메뉴 건너뛰기




Volumn 8, Issue 17, 2008, Pages 1508-1523

Inhibitors of 11β -HSD1: A potential treatment for the metabolic syndrome

Author keywords

11 hydroxysteroid dehydrogenase; Cortisol; Cushing's syndrome; Glucocorticoid excess; HPA axis; Metabolic syndrome

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE; 11BETA HYDROXYSTEROID DEHYDROGENASE INHIBITOR; 2 AMINO ADAMANTYL DERIVATIVE; 2 ANILINOTHIAZOLONE; 2 ANILINOTHIAZOLONE DERIVATIVE; 2 CYCLOALKYLAMINOTHIAZOLONE DERIVATIVE; 3 CHLORO 2 METHYL N [4 [2 (4 METHYL 1 PIPERAZINYL) 2 OXOETHYL] 2 THIAZOLYL]BENZENESULFONAMIDE; ANILINE DERIVATIVE; CARBENOXOLONE; CYCLOALKYLAMINO DERIVATIVE; GLYCYRRHETINIC ACID; INCB 13739; OXIDOREDUCTASE INHIBITOR; PERHYDROQUINOLYLBENZAMIDE; PF 915275; THIAZOLE DERIVATIVE; TRIFLUOROMETHYL DERIVATIVE; UNCLASSIFIED DRUG; 11BETA HYDROXYSTEROID DEHYDROGENASE 1; ENZYME INHIBITOR;

EID: 59149094004     PISSN: 15680266     EISSN: None     Source Type: Journal    
DOI: 10.2174/156802608786413528     Document Type: Review
Times cited : (22)

References (71)
  • 2
    • 0842277242 scopus 로고    scopus 로고
    • Grundy, S. M.; Brewer, H. B., Jr.; Cleeman, J. I.; Smith, S. C., Jr.; Lenfant, C. Definition of metabolic syndrome: Report of the National Heart, Lung, and Blood Institute/American Heart Association conference on scientific issues related to definition. Circulation 2004, 109, 433-438.
    • Grundy, S. M.; Brewer, H. B., Jr.; Cleeman, J. I.; Smith, S. C., Jr.; Lenfant, C. Definition of metabolic syndrome: Report of the National Heart, Lung, and Blood Institute/American Heart Association conference on scientific issues related to definition. Circulation 2004, 109, 433-438.
  • 3
    • 0019759637 scopus 로고
    • Transport of steroid hormones: Binding of 21 endogenous steroids to both testosterone-binding globulin and corticosteroid-binding globulin in human plasma
    • Dunn, J. F.; Nisula, B. C.; Rodbard, D. Transport of steroid hormones: binding of 21 endogenous steroids to both testosterone-binding globulin and corticosteroid-binding globulin in human plasma. J. Clin. Endocrinol. Metab. 1981, 53, 58-68.
    • (1981) J. Clin. Endocrinol. Metab , vol.53 , pp. 58-68
    • Dunn, J.F.1    Nisula, B.C.2    Rodbard, D.3
  • 4
    • 0041334187 scopus 로고    scopus 로고
    • 11β-Hydroxysteroid dehydrogenase: Unexpected connections
    • Walker, E. A.; Stewart, P. M. 11β-Hydroxysteroid dehydrogenase: unexpected connections. Trends Endocrinol. Metab. 2003, 14, 334-339.
    • (2003) Trends Endocrinol. Metab , vol.14 , pp. 334-339
    • Walker, E.A.1    Stewart, P.M.2
  • 5
    • 0030998776 scopus 로고    scopus 로고
    • Regulation of phosphoenolpyruvate carboxykinase (GTP) gene expression
    • Hanson, R. W.; Reshef, L. Regulation of phosphoenolpyruvate carboxykinase (GTP) gene expression. Annu. Rev. Biochem. 1997, 66, 581-611.
