Fibroblast growth factor 21: A “rheostat” for metabolic regulation?

A feed-forward regulatory loop in adipose tissue promotes signaling by the hepatokine FGF21

(2021) Myoung Sook Han et al.   GENES & DEVELOPMENT

A novel GLP-1 and FGF21 dual agonist has therapeutic potential for diabetes and non-alcoholic steatohepatitis

(2021) Qi Pan et al.   EBioMedicine

Efruxifermin in non-alcoholic steatohepatitis: a randomized, double-blind, placebo-controlled, phase 2a trial

(2021) Stephen A. Harrison et al.   NATURE MEDICINE

Th2 Cytokines Increase the Expression of Fibroblast Growth Factor 21 in the Liver

(2021) Seul-Gi Kang et al.   Cells

Targeting FGF21 for the Treatment of Nonalcoholic Steatohepatitis

(2020) Mohammad Zarei et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Fasting-induced FGF21 signaling activates hepatic autophagy and lipid degradation via JMJD3 histone demethylase

(2020) Sangwon Byun et al.   Nature Communications

The Effects of B1344, a Novel Fibroblast Growth Factor 21 Analog, on Nonalcoholic Steatohepatitis in Nonhuman Primates

(2020) Aoyuan Cui et al.   DIABETES

Development of a long acting FGF21 analogue-albumin fusion protein and its anti-diabetic effects

(2020) Hiroshi Watanabe et al.   JOURNAL OF CONTROLLED RELEASE

A Genetic Model to Study the Contribution of Brown and Brite Adipocytes to Metabolism

(2020) Tenagne D. Challa et al.   Cell Reports

FGF21 Signals to Glutamatergic Neurons in the Ventromedial Hypothalamus to Suppress Carbohydrate Intake

(2020) Sharon O. Jensen-Cody et al.   Cell Metabolism

Fibroblast growth factor-21 potentiates glucose transport in skeletal muscle fibers

(2020) G Rosales-Soto et al.   JOURNAL OF MOLECULAR ENDOCRINOLOGY

The therapeutic potential of FGF21 in metabolic diseases: from bench to clinic

(2020) Leiluo Geng et al.   Nature Reviews Endocrinology

Hypoxia-Induced Adipose Lipolysis Requires Fibroblast Growth Factor 21

(2020) Guicheng Wu et al.   Frontiers in Pharmacology

Discovery of a novel fibroblast activation protein (FAP) inhibitor, BR103354, with anti-diabetic and anti-steatotic effects

(2020) Jae Min Cho et al.   Scientific Reports

Liver-derived fibroblast growth factor 21 mediates effects of glucagon-like peptide-1 in attenuating hepatic glucose output

(2019) Junling Liu et al.   EBioMedicine

YIPF6 controls sorting of FGF21 into COPII vesicles and promotes obesity

(2019) Lirui Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

FGF21 Signals Protein Status to the Brain and Adaptively Regulates Food Choice and Metabolism

(2019) Cristal M. Hill et al.   Cell Reports

Fibroblast growth factor 21 protects against lipotoxicity-induced pancreatic β-cell dysfunction via regulation of AMPK signaling and lipid metabolism

(2019) Ting Xie et al.   CLINICAL SCIENCE

Paracrine-endocrine FGF chimeras as potent therapeutics for metabolic diseases

(2019) Longwei Zhao et al.   EBioMedicine

The integrative biology of type 2 diabetes

(2019) Michael Roden et al.   NATURE

Liver Plays a Major Role in FGF-21 Mediated Glucose Homeostasis

(2018) Mingyao Liu et al.   CELLULAR PHYSIOLOGY AND BIOCHEMISTRY

A biparatopic agonistic antibody that mimics fibroblast growth factor 21 ligand activity

(2018) Sally Yu Shi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Fibroblast growth factor-21 prevents diabetic cardiomyopathy via AMPK-mediated antioxidation and lipid-lowering effects in the heart

(2018) Hong Yang et al.   Cell Death & Disease

FGF21 is a Hormonal Mediator of the Human “Thrifty” Metabolic Phenotype

(2018) Karyne L. Vinales et al.   DIABETES

Agonistic β-Klotho antibody mimics fibroblast growth factor 21 (FGF21) functions

(2018) Xiaoshan Min et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structures of β-klotho reveal a ‘zip code’-like mechanism for endocrine FGF signalling

(2018) Sangwon Lee et al.   NATURE

Pancreatic fibroblast growth factor 21 protects against type 2 diabetes in mice by promoting insulin expression and secretion in a PI3K/Akt signaling-dependent manner

