-
1
-
-
77950664531
-
11β-Hydroxysteroid dehydrogenase type 1 inhibitors as promising therapeutic drugs for diabetes: Status and development
-
Ge, R.; Huang, Y.; Liang, G.; Li, X. 11β-Hydroxysteroid dehydrogenase type 1 inhibitors as promising therapeutic drugs for diabetes: status and development Curr. Med. Chem. 2010, 17, 412-422
-
(2010)
Curr. Med. Chem.
, vol.17
, pp. 412-422
-
-
Ge, R.1
Huang, Y.2
Liang, G.3
Li, X.4
-
2
-
-
77955590502
-
11β-Hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes
-
Morgan, S. A.; Tomlinson, J. W. 11β-Hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes Expert Opin. Invest. Drugs 2010, 19, 1067-1076
-
(2010)
Expert Opin. Invest. Drugs
, vol.19
, pp. 1067-1076
-
-
Morgan, S.A.1
Tomlinson, J.W.2
-
3
-
-
84871025881
-
Molecular target of the metabolic syndrome. 11β-HSD1 an adipocyte function
-
Masuzaki, H.; Yasue, S.; Nakao, K. Molecular target of the metabolic syndrome. 11β-HSD1 an adipocyte function Card. Pract. 2005, 16, 179-186
-
(2005)
Card. Pract.
, vol.16
, pp. 179-186
-
-
Masuzaki, H.1
Yasue, S.2
Nakao, K.3
-
4
-
-
68549139946
-
The pathogenetic role of cortisol in the metabolic syndrome: A hypothesis
-
Anagnostis, P.; Athyros, V. G.; Tziomalos, K.; Karagiannis, A.; Mikhailidis, D. P. The pathogenetic role of cortisol in the metabolic syndrome: a hypothesis J. Clin. Endocrinol. Metab. 2009, 94, 2692-2701
-
(2009)
J. Clin. Endocrinol. Metab.
, vol.94
, pp. 2692-2701
-
-
Anagnostis, P.1
Athyros, V.G.2
Tziomalos, K.3
Karagiannis, A.4
Mikhailidis, D.P.5
-
5
-
-
84863086678
-
Discovery of a Potent, Selective, and Orally Bioavailable Acidic 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitor: Discovery of 2-[(3S)-1-[5-(Cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3- piperidyl]acetic Acid (AZD4017)
-
Scott, J. S.; Bowker, S. S.; deSchoolmeester, J.; Gerhardt, S.; Hargreaves, D.; Kilgour, E.; Lloyd, A.; Mayers, R. M.; McCoull, W.; Newcombe, N. J.; Ogg, D.; Packer, M. J.; Rees, A.; Revill, J.; Schofield, P.; Selmi, N.; Swales, J. G.; Whittamore, P. R. O. Discovery of a Potent, Selective, and Orally Bioavailable Acidic 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitor: Discovery of 2-[(3S)-1-[5-(Cyclohexylcarbamoyl)-6- propylsulfanylpyridin-2-yl]-3-piperidyl]acetic Acid (AZD4017) J. Med. Chem. 2012, 55, 5951-5964
-
(2012)
J. Med. Chem.
, vol.55
, pp. 5951-5964
-
-
Scott, J.S.1
Bowker, S.S.2
Deschoolmeester, J.3
Gerhardt, S.4
Hargreaves, D.5
Kilgour, E.6
Lloyd, A.7
Mayers, R.M.8
McCoull, W.9
Newcombe, N.J.10
Ogg, D.11
Packer, M.J.12
Rees, A.13
Revill, J.14
Schofield, P.15
Selmi, N.16
Swales, J.G.17
Whittamore, P.R.O.18
-
6
-
-
84867574474
-
Optimisation of Pharmacokinetic Properties in a Neutral Series of 11β-HSD1 Inhibitors
-
Scott, J. S.; Gill, A. L.; Godfrey, L.; Groombridge, S. D.; Rees, A.; Revill, J.; Schofield, P.; Sörme, P.; Stocker, A.; Swales, J. G.; Whittamore, P. R. O. Optimisation of Pharmacokinetic Properties in a Neutral Series of 11β-HSD1 Inhibitors Bioorg. Med. Chem. Lett. 2012, 22, 6756-6761
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 6756-6761
-
-
Scott, J.S.1
Gill, A.L.2
Godfrey, L.3
Groombridge, S.D.4
Rees, A.5
Revill, J.6
Schofield, P.7
Sörme, P.8
Stocker, A.9
Swales, J.G.10
Whittamore, P.R.O.11
-
7
-
-
33947485697
-
A mathematical contribution to structure-activity studies
-
Free, S. M., Jr.; Wilson, J. W. A mathematical contribution to structure-activity studies J. Med. Chem. 1964, 7, 395-399
-
(1964)
