1 1 1 Higashi Mita, Tama ku, Kawasaki, Kanagawa 214 8571, Japan
    Biochim Biophys Acta 1774:1289-98. 2007
    ..FABP) and Cellular retinol binding protein (CRBP-II) were in the jejunum, and the Bile acid binding protein (BABP) was only observed in the ileum...
  42. doi Karavilagenin C derivatives as antimalarials
    Cátia Ramalhete
    iMed UL, Faculty of Pharmacy, University of Lisbon, Av das Forcas Armadas, 1600 083 Lisbon, Portugal
    Bioorg Med Chem 19:330-8. 2011
    ..for their in vitro antimalarial activity against the chloroquine-sensitive (3D7) and the chloroquine-resistant (Dd2) strains of Plasmodium falciparum. Compound 1 exhibited a moderate activity and 17 was inactive...
  43. doi In vitro metabolism and identification of human enzymes involved in the metabolism of methylnaltrexone
    Zeen Tong
    Pfizer Inc, Collegeville, PA 19426, USA
    Drug Metab Dispos 38:801-7. 2010
    ..5beta-Cholanic acid 3alpha,7alpha-diol, the AKR1C2 inhibitor, and medroxyprogesterone acetate, an inhibitor of AKR1C1, AKR1C2, and AKR1C4, inhibited MNTX reduction ..
  44. ncbi [[1]Benzothieno[3,2-b]pyridin-4-yl-amine--synthesis and investigation of activity against malaria]
    K Görlitzer
    Institut fur Pharmazeutische Chemie, der Universitätsklinik GieBen, Germany
    Pharmazie 59:506-12. 2004
    ..Testing against the chloroquine sensitive 3D7 and the chloroquine resistant Dd2 strain resulted in IC50 values of 150 nM and 210 nM, respectively...
  45. pmc Recombinant Plasmodium falciparum reticulocyte homology protein 4 binds to erythrocytes and blocks invasion
    Deepak Gaur
    Laboratory of Malaria and Vector Research, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Twinbrook III, 12735 Twinbrook Parkway, Bethesda, MD 20892 8132, USA
    Proc Natl Acad Sci U S A 104:17789-94. 2007
    ..Invasion by the parasite clone, Dd2, requires sialic acid on the erythrocyte surface; Dd2/NM is a variant selected for its ability to invade ..
  46. ncbi Peritoneal dialysis is the better therapy choice for successful anti-hepatitis B vaccination
    Juraj Svác
    Logman A S, Bratislava, Slovak Republic
    Adv Perit Dial 21:151-3. 2005
    ..The endpoints were the number of patients with a protective HBAb titer and the number with newly diagnosed hepatitis B. In PD patients, we calculated Kt/V on regular basis...
  47. ncbi Sterol regulatory element-binding protein-1c is responsible for cholesterol regulation of ileal bile acid-binding protein gene in vivo. Possible involvement of liver-X-receptor
    Isabelle Zaghini
    Physiologie de la Nutrition, Ecole Nationale Supérieure de Biologie Appliquée à la Nutrition et à l Alimentation ENSBANA, FRE 2049 CNRS Université de Bourgogne, F 21000, Dijon, France
    J Biol Chem 277:1324-31. 2002
    Ileal bile acid-binding protein (I-BABP) is a cytosolic protein that binds bile acid (BA) specifically. In the ileum, it is thought to be implied in their enterohepatic circulation...
  48. ncbi Androgen metabolism via 17beta-hydroxysteroid dehydrogenase type 3 in mammalian and non-mammalian vertebrates: comparison of the human and the zebrafish enzyme
    R Mindnich
    GSF National Research Center for Environment and Health, Institute of Experimental Genetics, Genome Analysis Center, Ingolstaedter Landstr 1, 85764 Neuherberg, Germany
    J Mol Endocrinol 35:305-16. 2005
    ..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...
  49. ncbi Molecular docking simulations of steroid substrates into human cytosolic hydroxysteroid dehydrogenases (AKR1C1 and AKR1C2): insights into positional and stereochemical preferences
    Yi Jin
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, 19104 6084, USA
    Steroids 71:380-91. 2006
    AKR1C1 and AKR1C2 are human cytosolic hydroxysteroid dehydrogenases, which play pivotal roles in the metabolism and action of natural and synthetic steroid hormones...
