Targeting hepatic glucose metabolism in the treatment of type 2 diabetes

Effects of multiple ascending doses of the glucagon receptor antagonist PF-06291874 in patients with type 2 diabetes mellitus

(2016) D. J. Kazierad et al.   DIABETES OBESITY & METABOLISM

The pathogenesis of insulin resistance: integrating signaling pathways and substrate flux

(2016) Varman T. Samuel et al.   JOURNAL OF CLINICAL INVESTIGATION

Development of potent small-molecule inhibitors to drug the undruggable steroid receptor coactivator-3

(2016) Xianzhou Song et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The nuclear retinoid-related orphan receptor-α regulates adipose tissue glyceroneogenesis in addition to hepatic gluconeogenesis

(2015) Sarah Kadiri et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Mitochondrial pyruvate transport: a historical perspective and future research directions

(2015) Kyle S. McCommis et al.   BIOCHEMICAL JOURNAL

Hepatic Acetyl CoA Links Adipose Tissue Inflammation to Hepatic Insulin Resistance and Type 2 Diabetes

(2015) Rachel J. Perry et al.   CELL

Hepatic Mitochondrial Pyruvate Carrier 1 Is Required for Efficient Regulation of Gluconeogenesis and Whole-Body Glucose Homeostasis

(2015) Lawrence R. Gray et al.   Cell Metabolism

Loss of Mitochondrial Pyruvate Carrier 2 in the Liver Leads to Defects in Gluconeogenesis and Compensation via Pyruvate-Alanine Cycling

(2015) Kyle S. McCommis et al.   Cell Metabolism

Evaluation of Efficacy and Safety of the Glucagon Receptor Antagonist LY2409021 in Patients With Type 2 Diabetes: 12- and 24-Week Phase 2 Studies

(2015) Christof M. Kazda et al.   DIABETES CARE

AMG 151 (ARRY-403), a novel glucokinase activator, decreases fasting and postprandial glycaemia in patients with type 2 diabetes

(2015) L. Katz et al.   DIABETES OBESITY & METABOLISM

Short-term administration of the glucagon receptor antagonist LY2409021 lowers blood glucose in healthy people and in those with type 2 diabetes

(2015) R. P. Kelly et al.   DIABETES OBESITY & METABOLISM

Effects of piragliatin, a glucokinase activator, on fasting and postprandial plasma glucose in patients with type 2 diabetes mellitus

(2015) Jianguo Zhi et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Glucagon receptor antagonism induces increased cholesterol absorption

(2015) Hong-Ping Guan et al.   JOURNAL OF LIPID RESEARCH

Empagliflozin, Cardiovascular Outcomes, and Mortality in Type 2 Diabetes

(2015) Bernard Zinman et al.   NEW ENGLAND JOURNAL OF MEDICINE

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses

(2015) Ariane Hammitzsch et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Controlled-release mitochondrial protonophore reverses diabetes and steatohepatitis in rats

(2015) R. J. Perry et al.   SCIENCE

Protein tyrosine phosphatase 1B (PTP1B): A key regulator and therapeutic target in liver diseases

(2015) Pei-Jie Chen et al.   TOXICOLOGY

Metformin: From Mechanisms of Action to Therapies

(2014) Marc Foretz et al.   Cell Metabolism

Thiazolidinediones and the Promise of Insulin Sensitization in Type 2 Diabetes

(2014) Raymond E. Soccio et al.   Cell Metabolism

Akt-Dependent Phosphorylation of Hepatic FoxO1 Is Compartmentalized on a WD40/ProF Scaffold and Is Selectively Inhibited by aPKC in Early Phases of Diet-Induced Obesity

(2014) M. P. Sajan et al.   DIABETES

Cdkn2a/p16Ink4a Regulates Fasting-Induced Hepatic Gluconeogenesis Through the PKA-CREB-PGC1  Pathway