    • (1997) Annu. Rev. Biochem , vol.66 , pp. 581-611
    • Hanson, R.W.1    Reshef, L.2
  • 6
    • 0033305631 scopus 로고    scopus 로고
    • Differentiation of adipose stromal cells: The roles of glucocorticoids and 11β-hydroxysteroid dehydrogenase
    • Bujalska, I. J.; Kumar, S.; Hewison, M.; Stewart, P. M. Differentiation of adipose stromal cells: the roles of glucocorticoids and 11β-hydroxysteroid dehydrogenase. Endocrinology 1999, 140, 3188-3196.
    • (1999) Endocrinology , vol.140 , pp. 3188-3196
    • Bujalska, I.J.1    Kumar, S.2    Hewison, M.3    Stewart, P.M.4
  • 10
    • 0035798621 scopus 로고    scopus 로고
    • Improved lipid and lipoprotein profile, hepatic insulin sensitivity, and glucose tolerance in 11β-hydroxysteroid dehydrogenase type 1 null mice
    • Morton, N. M.; Holmes, M. C.; Fievet, C.; Staels, B.; Tailleux, A.; Mullins, J. J.; Seckl, J. R. Improved lipid and lipoprotein profile, hepatic insulin sensitivity, and glucose tolerance in 11β-hydroxysteroid dehydrogenase type 1 null mice. J. Biol. Chem. 2001, 276, 41293-41300.
    • (2001) J. Biol. Chem , vol.276 , pp. 41293-41300
    • Morton, N.M.1    Holmes, M.C.2    Fievet, C.3    Staels, B.4    Tailleux, A.5    Mullins, J.J.6    Seckl, J.R.7
  • 12
    • 4544260173 scopus 로고    scopus 로고
    • Overexpression of 11β-hydroxysteroid dehydrogenase-1 in adipose tissue is associated with acquired obesity and features of insulin resistance: Studies in young adult monozygotic twins
    • Kannisto, K.; Pietiläinen, K. H.; Ehrenborg, E.; Rissanen, A.; Kaprio, J.; Hamsten, A.; Yki-Järvinen, H. Overexpression of 11β-hydroxysteroid dehydrogenase-1 in adipose tissue is associated with acquired obesity and features of insulin resistance: Studies in young adult monozygotic twins. J. Clin. Endocrinol. Metab. 2004, 89, 4414-4421.
    • (2004) J. Clin. Endocrinol. Metab , vol.89 , pp. 4414-4421
    • Kannisto, K.1    Pietiläinen, K.H.2    Ehrenborg, E.3    Rissanen, A.4    Kaprio, J.5    Hamsten, A.6    Yki-Järvinen, H.7
  • 15
    • 19644401171 scopus 로고    scopus 로고
    • Taking glucocorticoids by prescription is associated with subsequent cardiovascular disease
    • Wei, L.; MacDonald, T. M.; Walker, B. R. Taking glucocorticoids by prescription is associated with subsequent cardiovascular disease. Ann. Intern. Med. 2004, 141, 764-770.
    • (2004) Ann. Intern. Med , vol.141 , pp. 764-770
    • Wei, L.1    MacDonald, T.M.2    Walker, B.R.3
  • 16
    • 0038305844 scopus 로고    scopus 로고
    • Cardiovascular risk factors and common carotid artery caliber and stiffness in patients with Cushing's disease during active disease and 1 year after disease remission
    • Faggiano, A.; Pivonello, R.; Spiezia, S.; De Martino, M. C.; Filippella, M.; Di Somma, C.; Lombardi, G.; Colao, A. Cardiovascular risk factors and common carotid artery caliber and stiffness in patients with Cushing's disease during active disease and 1 year after disease remission. J. Clin. Endocrinol. Metab. 2003, 88, 2527-2533.
    • (2003) J. Clin. Endocrinol. Metab , vol.88 , pp. 2527-2533
    • Faggiano, A.1    Pivonello, R.2    Spiezia, S.3    De Martino, M.C.4    Filippella, M.5    Di Somma, C.6    Lombardi, G.7    Colao, A.8
  • 19
    • 0025815544 scopus 로고
    • The endocrine effects of long-term treatment with mifepristone (RU 486)
    • Lamberts, S. W.; Koper, J. W.; de, J. F. H. The endocrine effects of long-term treatment with mifepristone (RU 486). J. Clin. Endocrinol. Metab. 1991, 73, 187-191.
