95 related articles for article (PubMed ID: 20850205)
1. Structure-based optimization and biological evaluation of human 20α-hydroxysteroid dehydrogenase (AKR1C1) salicylic acid-based inhibitors.
El-Kabbani O; Scammells PJ; Day T; Dhagat U; Endo S; Matsunaga T; Soda M; Hara A
Eur J Med Chem; 2010 Nov; 45(11):5309-17. PubMed ID: 20850205
[TBL] [Abstract][Full Text] [Related]
2. Structure-guided design, synthesis, and evaluation of salicylic acid-based inhibitors targeting a selectivity pocket in the active site of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1).
El-Kabbani O; Scammells PJ; Gosling J; Dhagat U; Endo S; Matsunaga T; Soda M; Hara A
J Med Chem; 2009 May; 52(10):3259-64. PubMed ID: 19397269
[TBL] [Abstract][Full Text] [Related]
3. Probing the inhibitor selectivity pocket of human 20α-hydroxysteroid dehydrogenase (AKR1C1) with X-ray crystallography and site-directed mutagenesis.
El-Kabbani O; Dhagat U; Soda M; Endo S; Matsunaga T; Hara A
Bioorg Med Chem Lett; 2011 Apr; 21(8):2564-7. PubMed ID: 21414777
[TBL] [Abstract][Full Text] [Related]
4. Factorizing the role of a critical leucine residue in the binding of substrate to human 20alpha-hydroxysteroid dehydrogenase (AKR1C1): molecular modeling and kinetic studies of the Leu308Val mutant enzyme.
Dhagat U; Endo S; Soda M; Hara A; El-Kabbani O
Bioorg Med Chem Lett; 2010 Sep; 20(17):5274-6. PubMed ID: 20656485
[TBL] [Abstract][Full Text] [Related]
5. A salicylic acid-based analogue discovered from virtual screening as a potent inhibitor of human 20alpha-hydroxysteroid dehydrogenase.
Dhagat U; Carbone V; Chung RP; Matsunaga T; Endo S; Hara A; El-Kabbani O
Med Chem; 2007 Nov; 3(6):546-50. PubMed ID: 18045204
[TBL] [Abstract][Full Text] [Related]
6. Inhibitors of human 20α-hydroxysteroid dehydrogenase (AKR1C1).
El-Kabbani O; Dhagat U; Hara A
J Steroid Biochem Mol Biol; 2011 May; 125(1-2):105-11. PubMed ID: 21050889
[TBL] [Abstract][Full Text] [Related]
7. Derivatives of pyrimidine, phthalimide and anthranilic acid as inhibitors of human hydroxysteroid dehydrogenase AKR1C1.
Brozic P; Cesar J; Kovac A; Davies M; Johnson AP; Fishwick CW; Lanisnik Rizner T; Gobec S
Chem Biol Interact; 2009 Mar; 178(1-3):158-64. PubMed ID: 19007763
[TBL] [Abstract][Full Text] [Related]
8. Characterization of homogeneous recombinant rat ovarian 20alpha-hydroxysteroid dehydrogenase: fluorescent properties and inhibition profile.
Ma H; Penning TM
Biochem J; 1999 Aug; 341 ( Pt 3)(Pt 3):853-9. PubMed ID: 10417353
[TBL] [Abstract][Full Text] [Related]
9. Progestins as inhibitors of the human 20-ketosteroid reductases, AKR1C1 and AKR1C3.
Beranič N; Gobec S; Rižner TL
Chem Biol Interact; 2011 May; 191(1-3):227-33. PubMed ID: 21182831
[TBL] [Abstract][Full Text] [Related]
10. Selective loss of AKR1C1 and AKR1C2 in breast cancer and their potential effect on progesterone signaling.
Ji Q; Aoyama C; Nien YD; Liu PI; Chen PK; Chang L; Stanczyk FZ; Stolz A
Cancer Res; 2004 Oct; 64(20):7610-7. PubMed ID: 15492289
[TBL] [Abstract][Full Text] [Related]
11. Selective and potent inhibitors of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) that metabolizes neurosteroids derived from progesterone.