(2014) K. Bantubungi et al.   DIABETES

Management of Hyperglycemia in Type 2 Diabetes, 2015: A Patient-Centered Approach: Update to a Position Statement of the American Diabetes Association and the European Association for the Study of Diabetes

(2014) Silvio E. Inzucchi et al.   DIABETES CARE

Two novel glucagon receptor antagonists prove effective therapeutic agents in high-fat-fed and obese diabetic mice

(2014) F. P. M. O'Harte et al.   DIABETES OBESITY & METABOLISM

Metformin in Patients With Type 2 Diabetes and Kidney Disease

(2014) Silvio E. Inzucchi et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Targeted deletion of kidney glucose-6 phosphatase leads to nephropathy

(2014) Julie Clar et al.   KIDNEY INTERNATIONAL

Regulation of Substrate Utilization by the Mitochondrial Pyruvate Carrier

(2014) Nathaniel M. Vacanti et al.   MOLECULAR CELL

USP7 Attenuates Hepatic Gluconeogenesis Through Modulation of FoxO1 Gene Promoter Occupancy

(2014) Jessica A. Hall et al.   MOLECULAR ENDOCRINOLOGY

A phase 2 trial of the GSK-3 inhibitor tideglusib in progressive supranuclear palsy

(2014) Eduardo Tolosa et al.   MOVEMENT DISORDERS

Metformin suppresses gluconeogenesis by inhibiting mitochondrial glycerophosphate dehydrogenase

(2014) Anila K. Madiraju et al.   NATURE

Cyclin D1–Cdk4 controls glucose metabolism independently of cell cycle progression

(2014) Yoonjin Lee et al.   NATURE

Targeting the disordered C terminus of PTP1B with an allosteric inhibitor

(2014) Navasona Krishnan et al.   Nature Chemical Biology

REV-ERB and ROR nuclear receptors as drug targets

(2014) Douglas J. Kojetin et al.   NATURE REVIEWS DRUG DISCOVERY

The Hepatoselective Glucokinase Activator PF-04991532 Ameliorates Hyperglycemia without Causing Hepatic Steatosis in Diabetic Rats

(2014) Derek M. Erion et al.   PLoS One

SIRT1 and other sirtuins in metabolism

(2014) Hung-Chun Chang et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

A link between hepatic glucose production and peripheral energy metabolism via hepatokines

(2014) Aya Abdul-Wahed et al.   Molecular Metabolism

Options for Combination Therapy in Type 2 Diabetes: Comparison of the ADA/EASD Position Statement and AACE/ACE Algorithm

(2013) Timothy Bailey   AMERICAN JOURNAL OF MEDICINE

Glucose homeostasis, obesity and diabetes

(2013) Gul Bano   BEST PRACTICE & RESEARCH CLINICAL OBSTETRICS & GYNAECOLOGY

Reversal of Hypertriglyceridemia, Fatty Liver Disease, and Insulin Resistance by a Liver-Targeted Mitochondrial Uncoupler

(2013) Rachel J. Perry et al.   Cell Metabolism

Targeting Pyruvate Carboxylase Reduces Gluconeogenesis and Adiposity and Improves Insulin Resistance

(2013) N. Kumashiro et al.   DIABETES

Epidemiology and Molecular Mechanisms Tying Obesity, Diabetes, and the Metabolic Syndrome With Cancer

(2013) E. J. Gallagher et al.   DIABETES CARE

Dose-ranging study with the glucokinase activator AZD1656 as monotherapy in Japanese patients with type 2 diabetes mellitus

(2013) A. Kiyosue et al.   DIABETES OBESITY & METABOLISM

Inducible liver-specific knockdown of protein tyrosine phosphatase 1B improves glucose and lipid homeostasis in adult mice