  50. doi Overexpression of aldo-keto reductase 1C2 is associated with disease progression in patients with prostatic cancer
    Kuo Hsuan Huang
    Institute of Medicine, Department of Family Medicine, Chung Shan Medical University, Taichung, Taiwan
    Histopathology 57:384-94. 2010
    ..The aim was to investigate the relationship between AKR1C expression and disease progression in prostatic cancer...
  51. pmc Malaria drug resistance is associated with defective DNA mismatch repair
    Meryl A Castellini
    Department of Pathology, Anatomy and Cell Biology, Thomas Jefferson University, Philadelphia, PA 19107, USA
    Mol Biochem Parasitol 177:143-7. 2011
    ..We report that two ARMD parasites, W2 and Dd2, have defective MMR, as do the chloroquine-resistant parasites T9-94, 7C12, and 7G8...
  52. pmc Stereospecific reduction of 5β-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 5β-reductase pathway
    Yi Jin
    Department of Pharmacology and Centers of Excellence in Environmental Toxicology and Cancer Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6084, USA
    Biochem J 437:53-61. 2011
    ....
  53. doi Plasmodium falciparum MLH is schizont stage specific endonuclease
    Mohammed Tarique
    Malaria Group, International Centre for Genetic Engineering and Biotechnology, Aruna Asaf Ali Marg, New Delhi 110067, India
    Mol Biochem Parasitol 181:153-61. 2012
    ..Using immunofluorescence assay we report that the peak expression of MLH in both 3D7 and Dd2 strains of P...
  54. pmc The Danish Centre for Strategic Research in Type 2 Diabetes (DD2) study: Collection of baseline data from the first 580 patients
    Reimar Wernich Thomsen
    Department of Clinical Epidemiology, Aarhus University Hospital, Aarhus
    Clin Epidemiol 4:43-8. 2012
    ..overview of the baseline data collected in the nationwide Danish Centre for Strategic Research in Type 2 Diabetes (DD2) project. The paper presents descriptive data from the first 580 patients enrolled in the DD2...
  55. pmc The Danish Centre for Strategic Research in Type 2 Diabetes (DD2) study: expected outcome from the DD2 project and two intervention studies
    Henning Beck-Nielsen
    Diabetes Research Centre, Odense University Hospital, Odense
    Clin Epidemiol 4:21-6. 2012
    The overall aim of the Danish Centre for Strategic Research in Type 2 Diabetes (DD2) is to near-normalize metabolic control in newly diagnosed patients with type 2 diabetes (T2D) using an individualized treatment approach...
  56. ncbi QSAR and pharmacophore modeling of natural and synthetic antimalarial prodiginines
    Baljinder Singh
    Medicinal Chemistry Division, Indian Institute of Integrative Medicine, Canal Road, Jammu 180001, India
    Curr Comput Aided Drug Des 9:350-9. 2013
    ..potent in vitro as well as in vivo antimalarial activity against chloroquine sensitive D6 and multi-drug resistant Dd2 strains of Plasmodium falciparum...
  57. pmc A new bioactive diterpene glycoside from Molinaea retusa from the Madagascar dry forest
    Alexander L Eaton
    Department of Chemistry, Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, Virginia 24061, USA
    Nat Prod Commun 8:1201-3. 2013
    ..Compounds 2 and 3 also had moderate antiplasmodial activities, with IC50 values of 4.0 and 6.4 microM, respectively, against Plasmodium falciparum, Dd2 strain. The structures were determined using spectroscopic methods.
  58. doi Emergence of pyrido quinoxalines as new family of antimalarial agents
    A Chandra Shekhar
    Fluoroorganic Division, CSIR Indian Institute of Chemical Technology, Hyderabad 500 007, India
    Eur J Med Chem 77:280-7. 2014
    ..and evaluated their antimalarial activity in vitro against chloroquine sensitive (3D7) and drug resistant (Dd2) strains of Plasmodium falciparum...
