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Ligand cortisone

Basic Ligand Information

Molecular Structure

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Roles as Enzyme Ligand

In Vivo Substrate in Enzyme-catalyzed Reactions (9 results)

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Show Natural Substrate (9 entries)

EC NUMBER

LITERATURE

REACTION DIAGRAM

PROVEN IN VIVO REACTION

ENZYME 3D STRUCTURE

1.1.1.146

285967

cortisone + NAD(P)H = cortisol + NAD(P)+

-

1.1.1.146

762494

cortisone + NADH + H+ = cortisol + NAD+

-

1.1.1.146

760685, 740144, 740377, 740915, 739986, 740803, 740917, 740806, 740142, 740155, 740840, 741297, 760868, 760876, 761754, 761758, 762406, 760680, 760682, 761908, 740132, 741066, 761543, 760956, 761665

cortisone + NADPH + H+ = cortisol + NADP+

-

1.1.1.146

654889, 669640, 656133, 654698, 656227, 657396, 668379, 655162, 657253, 655216, 654637, 656356, 670065, 669730, 667835, 668636, 668296, 670253, 670263, 667956, 667962, 668297, 668424, 668505, 669397, 670261, 667148, 670264, 669504

cortisone + NADPH = cortisol + NADP+

-

1.1.1.146

700178

cortisone + NADPH = cortisol + NADP+ + H+

-

1.1.1.146

655218

cortisone + NADPH = cortisole + NADP+

-

1.1.1.146

6 entries

1.1.1.B40

669907

cortisone + NADPH = cortisol + NADP+

-

1.3.1.3

725399

cortisone + NADPH + H+ = 11beta,21dihydroxy-pregnan-3,11,20-trione + NADP+

-

1.3.1.3

705710

cortisone + NADPH + H+ = 17,21-dihydroxy-5beta-pregnane-3,11,20-trione + NADP+

-

1.3.1.3

2 entries

In Vivo Product in Enzyme-catalyzed Reactions (6 results)

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Show Natural Product (6 entries)

EC NUMBER

LITERATURE

REACTION DIAGRAM

PROVEN IN VIVO REACTION

ENZYME 3D STRUCTURE

1.1.1.146

-

cortisol + NAD+ = cortisone + NADH

-

1.1.1.146

-

cortisol + NAD+ = cortisone + NADH + H+

-

1.1.1.146

-

cortisol + NADP+ = cortisone + NADPH

-

1.1.1.146

-

cortisol + NADP+ = cortisone + NADPH + H+

-

1.1.1.B40

-

cortisol + beta-NAD+ = cortisone + beta-NADH

-

1.1.1.B40

-

cortisol + NAD+ = cortisone + NADH

-

1.1.1.146

4 entries

1.1.1.B40

2 entries

Substrate in Enzyme-catalyzed Reactions (24 results)

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Show Substrate (24 entries)

EC NUMBER

LITERATURE

REACTION DIAGRAM

REACTION

ENZYME 3D STRUCTURE

1.1.1.146

285967

cortisone + NAD(P)H = cortisol + NAD(P)+

-

1.1.1.146

762494

cortisone + NADH + H+ = cortisol + NAD+

-

1.1.1.146

691282, 710841, 711387, 711399, 711632, 711737, 711800, 712257, 713012, 713232, 740144, 740377, 740915, 691258, 691263, 691275, 691279, 691281, 691284, 693550, 711377, 711383, 711951, 739986, 740803, 740917, 740806, 710777, 711471, 711752, 711907, 740142, 740155, 740840, 741248, 741297, 760685, 760868, 760876, 761754, 761758, 762406, 760680, 760682, 761908, 740132, 741066, 761543, 760956, 761665

cortisone + NADPH + H+ = cortisol + NADP+

-

1.1.1.146

656133, 691282, 697498, 697563, 697625, 699469, 691281, 655218, 670065, 690401, 698167, 654637, 654698, 656227, 657253, 657396, 692338, 693544, 696736, 668379, 655162, 655216, 656356, 669730, 667835, 668296, 668636, 669640, 669504, 670261, 670253, 670263, 667956, 667962, 668297, 668424, 668505, 669397, 667673, 667148, 670264, 697737, 698026, 691275, 654889

cortisone + NADPH = cortisol + NADP+

-

1.1.1.146

700178

cortisone + NADPH = cortisol + NADP+ + H+

-

1.1.1.146

655218

cortisone + NADPH = cortisole + NADP+

-

1.1.1.146

6 entries

1.1.1.149

285979, 285994

cortisone + NADH = ? + NAD+

-

1.1.1.201

656659

cortisone + NADP+ = ? + NADPH

-

1.1.1.53

287101, 287085, 287093, 287100, 287087, 287090, 287094

cortisone + NAD(P)H = 17alpha,20beta,21-trihydroxy-pregn-4-ene-3,11-dione + NAD(P)+

-

1.1.1.53

725963

cortisone + NADPH + H+ = 20beta-hydroxycortisone + NADP+

-

1.1.1.B40

743434

cortisone + beta-NADPH = cortisol + beta-NADP+

-

1.1.1.B40

669907

cortisone + NADPH = cortisol + NADP+

-

1.1.1.53

2 entries

1.1.1.B40

2 entries

1.14.13.54

7390

Cortisone + NADPH + O2 = ?

-

1.14.15.8

744148

cortisone + reduced adrenodoxin + O2 = 15beta-hydroxycortisone + oxidized adrenodoxin + H2O

-

1.3.1.22

390765

17alpha,21-dihydroxypregn-4-ene-3,11,20-trione + NADPH = 17alpha,21-dihydroxy-5alpha-pregnan-3,11,20-trione + NADP+

-

1.3.1.3

725399

cortisone + NADPH + H+ = 11beta,21dihydroxy-pregnan-3,11,20-trione + NADP+

-

1.3.1.3

705710

cortisone + NADPH + H+ = 17,21-dihydroxy-5beta-pregnane-3,11,20-trione + NADP+

-

1.3.1.3

726492

cortisone + NADPH + H+ = ?

-

1.3.1.3

390646, 390647, 390590

cortisone + NADPH = 11beta,21dihydroxy-pregnan-3,11,20-trione + NADP+

-

1.3.1.3

687723

cortisone + NADPH = 5beta-17,21dihydroxy-pregnan-3,11,20-trione + NADP+

-

1.3.1.3

390591, 390594, 390595

cortisone + NADPH = ?

-

1.3.1.3

6 entries

1.3.99.4

391392, 391375

cortisone + acceptor = 1,4-pregnene-17alpha,21-diol-3,11,20-trione + reduced acceptor

-

2.8.2.15

760621

3'-phosphoadenylyl sulfate + cortisone = adenosine 3',5'-bisphosphate + ?