    • (1991) J. Clin. Endocrinol. Metab , vol.73 , pp. 187-191
    • Lamberts, S.W.1    Koper, J.W.2    de, J.F.H.3
  • 20
    • 0942288395 scopus 로고    scopus 로고
    • Licorice root: Possible mechanisms of antitoxicant, anti-carcinogen, and antitumor properties (A Review)
    • Pavlova, S. I.; Uteshev, B. S.; Sergeev, A. V. Licorice root: possible mechanisms of antitoxicant, anti-carcinogen, and antitumor properties (A Review). Pharm. Chem. J. 2003, 37, 314-317.
    • (2003) Pharm. Chem. J , vol.37 , pp. 314-317
    • Pavlova, S.I.1    Uteshev, B.S.2    Sergeev, A.V.3
  • 21
    • 0034056308 scopus 로고    scopus 로고
    • In the search for specific inhibitors of human 11β-hydroxysteroid-dehydrogenases (11β-HSDs): Chenodeoxycholic acid selectively inhibits 11β-HSD-I
    • Diederich, S.; Grossmann, C.; Hanke, B.; Quinkler, M.; Herrmann, M.; Bahr, V.; Oelkers, W. In the search for specific inhibitors of human 11β-hydroxysteroid-dehydrogenases (11β-HSDs): chenodeoxycholic acid selectively inhibits 11β-HSD-I. Eur. J. Endocrinol. 2000, 142, 200-207.
    • (2000) Eur. J. Endocrinol , vol.142 , pp. 200-207
    • Diederich, S.1    Grossmann, C.2    Hanke, B.3    Quinkler, M.4    Herrmann, M.5    Bahr, V.6    Oelkers, W.7
  • 22
    • 37149046570 scopus 로고    scopus 로고
    • Carbenoxolone treatment attenuates symptoms of metabolic syndrome and atherogenesis in obese, hyperlipidemic mice
    • Nuotio-Antar, A. M.; Hachey, D. L.; Hasty, A. H. Carbenoxolone treatment attenuates symptoms of metabolic syndrome and atherogenesis in obese, hyperlipidemic mice. Am. J. Physiol. Endocrinol. Metab. 2007, 293, E1517-1528.
    • (2007) Am. J. Physiol. Endocrinol. Metab , vol.293
    • Nuotio-Antar, A.M.1    Hachey, D.L.2    Hasty, A.H.3
  • 23
    • 0028839840 scopus 로고
    • Carbenoxolone increases hepatic insulin sensitivity in man: A novel role for 11-oxosteroid reductase in enhancing glucocorticoid receptor activation
    • Walker, B. R.; Connacher, A. A.; Lindsay, R. M.; Webb, D. J.; Edwards, C. R. W. Carbenoxolone increases hepatic insulin sensitivity in man: a novel role for 11-oxosteroid reductase in enhancing glucocorticoid receptor activation. J. Clin. Endocrinol. Metab. 1995, 80, 3155-3159.
    • (1995) J. Clin. Endocrinol. Metab , vol.80 , pp. 3155-3159
    • Walker, B.R.1    Connacher, A.A.2    Lindsay, R.M.3    Webb, D.J.4    Edwards, C.R.W.5
  • 24
    • 0037238379 scopus 로고    scopus 로고
    • Effects of the 11β-hydroxysteroid dehydrogenase inhibitor carbenoxolone on insulin sensitivity in men with type 2 diabetes
    • Andrews, R. C.; Rooyackers, O.; Walker, B. R. Effects of the 11β-hydroxysteroid dehydrogenase inhibitor carbenoxolone on insulin sensitivity in men with type 2 diabetes. J. Clin. Endocrinol. Metab. 2003, 88, 285-291.
    • (2003) J. Clin. Endocrinol. Metab , vol.88 , pp. 285-291
    • Andrews, R.C.1    Rooyackers, O.2    Walker, B.R.3
  • 25
    • 0033105754 scopus 로고    scopus 로고
    • Kotelevtsev, Y.; Brown, R. W.; Fleming, S.; Kenyon, C.; Edwards, C. R. W.; Seckl, J. R.; Mullins, J. J. Hypertension in mice lacking 11β-hydroxysteroid dehydrogenase type 2. J. Clin. Invest. 1999, 103, 683-689.
