Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors.
暂无分享,去创建一个
Cristian Bodin | Andrew G Leach | James S. Scott | A. Leach | Frederick W Goldberg | James S Scott | Wendy L Snelson | Sam D Groombridge | Craig S Donald | Stuart N L Bennett | Pablo Morentin Gutierrez | Amy C Gyte | A. Gyte | Wendy L. Snelson | P. M. Gutierrez | S. Groombridge | S. Bennett | C. Bodin | F. Goldberg | Craig S. Donald
[1] M. Waring. Lipophilicity in drug discovery , 2010, Expert Opinion on Drug Discovery.
[2] C. Edwards,et al. Hypertension in mice lacking 11beta-hydroxysteroid dehydrogenase type 2. , 1999, The Journal of clinical investigation.
[3] R. Ge,et al. 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors as Promising Therapeutic Drugs for Diabetes: Status and Development , 2010 .
[4] Peter Willett,et al. Assessment of additive/nonadditive effects in structure-activity relationships: implications for iterative drug design. , 2008, Journal of medicinal chemistry.
[5] M. Véniant,et al. Time of the day for 11β‐HSD1 inhibition plays a role in improving glucose homeostasis in DIO mice , 2009, Diabetes, obesity & metabolism.
[6] Jiandong Zhang,et al. Crystal structure of murine 11 beta-hydroxysteroid dehydrogenase 1: an important therapeutic target for diabetes. , 2005, Biochemistry.
[7] A. Gill,et al. Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors. , 2012, Bioorganic & medicinal chemistry letters.
[8] E. Maser,et al. 11 Beta-hydroxysteroid dehydrogenase type 1 from human liver: dimerization and enzyme cooperativity support its postulated role as glucocorticoid reductase. , 2002, Biochemistry.
[9] Angelo D. Favia,et al. Substrate Binding Process and Mechanistic Functioning of Type 1 11β-Hydroxysteroid Dehydrogenase from Enhanced Sampling Methods , 2011, PloS one.
[10] J. Tomlinson,et al. 11β-Hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes , 2010, Expert opinion on investigational drugs.
[11] M. Hewison,et al. Functional Expression, Characterization, and Purification of the Catalytic Domain of Human 11-β-Hydroxysteroid Dehydrogenase Type 1* , 2001, The Journal of Biological Chemistry.
[12] Eliot Sugarman,et al. Maximizing lipophilic efficiency: the use of Free-Wilson analysis in the design of inhibitors of acetyl-CoA carboxylase. , 2012, Journal of medicinal chemistry.
[13] M. Waring. Defining optimum lipophilicity and molecular weight ranges for drug candidates-Molecular weight dependent lower logD limits based on permeability. , 2009, Bioorganic & medicinal chemistry letters.
[14] B. Potter,et al. Crystal structures of 11β-hydroxysteroid dehydrogenase type 1 and their use in drug discovery. , 2011, Future medicinal chemistry.
[15] D. Hosfield,et al. Conformational Flexibility in Crystal Structures of Human 11β-Hydroxysteroid Dehydrogenase Type I Provide Insights into Glucocorticoid Interconversion and Enzyme Regulation* , 2005, Journal of Biological Chemistry.
[16] S. Free,et al. A MATHEMATICAL CONTRIBUTION TO STRUCTURE-ACTIVITY STUDIES. , 1964, Journal of medicinal chemistry.
[17] Martin J Packer,et al. 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). , 2012, Journal of medicinal chemistry.
[18] D. Mikhailidis,et al. Clinical review: The pathogenetic role of cortisol in the metabolic syndrome: a hypothesis. , 2009, The Journal of clinical endocrinology and metabolism.