Higaki Y; Usami N; Shintani S; Ishikura S; El-Kabbani O; Hara A
Chem Biol Interact; 2003 Feb; 143-144():503-13. PubMed ID: 12604236
[TBL] [Abstract][Full Text] [Related]
12. Phytoestrogens as inhibitors of the human progesterone metabolizing enzyme AKR1C1.
Brozic P; Smuc T; Gobec S; Rizner TL
Mol Cell Endocrinol; 2006 Oct; 259(1-2):30-42. PubMed ID: 16962702
[TBL] [Abstract][Full Text] [Related]
13. Structure of aldehyde reductase in ternary complex with coenzyme and the potent 20alpha-hydroxysteroid dehydrogenase inhibitor 3,5-dichlorosalicylic acid: implications for inhibitor binding and selectivity.
Carbone V; Chung R; Endo S; Hara A; El-Kabbani O
Arch Biochem Biophys; 2008 Nov; 479(1):82-7. PubMed ID: 18782556
[TBL] [Abstract][Full Text] [Related]
14. New cyclopentane derivatives as inhibitors of steroid metabolizing enzymes AKR1C1 and AKR1C3.
Stefane B; Brozic P; Vehovc M; Rizner TL; Gobec S
Eur J Med Chem; 2009 Jun; 44(6):2563-71. PubMed ID: 19237229
[TBL] [Abstract][Full Text] [Related]
15. Selectivity determinants of inhibitor binding to human 20alpha-hydroxysteroid dehydrogenase: crystal structure of the enzyme in ternary complex with coenzyme and the potent inhibitor 3,5-dichlorosalicylic acid.
Dhagat U; Endo S; Sumii R; Hara A; El-Kabbani O
J Med Chem; 2008 Aug; 51(15):4844-8. PubMed ID: 18620380
[TBL] [Abstract][Full Text] [Related]
16. Human 20alpha-hydroxysteroid dehydrogenase: crystallographic and site-directed mutagenesis studies lead to the identification of an alternative binding site for C21-steroids.
Couture JF; Legrand P; Cantin L; Luu-The V; Labrie F; Breton R
J Mol Biol; 2003 Aug; 331(3):593-604. PubMed ID: 12899831
[TBL] [Abstract][Full Text] [Related]
17. Alanine scanning mutagenesis of the testosterone binding site of rat 3 alpha-hydroxysteroid dehydrogenase demonstrates contact residues influence the rate-determining step.
Heredia VV; Cooper WC; Kruger RG; Jin Y; Penning TM
Biochemistry; 2004 May; 43(19):5832-41. PubMed ID: 15134457
[TBL] [Abstract][Full Text] [Related]
18. Design, synthesis and evaluation of caffeic acid phenethyl ester-based inhibitors targeting a selectivity pocket in the active site of human aldo-keto reductase 1B10.
Soda M; Hu D; Endo S; Takemura M; Li J; Wada R; Ifuku S; Zhao HT; El-Kabbani O; Ohta S; Yamamura K; Toyooka N; Hara A; Matsunaga T
Eur J Med Chem; 2012 Feb; 48():321-9. PubMed ID: 22236472
[TBL] [Abstract][Full Text] [Related]
19. Structure-based design, synthesis and in vitro characterization of potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors based on 2-substitutions of estrone and D-homo-estrone.
Möller G; Deluca D; Gege C; Rosinus A; Kowalik D; Peters O; Droescher P; Elger W; Adamski J; Hillisch A
Bioorg Med Chem Lett; 2009 Dec; 19(23):6740-4. PubMed ID: 19836949
[TBL] [Abstract][Full Text] [Related]
20. Structure-activity study in the class of 6-(3'-hydroxyphenyl)naphthalenes leading to an optimization of a pharmacophore model for 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors.
Marchais-Oberwinkler S; Frotscher M; Ziegler E; Werth R; Kruchten P; Messinger J; Thole H; Hartmann RW
Mol Cell Endocrinol; 2009 Mar; 301(1-2):205-11. PubMed ID: 18950679
[TBL] [Abstract][Full Text] [Related]
[Next] [New Search]