    • Kotelevtsev, Y.; Brown, R. W.; Fleming, S.; Kenyon, C.; Edwards, C. R. W.; Seckl, J. R.; Mullins, J. J. Hypertension in mice lacking 11β-hydroxysteroid dehydrogenase type 2. J. Clin. Invest. 1999, 103, 683-689.
  • 26
  • 27
    • 15544380476 scopus 로고    scopus 로고
    • 11β-hydroxysteroid dehydrogenase-1 as a therapeutic target for metabolic diseases
    • Fotsch, C.; Askew, B. C.; Chen, J. J. 11β-hydroxysteroid dehydrogenase-1 as a therapeutic target for metabolic diseases. Expert Opin. Ther. Pat. 2005, 15, 289-303.
    • (2005) Expert Opin. Ther. Pat , vol.15 , pp. 289-303
    • Fotsch, C.1    Askew, B.C.2    Chen, J.J.3
  • 28
    • 38149133022 scopus 로고    scopus 로고
    • 11β-hydroxysteroid dehydrogenase-1 as therapeutic agents
    • Webster, S. P.; Pallin, D. P. 11β-hydroxysteroid dehydrogenase-1 as therapeutic agents. Expert Opin. Ther. Pat. 2007, 17, 1407-1422.
    • (2007) Expert Opin. Ther. Pat , vol.17 , pp. 1407-1422
    • Webster, S.P.1    Pallin, D.P.2
  • 29
    • 33846391295 scopus 로고    scopus 로고
    • 11β-hydroxysteroid dehydrogenase type 1 inhibitors
    • Boyle, C. D.; Kowalski, T. J.; Zhang, L. 11β-hydroxysteroid dehydrogenase type 1 inhibitors. Annu. Rep. Med. Chem. 2006, 41, 127-140.
    • (2006) Annu. Rep. Med. Chem , vol.41 , pp. 127-140
    • Boyle, C.D.1    Kowalski, T.J.2    Zhang, L.3
  • 30
    • 34447105433 scopus 로고    scopus 로고
    • Inhibition of 11β-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target
    • Wamil, M.; Seckl, J. R. Inhibition of 11β-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target. Drug Discovery Today 2007, 12, 504-520.
    • (2007) Drug Discovery Today , vol.12 , pp. 504-520
    • Wamil, M.1    Seckl, J.R.2
  • 31
    • 33744935789 scopus 로고    scopus 로고
    • Recent progress in 11β-hydroxysteroid dehydrogenase type 1 (11-β-HSD1) inhibitor development
    • Barf, T.; Williams, M. Recent progress in 11β-hydroxysteroid dehydrogenase type 1 (11-β-HSD1) inhibitor development. Drugs of the Future 2006, 31, 231-243.
    • (2006) Drugs of the Future , vol.31 , pp. 231-243
    • Barf, T.1    Williams, M.2
  • 38
    • 33846228383 scopus 로고    scopus 로고
    • Rohde, J. J.; Pliushchev, M. A.; Sorensen, B. K.; Wodka, D.; Shuai, Q.; Wang, J.; Fung, S.; Monzon, K. M.; Chiou, W. J.; Pan, L.; Deng, X.; Chovan, L. E.; Ramaiya, A.; Mullally, M.; Henry, R. F.; Stolarik, D. F.; Imade, H. M.; Marsh, K. C.; Beno, D. W. A.; Fey, T. A.; Droz, B. A.; Brune, M. E.; Camp, H. S.; Sham, H. L.; Frevert, E. U.; Jacobson, P. B.; Link, J. T. Discovery and Metabolic Stabilization of Potent and Selective 2-Amino-N-(adamant-2-yl) Acetamide 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors. J. Med. Chem. 2007, 50, 149-164.
