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

Jing Xu, David J. Lloyd, Clarence Hale, +13

Diabetes

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

Elizabeth A. Killion, Jinghong Wang, Junming Yie, +22

Science Translational Medicine

Glp-1r AgonistsAnti-obesity EffectsImmunologyAnti-gipr AntibodiesPharmacotherapy +18

Pharmacologic Effects of FGF21 Are Independent of the “Browning” of White Adipose Tissue

Murielle M. Véniant, Glenn Sivits, Joan Helmering, +5

Cell Metabolism

Metabolic SyndromeMetabolic DisorderMedicinePathologyFibroblast Growth Factor +8

Chronic glucose-dependent insulinotropic polypeptide receptor (GIPR) agonism desensitizes adipocyte GIPR activity mimicking functional GIPR antagonism

Elizabeth A. Killion, Michelle Chen, James R. Falsey, +10

Nature Communications

Long-Term Inhibition of the Glucagon Receptor with a Monoclonal Antibody in Mice Causes Sustained Improvement in Glycemic Control, with Reversible α-Cell Hyperplasia and Hyperglucagonemia

Wei Gu, Hai Yan, Katherine A. Winters, +12

Journal of Pharmacology and Experimental Therapeutics

Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors

David J. Lloyd, David J. St. Jean, Robert J. Kurzeja, +26

Nature

BiochemistryMedicineInsulin ManagementDiabetesAntidiabetic Effects +4

Glucagon receptor antagonist-mediated improvements in glycemic control are dependent on functional pancreatic GLP-1 receptor

Wei Gu, Katherine A. Winters, Alykhan Motani, +12

American Journal of Physiology-Endocrinology and Metabolism

Metabolic SyndromeGlucose ToleranceDiabetes ManagementMedicineInsulin Management +13

Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 3. Structure–Activity Relationships within the Aryl Carbinol Region of the <i>N</i>-Arylsulfonamido-<i>N</i>′-arylpiperazine Series

Nobuko Nishimura, Mark H. Norman, Longbin Liu, +17

Journal of Medicinal Chemistry

Molecular BiologyChemical BiologyStructure–activity RelationshipsInsulin SignalingMolecular Pharmacology +20

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

Lewis D. Pennington, Michael D. Bartberger, Michael D. Croghan, +29

Journal of Medicinal Chemistry

Molecular BiologyPeptide ScienceAnalytical UltracentrifugationChemical BiologyPharmaceutical Chemistry +20

Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 1. Discovery of a Novel Tool Compound for in Vivo Proof-of-Concept

Kate S. Ashton, Kristin L. Andrews, Marion C. Bryan, +21

Journal of Medicinal Chemistry

GlycobiologyMolecular BiologyExcessive Glucose TurnoverProtein ExpressionNovel Tool Compound +19