A Dozen Years of Discovery: Insights into the Physiology and Pharmacology of FGF21.

[1]  B. Neuschwander‐Tetri,et al.  Pegbelfermin (BMS‐986036), PEGylated FGF21, in Patients with Obesity and Type 2 Diabetes: Results from a Randomized Phase 2 Study , 2018, Obesity.

[2]  B. Neuschwander‐Tetri,et al.  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, The Lancet.

[3]  S. Kliewer,et al.  PPARγ-K107 SUMOylation regulates insulin sensitivity but not adiposity in mice , 2018, Proceedings of the National Academy of Sciences.

[4]  P. Gao,et al.  A2A Receptor Activation Attenuates Hypertensive Cardiac Remodeling via Promoting Brown Adipose Tissue-Derived FGF21. , 2018, Cell metabolism.

[5]  Matthew J. Potthoff,et al.  Fibroblast Growth Factor 21: A Versatile Regulator of Metabolic Homeostasis. , 2018, Annual review of nutrition.

[6]  B. Goodwin,et al.  FGF21 increases water intake, urine output and blood pressure in rats , 2018, PloS one.

[7]  S. Kliewer,et al.  The Hormone FGF21 Stimulates Water Drinking in Response to Ketogenic Diet and Alcohol. , 2018, Cell metabolism.

[8]  M. Gillum,et al.  FGF21, a liver hormone that inhibits alcohol intake in mice, increases in human circulation after acute alcohol ingestion and sustained binge drinking at Oktoberfest , 2018, bioRxiv.

[9]  E. Pardon,et al.  Structures of β-klotho reveal a ‘zip code’-like mechanism for endocrine FGF signalling , 2018, Nature.

[10]  M. Kuro-o Ageing-related receptors resolved , 2018, Nature.

[11]  Jeffrey R. Chabot,et al.  Once‐weekly administration of a long‐acting fibroblast growth factor 21 analogue modulates lipids, bone turnover markers, blood pressure and body weight differently in obese people with hypertriglyceridaemia and in non‐human primates , 2017, Diabetes, obesity & metabolism.

[12]  S. Kliewer,et al.  FGF19, FGF21, and an FGFR1/β-Klotho-Activating Antibody Act on the Nervous System to Regulate Body Weight and Glycemia. , 2017, Cell metabolism.

[13]  W. Wahli,et al.  A Specific ChREBP and PPARα Cross-Talk Is Required for the Glucose-Mediated FGF21 Response , 2017, Cell reports.

[14]  A. Xu,et al.  The FGF21-CCL11 Axis Mediates Beiging of White Adipose Tissues by Coupling Sympathetic Nervous System to Type 2 Immunity. , 2017, Cell metabolism.

[15]  G. FitzGerald,et al.  Fibroblast growth factor 21 (FGF21) is robustly induced by ethanol and has a protective role in ethanol associated liver injury , 2017, Molecular metabolism.

[16]  T. Hansen,et al.  FGF21 Is a Sugar-Induced Hormone Associated with Sweet Intake and Preference in Humans. , 2017, Cell metabolism.

[17]  Matthew J. Potthoff,et al.  FGF21 Regulates Metabolism Through Adipose-Dependent and -Independent Mechanisms. , 2017, Cell metabolism.

[18]  M. Stolina,et al.  FGF21 Is Not a Major Mediator for Bone Homeostasis or Metabolic Actions of PPARα and PPARγ Agonists , 2017, Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research.

[19]  I. Deary,et al.  Genome-wide association study of alcohol consumption and genetic overlap with other health-related traits in UK Biobank (N=112 117) , 2017, Molecular Psychiatry.

[20]  S. Kliewer,et al.  FGF21 Is an Exocrine Pancreas Secretagogue. , 2017, Cell metabolism.

[21]  P. O’Reilly,et al.  KLB is associated with alcohol drinking, and its gene product β-Klotho is necessary for FGF21 regulation of alcohol preference , 2016, Proceedings of the National Academy of Sciences.

[22]  M. Herman,et al.  A critical role for ChREBP-mediated FGF21 secretion in hepatic fructose metabolism , 2016, Molecular metabolism.

[23]  S. Flier,et al.  Elevated Serum Fibroblast Growth Factor 21 in Humans with Acute Pancreatitis , 2016, PloS one.

[24]  Min Zhang,et al.  Fibroblast growth factor 21 deficiency exacerbates chronic alcohol-induced hepatic steatosis and injury , 2016, Scientific Reports.

[25]  C. Musante,et al.  PF-05231023, a long-acting FGF21 analogue, decreases body weight by reduction of food intake in non-human primates , 2016, Journal of Pharmacokinetics and Pharmacodynamics.

[26]  J. Heeren,et al.  FGF21 Lowers Plasma Triglycerides by Accelerating Lipoprotein Catabolism in White and Brown Adipose Tissues. , 2016, Cell metabolism.