    • Rohde, J. J.; Pliushchev, M. A.; Sorensen, B. K.; Wodka, D.; Shuai, Q.; Wang, J.; Fung, S.; Monzon, K. M.; Chiou, W. J.; Pan, L.; Deng, X.; Chovan, L. E.; Ramaiya, A.; Mullally, M.; Henry, R. F.; Stolarik, D. F.; Imade, H. M.; Marsh, K. C.; Beno, D. W. A.; Fey, T. A.; Droz, B. A.; Brune, M. E.; Camp, H. S.; Sham, H. L.; Frevert, E. U.; Jacobson, P. B.; Link, J. T. Discovery and Metabolic Stabilization of Potent and Selective 2-Amino-N-(adamant-2-yl) Acetamide 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors. J. Med. Chem. 2007, 50, 149-164.
  • 39
    • 37349004141 scopus 로고    scopus 로고
    • Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic relationship with 4′-cyano-biphenyl-4-sulfonic acid (6-aminopyridin-2-yl)-amide (PF-915275), an inhibitor of 11β-hydroxysteroid dehydrogenase type 1, in cynomolgus monkeys
    • Bhat, B. G.; Hosea, N.; Fanjul, A.; Herrera, J.; Chapman, J.; Thalacker, F.; Stewart, P. M.; Rejto, P. A. Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic relationship with 4′-cyano-biphenyl-4-sulfonic acid (6-aminopyridin-2-yl)-amide (PF-915275), an inhibitor of 11β-hydroxysteroid dehydrogenase type 1, in cynomolgus monkeys. J. Pharmacol. Exp. Ther. 2008, 324, 299-305.
    • (2008) J. Pharmacol. Exp. Ther , vol.324 , pp. 299-305
    • Bhat, B.G.1    Hosea, N.2    Fanjul, A.3    Herrera, J.4    Chapman, J.5    Thalacker, F.6    Stewart, P.M.7    Rejto, P.A.8
  • 41
    • 26844460594 scopus 로고    scopus 로고
    • Gu, X.; Dragovic, J.; Koo, G. C.; Koprak, S. L.; LeGrand, C.; Mundt, S. S.; Shah, K.; Springer, M. S.; Tan, E. Y.; Thieringer, R.; Hermanowski-Vosatka, A.; Zokian, H. J.; Balkovec, J. M.; Waddell, S. T. Discovery of 4-heteroarylbicyclo[2.2.2] octyltriazoles as potent and selective inhibitors of 11β-HSD1: Novel therapeutic agents for the treatment of metabolic syndrome. Bioorg. Med. Chem. Lett. 2005, 15, 5266-5269.
    • Gu, X.; Dragovic, J.; Koo, G. C.; Koprak, S. L.; LeGrand, C.; Mundt, S. S.; Shah, K.; Springer, M. S.; Tan, E. Y.; Thieringer, R.; Hermanowski-Vosatka, A.; Zokian, H. J.; Balkovec, J. M.; Waddell, S. T. Discovery of 4-heteroarylbicyclo[2.2.2] octyltriazoles as potent and selective inhibitors of 11β-HSD1: Novel therapeutic agents for the treatment of metabolic syndrome. Bioorg. Med. Chem. Lett. 2005, 15, 5266-5269.
  • 42
    • 23944493717 scopus 로고    scopus 로고
    • Hermanowski-Vosatka, A.; Balkovec, J. M.; Cheng, K.; Chen, H. Y.; Hernandez, M.; Koo, G. C.; Le Grand, C. B.; Li, Z.; Metzger, J. M.; Mundt, S. S.; Noonan, H.; Nunes, C. N.; Olson, S. H.; Pikounis, B.; Ren, N.; Robertson, N.; Schaeffer, J. M.; Shah, K.; Springer, M. S.; Strack, A. M.; Strowski, M.; Wu, K.; Wu, T.; Xiao, J.; Zhang, B. B.; Wright, S. D.; Thieringer, R. 11 -HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice. J. Exp. Med. 2005, 202, 517-527.
    • Hermanowski-Vosatka, A.; Balkovec, J. M.; Cheng, K.; Chen, H. Y.; Hernandez, M.; Koo, G. C.; Le Grand, C. B.; Li, Z.; Metzger, J. M.; Mundt, S. S.; Noonan, H.; Nunes, C. N.; Olson, S. H.; Pikounis, B.; Ren, N.; Robertson, N.; Schaeffer, J. M.; Shah, K.; Springer, M. S.; Strack, A. M.; Strowski, M.; Wu, K.; Wu, T.; Xiao, J.; Zhang, B. B.; Wright, S. D.; Thieringer, R. 11 -HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice. J. Exp. Med. 2005, 202, 517-527.
