FGF21-based pharmacotherapy – potential utility for metabolic disorders

FGF-21 as a novel metabolic regulator

Kharitonenkov, A., Shiyanova, T. L., Koester, A., Ford, A. M., Micanovic, R., Galbreath, E. J., Sandusky, G. E., Hammond, L. J., Moyers, J. S., Owens, R. A., et al. (2005) · Journal of Clinical Investigation · doi:10.1172/jci23606 · Cited by 2,125

Endocrine Regulation of the Fasting Response by PPARα-Mediated Induction of Fibroblast Growth Factor 21

Inagaki, T., Dutchak, P., Zhao, G., Ding, X., Gautron, L., Parameswara, V., Li, Y., Goetz, R., Mohammadi, M., Esser, V., et al. (2007) · Cell Metabolism · doi:10.1016/j.cmet.2007.05.003 · Cited by 1,504

Hepatic Fibroblast Growth Factor 21 Is Regulated by PPARα and Is a Key Mediator of Hepatic Lipid Metabolism in Ketotic States

Badman, M. K., Pissios, P., Kennedy, A. R., Koukos, G., Flier, J. S., & Maratos-Flier, E. (2007) · Cell Metabolism · doi:10.1016/j.cmet.2007.05.002 · Cited by 1,495

FGF21 regulates PGC-1α and browning of white adipose tissues in adaptive thermogenesis

Fisher, F. M., Kleiner, S., Douris, N., Fox, E. C., Mepani, R. J., Verdeguer, F., Wu, J., Kharitonenkov, A., Flier, J. S., Maratos-Flier, E., et al. (2012) · Genes & Development · doi:10.1101/gad.177857.111 · Cited by 1,478

Fibroblast growth factor 21 reverses hepatic steatosis, increases energy expenditure, and improves insulin sensitivity in diet-induced obese mice

Xu, J., Lloyd, D. J., Hale, C., Stanislaus, S., Chen, M., Sivits, G., Vonderfecht, S., Hecht, R., Li, Y.-S., Lindberg, R. A., et al. (2009) · Diabetes · doi:10.2337/db08-0392 · Cited by 1,151

Fibroblast Growth Factor 21 Corrects Obesity in Mice

Coskun, T., Bina, H. A., Schneider, M. A., Dunbar, J. D., Hu, C. C., Chen, Y., Moller, D. E., & Kharitonenkov, A. (2008) · Endocrinology · doi:10.1210/en.2008-0816 · Cited by 1,031

The effects of LY2405319, an FGF21 analog, in obese human subjects with type 2 diabetes

Gaich, G., Chien, J. Y., Fu, H., Glass, L. C., Deeg, M. A., Holland, W. L., Kharitonenkov, A., Bumol, T., Schilske, H. K., & Moller, D. E. (2013) · Cell Metabolism · doi:10.1016/j.cmet.2013.08.005 · Cited by 885

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

Fisher, F. M., Chui, P. C., Antonellis, P. J., Bina, H. A., Kharitonenkov, A., Flier, J. S., & Maratos-Flier, E. (2010) · Diabetes · doi:10.2337/db10-0193 · Cited by 830

Irisin and FGF21 are cold-induced endocrine activators of brown fat function in humans

Lee, P., Linderman, J. D., Smith, S., Brychta, R. J., Wang, J., Idelson, C., Perron, R. M., Werner, C. D., Phan, G. Q., Kammula, U. S., et al. (2014) · Cell Metabolism · doi:10.1016/j.cmet.2013.12.017 · Cited by 802

Autophagy deficiency leads to protection from obesity and insulin resistance by inducing Fgf21 as a mitokine

Kim, K. H., Jeong, Y. T., Oh, H., Kim, S. H., Cho, J. M., Kim, Y.-N., Kim, S. S., Kim, D. H., Hur, K. Y., Kim, H. K., et al. (2013) · Nature Medicine · doi:10.1038/nm.3014 · Cited by 774

Tissue-specific Expression of βKlotho and Fibroblast Growth Factor (FGF) Receptor Isoforms Determines Metabolic Activity of FGF19 and FGF21

Kurosu, H., Choi, M., Ogawa, Y., Dickson, A. S., Goetz, R., Eliseenkova, A. V., Mohammadi, M., Rosenblatt, K. P., Kliewer, S. A., & Kuro-o, M. (2007) · Journal of Biological Chemistry · doi:10.1074/jbc.m704165200 · Cited by 748

The metabolic state of diabetic monkeys is regulated by fibroblast growth factor-21