[27]  Jeffrey R. Chabot,et al.  A Long-Acting FGF21 Molecule, PF-05231023, Decreases Body Weight and Improves Lipid Profile in Non-human Primates and Type 2 Diabetic Subjects. , 2016, Cell metabolism.

[28]  C. Benoist,et al.  Fibroblast Growth Factor 21 (FGF21) Protects against High Fat Diet Induced Inflammation and Islet Hyperplasia in Pancreas , 2016, PloS one.

[29]  E. Maratos-Flier,et al.  Understanding the Physiology of FGF21. , 2016, Annual review of physiology.

[30]  Bhavna S. Paratala,et al.  FGF21 Regulates Sweet and Alcohol Preference. , 2016, Cell metabolism.

[31]  M. Gillum,et al.  FGF21 Mediates Endocrine Control of Simple Sugar Intake and Sweet Taste Preference by the Liver. , 2016, Cell metabolism.

[32]  Scott D Covey,et al.  FGF21-Mediated Improvements in Glucose Clearance Require Uncoupling Protein 1. , 2015, Cell reports.

[33]  Yuan Zhang,et al.  Role of fibroblast growth factor 21 in the early stage of NASH induced by methionine- and choline-deficient diet. , 2015, Biochimica et biophysica acta.

[34]  Matthew J. Brauer,et al.  Sustained Brown Fat Stimulation and Insulin Sensitization by a Humanized Bispecific Antibody Agonist for Fibroblast Growth Factor Receptor 1/βKlotho Complex , 2015, EBioMedicine.

[35]  R. Gimeno,et al.  Discrete Aspects of FGF21 In Vivo Pharmacology Do Not Require UCP1. , 2015, Cell reports.

[36]  M. Véniant,et al.  Pharmacologic Effects of FGF21 Are Independent of the "Browning" of White Adipose Tissue. , 2015, Cell metabolism.

[37]  J. Flier,et al.  Central Fibroblast Growth Factor 21 Browns White Fat via Sympathetic Action in Male Mice. , 2015, Endocrinology.

[38]  Bing Zhou,et al.  FGF21 treatment ameliorates alcoholic fatty liver through activation of AMPK-SIRT1 pathway. , 2014, Acta biochimica et biophysica Sinica.

[39]  S. Kliewer,et al.  Circulating FGF21 Is Liver Derived and Enhances Glucose Uptake During Refeeding and Overfeeding , 2014, Diabetes.

[40]  D. Schuppan,et al.  Fibroblast growth factor 21 limits lipotoxicity by promoting hepatic fatty acid activation in mice on methionine and choline-deficient diets. , 2014, Gastroenterology.

[41]  S. Kliewer,et al.  FGF21 acts centrally to induce sympathetic nerve activity, energy expenditure, and weight loss. , 2014, Cell metabolism.

[42]  S. Bornstein,et al.  FGF21 Maintains Glucose Homeostasis by Mediating the Cross Talk Between Liver and Brain During Prolonged Fasting , 2014, Diabetes.

[43]  R. Mehmood,et al.  Silencing of the Fibroblast growth factor 21 gene is an underlying cause of acinar cell injury in mice lacking MIST1. , 2014, American journal of physiology. Endocrinology and metabolism.

[44]  H. Fu,et al.  The effects of LY2405319, an FGF21 analog, in obese human subjects with type 2 diabetes. , 2013, Cell metabolism.

[45]  S. Kliewer,et al.  FGF21 regulates circadian behavior and metabolism by acting on the nervous system , 2013, Nature medicine.

[46]  S. Kliewer,et al.  FGF21 contributes to neuroendocrine control of female reproduction , 2013, Nature Medicine.

[47]  B. Hansen,et al.  LY2405319, an Engineered FGF21 Variant, Improves the Metabolic Status of Diabetic Monkeys , 2013, PloS one.

[48]  S. Bornstein,et al.  Adiponectin mediates the metabolic effects of FGF21 on glucose homeostasis and insulin sensitivity in mice. , 2013, Cell metabolism.

[49]  P. Scherer,et al.  An FGF21-adiponectin-ceramide axis controls energy expenditure and insulin action in mice. , 2013, Cell metabolism.

[50]  Andrew D. Johnson,et al.  Genome-wide meta-analysis of observational studies shows common genetic variants associated with macronutrient intake1234 , 2013, The American journal of clinical nutrition.

[51]  Audrey Y. Chu,et al.  Novel locus including FGF21 is associated with dietary macronutrient intake. , 2013, Human molecular genetics.

[52]  R. Gimeno,et al.  The breadth of FGF21's metabolic actions are governed by FGFR1 in adipose tissue. , 2013, Molecular metabolism.

[53]  Nobuyuki Itoh,et al.  Autophagy deficiency leads to protection from obesity and insulin resistance by inducing Fgf21 as a mitokine , 2012, Nature Medicine.

[54]  T. Arora,et al.  Treating Diabetes and Obesity with an FGF21-Mimetic Antibody Activating the βKlotho/FGFR1c Receptor Complex , 2012, Science Translational Medicine.