  59. doi Understanding androgen action in adipose tissue
    Michael W O'Reilly
    Centre for Endocrinology, Diabetes and Metabolism, School of Clinical and Experimental Medicine, University of Birmingham, Edgbaston, Birmingham B15 2TT, UK Electronic address
    J Steroid Biochem Mol Biol 143:277-84. 2014
    ..In particular, AKR1C2 and AKR1C3 are crucial in the regulation of local androgen bioavailability within adipose tissue...
  60. doi Cyclopalladated organosilane-tethered thiosemicarbazones: novel strategies for improving antiplasmodial activity
    Muneebah Adams
    Department of Chemistry, University of Cape Town, Private Bag, Rondebosch 7701, South Africa
    Dalton Trans 45:5514-20. 2016
    ..evaluated for in vitro antiplasmodial activity against the chloroquine-sensitive (NF54) and chloroquine-resistant (Dd2) strains of the human malaria parasite Plasmodium falciparum...
  61. pmc The roles of AKR1C1 and AKR1C2 in ethyl-3,4-dihydroxybenzoate induced esophageal squamous cell carcinoma cell death
    Wei Li
    State Key Laboratory of Molecular Oncology, Cancer Hospital, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, China
    Oncotarget 7:21542-55. 2016
    ....
  62. pmc Highly active ozonides selected against drug resistant malaria
    Lis Lobo
    Universidade Nova de Lisboa, Universidade Nova de Lisboa, Lisboa, Portugal, Universidade Nova de Lisboa, Unidade de Ensino e Investigação de Parasitologia Médica, Global Health and Tropical Medicine, Lisboa, Portugal
    Mem Inst Oswaldo Cruz . 2016
    ..In vitro, LC50 was at least 10 times more efficient inhibiting P. falciparum multidrug resistant Dd2 strain than chloroquine and mefloquine and as efficient as artemisinin (ART), artesunate and dihydroartemisinin...
  63. ncbi Bioisosteric ferrocenyl-containing quinolines with antiplasmodial and antitrichomonal properties
    Muneebah Adams
    Department of Chemistry, University of Cape Town, Rondebosch 7701, Cape Town, South Africa
    Dalton Trans 45:19086-19095. 2016
    ..were screened for their antiplasmodial activity against the chloroquine-sensitive (NF54) and CQ-resistant (Dd2) strains of P. falciparum, as well as for their cytotoxicity against Chinese Hamster Ovarian (CHO) cells...
  64. ncbi Kinetics of allopregnanolone formation catalyzed by human 3 alpha-hydroxysteroid dehydrogenase type III (AKR1C2)
    John W Trauger
    Department of Molecular Neuroscience, Merck Research Laboratories, 3535 General Atomics Court, San Diego, California 92121, USA
    Biochemistry 41:13451-9. 2002
    ..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...
  65. ncbi Human type 3 3alpha-hydroxysteroid dehydrogenase (aldo-keto reductase 1C2) and androgen metabolism in prostate cells
    Tea Lanisnik Rizner
    Department of Pharmacology, University of Pennsylvania School of Medicine, 3620 Hamilton Walk, Philadelphia, PA 19104 6084, USA
    Endocrinology 144:2922-32. 2003
    ..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 ..
  66. ncbi Determination of lipophilic descriptors of antihelmintic 6,7-diaryl-pteridine derivatives useful for bioactivity predictions
    Mario Reta
    Departamento de Quimica, Universidad Nacional de Rio Cuarto, Agencia Postal No 3, 5800 Rio Cuarto, Argentina
    Biomed Chromatogr 17:365-72. 2003
    ..PC.DD2), using acetonitrile-aqueous buffer pH = 7.45 as mobile phase, were obtained...
  67. ncbi Molecular characterization of two monkey dihydrodiol dehydrogenases
    Yu Higaki
    Laboratory of Biochemistry, Gifu Pharmaceutical University, Mitahora Higashi, Japan
    Drug Metab Pharmacokinet 17:348-56. 2002
    ..In addition, no mRNA for an enzyme corresponding to another isoenzyme (AKR1C2) of the human enzyme was detected in livers of the two monkey strains...