-

2.8.2.2

645774

3'-phosphoadenylylsulfate + cortisone = adenosine 3',5'-bisphosphate + cortisone sulfate

-

Product in Enzyme-catalyzed Reactions (12 results)

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Show Product (12 entries)

EC NUMBER

LITERATURE

REACTION DIAGRAM

REACTION

ENZYME 3D STRUCTURE

1.1.1.146

-

11-dehydrocorticosterone + NADPH + H+ = cortisone + NADP+

-

1.1.1.146

-

corticosterone + NAD+ = cortisone + NADH + H+

-

1.1.1.146

-

cortisol + NAD+ = cortisone + NADH

-

1.1.1.146

-

cortisol + NAD+ = cortisone + NADH + H+

-

1.1.1.146

-

cortisol + NADP+ = cortisone + NADPH

-

1.1.1.146

-

cortisol + NADP+ = cortisone + NADPH + H+

-

1.1.1.146

6 entries

1.1.1.151

286004

17alpha-hydroxy-pregn-4-ene-3,11,20,21-tetraone + NADPH = 17alpha,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADP+

-

1.1.1.B40

-

cortisol + beta-NAD+ = cortisone + beta-NADH

-

1.1.1.B40

-

cortisol + NAD+ = cortisone + NADH

-

1.1.1.B40

-

cortisol + NAD+ = cortisone + NADH + H+

-

1.1.1.B40

3 entries

1.14.15.4

285398

cortisol + reduced adrenal ferredoxin + O2 = cortisone + oxidized adrenal ferredoxin + H2O

-

3.1.6.2

-

cortisone 21-sulfate + H2O = cortisone + sulfate

-

Activator in Enzyme-catalyzed Reactions (3 results)

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Show Activating Compound (3 entries)

COMMENTARY

EC NUMBER

LITERATURE

ENZYME 3D STRUCTURE

5fold activation

1.1.1.141

285931

-

subcutaneously

1.13.11.52

666138

-

administration of cortisone to 8-day-old pups augments lactase activity

3.2.1.108

683869

-

3 entries

Inhibitor in Enzyme-catalyzed Reactions (6 results)

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Show Inhibitors (6 entries)

COMMENTARY

EC NUMBER

LITERATURE

ENZYME 3D STRUCTURE

i.e. cortisone

1.1.1.21

695881

-

competitive

1.1.1.213

347982

-

-

1.1.1.50

389527

-

-

1.3.1.42

678118

-

-

2.8.2.15

645722

-

-

3 entries

cortisol as substrate, weak, 0.012 mM

2.8.2.18

645769

-

Enzyme Kinetic Parameters

k_cat Value (Turnover Number) (10 results)

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Show Turnover Number (10 entries)

COMMENTARY

EC NUMBER

LITERATURE

TURNOVER NUMBER [1/S]

TURNOVER NUMBER MAXIMUM [1/S]

37°C, pH 7.4, recombinant 11beta-HSD1 expressed in Escherichia coli

1.1.1.146

656133

0.3

-

37°C, pH 7.4, recombinant 11beta-HSD1 expressed in Escherichia coli

1.1.1.146

656133

0.4

-

37°C, pH 7.4, recombinant 11beta-HSD1 expressed in Escherichia coli

2 entries

NADH

1.1.1.53

287087

0.333

-

-

1.3.1.3

390591

0.0375

-

mutant P133R, pH not specified in the publication, temperature not specified in the publication

1.3.1.3

725399

0.01

-

pH 6.0, 37°C

1.3.1.3

726492

0.195

-

pH 6.0, 37°C, mutant P133R

1.3.1.3

725399

0.01

-

pH 6.0, 37°C, wild-type enzyme

1.3.1.3

725399

0.165

-

wild-type, pH not specified in the publication, temperature not specified in the publication

1.3.1.3

725399

0.17

-

pH 7.5, 37°C cosubstrate ethanol

2.8.2.2

645774

0.15

-

K_M Value (37 results)

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Show KM Value (37 entries)

COMMENTARY

EC NUMBER

KM VALUE [MM]

KM VALUE MAXIMUM [MM]

LITERATURE

pH 7.4, 28°C

1.1.1.146

0.0044

-

695146

at pH 7.5 and 37°C

1.1.1.146

0.193

-

761908

37°C, pH 7.4, V149R mutant 11beta-HSD1, V149E mutant 11beta-HSD1, and N-terminal 15 amino acid truncated V149R and V149E mutant 11beta-HSD1

1.1.1.146

0.1

-

654698

37°C, pH 7.4, reduction of cortisone in intact HEK-293 cells transfected with 11beta-HSD1

1.1.1.146

0.0008

-

656227

37°C, pH 7.4, reduction of cortisone by lysates of HEK-293 cells transfected with 11beta-HSD1

1.1.1.146

0.00034

-

656227

37°C, pH 7.4, recombinant 11beta-HSD1 measured in intact COS cells transfected with 11beta-HSD1

1.1.1.146

0.0003

-

656133

37°C, pH 7.4, recombinant 11beta-HSD1 measured in intact COS cells transfected with 11beta-HSD1

1.1.1.146

0.00028

-

656133

37°C, pH 7.4, recombinant 11beta-HSD1 measured in extracts of COS cells transfected with 11beta-HSD1

1.1.1.146

0.009

-

656133

37°C, pH 7.4, recombinant 11beta-HSD1 measured in extracts of COS cells transfected with 11beta-HSD1

1.1.1.146

0.008

-

656133

37°C, pH 7.4, recombinant 11beta-HSD1 measured in intact COS cells transfected with 11beta-HSD1

2 entries

37°C, pH 7.4, recombinant 11beta-HSD1 measured in extracts of COS cells transfected with 11beta-HSD1

2 entries

37°C, pH 7.4, recombinant 11beta-HSD1 expressed in Pichia pastoris

1.1.1.146

0.002

-

656133

37°C, pH 7.4, recombinant 11beta-HSD1 expressed in Escherichia coli

1.1.1.146

0.0008

-

656133

37°C, pH 7.4, recombinant 11beta-HSD1 expressed in Escherichia coli

1.1.1.146

0.0006

-

656133

37°C, pH 7.4, recombinant 11beta-HSD1 expressed in Escherichia coli

2 entries

37°C, pH 7.4, recombinant 11beta-HSD1

1.1.1.146

0.0006

-

657253

37°C, pH 7.4, Hill coefficient of 1.6

1.1.1.146

0.014

-

654637

kidney enzyme, pH 7.4, 37°C

1.1.1.146

0.0008

-

654889

liver enzyme, pH 7.4, 37°C

1.1.1.146

0.01

-

654889

NADH, pH 6.3

1.1.1.149

0.022

-

285979

pH 7.3, 28°C

1.1.1.53

0.142

-

725963

-

1.1.1.53

0.318

-

287090

immobilized enzyme

1.1.1.53

0.085

0.098

287087, 287085

free enzyme

1.1.1.53

0.042

0.048

287087, 287085

-

1.1.1.53

0.024

-

287093

pH 7.4, 37°C, recombinant isozyme 11beta-HSD1

1.1.1.B40

0.00157

-

669907

pH 7.4, 37°C, recombinant isozyme 11beta-HSD1

1.1.1.B40

0.00136

-

669907

pH 7.4, 37°C, recombinant isozyme 11beta-HSD1

1.1.1.B40

0.00064

-

669907

pH 7.4, 37°C, recombinant isozyme 11beta-HSD1

1.1.1.B40

0.00057

-

669907

pH 7.4, 37°C, recombinant isozyme 11beta-HSD1

1.1.1.B40

0.00052

-

669907

pH 7.4, 37°C, recombinant isozyme 11beta-HSD1

5 entries

-

1.3.1.22

0.14

-

390765

wild-type, pH not specified in the publication, temperature not specified in the publication

1.3.1.3

0.0151

-

725399

pH 6.0, 37°C, wild-type enzyme

1.3.1.3

0.0151

-

725399

pH 6.0, 37°C, mutant P133R

1.3.1.3

0.0013

-

725399

pH 6.0, 37°C

1.3.1.3

0.0151

-

726492

-

1.3.1.3

0.0015

-

390590

mutant P133R, pH not specified in the publication, temperature not specified in the publication

