Publications by authors named "Jean Whaley"

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Discovery of liver-selective glucokinase activators comprising N-(4-alkylthiazol-2-yl)benzamides and N-(3-alkyl-1,2,4-thiadiazol-5-yl)benzamides for the treatment of metabolic disorders.
David S Yoon, Shung Wu, Sean S Chen, Rebecca A Smirk, Robert P Brigance, Jean Whaley

Bioorg Med Chem Lett· July 2025

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Discovery of (BMS-986172) as a Highly Potent MGAT2 Inhibitor that Achieved Targeted Efficacious Exposures at a Low Human Dose for the Treatment of Metabolic Disorders.
Wei Meng, Robert Brigance, James Mignone, Lidet Negash, Guohua Zhao, Jean Whaley

J Med Chem· September 2023

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Discovery of novel pyridinones as MGAT2 inhibitors for the treatment of metabolic disorders.
Fang Moore, Wei Wang, Guohua Zhao, James Mignone, Wei Meng, Jean M Whaley

Bioorg Med Chem Lett· July 2023

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Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities.
Elizabeth A Jurica, Ximao Wu, Kristin N Williams, Lauren E Haque, Richard A Rampulla, Jean M Whaley

Bioorg Med Chem· May 2023

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Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1-pyrazol-1-yl)methyl)phosphonate (BMS-820132).
Yan Shi, Ying Wang, Wei Meng, Robert P Brigance, Denis E Ryono, Jean Whaley

J Med Chem· March 2022

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Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
Huji Turdi, Hannguang Chao, Jon J Hangeland, Saleem Ahmad, Wei Meng, Jean M Whaley

J Med Chem· October 2021

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SGLT2 knockout prevents hyperglycemia and is associated with reduced pancreatic β-cell death in genetically obese mice.
Michael J Jurczak, Saumya Saini, Simona Ioja, Diana K Costa, Nnamdi Udeh, Jean M Whaley

Islets· May 2019

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Unique pharmacology of a novel allosteric agonist/sensitizer insulin receptor monoclonal antibody.
Simon A Hinke, Anne M Cieniewicz, Thomas Kirchner, Katharine D'Aquino, Rupesh Nanjunda, Jean M Whaley

Mol Metab· April 2018

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Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.
Jun Shi, Zhengxiang Gu, Elizabeth Anne Jurica, Ximao Wu, Lauren E Haque, Jean M Whaley

J Med Chem· February 2018

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Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.
Elizabeth A Jurica, Ximao Wu, Kristin N Williams, Andres S Hernandez, David S Nirschl, Jean M Whaley

J Med Chem· February 2017

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Novel Monoclonal Antibody Is an Allosteric Insulin Receptor Antagonist That Induces Insulin Resistance.
Anne M Cieniewicz, Thomas Kirchner, Simon A Hinke, Rupesh Nanjunda, Katharine D'Aquino, Jean M Whaley

Diabetes· January 2017

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Nonclinical toxicology assessments support the chronic safety of dapagliflozin, a first-in-class sodium-glucose cotransporter 2 inhibitor.
Mark Tirmenstein, Thomas E Dorr, Evan B Janovitz, Deborah Hagan, Lynn M Abell, Jean M Whaley

Int J Toxicol· June 2014

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Carcinogenicity risk assessment supports the chronic safety of dapagliflozin, an inhibitor of sodium-glucose co-transporter 2, in the treatment of type 2 diabetes mellitus.
Timothy P Reilly, Michael J Graziano, Evan B Janovitz, Thomas E Dorr, Craig Fairchild, Jean M Whaley

Diabetes Ther· June 2014

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Targeting the kidney and glucose excretion with dapagliflozin: preclinical and clinical evidence for SGLT2 inhibition as a new option for treatment of type 2 diabetes mellitus.
Jean M Whaley, Mark Tirmenstein, Timothy P Reilly, Simon M Poucher, Joanne Saye

Diabetes Metab Syndr Obes· October 2012

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Targeting renal glucose reabsorption for the treatment of type 2 diabetes mellitus using the SGLT2 inhibitor dapagliflozin.
Serge A Jabbour, Jean M Whaley, Mark Tirmenstein, Simon M Poucher, Timothy P Reilly

Postgrad Med· July 2012

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Acute and chronic effects of SGLT2 blockade on glomerular and tubular function in the early diabetic rat.
Scott C Thomson, Timo Rieg, Cynthia Miracle, Hadi Mansoury, Jean Whaley

Am J Physiol Regul Integr Comp Physiol· January 2012

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SGLT2 deletion improves glucose homeostasis and preserves pancreatic beta-cell function.
Michael J Jurczak, Hui-Young Lee, Andreas L Birkenfeld, Francois R Jornayvaz, David W Frederick, Jean M Whaley

Diabetes· March 2011

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Glucose dynamics and mechanistic implications of SGLT2 inhibitors in animals and humans.
James F List, Jean M Whaley

Kidney Int Suppl· March 2011

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SGLT2 mediates glucose reabsorption in the early proximal tubule.
Volker Vallon, Kenneth A Platt, Robyn Cunard, Jana Schroth, Jean Whaley

J Am Soc Nephrol· January 2011

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Quantitative PCR tissue expression profiling of the human SGLT2 gene and related family members.
Jian Chen, Sandy Williams, Samantha Ho, Howard Loraine, Deborah Hagan, Jean M Whaley

Diabetes Ther· December 2010

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Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity.
Claudio Mapelli, Sesha I Natarajan, Jean-Philippe Meyer, Margarita M Bastos, Michael S Bernatowicz, Jean M Whaley

J Med Chem· December 2009

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Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.
Bruce A Ellsworth, Wei Meng, Manorama Patel, Ravindar N Girotra, Gang Wu, Jean M Whaley

Bioorg Med Chem Lett· September 2008

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Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats.
Songping Han, Deborah L Hagan, Joseph R Taylor, Li Xin, Wei Meng, Jean M Whaley

Diabetes· June 2008

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Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
Wei Meng, Bruce A Ellsworth, Alexandra A Nirschl, Peggy J McCann, Manorama Patel, Jean M Whaley

J Med Chem· March 2008

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The dual peroxisome proliferator-activated receptor alpha/gamma activator muraglitazar prevents the natural progression of diabetes in db/db mice.
Effie Tozzo, Randolph Ponticiello, JoAnn Swartz, Dennis Farrelly, Rachel Zebo, Jean Whaley

J Pharmacol Exp Ther· April 2007

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