  • 45
    • 14244252559 scopus 로고    scopus 로고
    • Conformational Flexibility in Crystal Structures of Human 11 -Hydroxysteroid Dehydrogenase Type I Provide Insights into Glucocorticoid Interconversion and Enzyme Regulation
    • Hosfield, D. J.; Wu, Y.; Skene, R. J.; Hilgers, M.; Jennings, A.; Snell, G. P.; Aertgeerts, K. Conformational Flexibility in Crystal Structures of Human 11 -Hydroxysteroid Dehydrogenase Type I Provide Insights into Glucocorticoid Interconversion and Enzyme Regulation. J. Biol. Chem. 2005, 280, 4639-4648.
    • (2005) J. Biol. Chem , vol.280 , pp. 4639-4648
    • Hosfield, D.J.1    Wu, Y.2    Skene, R.J.3    Hilgers, M.4    Jennings, A.5    Snell, G.P.6    Aertgeerts, K.7
  • 46
    • 18244364603 scopus 로고    scopus 로고
    • Crystal Structure of Murine 11β-Hydroxysteroid Dehydrogenase 1: An Important Therapeutic Target for Diabetes
    • Zhang, J.; Osslund, T. D.; Plant, M. H.; Clogston, C. L.; Nybo, R. E.; Xiong, F.; Delaney, J. M.; Jordan, S. R. Crystal Structure of Murine 11β-Hydroxysteroid Dehydrogenase 1: An Important Therapeutic Target for Diabetes. Biochemistry 2005, 44, 6948-6957.
    • (2005) Biochemistry , vol.44 , pp. 6948-6957
    • Zhang, J.1    Osslund, T.D.2    Plant, M.H.3    Clogston, C.L.4    Nybo, R.E.5    Xiong, F.6    Delaney, J.M.7    Jordan, S.R.8
  • 47
    • 35148832557 scopus 로고    scopus 로고
    • Yuan, C.; St. Jean, D. J., Jr.; Liu, Q.; Cai, L.; Li, A.; Han, N.; Moniz, G.; Askew, B.; Hungate, R. W.; Johansson, L.; Tedenborg, L.; Pyring, D.; Williams, M.; Hale, C.; Chen, M.; Cupples, R.; Zhang, J.; Jordan, S.; Bartberger, M. D.; Sun, Y.; Emery, M.; Wang, M.; Fotsch, C. The Discovery of 2-Anilinothiazolones as 11β-HSD1 Inhibitors. Bioorg. Med. Chem. Lett. 2007, 17, 6056-6061.
    • Yuan, C.; St. Jean, D. J., Jr.; Liu, Q.; Cai, L.; Li, A.; Han, N.; Moniz, G.; Askew, B.; Hungate, R. W.; Johansson, L.; Tedenborg, L.; Pyring, D.; Williams, M.; Hale, C.; Chen, M.; Cupples, R.; Zhang, J.; Jordan, S.; Bartberger, M. D.; Sun, Y.; Emery, M.; Wang, M.; Fotsch, C. The Discovery of 2-Anilinothiazolones as 11β-HSD1 Inhibitors. Bioorg. Med. Chem. Lett. 2007, 17, 6056-6061.
  • 48
    • 43949124158 scopus 로고    scopus 로고
    • 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. 2-Amino-1,3-thiazol-4(5H)-ones as Potent and Selective 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Enzyme-Ligand Co-Crystal Structure and Demonstration of Pharmacodynamic Effects in C57Bl/6 Mice. J. Med. Chem. 2008, 51, 2933-2943.
    • 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. 2-Amino-1,3-thiazol-4(5H)-ones as Potent and Selective 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Enzyme-Ligand Co-Crystal Structure and Demonstration of Pharmacodynamic Effects in C57Bl/6 Mice. J. Med. Chem. 2008, 51, 2933-2943.
  • 49
    • 60349127107 scopus 로고    scopus 로고
    • i of 140 nM.