(2013) C. Owen et al.   DIABETOLOGIA

Small molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases

(2013) Frank J. Dekker et al.   DRUG DISCOVERY TODAY

AMPK, insulin resistance, and the metabolic syndrome

(2013) Neil B. Ruderman et al.   JOURNAL OF CLINICAL INVESTIGATION

Forkhead box class O transcription factors in liver function and disease

(2013) Irina Tikhanovich et al.   JOURNAL OF GASTROENTEROLOGY AND HEPATOLOGY

Autophagy in the liver

(2013) Patrice Codogno et al.   JOURNAL OF HEPATOLOGY

AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans

(2013) Biljana Georgievska et al.   JOURNAL OF NEUROCHEMISTRY

Pathophysiology and treatment of type 2 diabetes: perspectives on the past, present, and future

(2013) Steven E Kahn et al.   LANCET

Biguanides suppress hepatic glucagon signalling by decreasing production of cyclic AMP

(2013) Russell A. Miller et al.   NATURE

Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors

(2013) David J. Lloyd et al.   NATURE

Direct assessment of hepatic mitochondrial oxidative and anaplerotic fluxes in humans using dynamic 13C magnetic resonance spectroscopy

(2013) Douglas E Befroy et al.   NATURE MEDICINE

Single phosphorylation sites in Acc1 and Acc2 regulate lipid homeostasis and the insulin-sensitizing effects of metformin

(2013) Morgan D Fullerton et al.   NATURE MEDICINE

Identification of a Mitochondrial Target of Thiazolidinedione Insulin Sensitizers (mTOT)—Relationship to Newly Identified Mitochondrial Pyruvate Carrier Proteins

(2013) Jerry R. Colca et al.   PLoS One

Thiazolidinediones are acute, specific inhibitors of the mitochondrial pyruvate carrier

(2013) A. S. Divakaruni et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Metformin: an old but still the best treatment for type 2 diabetes

(2013) Lilian Beatriz Aguayo Rojas et al.   Diabetology & Metabolic Syndrome

Fine-Tuning Multiprotein Complexes Using Small Molecules

(2012) Andrea D. Thompson et al.   ACS Chemical Biology

Efficacy and Safety Profile Evaluation of Acarbose Alone and in Association With Other Antidiabetic Drugs: A Systematic Review

(2012) Giuseppe Derosa et al.   CLINICAL THERAPEUTICS

Novel Small-Molecule PGC-1  Transcriptional Regulator With Beneficial Effects on Diabetic db/db Mice

(2012) L.-N. Zhang et al.   DIABETES

Discovery of a Novel Glucagon Receptor Antagonist N-[(4-{(1S)-1-[3-(3, 5-Dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the Treatment of Type II Diabetes

(2012) Yusheng Xiong et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Deacetylase Sirt6 Activates the Acetyltransferase GCN5 and Suppresses Hepatic Gluconeogenesis

(2012) John E. Dominy et al.   MOLECULAR CELL

Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists

(2012) Laura A. Solt et al.   NATURE

CITED2 links hormonal signaling to PGC-1α acetylation in the regulation of gluconeogenesis

(2012) Mashito Sakai et al.   NATURE MEDICINE

Identification of Small Molecule Activators of Cryptochrome

(2012) T. Hirota et al.   SCIENCE

Identification and Functional Expression of the Mitochondrial Pyruvate Carrier

(2012) S. Herzig et al.   SCIENCE

A Mitochondrial Pyruvate Carrier Required for Pyruvate Uptake in Yeast, Drosophila, and Humans

(2012) D. K. Bricker et al.   SCIENCE

Regulation of Hepatic Glucose Uptake and Storage In Vivo

(2012) Mary Courtney Moore et al.   Advances in Nutrition

TCF7L2 Modulates Glucose Homeostasis by Regulating CREB- and FoxO1-Dependent Transcriptional Pathway in the Liver

(2012) Kyoung-Jin Oh et al.   PLoS Genetics

Class IIa Histone Deacetylases Are Hormone-Activated Regulators of FOXO and Mammalian Glucose Homeostasis

