C. Hale

发表

Discovery of Small-Molecule Glucokinase Regulatory Protein Modulators That Restore Glucokinase Activity

R. Wahl, R. Kurzeja, Joon-Hee Han, 2014, Journal of biomolecular screening.

FGF21 acts as a negative regulator of bile acid synthesis.

Jing Xu, M. Véniant, C. Hale, 2018, The Journal of endocrinology.

Development of 11β -HSD1 Inhibitors for the Treatment of Type 2 Diabetes

Minghan Wang, C. Hale, 2008 .

Discovery of a potent, orally active 11beta-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).

Jiandong Zhang, R. Syed, R. Hungate, 2010, Journal of medicinal chemistry.

GIPR antagonist antibodies conjugated to GLP-1 peptide are bispecific molecules that decrease weight in obese mice and monkeys

J. Harrold, M. Stolina, Shu-Chen Lu, 2021, Cell reports. Medicine.

Structure-activity relationships of a series of pyrrolo[3,2-d]pyrimidine derivatives and related compounds as neuropeptide Y5 receptor antagonists.

N. Chen, Z. Chen, V. Santora, 2000, Journal of medicinal chemistry.

Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists.

N. Chen, C. Fotsch, M. Norman, 2001, Journal of medicinal chemistry.

High capacity homogeneous non-radioactive cortisol detection assays for human 11beta-hydroxysteroid dehydrogenase type 1.

D. Powers, R. Kurzeja, Minghan Wang, 2007, Assay and drug development technologies.

A high-throughput microfluidic assay for SH2 domain-containing inositol 5-phosphatase 2.

J. McCarter, R. Kurzeja, Minghan Wang, 2006, Assay and drug development technologies.

Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.

Kristin L. Andrews, Jiandong Zhang, S. Chmait, 2015, Journal of medicinal chemistry.

Antidiabetic effects of 11β‐HSD1 inhibition in a mouse model of combined diabetes, dyslipidaemia and atherosclerosis

M. Véniant, Minghan Wang, M. Wang, 2009, Diabetes, obesity & metabolism.

Lack of overt FGF21 resistance in two mouse models of obesity and insulin resistance.

N. Chinookoswong, Jing Xu, M. Véniant, 2012, Endocrinology.

Lack of Overt FGF 21 Resistance in Two Mouse Models of Obesity and Insulin Resistance

N. Chinookoswong, Jing Xu, M. Véniant, 2011 .

Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.

Jiandong Zhang, R. Hungate, M. Véniant, 2008, Journal of medicinal chemistry.

A Volumetric Method for Quantifying Atherosclerosis in Mice by Using MicroCT: Comparison to En Face

M. Véniant, J. Turk, David M. Weinstein, 2011, PloS one.

FGF21 Promotes Metabolic Homeostasis via White Adipose and Leptin in Mice

Jing Xu, M. Véniant, S. Vonderfecht, 2012, PloS one.

FGF21 Reverses Hepatic Steatosis, Increases Energy Expenditure and Improves Insulin Sensitivity in Diet-induced Obese Mice

Jason K. Kim, R. Lindberg, M. Véniant, 2008 .

Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.

N. Chen, C. Fotsch, A. Bannon, 2005, Bioorganic & medicinal chemistry letters.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket.

S. Chmait, M. Bartberger, S. Jordan, 2014, Journal of medicinal chemistry.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.

R. Kunz, Jiandong Zhang, S. Chmait, 2014, Journal of medicinal chemistry.

Time of the day for 11β‐HSD1 inhibition plays a role in improving glucose homeostasis in DIO mice

M. Véniant, C. Fotsch, R. Komorowski, 2009, Diabetes, obesity & metabolism.

Structural Characterization and Pharmacodynamic Effects of an Orally Active 11β‐Hydroxysteroid Dehydrogenase Type 1 Inhibitor

Zhulun Wang, Haoda Xu, Xiaoshan Min, 2007, Chemical biology & drug design.