Kharitonenkov, A., Wroblewski, V. J., Koester, A., Chen, Y.-F., Clutinger, C. K., Tigno, X. T., Hansen, B. C., Shanafelt, A. B., & Etgen, G. J. (2007) · Endocrinology · doi:10.1210/en.2006-1168 · Cited by 738

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

Potthoff, M. J., Inagaki, T., Satapati, S., Ding, X., He, T., Goetz, R., Mohammadi, M., Finck, B. N., Mangelsdorf, D. J., Kliewer, S. A., et al. (2009) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0904187106 · Cited by 704

Adiponectin mediates the metabolic effects of FGF21 on glucose homeostasis and insulin sensitivity in mice

Lin, Z., Tian, H., Lam, K. S. L., Lin, S., Hoo, R. C. L., Konishi, M., Itoh, N., Wang, Y., Bornstein, S. R., Xu, A., et al. (2013) · Cell Metabolism · doi:10.1016/j.cmet.2013.04.005 · Cited by 691

βKlotho is required for metabolic activity of fibroblast growth factor 21

Ogawa, Y., Kurosu, H., Yamamoto, M., Nandi, A., Rosenblatt, K. P., Goetz, R., Eliseenkova, A. V., Mohammadi, M., & Kuro-o, M. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0701600104 · Cited by 617

Increased Fibroblast Growth Factor 21 in Obesity and Nonalcoholic Fatty Liver Disease

Dushay, J., Chui, P. C., Gopalakrishnan, G. S., Varela–Rey, M., Crawley, M., Fisher, F. M., Badman, M. K., Martinez–Chantar, M. L., & Maratos–Flier, E. (2010) · Gastroenterology · doi:10.1053/j.gastro.2010.04.054 · Cited by 607

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

Chau, M. D. L., Gao, J., Yang, Q., Wu, Z., & Gromada, J. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1006962107 · Cited by 557

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

Bookout, A. L., de Groot, M. H. M., Owen, B. M., Lee, S., Gautron, L., Lawrence, H. L., Ding, X., Elmquist, J. K., Takahashi, J. S., Mangelsdorf, D. J., et al. (2013) · Nature Medicine · doi:10.1038/nm.3249 · Cited by 545

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

Dutchak, P. A., Katafuchi, T., Bookout, A. L., Choi, J. H., Yu, R. T., Mangelsdorf, D. J., & Kliewer, S. A. (2012) · Cell · doi:10.1016/j.cell.2011.11.062 · Cited by 537

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

Holland, W., Adams, A., Brozinick, J., Bui, H., Miyauchi, Y., Kusminski, C., Bauer, S., Wade, M., Singhal, E., Cheng, C. C., et al. (2013) · Cell Metabolism · doi:10.1016/j.cmet.2013.03.019 · Cited by 525

The Circulating Metabolic Regulator FGF21 Is Induced by Prolonged Fasting and PPARα Activation in Man

Gälman, C., Lundåsen, T., Kharitonenkov, A., Bina, H. A., Eriksson, M., Hafström, I., Dahlin, M., Åmark, P., Angelin, B., & Rudling, M. (2008) · Cell Metabolism · doi:10.1016/j.cmet.2008.06.014 · Cited by 512

Fibroblast Growth Factor-21 Improves Pancreatic β-Cell Function and Survival by Activation of Extracellular Signal–Regulated Kinase 1/2 and Akt Signaling Pathways

Wente, W., Efanov, A. M., Brenner, M. B., Kharitonenkov, A., Koster, A. M., Sandusky, G. E., Sewing, S., Treinies, I., Zitzer, H., & Gromada, J. (2006) · Diabetes · doi:10.2337/db05-1435 · Cited by 497

Fibroblast growth factor 21 promotes bone loss by potentiating the effects of peroxisome proliferator-activated receptor γ

Wei, W., Dutchak, P. A., Wang, X., Ding, X., Wang, X., Bookout, A. L., Goetz, R., Mohammadi, M., Gerard, R. D., Dechow, P. C., et al. (2012) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1200797109 · Cited by 426

The starvation hormone, fibroblast growth factor-21, extends lifespan in mice

Zhang, Y., Xie, Y., Berglund, E. D., Coate, K. C., He, T. T., Katafuchi, T., Xiao, G., Potthoff, M. J., Wei, W., Wan, Y., et al. (2012) · eLife · doi:10.7554/elife.00065 · Cited by 420

Inhibition of Growth Hormone Signaling by the Fasting-Induced Hormone FGF21

Inagaki, T., Lin, V. Y., Goetz, R., Mohammadi, M., Mangelsdorf, D. J., & Kliewer, S. A. (2008) · Cell Metabolism · doi:10.1016/j.cmet.2008.05.006 · Cited by 409