    • i of 140 nM.
  • 50
    • 13644269232 scopus 로고    scopus 로고
    • The Crystal Structure of Guinea Pig 11β-Hydroxysteroid Dehydrogenase Type 1 Provides a Model for Enzyme-Lipid Bilayer Interactions
    • Ogg, D.; Elleby, B.; Norström, C.; Stefansson, K.; Abrahmsén, L.; Oppermann, U.; Svensson, S. The Crystal Structure of Guinea Pig 11β-Hydroxysteroid Dehydrogenase Type 1 Provides a Model for Enzyme-Lipid Bilayer Interactions. J. Biol. Chem. 2005, 280, 3789-3794.
    • (2005) J. Biol. Chem , vol.280 , pp. 3789-3794
    • Ogg, D.1    Elleby, B.2    Norström, C.3    Stefansson, K.4    Abrahmsén, L.5    Oppermann, U.6    Svensson, S.7
  • 51
    • 60349130691 scopus 로고    scopus 로고
    • Unpublished results
    • Unpublished results.
  • 55
    • 60349120801 scopus 로고    scopus 로고
    • Veniant, M. H., C.; Komorowski, R.; Chen, M. M.; St. Jean, D. J., Jr.; Fotsch, C.; Wang, M. Time of day for 11β-HSD1 inhibition plays a role in improving glucose homeostasis in DIO mice. Diabetes Obes. Metabol. 2008, in press.
    • Veniant, M. H., C.; Komorowski, R.; Chen, M. M.; St. Jean, D. J., Jr.; Fotsch, C.; Wang, M. Time of day for 11β-HSD1 inhibition plays a role in improving glucose homeostasis in DIO mice. Diabetes Obes. Metabol. 2008, in press.
  • 56
    • 0035111323 scopus 로고    scopus 로고
    • Intracellular regeneration of glucocorticoids by 11β-hydroxysteroid dehydrogenase (112b-HSD)-1 plays a key role in regulation of the hypothalamic-pituitary-adrenal axis: Analysis of 11β-HSD-1-deficient mice
    • Harris, H. J.; Kotelevtsev, Y.; Mullins, J. J.; Seckl, J. R.; Holmes, M. C. Intracellular regeneration of glucocorticoids by 11β-hydroxysteroid dehydrogenase (112b-HSD)-1 plays a key role in regulation of the hypothalamic-pituitary-adrenal axis: analysis of 11β-HSD-1-deficient mice. Endocrinology 2001, 142, 114-120.
    • (2001) Endocrinology , vol.142 , pp. 114-120
    • Harris, H.J.1    Kotelevtsev, Y.2    Mullins, J.J.3    Seckl, J.R.4    Holmes, M.C.5
  • 58
    • 0037374775 scopus 로고    scopus 로고
    • Is 11β-hydroxysteroid dehydrogenase type 1 a therapeutic target? Effects of carbenoxolone in lean and obese Zucker rats
    • Livingstone, D. E. W.; Walker, B. R. Is 11β-hydroxysteroid dehydrogenase type 1 a therapeutic target? Effects of carbenoxolone in lean and obese Zucker rats. J. Pharmacol. Exp. Ther. 2003, 305, 167-172.
    • (2003) J. Pharmacol. Exp. Ther , vol.305 , pp. 167-172
    • Livingstone, D.E.W.1    Walker, B.R.2
  • 60
    • 60349101988 scopus 로고    scopus 로고
    • AMG 221 is an orally-administered agent being evaluated for treatment of metabolic disorders, including type 2 diabetes. Retrieved 3/21/ 2008, from http://www.amgen.com/science/ pipe_AMG221.html
    • "AMG 221 is an orally-administered agent being evaluated for treatment of metabolic disorders, including type 2 diabetes." Retrieved 3/21/ 2008, from http://www.amgen.com/science/ pipe_AMG221.html
  • 61
    • 39049131253 scopus 로고    scopus 로고
    • Modulation of 11β-Hydroxysteroid Dehydrogenase (11βHSD) Activity Biomarkers and Pharmacokinetics of PF-00915275, a Selective 11βHSD1 Inhibitor
    • Courtney, R.; Stewart, P. M.; Toh, M.; Ndongo, M. N.; Calle, R. A.; Hirshberg, B. Modulation of 11β-Hydroxysteroid Dehydrogenase (11βHSD) Activity Biomarkers and Pharmacokinetics of PF-00915275, a Selective 11βHSD1 Inhibitor. J. Clin. Endocrinol. Metab. 2008, 93, 550-556.