1.3.1.3

0.0013

-

725399

-

1.3.1.3

0.0217

-

390591

-

1.3.1.3

0.034

-

390647

-

2 entries

i.e. 4-pregnene-17alpha,21diol-3,11,20-trione

1.3.99.4

0.0256

-

391375

K_i Value (1 result)

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Show KI Value (1 entry)

COMMENTARY

EC NUMBER

KI VALUE [MM]

KI VALUE MAXIMUM [MM]

LITERATURE

androsterone oxidation

1.1.1.213

0.285

-

347982

IC₅₀ Value (1 result)

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Show IC50 Value (1 entry)

COMMENTARY

EC NUMBER

IC50 VALUE

IC50 VALUE MAXIMUM

LITERATURE

in 0.1 M potassium phosphate, pH 7.4, at 25°C

1.1.1.21

0.0022

-

695881

References & Links

Literature References (137)

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Show Reference (137 entries)

BRENDA REFERENCE ID

PUBMED ID

TITLE

YEAR

AUTHORS

JOURNAL

VOLUME

PAGES

7390

3486863

Studies on steroid monooxygenase from Cylindrocarpon radicicola ATCC 11011. Purification and characterization

1986

Itagaki, E.

J. Biochem.

99

815-824

285398

2337351

Lipid regulation of bovine cytochrome P45011beta activity

1990

Seybert, D.

Arch. Biochem. Biophys.

279

188-194

285931

2059213

Regulation of synthesis and activity of NAD+-dependent 15-hydroxy-prostaglandin dehydrogenase (15-PGDH) by dexamethasone and phorbol ester in human erythroleukemia (HEL) cells

1991

Xun, C.Q.; Ensor, C.M.; Tai, H.H.

Biochem. Biophys. Res. Commun.

177

1258-1265

285967

4384445

Metabolism of 11-oxogenated steroids. Metabolism in vitro by preparations of liver

1968

Bush, I.E.; Hunter, S.A.; Meigs, R.A.

Biochem. J.

107

239-258

285979

2722736

Purification and characterization of a novel form of 20alpha-hydroxysteroid dehydrogenase from Clostridium scindens

1989

Krafft, A.E.; Hylemon, P.B.

J. Bacteriol.

171

2925-2932

285994

3475510

Cofactor requirements of steroid-17-20-desmolase and 20alpha-hydroxysteroid dehydrogenase ativities in cell extracts of Clostridium scindens

1987

Krafft, A.E.; Winter, J.; Bokkenheuser, V.D.; Hylemon, P.B.

J. Steroid Biochem.

28

49-54

286004

14253469

The 21-hydroxysteroid dehydrogenases of liver. A nicotinamide adenine dinucleotide phosphate dehydrogenase and two nicotinamide adenine dinucleotide dehydrogenases

1965

Monder, C.; White, A.

J. Biol. Chem.

240

71-77

287085

3474489

Properties of immobilized subunits of 20beta-hydroxysteroid dehydrogenase

1987

Carrea, G.; Pasta, P.

Methods Enzymol.

135

475-483

287087

-

Enzyme-catalyzed steroid transformations in water-organic solvent two-phase systems

1987

Carrea, G.; Cremonesi, P.

Methods Enzymol.

136

150-157

287090

6928375

Bifunctional enzyme activity at the same active site: study of 3alpha and 20beta activity by affinity alkylation of 3alpha, 20beta-hydroxysteroid dehydrogenase with 17-(bromoacetoxy)steroids

1980

Sweet, F.; Samant, B.R.

Biochemistry

19

978-986

287093

718844

Comparison of the 3alpha-and 20beta-hydroxysteroid dehydrogenase activities of the cortisone reductase of Streptomyces hydrogenans

1978

Edwards, C.A.F.; Orr, J.C.

Biochemistry

17

4370-4376

287094

833119

20beta-Hydroxysteroid oxidoreductase. Kinetics and binding of corticosteroids and corticosteroid-21-aldehydes

1977

Szymanski, E.S.; Furfine, C.S.

J. Biol. Chem.

252

205-211

287100

1396701

Short-chain dehydrogenases. Proteolysis and chemical modification of prokaryotic 3alpha/20beta-hydroxysteroid, insect alcohol and human 15-hydroxyprostaglandin dehydrogenase

1992

Krook, M.; Prozorovski, V.; Atrian, S.; Gonzalez-Duarte, R.; Jörnvall, H.

Eur. J. Biochem.

209

233-239

287101

9808673

20beta-Hydroxysteroid dehydrogenase catalyzes ketone-reduction of acetohexamide, an oral antidiabetic drug, in liver microsomes of adult male rats

1998

Takada, H.; Otagiri, M.; Imamura, Y.

J. Pharmacol. Exp. Ther.

287

504-507

347982

6435601

Purification and properties of a 3alpha-hydroxysteroid dehydrogenase of rat liver cytosol and its inhibition by anti-inflammatory drugs

1984

Penning, T.M.; Mukharji, I.; Barrows, S.; Talalay, P.

Biochem. J.

222

601-611

389527

3170514

Purification and characterization of NADP+-dependent 3alpha-hydroxysteroid dehydrogenase from mouse liver cytosol

1988

Hara, A.; Inoue, Y.; Nakagawa, M.; Naganeo, F.; Sawada, H.

J. Biochem.

103

1027-1034

390590

3828348

Identification of cortisone 5beta-reductase as DELTA4-3-ketosteroid 5beta-reductase

1987

Furuebisu, M.; Deguchi, S.; Okuda, K.

Biochim. Biophys. Acta

912

110-114

390591

6736016

Purification and characterization of DELTA 4-3-ketosteroid 5beta-reductase

1984

Okuda, A.; Okuda, K.

J. Biol. Chem.

259

7519-7524

390594

13376613

Separation of DELTA4-5alpha- and DELTA4-5beta-hydrogenases from rat liver homogenates

1956

Forchielli, E.; Dorfmann, R.I.

J. Biol. Chem.

223

443-448

390595

4396256

Steroid DELTA4-reductases of pig liver: partial purification of testosterone 5beta-reductase

1971

Nduaguba, J.C.; Clark, A.F.

Can. J. Biochem.

49

385-392

390646

13805063

The DELTA4-hydrogenases of guinea pig adrenal gland

1960

Brown-Grant, K.; Forchielli, E.; Dorfman, R.I.

J. Biol. Chem.

235

1317-1320

390647

13416214

The enzymatic reduction of DELTA4-3-ketosteroids

1957

Tomkins, G.M.

J. Biol. Chem.

225

13-24

390765

-

Some characteristics of the microsomal steroid reductase (5alpha) of rat liver

1960

McGuire, J.S.; Hollis, V.W.; Tomkins, G.M.

J. Biol. Chem.

235

3112-3117

391375

2317517

Purification and characterization of 3-ketosteroid-delta 1-dehydrogenase from Nocardia corallina

1990

Itagaki, E.; Wakabayashi, T.; Hatta, T.

Biochim. Biophys. Acta

1038

60-67

391392

8586617

Purification and characterization of the 3-ketosteroid-DELTA1-dehydrogenase of Arthrobacter simplex produced in Streptomyces lividans

1995

Choi, K.P.; Molnar, I.; Yamashita, M.; Murooka, Y.

J. Biochem.

117

1043-1049

645722

737567

Enzymatic sulfation of steroids. V. Partial purification and some properties of sulfotransferase III, the major glucocorticoid sulfotransferase of liver cytosol from male rats

1978

Singer, S.S.; Gebhart, J.; Hess, E.

Can. J. Biochem.