[55]  S. Kliewer,et al.  βKlotho is required for fibroblast growth factor 21 effects on growth and metabolism. , 2012, Cell metabolism.

[56]  Katherine A. Winters,et al.  Long-acting FGF21 has enhanced efficacy in diet-induced obese mice and in obese rhesus monkeys. , 2012, Endocrinology.

[57]  Jing Xu,et al.  FGF21 Promotes Metabolic Homeostasis via White Adipose and Leptin in Mice , 2012, PloS one.

[58]  S. Kliewer,et al.  Fibroblast growth factor 21 promotes bone loss by potentiating the effects of peroxisome proliferator-activated receptor γ , 2012, Proceedings of the National Academy of Sciences.

[59]  S. Kliewer,et al.  Fibroblast Growth Factor-21 Regulates PPARγ Activity and the Antidiabetic Actions of Thiazolidinediones , 2012, Cell.

[60]  B. Spiegelman,et al.  FGF21 regulates PGC-1α and browning of white adipose tissues in adaptive thermogenesis. , 2012, Genes & development.

[61]  Jun Li,et al.  Amelioration of Type 2 Diabetes by Antibody-Mediated Activation of Fibroblast Growth Factor Receptor 1 , 2011, Science Translational Medicine.

[62]  F. Villarroya,et al.  Thermogenic Activation Induces FGF21 Expression and Release in Brown Adipose Tissue* , 2011, The Journal of Biological Chemistry.

[63]  M. Schwartz,et al.  Fibroblast Growth Factor 21 Action in the Brain Increases Energy Expenditure and Insulin Sensitivity in Obese Rats , 2010, Diabetes.

[64]  F. Villarroya,et al.  Hepatic FGF21 expression is induced at birth via PPARalpha in response to milk intake and contributes to thermogenic activation of neonatal brown fat. , 2010, Cell metabolism.

[65]  J. Flier,et al.  Fibroblast growth factor 21-deficient mice demonstrate impaired adaptation to ketosis. , 2009, Endocrinology.

[66]  E. Fazio,et al.  Fibroblast growth factor 21 reduces the severity of cerulein-induced pancreatitis in mice. , 2009, Gastroenterology.

[67]  M. Konishi,et al.  Fibroblast growth factor 21 regulates lipolysis in white adipose tissue but is not required for ketogenesis and triglyceride clearance in liver. , 2009, Endocrinology.

[68]  S. Kliewer,et al.  FGF21 induces PGC-1α and regulates carbohydrate and fatty acid metabolism during the adaptive starvation response , 2009, Proceedings of the National Academy of Sciences.

[69]  M. Mohammadi,et al.  The FGF family: biology, pathophysiology and therapy , 2009, Nature Reviews Drug Discovery.

[70]  Jason K. Kim,et al.  Fibroblast Growth Factor 21 Reverses Hepatic Steatosis, Increases Energy Expenditure, and Improves Insulin Sensitivity in Diet-Induced Obese Mice , 2009, Diabetes.

[71]  D. Moller,et al.  Fibroblast growth factor 21 corrects obesity in mice. , 2008, Endocrinology.

[72]  Yuichi Akasaki,et al.  FGF21 is an Akt‐regulated myokine , 2008, FEBS letters.

[73]  W. Pan,et al.  The fasting polypeptide FGF21 can enter brain from blood , 2007, Peptides.

[74]  T. Bengtsson,et al.  Unexpected evidence for active brown adipose tissue in adult humans. , 2007, American journal of physiology. Endocrinology and metabolism.

[75]  S. Kliewer,et al.  Endocrine regulation of the fasting response by PPARalpha-mediated induction of fibroblast growth factor 21. , 2007, Cell metabolism.

[76]  J. Flier,et al.  Hepatic fibroblast growth factor 21 is regulated by PPARalpha and is a key mediator of hepatic lipid metabolism in ketotic states. , 2007, Cell metabolism.

[77]  Yun-Fei Chen,et al.  The metabolic state of diabetic monkeys is regulated by fibroblast growth factor-21. , 2007, Endocrinology.

[78]  J. Gromada,et al.  FGF-21 as a novel metabolic regulator. , 2005, The Journal of clinical investigation.

[79]  M. Konishi,et al.  Identification of a novel FGF, FGF-21, preferentially expressed in the liver. , 2000, Biochimica et biophysica acta.

[80]  S. Leibowitz Paraventricular nucleus: A primary site mediating adrenergic stimulation of feeding and drinking , 1978, Pharmacology Biochemistry and Behavior.

[81]  Jeffrey R. Chabot,et al.  Once-weekly administration of a long-acting FGF 21 analogue modulates lipids , bone turnover markers , blood pressure , and body weight differently in obese hypertriglyceridemic subjects and in non-human primates , 2017 .

[82]  A. Papavassiliou,et al.  Brown Adipose Tissue Responds to Cold and Adrenergic Stimulation by Induction of FGF21 , 2011, Molecular medicine.