    • (2008) J. Clin. Endocrinol. Metab , vol.93 , pp. 550-556
    • Courtney, R.1    Stewart, P.M.2    Toh, M.3    Ndongo, M.N.4    Calle, R.A.5    Hirshberg, B.6
  • 62
    • 60349108327 scopus 로고    scopus 로고
    • Pfizer. NCT00427401: A Study To Evaluate PF-00915275 In Subjects With Type 2 Diabetes Mellitus For 4-Weeks. from www.clinicaltrials.gov
    • Pfizer. "NCT00427401: A Study To Evaluate PF-00915275 In Subjects With Type 2 Diabetes Mellitus For 4-Weeks." from www.clinicaltrials.gov
  • 64
    • 50249094821 scopus 로고    scopus 로고
    • 11β-HSD1 inhibitors for type 2 diabetes: A systematic development strategy to assess pharmacodynamic activity and obtain proof-of-concept in man
    • Boston, MA, February 28
    • Huber, R. 11β-HSD1 inhibitors for type 2 diabetes: a systematic development strategy to assess pharmacodynamic activity and obtain proof-of-concept in man. IBC's Targeting metabolic syndrome, Boston, MA 2007, February 28.
    • (2007) IBC's Targeting metabolic syndrome
    • Huber, R.1
  • 66
    • 60349121535 scopus 로고    scopus 로고
    • Incyte's Product Pipeline. Retrieved 3/21/2008, from http://www.incyte.com/drugs_product_pipeline.html.
    • "Incyte's Product Pipeline." Retrieved 3/21/2008, from http://www.incyte.com/drugs_product_pipeline.html.
  • 68
    • 26044458939 scopus 로고    scopus 로고
    • Increased expression of 11β-hydroxysteroid dehydrogenase type I in type 2 diabetic myotubes
    • Abdallah, B. M.; Beck-Nielsen, H.; Gaster, M. Increased expression of 11β-hydroxysteroid dehydrogenase type I in type 2 diabetic myotubes. Eur. J. Clin. Invest. 2005, 35, 627-634.
    • (2005) Eur. J. Clin. Invest , vol.35 , pp. 627-634
    • Abdallah, B.M.1    Beck-Nielsen, H.2    Gaster, M.3
  • 69
    • 0035836756 scopus 로고    scopus 로고
    • Lack of tissue glucocorticoid reactivation in 11β-hydroxysteroid dehydrogenase type 1 knockout mice ameliorates age-related learning impairments
    • Yau, J. L.; Noble, J.; Kenyon, C. J.; Hibberd, C.; Kotelevtsev, Y.; Mullins, J. J.; Seckl, J. R. Lack of tissue glucocorticoid reactivation in 11β-hydroxysteroid dehydrogenase type 1 knockout mice ameliorates age-related learning impairments. Proc. Natl. Acad. Sci. USA 2001, 98, 4716-4721.
    • (2001) Proc. Natl. Acad. Sci. USA , vol.98 , pp. 4716-4721
    • Yau, J.L.1    Noble, J.2    Kenyon, C.J.3    Hibberd, C.4    Kotelevtsev, Y.5    Mullins, J.J.6    Seckl, J.R.7
  • 70
    • 85047691378 scopus 로고    scopus 로고
    • 11β-hydroxysteroid dehydrogenase type 1 as a novel therapeutic target in metabolic and neurodegenerative disease
    • Walker, B. R.; Seckl, J. R. 11β-hydroxysteroid dehydrogenase type 1 as a novel therapeutic target in metabolic and neurodegenerative disease. Expert Opin. Ther. Targets 2003, 7, 771-783.
    • (2003) Expert Opin. Ther. Targets , vol.7 , pp. 771-783
    • Walker, B.R.1    Seckl, J.R.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.