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

Ding, X., Boney-Montoya, J., Owen, B. M., Bookout, A. L., Coate, K. C., Mangelsdorf, D. J., & Kliewer, S. A. (2012) · Cell Metabolism · doi:10.1016/j.cmet.2012.08.002 · Cited by 403

Fibroblast Growth Factor 21-Deficient Mice Demonstrate Impaired Adaptation to Ketosis

Badman, M. K., Koester, A., Flier, J. S., Kharitonenkov, A., & Maratos-Flier, E. (2009) · Endocrinology · doi:10.1210/en.2009-0532 · Cited by 362

Life Extension in the Dwarf Mouse

Bartke, A., & Brown‐Borg, H. M. (2004) · Current topics in developmental biology/Current Topics in Developmental Biology · doi:10.1016/s0070-2153(04)63006-7 · Cited by 360

Fibroblast growth factor 21 regulates lipolysis in white adipose tissue but is not required for ketogenesis and triglyceride clearance in liver

Hotta, Y., Nakamura, H., Konishi, M., Murata, Y., Takagi, H., Matsumura, S., Inoue, K., Fushiki, T., & Itoh, N. (2009) · Endocrinology · doi:10.1210/en.2009-0119 · Cited by 352

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

Xu, J., Stanislaus, S., Chinookoswong, N., Lau, Y. Y., Hager, T., Patel, J., Ge, H., Weiszmann, J., Lu, S.-C., Graham, M., et al. (2009) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.00348.2009 · Cited by 340

FGF‐21/FGF‐21 receptor interaction and activation is determined by βKlotho

Kharitonenkov, A., Dunbar, J. D., Bina, H. A., Bright, S. W., Moyers, J. S., Zhang, C., Ding, L., Micanovic, R., Mehrbod, S. F., Knierman, M. D., et al. (2007) · Journal of Cellular Physiology · doi:10.1002/jcp.21357 · Cited by 333

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

Berglund, E. D., Li, C. Y., Bina, H. A., Lynes, S. E., Michael, M. D., Shanafelt, A. B., Kharitonenkov, A., & Wasserman, D. H. (2009) · Endocrinology · doi:10.1210/en.2009-0221 · Cited by 297

Adipose Fibroblast Growth Factor 21 Is Up-Regulated by Peroxisome Proliferator-Activated Receptor γ and Altered Metabolic States

Muise, E. S., Azzolina, B., Kuo, D. W., El-Sherbeini, M., Tan, Y., Yuan, X., Mu, J., Thompson, J. R., Berger, J. P., & Wong, K. K. (2008) · Molecular Pharmacology · doi:10.1124/mol.108.044826 · Cited by 294

Acute Exercise Induces FGF21 Expression in Mice and in Healthy Humans

Kim, K. H., Kim, S. H., Min, Y.-K., Yang, H.-M., Lee, J.-B., & Lee, M.-S. (2013) · PLoS ONE · doi:10.1371/journal.pone.0063517 · Cited by 290

Fibroblast Growth Factor 21 Action in the Brain Increases Energy Expenditure and Insulin Sensitivity in Obese Rats

Sarruf, D. A., Thaler, J. P., Morton, G. J., German, J. P., Fischer, J. D., Ogimoto, K., & Schwartz, M. W. (2010) · Diabetes · doi:10.2337/db09-1878 · Cited by 287

The fasting polypeptide FGF21 can enter brain from blood

Hsuchou, H., Pan, W., & Kastin, A. J. (2007) · Peptides · doi:10.1016/j.peptides.2007.10.007 · Cited by 280

The breadth of FGF21's metabolic actions are governed by FGFR1 in adipose tissue

Adams, A. C., Yang, C., Coskun, T., Cheng, C. C., Gimeno, R. E., Luo, Y., & Kharitonenkov, A. (2013) · Molecular Metabolism · doi:10.1016/j.molmet.2012.08.007 · Cited by 266

Adiponectin, driver or passenger on the road to insulin sensitivity?

