Crystal structures of 11β-hydroxysteroid dehydrogenase type 1 and their use in drug discovery

The development and SAR of pyrrolidine carboxamide 11β-HSD1 inhibitors

(2010) Hengmiao Cheng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors

(2010) Daqing Sun et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of Adamantyl Ethanone Derivatives as Potent 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors

(2010) Xiangdong Su et al.   ChemMedChem

The 11- -Hydroxysteroid Dehydrogenase Type 1 Inhibitor INCB13739 Improves Hyperglycemia in Patients With Type 2 Diabetes Inadequately Controlled by Metformin Monotherapy

(2010) J. Rosenstock et al.   DIABETES CARE

Discovery of a Potent, Orally Active 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor for Clinical Study: Identification of (S)-2-((1S,2S,4R)-Bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221)

(2010) Murielle M. Véniant et al.   JOURNAL OF MEDICINAL CHEMISTRY

11 -Hydroxysteroid Dehydrogenase Type 1 Expression Is Increased in the Aged Mouse Hippocampus and Parietal Cortex and Causes Memory Impairments

(2010) M. C. Holmes et al.   JOURNAL OF NEUROSCIENCE

Partial Deficiency or Short-Term Inhibition of 11 -Hydroxysteroid Dehydrogenase Type 1 Improves Cognitive Function in Aging Mice

(2010) K. Sooy et al.   JOURNAL OF NEUROSCIENCE

Targeting the pre-receptor metabolism of cortisol as a novel therapy in obesity and diabetes

(2010) Laura L. Gathercole et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

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

(2009) Michael Siu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors

(2009) Dustin L. McMinn et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11β-HSD1 inhibitors

(2009) Yosup Rew et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

11β-hydroxysteroid dehydrogenase type 1 inhibitors: a review of recent patents

(2009) Craig D Boyle et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Efficacious 11β-Hydroxysteroid Dehydrogenase Type I Inhibitors in the Diet-Induced Obesity Mouse Model

(2009) Zhao-Kui Wan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Obesity and corticosteroids: 11β-Hydroxysteroid type 1 as a cause and therapeutic target in metabolic disease

(2009) Nicholas Michael Morton   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Mutations of key hydrophobic surface residues of 11β-hydroxysteroid dehydrogenase type 1 increase solubility and monodispersity in a bacterial expression system

(2009) Alexander J. Lawson et al.   PROTEIN SCIENCE

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

(2008) Hua Tu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery and Initial SAR of Arylsulfonylpiperazine Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1)

(2008) Daqing Sun et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2008) Haixia Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2008) Yuping Zhu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

11-Beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors in Type 2 diabetes mellitus and obesity

(2008) Katherine A Hughes et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Piperazine Sulfonamides as Potent, Selective, and Orally Available 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors with Efficacy in the Rat Cortisone-Induced Hyperinsulinemia Model

(2008) Jason Xiang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel, Potent Benzamide Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Exhibiting Oral Activity in an Enzyme Inhibition ex Vivo Model▽

(2008) Lisa D. Julian et al.   JOURNAL OF MEDICINAL CHEMISTRY

Further Studies with the 2-Amino-1,3-thiazol-4(5H)-one Class of 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Reducing Pregnane X Receptor Activity and Exploring Activity in a Monkey Pharmacodynamic Model

(2008) Christopher Fotsch et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2008) Lars Johansson et al.   JOURNAL OF MEDICINAL CHEMISTRY