  68. pmc Chloroquine-resistant isoforms of the Plasmodium falciparum chloroquine resistance transporter acidify lysosomal pH in HEK293 cells more than chloroquine-sensitive isoforms
    David C Reeves
    Department of Physiology and Biophysics, Albert Einstein College of Medicine of Yeshiva University, 1300 Morris Park Avenue, Bronx, NY 10461, USA
    Mol Biochem Parasitol 150:288-99. 2006
    ..falciparum chloroquine resistance transporter (PfCRT). We expressed chloroquine-sensitive (HB3) and resistant (Dd2) pfcrt alleles in HEK293 human embryonic kidney cells...
  69. ncbi Conformational changes of chicken liver bile acid-binding protein bound to anionic lipid membrane are coupled to the lipid phase transitions
    María Belén Decca
    Centro de Investigaciones en Quimica Biologica de Cordoba, UNC CONICET, Departamento de Quimica Biologica, Facultad de Ciencias Quimicas, Universidad Nacional de Cordoba, Ciudad Universitaria, Cordoba, Republica Argentina
    Biochim Biophys Acta 1768:1583-91. 2007
    Chicken liver bile acid-binding protein (L-BABP) binds to anionic lipid membranes by electrostatic interactions and acquires a partly folded state [Nolan, V., Perduca, M., Monaco, H., Maggio, B. and Montich, G. G. (2003) Biochim. Biophys...
  70. ncbi Short report: polymorphisms in the pfcrt and pfmdr1 genes of Plasmodium falciparum and in vitro susceptibility to amodiaquine and desethylamodiaquine
    Diego F Echeverry
    International Center for Medical Research and Training CIDEIM, Cali, Valle, Colombia
    Am J Trop Med Hyg 77:1034-8. 2007
    ..The lowest susceptibility found to amodiaquine was observed in an isolate carrying a pfcrt and pfmdr1 Dd2-like haplotype, whereas a pfcrt haplotype related to the 7G8 Brazilian strain was found in a Colombian isolate with ..
  71. doi The MYB98 subcircuit of the synergid gene regulatory network includes genes directly and indirectly regulated by MYB98
    Jayson A Punwani
    Department of Biology, University of Utah, 257 South 1400 East, Salt Lake City, UT 84112 0840, USA
    Plant J 55:406-14. 2008
    ..We also show that five of the CRP810 genes, which include DD2, lack a functional GTAACNT element, suggesting that they are not directly regulated by MYB98...
  72. ncbi [Multiplex PCR for analysis of the Plasmodium falciparum drug resistance molecular markers]
    Guo Qing Zhang
    National Institute of Parasitic Diseases, Chinese Center for Disease Control and Prevention, Shanghai 200025, China
    Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi 25:451-6. 2007
    ..To develop a multiplex PCR protocol for amplification of five Plasmodium falciparum drug resistance related genes, thereby facilitate the rapid and high throughput analysis of the drug resistance molecular markers...
  73. doi Antimalarial activity of natural product extracts from Papua New Guinean and Australian plants against Plasmodium falciparum
    Liza S Fernandez
    Discovery Biology, Eskitis Institute for Cell and Molecular Therapies, Griffith University, Brisbane, Australia
    Phytother Res 22:1409-12. 2008
    ..and Australia was screened for in vitro activity against the chloroquine-sensitive 3D7 and chloroquine-resistant Dd2 strains of Plasmodium falciparum...
  74. pmc Comprehensive study of proteasome inhibitors against Plasmodium falciparum laboratory strains and field isolates from Gabon
    Andrea Kreidenweiss
    Medical Research Unit, Albert Schweitzer Hospital, BP118 Lambaréné, Gabon
    Malar J 7:187. 2008
    ..falciparum. Subsequently, a selection of inhibitors was tested in field isolates from Lambaréné, Gabon...