J. Med. Chem.
, vol.7
, pp. 395-399
-
-
Free Jr., S.M.1
Wilson, J.W.2
-
8
-
-
84856397312
-
Maximizing lipophilic efficiency: The use of free-wilson analysis in the design of inhibitors of acetyl-CoA carboxylase
-
Freeman-Cook, K. D.; Amor, P.; Bader, S.; Buzon, L. M.; Coffey, S. B.; Corbett, J. W.; Dirico, K. J.; Doran, S. D.; Elliott, R. L.; Esler, W.; Guzman-Perez, A.; Henegar, K. E.; Houser, J. A.; Jones, C. S.; Limberakis, C.; Loomis, K.; McPherson, K.; Murdande, S.; Nelson, K. L.; Phillion, D.; Pierce, B. S.; Song, W.; Sugarman, E.; Tapley, S.; Tu, M.; Zhao, Z. Maximizing lipophilic efficiency: The use of free-wilson analysis in the design of inhibitors of acetyl-CoA carboxylase J. Med. Chem. 2012, 55, 935-942
-
(2012)
J. Med. Chem.
, vol.55
, pp. 935-942
-
-
Freeman-Cook, K.D.1
Amor, P.2
Bader, S.3
Buzon, L.M.4
Coffey, S.B.5
Corbett, J.W.6
Dirico, K.J.7
Doran, S.D.8
Elliott, R.L.9
Esler, W.10
Guzman-Perez, A.11
Henegar, K.E.12
Houser, J.A.13
Jones, C.S.14
Limberakis, C.15
Loomis, K.16
McPherson, K.17
Murdande, S.18
Nelson, K.L.19
Phillion, D.20
Pierce, B.S.21
Song, W.22
Sugarman, E.23
Tapley, S.24
Tu, M.25
Zhao, Z.26
more..
-
9
-
-
57349117629
-
Assessment of Additive/Nonadditive Effects in Structure-Activity Relationships: Implications for Iterative Drug Design
-
Patel, Y.; Gillet, V. J.; Howe, T.; Pastor, J.; Oyarzabal, J.; Willett, P. Assessment of Additive/Nonadditive Effects in Structure-Activity Relationships: Implications for Iterative Drug Design J. Med. Chem. 2008, 51, 7552-7562
-
(2008)
J. Med. Chem.
, vol.51
, pp. 7552-7562
-
-
Patel, Y.1
Gillet, V.J.2
Howe, T.3
Pastor, J.4
Oyarzabal, J.5
Willett, P.6
-
10
-
-
79953235168
-
Crystal structures of 11β-hydroxysteroid dehydrogenase type 1 and their use in drug discovery
-
Thomas, M. P.; Potter, B. V. L. Crystal structures of 11β-hydroxysteroid dehydrogenase type 1 and their use in drug discovery Future Med. Chem. 2011, 3, 367-390
-
(2011)
Future Med. Chem.