56

1028-1035

645769

6936065

Enzymatic sulfation of steroids. XI. The extensive purification and some properties of hepatic sulfotransferase III from female rats

1980

Singer, S.S.; Bruns, L.

Can. J. Biochem.

58

660-666

645774

6935986

The identity of alcohol sulfotransferases with hydroxysteroid sulfotransferases

1980

Lyon, E.S.; Jakoby, W.B.

Arch. Biochem. Biophys.

202

474-481

654637

11841241

11 beta-Hydroxysteroid dehydrogenase type 1 from human liver: dimerization and enzyme cooperativity support its postulated role as glucocorticoid reductase

2002

Maser, E.; Volker, B.; Friebertshauser, J.

Biochemistry

41

2459-2465

654698

12680765

Functional characterization of the human 11 beta-hydroxysteroid dehydrogenase 1B (11 beta-HSD 1B) variant

2003

Blum, A.; Raum, A.; Maser, E.

Biochemistry

42

4108-4117

654889

14732482

Characterisation of 11beta-hydroxysteroid dehydrogenases in feline kidney and liver

2004

Schipper, L.; Spee, B.; Rothuizen, J.; Woutersen-van Nijnanten, F.; Fink-Gremmels, J.

Biochim. Biophys. Acta

1688

68-77

655162

15172126

Expression of 11beta-hydroxysteroid dehydrogenase types 1 and 2 in colorectal cancer

2004

Zbankova, S.; Bryndova, J.; Kment, M.; Pacha, J.

Cancer Lett.

210

95-100

655216

12604230

Purification, characterization and NNK carbonyl reductase activities of 11beta-hydroxysteroid dehydrogenase type 1 from human liver: enzyme cooperativity and significance in the detoxification of a tobacco-derived carcinogen

2003

Maser, E.; Friebertshauser, J.; Volker, B.

Chem. Biol. Interact.

143-144

435-448

655218

12604233

The critical role of the N-terminus of 11beta-hydroxysteroid dehydrogenase type 1, as being encoded by exon 1, for enzyme stabilization and activity

2003

Blum, A.; Maser, E.

Chem. Biol. Interact.

143-144

469-480

656133

12397058

Comparative enzymology of 11beta -hydroxysteroid dehydrogenase type 1 from glucocorticoid resistant (guinea pig) versus sensitive (human) species

2003

Shafqat, N.; Elleby, B.; Svensson, S.; Shafqat, J.; Jornvall, H.; Abrahmsen, L.; Oppermann, U.

J. Biol. Chem.

278

2030-2035

656227

15152005

Appropriate function of 11beta-hydroxysteroid dehydrogenase type 1 in the endoplasmic reticulum lumen is dependent on its N-terminal region sharing similar topological determinants with 50-kDa esterase

2004

Frick, C.; Atanasov, A.G.; Arnold, P.; Ozols, J.; Odermatt, A.

J. Biol. Chem.

279

31131-31138

656356

15330095

Membrane protein isolation by in situ solubilization, partitioning and affinity adsorption in aqueous two-phase systems. Purification of the human type 1 11beta-hydroxysteroid dehydrogenase

2004

Roobol-Boza, M.; Dolby, V.; Doverskog, M.; Barrefelt, A.; Lindqvist, F.; Oppermann, U.C.; Kohler Van Alstine, K.; Tjerneld, F.

J. Chromatogr. A

1043

217-223

656659

15276626

Purification and characterization of 7beta-hydroxysteroid dehydrogenase from rabbit liver microsomes

2004

Shiotsuki, H.; Maeda, Y.; Chijiiwa, K.

J. Steroid Biochem. Mol. Biol.

91

185-190

657253

12460758

Purification of full-length recombinant human and rat type 1 11beta-hydroxysteroid dehydrogenases with retained oxidoreductase activities

2002

Nobel, C.S.I.; Dunas, F.; Abrahmsen, L.B.

Protein Expr. Purif.

26

349-356

657396

15033547

The novel anticancer drug oracin: different stereospecificity and cooperativity for carbonyl reduction by purified human liver 11beta-hydroxysteroid dehydrogenase type 1

2004

Wsol, V.; Szotakova, B.; Skalova, L.; Maser, E.

Toxicology

197

253-261

666138

5074346

D-Tryptophan pyrrolase activity in the liver and the intestine of the rat

1972

Loh, H.H.; Berg, C.P.

J. Nutr.

102

1331-1339

667148

12700160

Regulation of 11beta-hydroxysteroid dehydrogenase enzymes in the rat kidney by estradiol

2003

Gomez-Sanchez, E.P.; Venkataseshu, G.; Chen, Y.J.; Liu, Y.; Zhou, M.Y.; Toroslu, C.; Romero, D.G.; Hughson, M.D.; de Rodriguez, A.; Gomez-Sanchez, C.E.

Am. J. Physiol. Endocrinol. Metab.

285

E272-E279

667673

15865440

Crystal structure of murine 11 beta-hydroxysteroid dehydrogenase 1: an important therapeutic target for diabetes

2005

Zhang, J.; Osslund, T.D.; Plant, M.H.; Clogston, C.L.; Nybo, R.E.; Xiong, F.; Delaney, J.M.; Jordan, S.R.

Biochemistry

44

6948-6957

667835

16580270

The role of tyrosine 177 in human 11beta-hydroxysteroid dehydrogenase type 1 in substrate and inhibitor binding: an unlikely hydrogen bond donor for the substrate

2006

Kim, K.W.; Wang, Z.; Busby, J.; Tsuruda, T.; Chen, M.; Hale, C.; Castro, V.M.; Svensson, S.; Nybo, R.; Xiong, F.; Wang, M.

Biochim. Biophys. Acta

1764

824-830

667956

15911270

Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I

2005

Xiang, J.; Ipek, M.; Suri, V.; Massefski, W.; Pan, N.; Ge, Y.; Tam, M.; Xing, Y.; Tobin, J.F.; Xu, X.; Tam, S.

Bioorg. Med. Chem. Lett.

15

2865-2869

667962

16039856

Adamantyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1

2005

Olson, S.; Aster, S.D.; Brown, K.; Carbin, L.; Graham, D.W.; Hermanowski-Vosatka, A.; LeGrand, C.B.; Mundt, S.S.; Robbins, M.A.; Schaeffer, J.M.; Slossberg, L.H.; Szymonifka, M.J.; Thieringer, R.; Wright, S.D.; Balkovec, J.M.

Bioorg. Med. Chem. Lett.

15

4359-4362

668296

16181237

In vivo activity of 11beta-hydroxysteroid dehydrogenase type 1 and free fatty acid-induced insulin resistance

2005

Mai, K.; Kullmann, V.; Bobbert, T.; Maser-Gluth, C.; Moehlig, M.; Baehr, V.; Pfeiffer, A.F.; Spranger, J.; Diederich, S.

Clin. Endocrinol. (Oxf.)

63

442-449

668297

17121533

11beta Hydroxysteroid dehydrogenase type 1 is expressed and is biologically active in human skeletal muscle

2006

Jang, C.; Obeyesekere, V.R.; Dilley, R.J.; Alford, F.P.; Inder, W.J.

Clin. Endocrinol. (Oxf.)

65

800-805

668379

17065337

Splanchnic cortisol production in dogs occurs primarily in the liver: evidence for substantial hepatic specific 11beta hydroxysteroid dehydrogenase type 1 activity

2006

Basu, R.; Edgerton, D.S.; Singh, R.J.; Cherrington, A.; Rizza, R.A.