  75. pmc Type 5 17beta-hydroxysteroid dehydrogenase/prostaglandin F synthase (AKR1C3): role in breast cancer and inhibition by non-steroidal anti-inflammatory drug analogs
    Michael C Byrns
    Department of Pharmacology, Center of Excellence in Environmental Toxicology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6084, United States
    Chem Biol Interact 178:221-7. 2009
    ..exploits the selective inhibition of AKR1C3 by indomethacin, which did not inhibit highly related AKR1C1 or AKR1C2. Using known structure-activity relationships for the inhibition of PGHS-1 and PGHS-2 by indole acetic acids we ..
  76. pmc New Insight in Loss of Gut Barrier during Major Non-Abdominal Surgery
    Joep P M Derikx
    Department of Surgery, University Hospital Maastricht and Nutrition and Toxicology Research Institute NUTRIM, Maastricht University, Maastricht, The Netherlands
    PLoS ONE 3:e3954. 2008
    ..Gut barrier loss has been implicated as a critical event in the occurrence of postoperative complications. We aimed to study the development of gut barrier loss in patients undergoing major non-abdominal surgery...
  77. doi Performance of a novel keratinocyte-based reporter cell line to screen skin sensitizers in vitro
    Roger Emter
    Givaudan Schweiz AG, Ueberlandstrasse 138, CH 8600 Duebendorf, Switzerland
    Toxicol Appl Pharmacol 245:281-90. 2010
    ..To this end, a luciferase reporter gene under control of a single copy of the ARE-element of the human AKR1C2 gene was stably inserted into HaCaT keratinocytes...
  78. doi Naturally occurring variants of human aldo-keto reductases with reduced in vitro metabolism of daunorubicin and doxorubicin
    Onkar S Bains
    Division of Pharmaceutics and Biopharmaceutics, Faculty of Pharmaceutical Sciences, University of British Columbia, Vancouver, British Columbia, Canada
    J Pharmacol Exp Ther 335:533-45. 2010
    ..These findings suggest that ns-SNPs in human AKR1C3, AKR1C4, and AKR7A2 significantly decrease the in vitro metabolism of DOX and DAUN...
  79. pmc AKR1C3 as a target in castrate resistant prostate cancer
    Adegoke O Adeniji
    Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104 6061, USA
    J Steroid Biochem Mol Biol 137:136-49. 2013
    ..inhibition of AKR1C3 will be important, however, due to the presence of closely related isoforms, AKR1C1 and AKR1C2 that are also involved in androgen inactivation...
  80. doi NMR investigation of the equilibrium partitioning of a water-soluble bile salt protein carrier to phospholipid vesicles
    Alberto Ceccon
    Department of Biotechnology, University of Verona, 37134, Verona, Italy
    Proteins 81:1776-91. 2013
    ..We applied NMR spectroscopy to study the partitioning of a water-soluble bile acid binding protein (BABP), belonging to the FABP family, between its free and lipid-vesicle-bound states...
  81. doi Antimalarial activity of compounds comprising a primary benzene sulfonamide fragment
    Katherine T Andrews
    Eskitis Institute for Drug Discovery, Griffith University, Don Young Road, Nathan, Queensland 4111, Australia Queensland Institute of Medical Research, Herston, Queensland 4029, Australia Electronic address
    Bioorg Med Chem Lett 23:6114-7. 2013
    ..We report the in vitro activity against Plasmodium falciparum drug sensitive (3D7) and resistant (Dd2) parasites for a panel of fourteen primary benzene sulfonamide compounds...
  82. pmc A process similar to autophagy is associated with cytocidal chloroquine resistance in Plasmodium falciparum
    David Gaviria
    Departments of Chemistry and of Biochemistry, Cellular and Molecular Biology, Georgetown University, Washington, District of Columbia, United States of America
    PLoS ONE 8:e79059. 2013
    ..loci (QTL) analysis of the progeny of a chloroquine sensitive (CQS; strain HB3)×chloroquine resistant (CQR; strain Dd2) genetic cross identifies distinct genetic architectures for CQR(CS) vs CQR(CC) phenotypes, including ..