(2018) Yingying Pan et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Pegbelfermin (BMS-986036), a PEGylated fibroblast growth factor 21 analogue, in patients with non-alcoholic steatohepatitis: a randomised, double-blind, placebo-controlled, phase 2a trial

(2018) Arun Sanyal et al.   LANCET

Pegbelfermin (BMS-986036), PEGylated FGF21, in Patients with Obesity and Type 2 Diabetes: Results from a Randomized Phase 2 Study

(2018) Edgar D. Charles et al.   Obesity

Neuronal SIRT1 regulates macronutrient-based diet selection through FGF21 and oxytocin signalling in mice

(2018) Sho Matsui et al.   Nature Communications

A Novel Fc-FGF21 With Improved Resistance to Proteolysis, Increased Affinity Toward β-Klotho, and Enhanced Efficacy in Mice and Cynomolgus Monkeys

(2017) Shanaka Stanislaus et al.   ENDOCRINOLOGY

Fibroblast growth factor 19 regulates skeletal muscle mass and ameliorates muscle wasting in mice

(2017) Bérengère Benoit et al.   NATURE MEDICINE

A Specific ChREBP and PPARα Cross-Talk Is Required for the Glucose-Mediated FGF21 Response

(2017) Alison Iroz et al.   Cell Reports

Efficacy of a combination of high and low dosage of PEGylated FGF-21 in treatment of diabetes in db/db mice

(2016) Pengfei Xu et al.   BIOMEDICINE & PHARMACOTHERAPY

FGF21 Regulates Sweet and Alcohol Preference

(2016) Saswata Talukdar et al.   Cell Metabolism

Defining the Nutritional and Metabolic Context of FGF21 Using the Geometric Framework

(2016) Samantha M. Solon-Biet et al.   Cell Metabolism

A Long-Acting FGF21 Molecule, PF-05231023, Decreases Body Weight and Improves Lipid Profile in Non-human Primates and Type 2 Diabetic Subjects

(2016) Saswata Talukdar et al.   Cell Metabolism

FGF21 Mediates Endocrine Control of Simple Sugar Intake and Sweet Taste Preference by the Liver

(2016) Stephanie von Holstein-Rathlou et al.   Cell Metabolism

Fibroblast growth factor 21 improves hepatic insulin sensitivity by inhibiting mammalian target of rapamycin complex 1 in mice

(2016) Qi Gong et al.   HEPATOLOGY

Biliverdin Reductase A Attenuates Hepatic Steatosis by Inhibition of Glycogen Synthase Kinase (GSK) 3β Phosphorylation of Serine 73 of Peroxisome Proliferator-activated Receptor (PPAR) α

(2016) Terry D. Hinds et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Fibroblast Activation Protein Cleaves and Inactivates Fibroblast Growth Factor 21

(2016) Diana Ronai Dunshee et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

PF-05231023, a long-acting FGF21 analogue, decreases body weight by reduction of food intake in non-human primates

(2016) W. Clayton Thompson et al.   JOURNAL OF PHARMACOKINETICS AND PHARMACODYNAMICS

Metabolic Responses to Dietary Protein Restriction Require an Increase in FGF21 that Is Delayed by the Absence of GCN2

(2016) Thomas Laeger et al.   Cell Reports

Fibroblast activation protein (FAP) as a novel metabolic target

(2016) Miguel Angel Sánchez-Garrido et al.   Molecular Metabolism

Human FGF-21 Is a Substrate of Fibroblast Activation Protein

(2016) Andrew L. Coppage et al.   PLoS One

Bilirubin Binding to PPARα Inhibits Lipid Accumulation

(2016) David E. Stec et al.   PLoS One

Circulating FGF21 proteolytic processing mediated by fibroblast activation protein

(2015) E. Y. Zhen et al.   BIOCHEMICAL JOURNAL

Role of fibroblast growth factor 21 in the early stage of NASH induced by methionine- and choline-deficient diet

(2015) Naoki Tanaka et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

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

(2015) Murielle M. Véniant et al.   Cell Metabolism

Central Fibroblast Growth Factor 21 Browns White Fat via Sympathetic Action in Male Mice

(2015) Nicholas Douris et al.   ENDOCRINOLOGY

FGF21 deletion exacerbates diabetic cardiomyopathy by aggravating cardiac lipid accumulation

(2015) Xiaoqing Yan et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

FGF21 and the late adaptive response to starvation in humans

(2015) Pouneh K. Fazeli et al.   JOURNAL OF CLINICAL INVESTIGATION

FGF21 mediates alcohol-induced adipose tissue lipolysis by activation of systemic release of catecholamine in mice