Diabetes

55

3013-3019

668424

16469798

Enhancement of cortisol-induced 11beta-hydroxysteroid dehydrogenase type 1 expression by interleukin 1beta in cultured human chorionic trophoblast cells

2006

Li, W.; Gao, L.; Wang, Y.; Duan, T.; Myatt, L.; Sun, K.

Endocrinology

147

2490-2495

668505

15926111

Characterization of 11beta-hydroxysteroid dehydrogenase activity in testicular tissue of control and GnRH-immunized boars as a possible regulator of spermatogenesis

2005

Claus, R.; Wagner, A.; Lambert, T.

Exp. Clin. Endocrinol. Diabetes

113

262-267

668636

16814782

Coffee inhibits the reactivation of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1: a glucocorticoid connection in the anti-diabetic action of coffee?

2006

Atanasov, A.G.; Dzyakanchuk, A.A.; Schweizer, R.A.; Nashev, L.G.; Maurer, E.M.; Odermatt, A.

FEBS Lett.

580

4081-4085

669397

15542590

The crystal structure of guinea pig 11beta-hydroxysteroid dehydrogenase type 1 provides a model for enzyme-lipid bilayer interactions

2005

Ogg, D.; Elleby, B.; Norstroem, C.; Stefansson, K.; Abrahmsen, L.; Oppermann, U.; Svensson, S.

J. Biol. Chem.

280

3789-3794

669504

16234247

Evidence that the 11 beta-hydroxysteroid dehydrogenase (11 beta-HSD1) is regulated by pentose pathway flux. Studies in rat adipocytes and microsomes

2006

McCormick, K.L.; Wang, X.; Mick, G.J.

J. Biol. Chem.

281

341-347

669640

16783599

Comparison of a homology model and the crystallographic structure of human 11beta-hydroxysteroid dehydrogenase type 1 (11betaHSD1) in a structure-based identification of inhibitors

2006

Miguet, L.; Zhang, Z.; Barbier, M.; Grigorov, M.G.

J. Comput. Aided Mol. Des.

20

67-81

669730

16751407

Local amplification of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1 promotes macrophage phagocytosis of apoptotic leukocytes

2006

Gilmour, J.S.; Coutinho, A.E.; Cailhier, J.F.; Man, T.Y.; Clay, M.; Thomas, G.; Harris, H.J.; Mullins, J.J.; Seckl, J.R.; Savill, J.S.; Chapman, K.E.

J. Immunol.

176

7605-7611

669907

16087724

Comparative enzymology of 11beta-hydroxysteroid dehydrogenase type 1 from six species

2005

Arampatzis, S.; Kadereit, B.; Schuster, D.; Balazs, Z.; Schweizer, R.A.; Frey, F.J.; Langer, T.; Odermatt, A.

J. Mol. Endocrinol.

35

89-101

670065

16460444

11beta-Hydroxysteroid dehydrogenase type 1-driven cortisone reactivation regulates plasminogen activator inhibitor type 1 in adipose tissue of obese women

2006

Ayachi, S.E.; Paulmyer-Lacroix, O.; Verdier, M.; Alessi, M.C.; Dutour, A.; Grino, M.

J. Thromb. Haemost.

4

621-627

670253

16412558

Why is 11beta-hydroxysteroid dehydrogenase type 1 facing the endoplasmic reticulum lumen? Physiological relevance of the membrane topology of 11beta-HSD1

2006

Odermatt, A.; Atanasov, A.G.; Balazs, Z.; Schweizer, R.A.; Nashev, L.G.; Schuster, D.; Langer, T.

Mol. Cell. Endocrinol.

248

15-23

670261

16337333

Cooperativity between 11beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase is based on a common pyridine nucleotide pool in the lumen of the endoplasmic reticulum

2006

Czegle, I.; Piccirella, S.; Senesi, S.; Csala, M.; Mandl, J.; Banhegyi, G.; Fulceri, R.; Benedetti, A.

Mol. Cell. Endocrinol.

248

24-25

670263

16431016

Active site variability of type 1 11beta-hydroxysteroid dehydrogenase revealed by selective inhibitors and cross-species comparisons

2006

Hult, M.; Shafqat, N.; Elleby, B.; Mitschke, D.; Svensson, S.; Forsgren, M.; Barf, T.; Vallgarda, J.; Abrahmsen, L.; Oppermann, U.

Mol. Cell. Endocrinol.

248

26-33

670264

16343739

11beta-Hydroxysteroid dehydrogenase type 1: purification from human liver and characterization as carbonyl reductase of xenobiotics

2006

Maser, E.; Wsol, V.; Martin, H.J.

Mol. Cell. Endocrinol.

248

34-37

678118

9585575

Reductive and oxidative half-reactions of morphinone reductase from Pseudomonas putida M10: a kinetic and thermodynamic analysis

1998

Craig, D.H.; Moody, P.C.; Bruce, N.C.; Scrutton, N.S.

Biochemistry

37

7598-7607

683869

18273561

Hormone induced expression of brush border lactase in suckling rat intestine

2008

Chaudhry, K.K.; Mahmood, S.; Mahmood, A.

Mol. Cell. Biochem.

312

11-16

687723

18407998

Crystal structure of human liver DELTA4-3-ketosteroid 5beta-reductase (AKR1D1) and implications for substrate binding and catalysis

2008

Di Costanzo, L.; Drury, J.E.; Penning, T.M.; Christianson, D.W.

J. Biol. Chem.

283

16830-16839

690401

17765862

An in vitro microdialysis methodology to study 11beta-hydroxysteroid dehydrogenase type 1 enzyme activity in liver microsomes

2007

Sun, L.; Stenken, J.A.; Yang, A.Y.; Zhao, J.J.; Musson, D.G.

Anal. Biochem.

370

26-37

691258

17442567

Piperidine amides as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors

2007

Flyren, K.; Bergquist, L.O.; Castro, V.M.; Fotsch, C.; Johansson, L.; St Jean, D.J.; Sutin, L.; Williams, M.

Bioorg. Med. Chem. Lett.

17

3421-3425

691263

18242087

Discovery of novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 by docking and pharmacophore modeling

2008

Yang, H.; Dou, W.; Lou, J.; Leng, Y.; Shen, J.

Bioorg. Med. Chem. Lett.

18

1340-1345

691275

18434143

Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1

2008

Aster, S.D.; Graham, D.W.; Kharbanda, D.; Patel, G.; Ponpipom, M.; Santorelli, G.M.; Szymonifka, M.J.; Mundt, S.S.; Shah, K.; Springer, M.S.; Thieringer, R.; Hermanowski-Vosatka, A.; Wright, S.D.; Xiao, J.; Zokian, H.; Balkovec, J.M.

Bioorg. Med. Chem. Lett.

18

2799-2804

691279

18485702

Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1

2008

Wang, H.; Ruan, Z.; Li, J.J.; Simpkins, L.M.; Smirk, R.A.; Wu, S.C.; Hutchins, R.D.; Nirschl, D.S.; Van Kirk, K.; Cooper, C.B.; Sutton, J.C.; Ma, Z.; Golla, R.; Seethala, R.; Salyan, M.E.; Nayeem, A.; Krystek, S.R.; Sheriff, S.; Camac, D.M.; Morin, P.E.; Carpenter, B.; Robl, J.A.; Zahler, R.; Gordon, D.A.; Hamann, L.G.

Bioorg. Med. Chem. Lett.

18

3168-3172

691281

18440811

4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I

2008

Zhu, Y.; Olson, S.H.; Hermanowski-Vosatka, A.; Mundt, S.; Shah, K.; Springer, M.; Thieringer, R.; Wright, S.; Xiao, J.; Zokian, H.; Balkovec, J.M.