  83. pmc Transcriptome-Wide Expression Profiling in Skin Fibroblasts of Patients with Joint Hypermobility Syndrome/Ehlers-Danlos Syndrome Hypermobility Type
    Nicola Chiarelli
    Department of Molecular and Translational Medicine, Division of Biology and Genetics, University of Brescia, Bres6cia, Italy
    PLoS ONE 11:e0161347. 2016
    ..g., CFD, AQP9, COLEC12, KCNQ5, PRLR), and essential for redox balance (e.g., ADH1C, AKR1C2, AKR1C3, MAOB, GSTM5)...
  84. pmc Furoquinoline Alkaloids and Methoxyflavones from the Stem Bark of Melicope madagascariensis (Baker) T.G. Hartley
    Vincent E Rasamison
    Centre National d Application de Recherches Pharmaceutiques, B P 702, 101, Antananarivo, Madagascar
    Nat Prod Bioprospect 6:261-265. 2016
    ..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...
  85. pmc Pre-receptor regulation of the androgen receptor
    Trevor M Penning
    Center of Excellence in Environmental Toxicology, Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia 19104 6084, USA
    Mol Cell Endocrinol 281:1-8. 2008
    ..Together these enzymes are involved in the pre-receptor regulation of androgen action. Inhibition of AKR1C2 would be desirable in cases of androgen insufficiency and inhibition of RL-HSD might be desirable in benign ..
  86. ncbi Spectrum of dentin dysplasia in a family: case report and literature review
    W K Seow
    University of Queensland Dental School, Brisbane, Australia
    Pediatr Dent 16:437-42. 1994
    The dentin dysplasias (DD), which may be classified as type 1 (DD1) or type 2 (DD2), form a group of rare, inherited dentin abnormalities that are clinically distinct from dentinogenesis imperfecta...
  87. ncbi Molecular cloning of human type 3 3 alpha-hydroxysteroid dehydrogenase that differs from 20 alpha-hydroxysteroid dehydrogenase by seven amino acids
    I Dufort
    Medical Research Council Group in Molecular Endocrinology, CHUL Research Center, Quebec, Canada
    Biochem Biophys Res Commun 228:474-9. 1996
    ..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...
  88. pmc Regulation of expression of human intestinal bile acid-binding protein in Caco-2 cells
    T Kanda
    Department of Surgery, Niigata University School of Medicine, 1 757 Asahimachi dori, Niigata 951, Japan
    Biochem J 330:261-5. 1998
    ..We examined whether bile acids affect human enterocyte gene expression of intestinal bile acid-binding protein (I-BABP), a component of this transport system...
  89. ncbi Cloning of genes by mRNA differential display induced during the hypersensitive reaction of soybean after inoculation with Pseudomonas syringae pv. glycinea
    K Seehaus
    Universitat Kaiserslautern, FB Biologie, Kaiserslautern, Germany
    Plant Mol Biol 38:1225-34. 1998
    ..Database searches revealed that the fragment DD1 encodes chalcone isomerase and DD2 was identified as ubiquitin. The fragment DD3 shares significant homology to the signalling molecule 14-3-3...
  90. ncbi Chloroquine resistance in Plasmodium falciparum and polymorphism of the CG2 gene
    L K Basco
    Institut de Recherche pour le Developpement, Laboratoire de Recherche sur le Paludisme, Laboratoire Associé Francophone 302, Organisation de Coordination pour la Lutte Contre les Endemies en Afrique Centrale, Yaounde, Cameroon
    J Infect Dis 180:1979-86. 1999
    A distinct genotype (designated Dd2-type profile) consisting of 12 point mutations and 3 repetitive regions of the CG2 gene, a candidate gene for chloroquine resistance, has been associated with in vitro resistance in laboratory-adapted ..
  91. pmc Human 3alpha-hydroxysteroid dehydrogenase isoforms (AKR1C1-AKR1C4) of the aldo-keto reductase superfamily: functional plasticity and tissue distribution reveals roles in the inactivation and formation of male and female sex hormones
    T M Penning
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6084, USA
    Biochem J 351:67-77. 2000
    ..The enzymes correspond to type 1 3alpha-HSD (AKR1C4), type 2 3alpha(17beta)-HSD (AKR1C3), type 3 3alpha-HSD (AKR1C2) and 20alpha(3alpha)-HSD (AKR1C1), and share at least 84% amino acid sequence identity...
  92. ncbi Photophysical process of hexadecyl 4-biphenylamino benzoate
    Z Chen
    Department of Chemistry, Shanxi University, Taiyuan, PR China
    Spectrochim Acta A Mol Biomol Spectrosc 57:419-22. 2001
    The photophysical properties of hexadecyl 4-biphenylamino benzoate (HBAB), the molecule of which possesses a polar end composed of donor (triphenylamino group) and acceptor (ester group) and a long non-polar alkyl tail, have been ..
  93. ncbi Cloning and expression of cDNA encoding hamster liver 3-hydroxyhexobarbital/17beta(3alpha)-hydroxysteroid dehydrogenase 1
    R Takenoshita
    Faculty of Pharmaceutical Sciences, Fukuoka University, 8 19 1 Nanakuma, Jonan ku, 814 0180, Fukuoka, Japan
    Chem Biol Interact 130:863-70. 2001
    ..and 74-76% identity to human liver bile acid binding protein/3alpha-hydroxysteroid dehydrogenase (DD2), human liver 3alpha-hydroxysteroid dehydrogenase type I (DD4) and type II (DD3), and rabbit ovary 20alpha-..
  94. ncbi The human kidney is a progesterone-metabolizing and androgen-producing organ
    M Quinkler
    Department of Endocrinology, Klinikum Benjamin Franklin, Free University, 12200 Berlin, Germany
    J Clin Endocrinol Metab 88:2803-9. 2003
    ..analysis demonstrated the expression of 5 alpha-reductase type 1, 5 beta-reductase, aldo-keto-reductase (AKR) 1C1, AKR1C2, AKR1C3, 3 beta-hydroxysteroid dehydrogenase (3 beta-HSD) type 2, and 17 alpha-hydroxylase/17,20-lyase (P450c17)...
  95. ncbi Structure-function relationships in 3alpha-hydroxysteroid dehydrogenases: a comparison of the rat and human isoforms
    Trevor M Penning
    Department of Pharmacology, School of Medicine, University of Pennsylvania, 3620 Hamilton Walk, Philadelphia, PA 19104, USA
    J Steroid Biochem Mol Biol 85:247-55. 2003
    ..The X-ray crystal structures of AKR1C9 and AKR1C2 (human type 3 3alpha-HSD, bile acid binding protein and peripheral 3alpha-HSD) reveal that the AKR1C2 structure ..
  96. ncbi Simultaneous measurements of blood pressures in right and left brachial arteries
    Gad Mendelson
    Shoham Geriatrics Center, Pardes Hanna, Israel
    Cardiol Rev 12:276-8. 2004
    ..and 171 men, mean age 79 +/- 10 years, 2 geriatricians simultaneously measured brachial artery blood pressure (BABP) with the patient in the sitting position...
  97. ncbi Carbonyl reduction of naltrexone and dolasetron by oxidoreductases isolated from human liver cytosol
    U Breyer-Pfaff
    Institut fur Pharmakologie und Toxikologie, Abteilung Toxikologie, Eberhard Karls Universitat Tubingen, Wilhelmstrasse 56, 72074 Tubingen, Germany
    J Pharm Pharmacol 56:1601-6. 2004
    ..AKR1C1, AKR1C2, and AKR1C4 were able to reduce both substrates...
  98. ncbi Chicken liver bile acid-binding protein is in a compact partly folded state at acidic pH. Its relevance to the interaction with lipid membranes
    Verónica Nolan
    Departamento de Quimica Biologica, Facultad de Ciencias Quimicas, Universidad Nacional de Córdoba CIQUIBIC CONICET Pabellón Argentina, Ciudad Universitaria 5000 Córdoba, Argentina
    Biochemistry 44:8486-93. 2005
    ..the far- and near-UV, Fourier transform infrared spectroscopy, and size-exclusion chromatography, we found that L-BABP was partly unfolded at pH 2.5 and low ionic strength, retaining some of its secondary structure. Addition of 0...