(2015) Cuiqing Zhao et al.   JOURNAL OF LIPID RESEARCH

Glucocorticoids Regulate the Metabolic Hormone FGF21 in a Feed-Forward Loop

(2015) Rucha Patel et al.   MOLECULAR ENDOCRINOLOGY

Sustained Brown Fat Stimulation and Insulin Sensitization by a Humanized Bispecific Antibody Agonist for Fibroblast Growth Factor Receptor 1/βKlotho Complex

(2015) Ganesh Kolumam et al.   EBioMedicine

Pharmacokinetics (PK), Pharmacodynamics (PD) and Integrated PK/PD Modeling of a Novel Long Acting FGF21 Clinical Candidate PF-05231023 in Diet-Induced Obese and Leptin-Deficient Obese Mice

(2015) Yan Weng et al.   PLoS One

Methionine restriction restores a younger metabolic phenotype in adult mice with alterations in fibroblast growth factor 21

(2014) Emma K. Lees et al.   AGING CELL

FGF21 Acts Centrally to Induce Sympathetic Nerve Activity, Energy Expenditure, and Weight Loss

(2014) Bryn M. Owen et al.   Cell Metabolism

FGF21 Maintains Glucose Homeostasis by Mediating the Cross Talk Between Liver and Brain During Prolonged Fasting

(2014) Q. Liang et al.   DIABETES

Circulating FGF21 Is Liver Derived and Enhances Glucose Uptake During Refeeding and Overfeeding

(2014) K. R. Markan et al.   DIABETES

Fibroblast growth factor 21 participates in adaptation to endoplasmic reticulum stress and attenuates obesity-induced hepatic metabolic stress

(2014) Seong Hun Kim et al.   DIABETOLOGIA

Orphan Nuclear Receptor Nur77 Mediates Fasting-Induced Hepatic Fibroblast Growth Factor 21 Expression

(2014) Ae-Kyung Min et al.   ENDOCRINOLOGY

Liver-Enriched Transcription Factor CREBH Interacts With Peroxisome Proliferator-Activated Receptor α to Regulate Metabolic Hormone FGF21

(2014) Hyunbae Kim et al.   ENDOCRINOLOGY

Fibroblast Growth Factor 21 Limits Lipotoxicity by Promoting Hepatic Fatty Acid Activation in Mice on Methionine and Choline-Deficient Diets

(2014) Ffolliott M. Fisher et al.   GASTROENTEROLOGY

FGF21 is an endocrine signal of protein restriction

(2014) Thomas Laeger et al.   JOURNAL OF CLINICAL INVESTIGATION

Fasting increases serum bilirubin levels in clinically normal, healthy males but not females: a retrospective study from phase I clinical trial participants

(2014) Paul M Griffin et al.   JOURNAL OF CLINICAL PATHOLOGY

Glucagon Stimulates Hepatic FGF21 Secretion through a PKA- and EPAC-Dependent Posttranscriptional Mechanism

(2014) Holly A. Cyphert et al.   PLoS One

Adiponectin Mediates the Metabolic Effects of FGF21 on Glucose Homeostasis and Insulin Sensitivity in Mice

(2013) Zhuofeng Lin et al.   Cell Metabolism

An FGF21-Adiponectin-Ceramide Axis Controls Energy Expenditure and Insulin Action in Mice

(2013) William L. Holland et al.   Cell Metabolism

The Effects of LY2405319, an FGF21 Analog, in Obese Human Subjects with Type 2 Diabetes

(2013) Gregory Gaich et al.   Cell Metabolism

Pegylated Fgf21 rapidly normalizes insulin-stimulated glucose utilization in diet-induced insulin resistant mice

(2013) Raul C. Camacho et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Retinoic Acid Receptor β Stimulates Hepatic Induction of Fibroblast Growth Factor 21 to Promote Fatty Acid Oxidation and Control Whole-body Energy Homeostasis in Mice

(2013) Yu Li et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

FGF21 regulates metabolism and circadian behavior by acting on the nervous system

(2013) Angie L Bookout et al.   NATURE MEDICINE

Rational Design of a Fibroblast Growth Factor 21-Based Clinical Candidate, LY2405319

(2013) Alexei Kharitonenkov et al.   PLoS One

LY2405319, an Engineered FGF21 Variant, Improves the Metabolic Status of Diabetic Monkeys

(2013) Andrew C. Adams et al.   PLoS One

Fibroblast growth factor 21 protects against cardiac hypertrophy in mice

(2013) A. Planavila et al.   Nature Communications

Fibroblast Growth Factor-21 Regulates PPARγ Activity and the Antidiabetic Actions of Thiazolidinediones