Bioorg. Med. Chem. Lett.

18

3405-3411

691282

18440812

Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I

2008

Zhu, Y.; Olson, S.H.; Graham, D.; Patel, G.; Hermanowski-Vosatka, A.; Mundt, S.; Shah, K.; Springer, M.; Thieringer, R.; Wright, S.; Xiao, J.; Zokian, H.; Dragovic, J.; Balkovec, J.M.

Bioorg. Med. Chem. Lett.

18

3412-3416

691284

18511278

Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1)

2008

Sun, D.; Wang, Z.; Di, Y.; Jaen, J.C.; Labelle, M.; Ma, J.; Miao, S.; Sudom, A.; Tang, L.; Tomooka, C.S.; Tu, H.; Ursu, S.; Walker, N.; Yan, X.; Ye, Q.; Powers, J.P.

Bioorg. Med. Chem. Lett.

18

3513-3516

692338

17306259

The selectivity of tyrosine 280 of human 11beta-hydroxysteroid dehydrogenase type 1 in inhibitor binding

2007

Kim, K.W.; Wang, Z.; Busby, J.; Tsuruda, T.; Chen, M.; Hale, C.; Castro, V.M.; Svensson, S.; Nybo, R.; Xiong, F.; Wang, M.

FEBS Lett.

581

995-999

693544

18419108

2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice

2008

Johansson, L.; Fotsch, C.; Bartberger, M.D.; Castro, V.M.; Chen, M.; Emery, M.; Gustafsson, S.; Hale, C.; Hickman, D.; Homan, E.; Jordan, S.R.; Komorowski, R.; Li, A.; McRae, K.; Moniz, G.; Matsumoto, G.; Orihuela, C.; Palm, G.; Veniant, M.; Wang, M.; Williams, M.; Zhang, J.

J. Med. Chem.

51

2933-2943

693550

18553955

Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model

2008

Julian, L.D.; Wang, Z.; Bostick, T.; Caille, S.; Choi, R.; Degraffenreid, M.; Di, Y.; He, X.; Hungate, R.W.; Jaen, J.C.; Liu, J.; Monshouwer, M.; McMinn, D.; Rew, Y.; Sudom, A.; Sun, D.; Tu, H.; Ursu, S.; Walker, N.; Yan, X.; Ye, Q.; Powers, J.P.

J. Med. Chem.

51

3953-3960

695146

17825335

5Alpha-androstane-3beta,7alpha,17beta-triol and 5alpha-androstane-3beta,7beta,17beta-triol as substrates for the human 11beta-hydroxysteroid dehydrogenase type 1

2007

Hennebert, O.; Le Mee, S.; Pernelle, C.; Morfin, R.

Steroids

72

855-864

695881

19464995

Kinetic studies of AKR1B10, human aldose reductase-like protein: endogenous substrates and inhibition by steroids

2009

Endo, S.; Matsunaga, T.; Mamiya, H.; Ohta, C.; Soda, M.; Kitade, Y.; Tajima, K.; Zhao, H.T.; El-Kabbani, O.; Hara, A.

Arch. Biochem. Biophys.

487

1-9

696736

18789704

Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1

2008

Tu, H.; Powers, J.P.; Liu, J.; Ursu, S.; Sudom, A.; Yan, X.; Xu, H.; Meininger, D.; Degraffenreid, M.; He, X.; Jaen, J.C.; Sun, D.; Labelle, M.; Yamamoto, H.; Shan, B.; Walker, N.P.; Wang, Z.

Bioorg. Med. Chem.

16

8922-8931

697498

18336279

The role of 11beta-hydroxysteroid dehydrogenase in metabolic disease and therapeutic potential of 11beta-HSD1 inhibitors

2008

Saiah, E.

Curr. Med. Chem.

15

642-649

697563

18779947

11beta-Hydroxysteroid dehydrogenase type 1 regulates insulin and glucagon secretion in pancreatic islets

2008

Swali, A.; Walker, E.A.; Lavery, G.G.; Tomlinson, J.W.; Stewart, P.M.

Diabetologia

51

2003-2011

697625

18467433

Insulin and dexamethasone dynamically regulate adipocyte 11beta-hydroxysteroid dehydrogenase type 1

2008

Balachandran, A.; Guan, H.; Sellan, M.; van Uum, S.; Yang, K.

Endocrinology

149

4069-4079

697737

18653260

Structure-based virtual screening for identification of novel 11beta-HSD1 inhibitors

2009

Yang, H.; Shen, Y.; Chen, J.; Jiang, Q.; Leng, Y.; Shen, J.

Eur. J. Med. Chem.

44

1167-1171

698026

19535018

Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 by plant extracts used as traditional antidiabetic medicines

2009

Gumy, C.; Thurnbichler, C.; Aubry, E.M.; Balazs, Z.; Pfisterer, P.; Baumgartner, L.; Stuppner, H.; Odermatt, A.; Rollinger, J.M.

Fitoterapia

80

200-205

698167

19129713

Expression and activity of 11beta-hydroxysteroid dehydrogenase type 1 enzyme in subcutaneous and visceral adipose tissue of prepubertal children

2009

Mericq, V.; Medina, P.; Bouwman, C.; Johnson, M.C.; Godoy, J.; Lopez, T.; Iniguez, G.

Horm. Res.

71

89-93

699469

19673466

Efficacious 11beta-hydroxysteroid dehydrogenase type I inhibitors in the diet-induced obesity mouse model

2009

Wan, Z.K.; Chenail, E.; Xiang, J.; Li, H.Q.; Ipek, M.; Bard, J.; Svenson, K.; Mansour, T.S.; Xu, X.; Tian, X.; Suri, V.; Hahm, S.; Xing, Y.; Johnson, C.E.; Li, X.; Qadri, A.; Panza, D.; Perreault, M.; Tobin, J.F.; Saiah, E.

J. Med. Chem.

52

5449-5461

700178

18973788

The role and regulation of 11beta-hydroxysteroid dehydrogenase type 1 in the inflammatory response

2009

Chapman, K.E.; Coutinho, A.E.; Gray, M.; Gilmour, J.S.; Savill, J.S.; Seckl, J.R.

Mol. Cell. Endocrinol.

301

123-131

705710

18848863

Structure and catalytic mechanism of human steroid 5beta-reductase (AKR1D1)

2009

Di Costanzo, L.; Drury, J.E.; Christianson, D.W.; Penning, T.M.

Mol. Cell. Endocrinol.

301

191-198

710777

19701236

Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro

2009

Zhang, X.; Zhou, Y.; Shen, Y.; Du, L.L.; Chen, J.H.; Leng, Y.; Shen, J.H.

Acta Pharmacol. Sin.

30

1344-1350

710841

19497289

Cell-based assay for screening 11beta-hydroxysteroid dehydrogenase 1 inhibitors

2009

Cho, Y.S.; Kim, C.H.; Cheon, H.G.

Anal. Biochem.

392

110-116

711377

19181519

Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1)

2009

Sun, D.; Wang, Z.; Cardozo, M.; Choi, R.; Degraffenreid, M.; Di, Y.; He, X.; Jaen, J.C.; Labelle, M.; Liu, J.; Ma, J.; Miao, S.; Sudom, A.; Tang, L.; Tu, H.; Ursu, S.; Walker, N.; Yan, X.; Ye, Q.; Powers, J.P.

Bioorg. Med. Chem. Lett.