, vol.3
, pp. 367-390
-
-
Thomas, M.P.1
Potter, B.V.L.2
-
11
-
-
0035877598
-
Functional Expression, Characterization, and Purification of the Catalytic Domain of Human 11-beta-Hydroxysteroid Dehydrogenase Type 1
-
Walker, E. A.; Clark, A. M.; Hewison, M.; Ride, J. P.; Stewart, P. M. Functional Expression, Characterization, and Purification of the Catalytic Domain of Human 11-beta-Hydroxysteroid Dehydrogenase Type 1 J. Biol. Chem. 2001, 276, 21343-21350
-
(2001)
J. Biol. Chem.
, vol.276
, pp. 21343-21350
-
-
Walker, E.A.1
Clark, A.M.2
Hewison, M.3
Ride, J.P.4
Stewart, P.M.5
-
12
-
-
0037133133
-
11β-Hydroxysteroid Dehydrogenase Type 1 from Human Liver: Dimerization and Enzyme Cooperativity Support Its Postulated Role as Glucocorticoid Reductase
-
Maser, E.; Voelker, B.; Friebertshaeuser, J. 11β-Hydroxysteroid Dehydrogenase Type 1 from Human Liver: Dimerization and Enzyme Cooperativity Support Its Postulated Role as Glucocorticoid Reductase Biochemistry 2002, 41, 2459-2465
-
(2002)
Biochemistry
, vol.41
, pp. 2459-2465
-
-
Maser, E.1
Voelker, B.2
Friebertshaeuser, J.3
-
13
-
-
14244252559
-
Conformational Flexibility in Crystal Structures of Human 11{beta}-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{beta}-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
-
14
-
-
80053102360
-
Substrate Binding Process and Mechanistic Functioning of Type 1 11β-Hydroxysteroid Dehydrogenase from Enhanced Sampling Methods
-
Favia, A. D.; Masetti, M.; Recanatini, M.; Cavalli, A. Substrate Binding Process and Mechanistic Functioning of Type 1 11β-Hydroxysteroid Dehydrogenase from Enhanced Sampling Methods PLoS ONE 2011, 6, e25375
-
(2011)
PLoS ONE
, vol.6
, pp. 25375
-
-
Favia, A.D.1
Masetti, M.2
Recanatini, M.3
Cavalli, A.4
-
15
-
-
18244364603
-
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 (N. Y.) 2005, 44, 6948-6957
-
(2005)
Biochemistry (N. Y.)
, 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
-
16
-
-
84871006287
-
-
Schrödinger, LLC: New York, NY
-
Maestro; Schrödinger, LLC: New York, NY, 2011; 9.2.
-
(2011)
Maestro
, vol.92
-
-
-
17
-
-
77749315417
-
Lipophilicity in drug discovery
-
Waring, M. J. Lipophilicity in drug discovery Expert Opin. Drug Discovery 2010, 5, 235-248
-
(2010)
Expert Opin. Drug Discovery
, vol.5
, pp. 235-248
-
-
Waring, M.J.1
-
18
-
-
65449179589
-
Defining optimum lipophilicity and molecular weight ranges for drug candidates-Molecular weight dependent lower logD limits based on permeability
-
Waring, M. J. Defining optimum lipophilicity and molecular weight ranges for drug candidates-Molecular weight dependent lower logD limits based on permeability Bioorg. Med. Chem. Lett. 2009, 19, 2844-2851
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 2844-2851
-
-
Waring, M.J.1
-
19
-
-
0033105754
-
Hypertension in mice lacking 11β-hydroxysteroid dehydrogenase type 2
-
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
-
(1999)
J. Clin. Invest.
, vol.103
, pp. 683-689
-
-
Kotelevtsev, Y.1
Brown, R.W.2
Fleming, S.3
Kenyon, C.4
Edwards, C.R.W.5
Seckl, J.R.6
Mullins, J.J.7
-
20
-
-
58149343771
-
Time of the day for 11β-HSD1 inhibition plays a role in improving glucose homeostasis in DIO mice
-
Veniant, M. M.; Hale, C.; Komorowski, R.; Chen, M. M.; St., J., D. J.; Fotsch, C.; Wang, M. Time of the day for 11β-HSD1 inhibition plays a role in improving glucose homeostasis in DIO mice Diabetes, Obes. Metab. 2009, 11, 109-117
-
(2009)
Diabetes, Obes. Metab.
, vol.11
, pp. 109-117
-
-
Veniant, M.M.1
Hale, C.2
Komorowski, R.3
Chen, M.M.4
St., J.D.J.5
Fotsch, C.6
Wang, M.7
|