(2011) Maria M. Mihaylova et al.   CELL

Hormonal Regulation of Hepatic Glucose Production in Health and Disease

(2011) Hua V. Lin et al.   Cell Metabolism

Control of Blood Glucose in the Absence of Hepatic Glucose Production During Prolonged Fasting in Mice: Induction of Renal and Intestinal Gluconeogenesis by Glucagon

(2011) E. Mutel et al.   DIABETES

FoxO6 Integrates Insulin Signaling With Gluconeogenesis in the Liver

(2011) Dae Hyun Kim et al.   DIABETES

Metformin and digestive disorders

(2011) M. Bouchoucha et al.   DIABETES & METABOLISM

Role of Bile Acid Sequestrants in the Treatment of Type 2 Diabetes

(2011) Y. Handelsman   DIABETES CARE

The role of dysregulated glucagon secretion in type 2 diabetes

(2011) D. D'Alessio   DIABETES OBESITY & METABOLISM

Hepatic Suppression ofFoxo1andFoxo3Causes Hypoglycemia and Hyperlipidemia in Mice

(2011) Kebin Zhang et al.   ENDOCRINOLOGY

The REV-ERBs and RORs: molecular links between circadian rhythms and lipid homeostasis

(2011) Laura A Solt et al.   Future Medicinal Chemistry

Separation of the gluconeogenic and mitochondrial functions of PGC-1  through S6 kinase

(2011) Y. Lustig et al.   GENES & DEVELOPMENT

Evidence for Irreversible Inhibition of Glycogen Synthase Kinase-3β by Tideglusib

(2011) Juan Manuel Domínguez et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Hepatic FoxOs Regulate Lipid Metabolism via Modulation of Expression of the Nicotinamide Phosphoribosyltransferase Gene

(2011) Rongya Tao et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of (S)-6-(3-Cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic Acid as a Hepatoselective Glucokinase Activator Clinical Candidate for Treating Type 2 Diabetes Mellitus

(2011) Jeffrey A. Pfefferkorn et al.   JOURNAL OF MEDICINAL CHEMISTRY

Impact of a Glycogen Phosphorylase Inhibitor and Metformin on Basal and Glucagon-Stimulated Hepatic Glucose Flux in Conscious Dogs

(2011) T. P. Torres et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Small Molecule Inhibition of the Steroid Receptor Coactivators, SRC-3 and SRC-1

(2011) Ying Wang et al.   MOLECULAR ENDOCRINOLOGY

The AMPK signalling pathway coordinates cell growth, autophagy and metabolism

(2011) Maria M. Mihaylova et al.   NATURE CELL BIOLOGY

GSK-3 Inhibitors: Preclinical and Clinical Focus on CNS

(2011) Hagit Eldar-Finkelman et al.   Frontiers in Molecular Neuroscience

GSK4112, a Small Molecule Chemical Probe for the Cell Biology of the Nuclear Heme Receptor Rev-erbα

(2010) Daniel Grant et al.   ACS Chemical Biology

Identification of SR3335 (ML-176): A Synthetic RORα Selective Inverse Agonist

(2010) Naresh Kumar et al.   ACS Chemical Biology

Cdc2-like Kinase 2 Is an Insulin-Regulated Suppressor of Hepatic Gluconeogenesis

(2010) Joseph T. Rodgers et al.   Cell Metabolism

The Coactivator SRC-1 Is an Essential Coordinator of Hepatic Glucose Production

(2010) Jean-Francois Louet et al.   Cell Metabolism

Pathogenesis of Fasting and Postprandial Hyperglycemia in Type 2 Diabetes: Implications for Therapy

(2010) R. A. Rizza   DIABETES

Effects of the novel Foxo1 inhibitor AS1708727 on plasma glucose and triglyceride levels in diabetic db/db mice

(2010) Hirotsugu Tanaka et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

FoxOs Function Synergistically to Promote Glucose Production

(2010) Rebecca A. Haeusler et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

AMPK-dependent Repression of Hepatic Gluconeogenesis via Disruption of CREB·CRTC2 Complex by Orphan Nuclear Receptor Small Heterodimer Partner