19

1522-1527

711383

19473839

N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275

2009

Siu, M.; Johnson, T.O.; Wang, Y.; Nair, S.K.; Taylor, W.D.; Cripps, S.J.; Matthews, J.J.; Edwards, M.P.; Pauly, T.A.; Ermolieff, J.; Castro, A.; Hosea, N.A.; LaPaglia, A.; Fanjul, A.N.; Vogel, J.E.

Bioorg. Med. Chem. Lett.

19

3493-3497

711387

19564108

4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice

2009

Zhang, X.; Zhou, Z.; Yang, H.; Chen, J.; Feng, Y.; Du, L.; Leng, Y.; Shen, J.

Bioorg. Med. Chem. Lett.

19

4455-4458

711399

20045318

Discovery of cyclicsulfonamide derivatives as 11beta-hydroxysteroid dehydrogenase 1 inhibitors

2010

Kim, S.H.; Ramu, R.; Kwon, S.W.; Lee, S.H.; Kim, C.H.; Kang, S.K.; Rhee, S.D.; Bae, M.A.; Ahn, S.H.; Ha, D.C.; Cheon, H.G.; Kim, K.Y.; Ahn, J.H.

Bioorg. Med. Chem. Lett.

20

1065-1069

711471

20851614

Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11beta-hydroxysteroid dehydrogenase 2 inhibitors

2010

Stanetty, C.; Czollner, L.; Koller, I.; Shah, P.; Gaware, R.; Cunha, T.D.; Odermatt, A.; Jordis, U.; Kosma, P.; Classen-Houben, D.

Bioorg. Med. Chem.

18

7522-7541

711632

20718744

Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice

2010

Feng, Y.; Huang, S.L.; Dou, W.; Zhang, S.; Chen, J.H.; Shen, Y.; Shen, J.H.; Leng, Y.

Br. J. Pharmacol.

161

113-126

711737

19336945

Sesquiterpenes from cultures of the basidiomycete Clitocybe conglobata and their 11 beta-hydroxysteroid dehydrogenase inhibitory activity

2009

Xu, D.; Sheng, Y.; Zhou, Z.Y.; Liu, R.; Leng, Y.; Liu, J.K.

Chem. Pharm. Bull.

57

433-435

711752

20486152

Discovery of adamantyl ethanone derivatives as potent 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors

2010

Su, X.; Pradaux-Caggiano, F.; Thomas, M.P.; Szeto, M.W.; Halem, H.A.; Culler, M.D.; Vicker, N.; Potter, B.V.

ChemMedChem

5

1026-1044

711800

20015040

11beta-hydroxysteroid dehydrogenase type 1 inhibitors as promising therapeutic drugs for diabetes: status and development

2010

Ge, R.; Huang, Y.; Liang, G.; Li, X.

Curr. Med. Chem.

17

412-422

711907

20346546

A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition

2010

Torres-Piedra, M.; Ortiz-Andrade, R.; Villalobos-Molina, R.; Singh, N.; Medina-Franco, J.L.; Webster, S.P.; Binnie, M.; Navarrete-Vazquez, G.; Estrada-Soto, S.

Eur. J. Med. Chem.

45

2606-2612

711951

19780703

Diazepane-acetamide derivatives as selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors

2009

Odermatt, A.

Expert Opin. Ther. Pat.

19

1477-1483

712257

19329984

Pentanol derivatives from basidiomycete Catathelasma imperiale and their 11beta-hydroxysteroid dehydrogenases inhibitory activity

2009

Zhang, L.; Shen, Y.; Zhu, H.J.; Wang, F.; Leng, Y.; Liu, J.K.

J. Antibiot.

62

239-242

713012

20614230

Fenofibrate but not fenofibric acid inhibits 11beta-hydroxysteroid dehydrogenase 1 in C2C12 myotubes

2010

Kim, C.H.; Ramu, R.; Ahn, J.H.; Bae, M.A.; Cho, Y.S.

Mol. Cell. Biochem.

344

91-98

713232

19879607

Rare merosesquiterpenoids from basidiomycete Craterellus odoratus and their inhibition of 11beta-hydroxysteroid dehydrogenases

2010

Zhang, L.; Shen, Y.; Wang, F.; Leng, Y.; Liu, J.K.

Phytochemistry

71

100-103

725399

20522910

Characterization of disease-related 5beta-reductase (AKR1D1) mutations reveals their potential to cause bile acid deficiency

2010

Drury, J.E.; Mindnich, R.; Penning, T.M.

J. Biol. Chem.

285

24529-24537

725963

22061621

Discovery of a novel enzyme mediating glucocorticoid catabolism in fish: 20beta-hydroxysteroid dehydrogenase type 2

2012

Tokarz, J.; Mindnich, R.; Norton, W.; Moeller, G.; Hrabe de Angelis, M.; Adamski, J.

Mol. Cell. Endocrinol.

349

202-213

726492

21255593

Substrate specificity and inhibitor analyses of human steroid 5beta-reductase (AKR1D1)

2011

Chen, M.; Drury, J.E.; Penning, T.M.

Steroids

76

484-490

739986

24055708

11beta-Hydroxysteroid dehydrogenase 1 contributes to the pro-inflammatory response of keratinocytes

2013

Itoi, S.; Terao, M.; Murota, H.; Katayama, I.

Biochem. Biophys. Res. Commun.

440

265-270

740132

26085523

Biological roles of hydroxysteroid (11-beta) dehydrogenase 1 (HSD11B1), HSD11B2, and glucocorticoid receptor (NR3C1) in sheep conceptus elongation

2015

Brooks, K.; Burns, G.; Spencer, T.E.

Biol. Reprod.

93

38

740142

23981897

Synthesis and biological analysis of benzazol-2-yl piperazine sulfonamides as 11beta-hydroxysteroid dehydrogenase 1 inhibitors

2013

Hofer, S.; Kratschmar, D.V.; Schernthanner, B.; Vuorinen, A.; Schuster, D.; Odermatt, A.; Easmon, J.

Bioorg. Med. Chem. Lett.

23

5397-5400

740144

24507919

3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11beta-hydroxysteroid dehydrogenase 1 inhibitor

2014

Lee, Y.; Shin, Y.J.; Ahn, S.K.

Bioorg. Med. Chem. Lett.

24

1421-1425

740155

25529735

Synthesis and biological evaluation of picolinamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1)

2015

Ryu, J.H.; Kim, S.; Han, H.Y.; Son, H.J.; Lee, H.J.; Shin, Y.A.; Kim, J.S.; Park, H.G.

Bioorg. Med. Chem. Lett.

25

695-700

740377

27145012

11beta-Hydroxysteroid dehydrogenase type 1 is expressed in neutrophils and restrains an inflammatory response in male mice

2016

Coutinho, A.E.; Kipari, T.M.; Zhang, Z.; Esteves, C.L.; Lucas, C.D.; Gilmour, J.S.; Webster, S.P.; Walker, B.R.; Hughes, J.; Savill, J.S.; Seckl, J.R.; Rossi, A.G.; Chapman, K.E.

Endocrinology

157

2928-2936

740803

25303491

11beta-hydroxysteroid dehydrogenase types 1 and 2 activity in subcutaneous adipose tissue in humans: implications in obesity and diabetes

2015

Dube, S.; Norby, B.J.; Pattan, V.; Carter, R.E.; Basu, A.; Basu, R.

J. Clin. Endocrinol. Metab.

100

E70-E76

740806

23814014

Resveratrol inhibits 11beta-hydroxysteroid dehydrogenase type 1 activity in rat adipose microsomes

2013

Tagawa, N.; Kubota, S.; Kato, I.; Kobayashi, Y.