Ye, R., & Scherer, P. E. (2013) · Molecular Metabolism · doi:10.1016/j.molmet.2013.04.001 · Cited by 251

Fibroblast Growth Factor 21 Mediates Specific Glucagon Actions

Habegger, K. M., Stemmer, K., Cheng, C., Müller, T. D., Heppner, K. M., Ottaway, N., Holland, J., Hembree, J. L., Smiley, D., Gelfanov, V., et al. (2013) · Diabetes · doi:10.2337/db12-1116 · Cited by 245

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

Fisher, F. M., Estall, J. L., Adams, A. C., Antonellis, P. J., Bina, H. A., Flier, J. S., Kharitonenkov, A., Spiegelman, B. M., & Maratos–Flier, E. (2011) · Endocrinology · doi:10.1210/en.2011-0281 · Cited by 231

FGF21 contributes to neuroendocrine control of female reproduction

Owen, B. M., Bookout, A. L., Ding, X., Lin, V. Y., Atkin, S. D., Gautron, L., Kliewer, S. A., & Mangelsdorf, D. J. (2013) · Nature Medicine · doi:10.1038/nm.3250 · Cited by 230

Apolipoprotein C-III and the Metabolic Basis for Hypertriglyceridemia and the Dense Low-Density Lipoprotein Phenotype

Zheng, C., Khoo, C., Furtado, J., & Sacks, F. M. (2010) · Circulation · doi:10.1161/circulationaha.109.875807 · Cited by 223

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

Foltz, I. N., Hu, S., King, C., Wu, X., Yang, C., Wang, W., Weiszmann, J., Stevens, J., Chen, J. S., Nuanmanee, N., et al. (2012) · Science Translational Medicine · doi:10.1126/scitranslmed.3004690 · Cited by 211

Fibroblast Growth Factor-21 Is Induced in Human Skeletal Muscles by Hyperinsulinemia

Hojman, P., Pedersen, M., Nielsen, A. R., Krogh-Madsen, R., Yfanti, C., Åkerstrom, T., Nielsen, S., & Pedersen, B. K. (2009) · Diabetes · doi:10.2337/db09-0713 · Cited by 198

Molecular determinants of FGF‐21 activity—synergy and cross‐talk with PPARγ signaling

Moyers, J. S., Shiyanova, T. L., Mehrbod, F., Dunbar, J. D., Noblitt, T. W., Otto, K. A., Reifel-Miller, A. E., & Kharitonenkov, A. (2006) · Journal of Cellular Physiology · doi:10.1002/jcp.20847 · Cited by 193

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

Wu, A.-L., Kolumam, G., Stawicki, S., Chen, Y., Li, J., Zavala-Solorio, J., Phamluong, K., Feng, B., Li, L., Marsters, S., et al. (2011) · Science Translational Medicine · doi:10.1126/scitranslmed.3002669 · Cited by 184

Fibroblast Growth Factor 21 Induces Glucose Transporter-1 Expression through Activation of the Serum Response Factor/Ets-Like Protein-1 in Adipocytes

Ge, X., Chen, C., Hui, X. H., Wang, Y., Lam, K. S. L., & Xu, A. (2011) · Journal of Biological Chemistry · doi:10.1074/jbc.m111.248591 · Cited by 181

FGF21 Requires βklotho to Act In Vivo

Adams, A. C., Cheng, C. C., Coskun, T., & Kharitonenkov, A. (2012) · PLoS ONE · doi:10.1371/journal.pone.0049977 · Cited by 181

High Plasma Level of Fibroblast Growth Factor 21 Is an Independent Predictor of Type 2 Diabetes

Chen, C., Cheung, B. M. Y., Tso, A. W. K., Wang, Y., Law, L. S., Ong, K. L., Wat, N. M. S., Xu, A., & Lam, K. S. L. (2011) · Diabetes Care · doi:10.2337/dc11-0294 · Cited by 181

Fibroblast Growth Factor 21 Reduces the Severity of Cerulein-Induced Pancreatitis in Mice

Johnson, C. L., Weston, J. Y., Chadi, S. A., Fazio, E. N., Huff, M. W., Kharitonenkov, A., Köester, A., & Pin, C. L. (2009) · Gastroenterology · doi:10.1053/j.gastro.2009.07.064 · Cited by 180

Differential Specificity of Endocrine FGF19 and FGF21 to FGFR1 and FGFR4 in Complex with KLB

Yang, C., Jin, C., Li, X., Wang, F., McKeehan, W. L., & Luo, Y. (2012) · PLoS ONE · doi:10.1371/journal.pone.0033870 · Cited by 173

LY2405319, an engineered FGF21 variant, improves the metabolic status of diabetic monkeys

Adams, A. C., Halstead, C. A., Hansen, B. C., Irizarry, A. R., Martin, J. A., Myers, S. R., Reynolds, V. L., Smith, H. W., Wroblewski, V. J., & Kharitonenkov, A. (2013) · PLoS ONE · doi:10.1371/journal.pone.0065763 · Cited by 169

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

Kharitonenkov, A., Beals, J. M., Micanovic, R., Strifler, B. A., Rathnachalam, R., Wroblewski, V. J., Li, S., