Structure-function aspects and inhibitor design of type 5 17²-hydroxysteroid dehydrogenase (AKR1C3)

Molecular and Cellular Endocrinology

Volumn 171, Issue 1-2, 2001, Pages 137-149

  Penning, Trevor M ^a   Burczynski, Michael E ^a   Jez, Joseph M ^a,b   Lin, Hseuh Kung ^a,c   Ma, Haiching ^a,d   Moore, Margaret ^a   Ratnam, Kapila ^a,e   Palackal, Nisha ^a  

^a UNIVERSITY OF PENNSYLVANIA   (United States)

^b SALK INSTITUTE FOR BIOLOGICAL STUDIES   (United States)

^c WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

^d UNIVERSITY OF PENNSYLVANIA   (United States)

^e Department of Infectious Disease ^*  (United States)

Author keywords

17 hydroxysteroid dehydrogenase; Aldo keto reductase; Inhibitors; Steroid hormones

Indexed keywords

20ALPHA DIHYDROPROGESTERONE; 3ALPHA HYDROXYSTEROID DEHYDROGENASE; 3ALPHA HYDROXYSTEROID DEHYDROGENASE 2; ALDO KETO REDUCTASE; ANDROSTANEDIOL; ANDROSTANOLONE; DELTA4 ANDROSTENE 3,17 DIONE; ESTRADIOL; ESTRONE; ETHYLENE OXIDE DERIVATIVE; ISOENZYME; OXIDOREDUCTASE; PROGESTERONE; PYRAZOLE DERIVATIVE; RECOMBINANT ENZYME; SPIRO COMPOUND; STEROID; STEROID CARBOXYLATE; STEROID HORMONE; TESTOSTERONE 17BETA DEHYDROGENASE; TESTOSTERONE 17BETA DEHYDROGENASE 5; TESTOSTERONE 17BETA DEHYDROGENASE INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; BINDING COMPETITION; BREAST CANCER; CATALYSIS; CONTROLLED STUDY; DRUG DESIGN; DRUG MECHANISM; ENZYME INHIBITION; ENZYME KINETICS; ENZYME SUBSTRATE; ESCHERICHIA COLI; HUMAN; MAMMARY GLAND; MOLECULAR CLONING; NONHUMAN; OXIDATION; PRIORITY JOURNAL; PROSTATE; PROSTATE CANCER; PROTEIN EXPRESSION; PROTEIN FAMILY; REDUCTION; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; STEROID METABOLISM; STRUCTURE ACTIVITY RELATION;

17-HYDROXYSTEROID DEHYDROGENASES; 20-ALPHA-DIHYDROPROGESTERONE; 3-ALPHA-HYDROXYSTEROID DEHYDROGENASE (B-SPECIFIC); 3-HYDROXYSTEROID DEHYDROGENASES; ANIMALS; BINDING SITES; BREAST NEOPLASMS; CLONING, MOLECULAR; ENZYME INHIBITORS; ESCHERICHIA COLI; ESTRADIOL; ESTRONE; FEMALE; GENE EXPRESSION; GENE LIBRARY; HUMANS; ISOENZYMES; LIVER; MALE; MAMMARY GLANDS, ANIMAL; MUTAGENESIS, SITE-DIRECTED; PROGESTERONE; PROSTATE; PROSTATIC NEOPLASMS; RATS; RECOMBINANT PROTEINS; REVERSE TRANSCRIPTASE POLYMERASE CHAIN REACTION; STRUCTURE-ACTIVITY RELATIONSHIP; TISSUE DISTRIBUTION; UTERUS;

EID: 0035931291     PISSN: 03037207     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0303-7207(00)00426-3     Document Type: Article

References (30)

1. 17β-hydroxysteroid dehydrogenase: Isozymes and mutations
2. The kinetic mechanism catalyzed by homogeneous rat liver 3α-hydroxysteroid dehydrogenase. Evidence for binary and ternary dead-end complexes containing non-steroidal anti-inflammatory drugs
3. +
4. + bound to 3α-hydroxysteroid/dihydrodiol dehydrogenase
5. Detection of a transient enzyme-steroid complex during active site-directed irreversible inhibition of 3-oxo-Δ-5-steroid isomerase
6. Expression and characterization of four recombinant human dihydrodiol dehydrogenase isoforms: Oxidation of trans-7, 8-dihydroxy-7, 8-dihydrobenzo[a]pyrene to the activated o-quinone metabolite benzo[a]pyrene-7, 8-dione
7. Molecular cloning of two human liver 3α-hydroxysteroid/dihydrodiol dehydrogenase isoenzymes that are identical with chlordecone reductase and bile-acid binder
8. Characteristics of a highly labile human type 5 17β-hydroxysteroid dehydrogenase
9. Localization of type 5 17β-hydroxysteroid dehydrogenase, 3β-hydroxysteroid dehydrogenase and androgen receptor in the human prostate by in situ hybridization and immunocytochemistry
10. Relationship of human liver dihydrodiol dehydrogenases to hepatic bile acid-binding protein and an oxidoreductase of human colon cells
11. Three dimensional structure of rat liver 3α-hydroxysteroid/dihydrodiol dehydrogenase: A member of the aldo-keto reductase superfamily
12. Comparitive anatomy of the aldo-keto reductase superfamily
13. Substrate specificity, gene structure, and tissue-specific distribution of multiple human 3α-hydroxysteroid dehydrogenases
14. The key role of 17β-hydroxysteroid dehydrogenases in sex steroid biology
15. Inhibition of 3(17)β-hydroxysteroid dehydrogenase from Pseudomonas testosteroni by steroidal A ring fused pyrazoles
16. Expression and characterization of recombinant type 2 3α-hydroxysteroid dehydrogenase (HSD) from human prostate: Demonstration of bifunctional 3α/17β-HSD activity and cellular distribution
17. Characterization of homogeneous recombinant rat ovarian 20α-hydroxysteroid dehydrogenase: Fluorescent properties and inhibition profile
18. Conversion of mammalian 3α-hydroxysteroid dehydrogenase to 20α-hydroxysteroid dehydrogenase using loop chimeras: Changing specificity from androgens to progestins
19. Overexpression and mutagenesis of the cDNA for rat liver 3α-hydroxysteroid/dihydrodiol dehydrogenase. Role of cysteines and tyrosines in catalysis
20. Cloning and sequencing of the cDNA for rat liver 3α-hydroxysteroid/dihydrodiol dehydrogenase
21. Molecular endocrinology of hydroxysteroid dehydrogenases
22. Purification and properties of a 3α-hydroxysteroid dehydrogenase of rat liver cytosol and its inhibition by anti-inflammatory drugs
23. Clues to the development of mechanism-based inactivators of 3α-hydroxysteroid dehydrogenase: Comparison of steroidal and nonsteroidal Michael acceptors and epoxides
24. Human 3α-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
25. Mutagenesis of 3α-hydroxysteroid dehydrogenase reveals a 'push-pull' mechanism for proton transfer in aldo-keto reductases
26. cloning and expression of the human hepatic bile acid-binding protein. A member of the monomeric reductase gene family
27. Stereoselective preparation of deuterated reduced nicotinamide adenine dinucleotides and substrates by enzymatic synthesis
28. Statistical estimations in enzyme kinetics
29. Expression cloning and characterization of human 17β-hydroxysteroid dehydrogenase type 2, a microsomal enzyme possessing 20α-hydroxysterold dehydrogenase activity