J. Endocrinol.

218

311-320

740840

24294985

Medicinal chemistry of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1)

2014

Scott, J.S.; Goldberg, F.W.; Turnbull, A.V.

J. Med. Chem.

57

4466-4486

740915

25151952

11beta-Hydroxysteroid dehydrogenase 1: Regeneration of active glucocorticoids is only part of the story

2015

Odermatt, A.; Klusonova, P.

J. Steroid Biochem. Mol. Biol.

151

85-92

740917

25066675

Endocrine disruptors and other inhibitors of 11beta-hydroxysteroid dehydrogenase 1 and 2: Tissue-specific consequences of enzyme inhibition

2016

Vitku, J.; Starka, L.; Bicikova, M.; Hill, M.; Heracek, J.; Sosvorova, L.; Hampl, R.

J. Steroid Biochem. Mol. Biol.

155

207-216

741066

25227721

11beta-Hydroxysteroid dehydrogenase enzymes modulate effects of glucocorticoids in rheumatoid arthritis synovial cells

2015

Schmidt, M.; Straub, R.H.

Neuroimmunomodulation

22

40-45

741248

26528718

Metabolic coupling determines the activity: comparison of 11beta-hydroxysteroid dehydrogenase 1 and its coupling between liver parenchymal cells and testicular Leydig cells

2015

Li, X.; Hu, G.; Li, X.; Wang, Y.Y.; Hu, Y.Y.; Zhou, H.; Latif, S.A.; Morris, D.J.; Chu, Y.; Zheng, Z.; Ge, R.S.

PLoS ONE

10

e0141767

741297

24404164

Green tea and one of its constituents, epigallocatechine-3-gallate, are potent inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1

2014

Hintzpeter, J.; Stapelfeld, C.; Loerz, C.; Martin, H.J.; Maser, E.

PLoS ONE

9

e84468

743434

26654513

Species differences of 11beta-hydroxysteroid dehydrogenase type 2 function in human and rat term placenta determined via LC-MS/MS

2016

Heussner, K.; Ruebner, M.; Huebner, H.; Rascher, W.; Menendez-Castro, C.; Hartner, A.; Fahlbusch, F.B.; Rauh, M.

Placenta

37

79-84

744148

25904128

Comparison of CYP106A1 and CYP106A2 from Bacillus megaterium - identification of a novel 11-oxidase activity

2015

Kiss, F.M.; Schmitz, D.; Zapp, J.; Dier, T.K.; Volmer, D.A.; Bernhardt, R.

Appl. Microbiol. Biotechnol.

99

8495-8514

760621

28782626

DELTA4-3-ketosteroids as a new class of substrates for the cytosolic sulfotransferases

2017

Hashiguchi, T.; Kurogi, K.; Shimohira, T.; Teramoto, T.; Liu, M.C.; Suiko, M.; Sakakibara, Y.

Biochim. Biophys. Acta

1861

2883-2890

760680

29738970

A novel derivatives of thiazol-4(5H)-one and their activity in the inhibition of 11beta-hydroxysteroid dehydrogenase type 1

2018

Studzinska, R.; Kolodziejska, R.; Kupczyk, D.; Plazinski, W.; Kosmalski, T.

Bioorg. Chem.

79

115-121

760682

30086417

Thiazolo[3,2-a]pyrimidin-5-one derivatives as a novel class of 11beta-hydroxysteroid dehydrogenase inhibitors

2018

Studzinska, R.; Kupczyk, D.; Plazinska, A.; Kolodziejska, R.; Kosmalski, T.; Modzelewska-Banachiewicz, B.

Bioorg. Chem.

81

21-26

760685

30245006

Design, synthesis, and biological evaluation of novel selective peptide inhibitors of 11beta-hydroxysteroid dehydrogenase 1

2018

Boudon, S.; Heidl, M.; Vuorinen, A.; Wandeler, E.; Campiche, R.; Odermatt, A.; Jackson, E.

Bioorg. Med. Chem.

26

5128-5139

760868

30796905

Expression and activity of the cortisol-activating enzyme 11beta-hydroxysteroid dehydrogenase type 1 is tissue and species-specific

2019

Dammann, C.; Stapelfeld, C.; Maser, E.

Chem. Biol. Interact.

303

57-61

760876

31366832

Discovery and biological evaluation of potent and orally active human 11beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes mellitus

2019

Koike, T.; Shiraki, R.; Sasuga, D.; Hosaka, M.; Kawano, T.; Fukudome, H.; Kurosawa, K.; Moritomo, A.; Mimasu, S.; Ishii, H.; Yoshimura, S.

Chem. Pharm. Bull.

67

824-838

760956

28932959

The role and regulation of the 11 beta-hydroxysteroid dehydrogenase enzyme system in patients with inflammatory bowel disease

2017

Hussey, M.; Holleran, G.; Smith, S.; Sherlock, M.; McNamara, D.

Digest. Dis. Sci.

62

3385-3390

761543

31674280

Structural assessment and identification of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors

2020

Ganjoo, A.; Tripathi, A.; Chetti, P.

J. Biomol. Struct. Dyn.

38

4928-4937

761665

31273032

11beta-Hydroxysteroid dehydrogenases control access of 7beta,27-dihydroxycholesterol to retinoid-related orphan receptor gamma

2019

Beck, K.R.; Inderbinen, S.G.; Kanagaratnam, S.; Kratschmar, D.V.; Jetten, A.M.; Yamaguchi, H.; Odermatt, A.

J. Lipid Res.

60

1535-1546

761754

28765040

The cortisol-activating enzyme 11beta-hydroxysteroid dehydrogenase type 1 in skeletal muscle in the pathogenesis of the metabolic syndrome

2017

Loerz, C.; Maser, E.

J. Steroid Biochem. Mol. Biol.

174

65-71

761758

30902677

Enzymatic interconversion of the oxysterols 7beta,25-dihydroxycholesterol and 7-keto,25-hydroxycholesterol by 11beta-hydroxysteroid dehydrogenase type 1 and 2

2019

Beck, K.R.; Kanagaratnam, S.; Kratschmar, D.V.; Birk, J.; Yamaguchi, H.; Sailer, A.W.; Seuwen, K.; Odermatt, A.

J. Steroid Biochem. Mol. Biol.

190

19-28

761908

31664610

Design, synthesis, molecular docking and in vitro evaluation of benzothiazole derivatives as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors

2020

Cabrera Perez, L.C.; Padilla-Martinez, I.I.; Cruz, A.; Correa Basurto, J.; Miliar Garcia, A.; Hernandez Zavala, A.A.; Gomez Lopez, M.; Rosales Hernandez, M.C.

Mol. Divers.

24

971-984

762406

33214595

Role of 11beta-hydroxysteroid dehydrogenase type 1 in the development of atopic dermatitis

2020

Lee, N.R.; Kim, B.J.; Lee, C.H.; Lee, Y.B.; Lee, S.; Hwang, H.J.; Kim, E.; Kim, S.H.; Lee, M.G.; Lee, S.E.; Lavery, G.G.; Choi, E.H.

Sci. Rep.

10

20237

762494

33387577

Species-specific differences in the inhibition of 11beta-hydroxysteroid dehydrogenase 2 by itraconazole and posaconazole

2021

Inderbinen, S.G.; Zogg, M.; Kley, M.; Smiesko, M.; Odermatt, A.

Toxicol. Appl. Pharmacol.

412

115387

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