(2010) Ji-Min Lee et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Metformin inhibits hepatic gluconeogenesis in mice independently of the LKB1/AMPK pathway via a decrease in hepatic energy state

(2010) Marc Foretz et al.   JOURNAL OF CLINICAL INVESTIGATION

Fructose-1,6-bisphosphatase Inhibitors. 2. Design, Synthesis, and Structure−Activity Relationship of a Series of Phosphonic Acid Containing Benzimidazoles that Function as 5′-Adenosinemonophosphate (AMP) Mimics

(2010) Qun Dang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Forkhead Box O1 Inhibitors for Treating Type 2 Diabetes: Improvement of Fasting Glycemia in Diabetic db/db Mice

(2010) T. Nagashima et al.   MOLECULAR PHARMACOLOGY

Cryptochrome mediates circadian regulation of cAMP signaling and hepatic gluconeogenesis

(2010) Eric E Zhang et al.   NATURE MEDICINE

SGLT2 inhibition — a novel strategy for diabetes treatment

(2010) Edward C. Chao et al.   NATURE REVIEWS DRUG DISCOVERY

Inhibition of PTP1B by Trodusquemine (MSI-1436) Causes Fat-specific Weight Loss in Diet-induced Obese Mice

(2010) Kristen A. Lantz et al.   Obesity

Targeted disruption of the CREB coactivator Crtc2 increases insulin sensitivity

(2010) Y. Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Novel therapeutics and targets for the treatment of diabetes

(2010) Thomas D Aicher et al.   Expert Review of Clinical Pharmacology

Nutrient-dependent regulation of PGC-1α's acetylation state and metabolic function through the enzymatic activities of Sirt1/GCN5

(2009) John E. Dominy et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Intestinal gluconeogenesis: key signal of central control of energy and glucose homeostasis

(2009) Gilles Mithieux et al.   CURRENT OPINION IN CLINICAL NUTRITION AND METABOLIC CARE

Sensitivity of Lipid Metabolism and Insulin Signaling to Genetic Alterations in Hepatic Peroxisome Proliferator-Activated Receptor-  Coactivator-1  Expression

(2009) J. L. Estall et al.   DIABETES

Inhibition of Protein Tyrosine Phosphatase-1B with Antisense Oligonucleotides Improves Insulin Sensitivity and Increases Adiponectin Concentrations in Monkeys

(2009) Michael M. Swarbrick et al.   ENDOCRINOLOGY

Assessing the potential of glucokinase activators in diabetes therapy

(2009) Franz M. Matschinsky   NATURE REVIEWS DRUG DISCOVERY

Therapies for hyperglycaemia-induced diabetic complications: from animal models to clinical trials

(2009) Nigel A. Calcutt et al.   NATURE REVIEWS DRUG DISCOVERY

Fasting hyperglycemia is not associated with increased expression of PEPCK or G6Pc in patients with Type 2 Diabetes

(2009) V. T. Samuel et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

New Inhibitors of Glycogen Phosphorylase as Potential Antidiabetic Agents

(2008) L. Somsak et al.   CURRENT MEDICINAL CHEMISTRY

Liver-Specific Deletion of Protein-Tyrosine Phosphatase 1B (PTP1B) Improves Metabolic Syndrome and Attenuates Diet-Induced Endoplasmic Reticulum Stress

(2008) M. Delibegovic et al.   DIABETES

COP1 Functions as a FoxO1 Ubiquitin E3 Ligase to Regulate FoxO1-mediated Gene Expression

(2008) Satomi Kato et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A brief introduction to FOXOlogy

(2008) B M Th Burgering   ONCOGENE

Gene expression-based screening identifies microtubule inhibitors as inducers of PGC-1  and oxidative phosphorylation

(2008) Z. Arany et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Absence of the SRC-2 Coactivator Results in a Glycogenopathy Resembling Von Gierke's Disease

(2008) A. R. Chopra et al.   SCIENCE