  99. pmc Disruption of a Plasmodium falciparum gene linked to male sexual development causes early arrest in gametocytogenesis
    Tetsuya Furuya
    Laboratory of Malaria and Vector Research, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, MD 20892 8132, USA
    Proc Natl Acad Sci U S A 102:16813-8. 2005
    A male gametocyte defect in the Plasmodium falciparum Dd2 parasite was previously discovered through the observation that all progeny clones in a Dd2 x HB3 genetic cross were the result of fertilization events between Dd2 female and HB3 ..
  100. ncbi 1,25-dihydroxyvitamin D3 and its receptor inhibit the chenodeoxycholic acid-dependent transactivation by farnesoid X receptor
    Yumiko Honjo
    Second Division, Department of Internal Medicine, Hamamatsu University School of Medicine, 1 20 1 Handayama, Hamamatsu, Shizuoka 431 3192, Japan
    J Endocrinol 188:635-43. 2006
    ..the natural promoter for the small heterodimer partner (SHP), bile salt export pump (BSEP), and ileum bile acid (I-BABP) gene...
  101. ncbi Relationship between immobilized artificial membrane chromatographic retention and human oral absorption of structurally diverse drugs
    Jignesh Kotecha
    Department of Quality Assurance, L M College of Pharmacy, P O Box 4011, Navrangpura, Ahmedabad 380009, India
    Int J Pharm 333:127-35. 2007
    ..The retention (capacity factor, k'(IAM) of each drug was measured by reverse phase HPLC using an IAM.PC.DD2 (1 cm x 3 mm i.d., 12 microm) column with an eluent of acetonitrile - 0.01 M phosphate buffer at pH 4.5-7.4...

Research Grants9

  1. Amy E Wright; Fiscal Year: 2014
    ..resulting in the identification of 165 fractions from 85 organisms that reproducibly inhibit the drug resistant Dd2 strain of Plasmodium falciparum at concentrations lower than 5 [unreadable]g/mL...
  2. Development of a Chloroquine Replacement Drug
    MICHAEL KEVIN RISCOE; Fiscal Year: 2010
    ..g., D6, Dd2, 7G8 and Tm90-C2B. PH128 is active by oral means of administration in P. berghei and P...
  3. ANTIMALARIAL ACTION AND RESISTANCE
    Donald Krogstad; Fiscal Year: 1991
    ..To accomplish this, a genomic DNA library from the resistant Dd2 parent strain will be hybridized to DNA from the resistant progeny...
  4. INTRACELLULAR TRANSPORT OF AMPHIPATHS
    Bruce Luxon; Fiscal Year: 2000
    ..by co-diffusion with soluble binding proteins like fatty acid binding protein (FABP) or bile acid binding protein (BABP)...
  5. Dihydrodiol dehydrogenase mediates cisplatin resistance
    Henry Simpkins; Fiscal Year: 2007
    ..Analysis of a human lung squamous cell carcinoma cell line (A549) which has a very high levels of endogenous DDH2 mRNA exhibited a degree of cisplatin resistance greater than that of the 2008/C13* cell line...
  6. Breast cancer and HRT: genetic susceptibility within th*
    Kathleen Malone; Fiscal Year: 2006
    ..polymorphisms (SNPs) and tagSNPs in the PGR gene, and the following progesterone metabolizing genes, AKR1C1, AKR1C2, AKR1C3, SRD5A1, SRD5A2, and the CYP3A4 gene...
  7. Symposium on Aldo-Keto Reductases & Toxicant Metabolism
    TREVOR PENNING; Fiscal Year: 2002
    ..abstract_text> ..
  8. Molecular Mechanisms of Multistage Carcinogenesis
    TREVOR PENNING; Fiscal Year: 2006
    ..By studying the discrete molecular events responsible for the causation of cancer this Program may lead to the early prevention and intervention of this disease. ..
  9. Novel Anti-Malarials by Combinatorial Pharmacogenomics
    Joseph DeRisi; Fiscal Year: 2006
    ..The compiled relationships from known anti-malarials, novel quinolines, and toxicology will then be used to guide and optimize additional synthesis efforts toward the ultimate goal of producing effective therapeutics. ..