The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors.

Jiandong Zhang, R. Hungate, Meredith Williams, 2007, Bioorganic & medicinal chemistry letters.

The selectivity of tyrosine 280 of human 11β‐hydroxysteroid dehydrogenase type 1 in inhibitor binding

Zhulun Wang, S. Svensson, Minghan Wang, 2007, FEBS letters.

Determination of prednisolone in human adipose tissue incubation medium using LC-MS/MS to support the measurement of 11beta-hydroxysteroid dehydrogenase activity.

M. Emery, I. McCaffery, J. Rossi, 2009, Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.

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.

Jiandong Zhang, E. Homan, Meredith Williams, 2008, Journal of medicinal chemistry.

Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis.

S. Chmait, M. Bartberger, S. Jordan, 2015, Journal of medicinal chemistry.

2-(S)-phenethylaminothiazolones as potent, orally efficacious inhibitors of 11beta-hydroxysteriod dehydrogenase type 1.

R. Hungate, M. Véniant, Minghan Wang, 2007, Journal of medicinal chemistry.

Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).

Michael G Kelly, J. Cheetham, M. Jarosinski, 2003, Bioorganic & medicinal chemistry letters.

Molecular targeting of the GK-GKRP pathway in diabetes

M. Véniant, A. Pellacani, C. Hale, 2015, Expert opinion on therapeutic targets.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series.

R. Kunz, S. Chmait, M. Bartberger, 2014, Journal of medicinal chemistry.

Long-acting MIC-1/GDF15 molecules to treat obesity: Evidence from mice to monkeys

Hantao Liu, Zhulun Wang, Xiaoshan Min, 2017, Science Translational Medicine.

Fibroblast Growth Factor 21 Reverses Hepatic Steatosis, Increases Energy Expenditure, and Improves Insulin Sensitivity in Diet-Induced Obese Mice

Jason K. Kim, Jing Xu, R. Lindberg, 2009, Diabetes.

Growth differentiation factor 15 as a potential therapeutic for treating obesity

M. Véniant, C. Hale, 2020, Molecular metabolism.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept.

R. Wahl, Jiandong Zhang, S. Chmait, 2014, Journal of medicinal chemistry.

Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors

R. Wahl, Jiandong Zhang, S. Chmait, 2013, Nature.

Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists.

C. Hulme, A. Bannon, J. Salon, 2006, Bioorganic & medicinal chemistry letters.

Characterization of Neuropeptide Y (NPY) Receptors

C. Hale, J. Marasco, W. Karbon, 1998 .

Anti-obesity effects of GIPR antagonists alone and in combination with GLP-1R agonists in preclinical models

D. Bates, C. Murawsky, Zhulun Wang, 2018, Science Translational Medicine.

11β‐Hydroxysteroid Dehydrogenase Type 1 as a Therapeutic Target for Type 2 Diabetes

D. Jean, C. Hale, 2011 .

The evolving systemic biomarker milieu in obese ZSF1 rat model of human cardiometabolic syndrome: Characterization of the model and cardioprotective effect of GDF15

M. Stolina, M. Véniant, Yinhong Chen, 2020, bioRxiv.

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.

Zhulun Wang, S. Svensson, Minghan Wang, 2006, Biochimica et biophysica acta.

Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.

C. Fotsch, Markian M Stec, N. Xi, 2004, Bioorganic & medicinal chemistry letters.

Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding.

J. Cheetham, K. Stark, C. Fotsch, 2003, Journal of medicinal chemistry.

Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.

M. Véniant, R. Subramanian, M. Emery, 2011, ACS medicinal chemistry letters.

Biochemical, biophysical, and pharmacological characterization of bacterially expressed human agouti-related protein.

V. Katta, J. Philo, J. Delaney, 1998, Biochemistry.

human GIPR ECD and Fab complex

Xiaoshan Min, Shu-Chen Lu, M. Véniant, 2018 .