(2012) Paul A. Dutchak et al.   CELL

βKlotho Is Required for Fibroblast Growth Factor 21 Effects on Growth and Metabolism

(2012) Xunshan Ding et al.   Cell Metabolism

Long-Acting FGF21 Has Enhanced Efficacy in Diet-Induced Obese Mice and in Obese Rhesus Monkeys

(2012) Murielle M. Véniant et al.   ENDOCRINOLOGY

Activation of the Farnesoid X Receptor Induces Hepatic Expression and Secretion of Fibroblast Growth Factor 21

(2012) Holly A. Cyphert et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Fasting-Induced FGF21 Is Repressed by LXR Activation via Recruitment of an HDAC3 Corepressor Complex in Mice

(2012) Amena Archer et al.   MOLECULAR ENDOCRINOLOGY

FGF21 Requires βklotho to Act In Vivo

(2012) Andrew C. Adams et al.   PLoS One

Rationale-Based Engineering of a Potent Long-Acting FGF21 Analog for the Treatment of Type 2 Diabetes

(2012) Randy Hecht et al.   PLoS One

Treating Diabetes and Obesity with an FGF21-Mimetic Antibody Activating the  Klotho/FGFR1c Receptor Complex

(2012) I. N. Foltz et al.   Science Translational Medicine

Fibroblast Growth Factor 21 (FGF21) in Human Cerebrospinal Fluid

(2011) Bee K. Tan et al.   DIABETES

Direct effects of FGF21 on glucose uptake in human skeletal muscle: implications for type 2 diabetes and obesity

(2011) Fredirick L. Mashili et al.   DIABETES-METABOLISM RESEARCH AND REVIEWS

Integrated Regulation of Hepatic Metabolism by Fibroblast Growth Factor 21 (FGF21)in Vivo

(2011) ffolliott M. Fisher et al.   ENDOCRINOLOGY

Amelioration of Type 2 Diabetes by Antibody-Mediated Activation of Fibroblast Growth Factor Receptor 1

(2011) A.-L. Wu et al.   Science Translational Medicine

Obesity Is a Fibroblast Growth Factor 21 (FGF21)-Resistant State

(2010) f. M. Fisher et al.   DIABETES

Thyroid Hormone Regulates Hepatic Expression of Fibroblast Growth Factor 21 in aPPARα-dependent Manner

(2010) Andrew C. Adams et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Regulation of FGF21 Expression and Secretion by Retinoic Acid Receptor-related Orphan Receptor α

(2010) Yongjun Wang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Research Resource: Comprehensive Expression Atlas of the Fibroblast Growth Factor System in Adult Mouse

(2010) Klementina Fon Tacer et al.   MOLECULAR ENDOCRINOLOGY

Fibroblast growth factor 21 regulates energy metabolism by activating the AMPK–SIRT1–PGC-1α pathway

(2010) Mary D. L. Chau et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Acute glucose-lowering and insulin-sensitizing action of FGF21 in insulin-resistant mouse models—association with liver and adipose tissue effects

(2009) Jing Xu et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Fibroblast Growth Factor 21 Controls Glycemia via Regulation of Hepatic Glucose Flux and Insulin Sensitivity

(2009) Eric D. Berglund et al.   ENDOCRINOLOGY

Fibroblast Growth Factor 21 Regulates Lipolysis in White Adipose Tissue But Is Not Required for Ketogenesis and Triglyceride Clearance in Liver

(2009) Yuhei Hotta et al.   ENDOCRINOLOGY

Inhibition of lipolysis may contribute to the acute regulation of plasma FFA and glucose by FGF21 inob/obmice

(2009) Xiaofan Li et al.   FEBS LETTERS

Peroxisome Proliferator-Activated Receptor  /  (PPAR / ) but Not PPAR  Serves as a Plasma Free Fatty Acid Sensor in Liver

(2009) L. M. Sanderson et al.   MOLECULAR AND CELLULAR BIOLOGY

The FGF family: biology, pathophysiology and therapy

(2009) Andrew Beenken et al.   NATURE REVIEWS DRUG DISCOVERY

FGF21 induces PGC-1  and regulates carbohydrate and fatty acid metabolism during the adaptive starvation response

(2009) M. J. Potthoff et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2008) J. Xu et al.   DIABETES

FGF21 attenuates lipolysis in human adipocytes - A possible link to improved insulin sensitivity

(2008) Peter Arner et al.   FEBS LETTERS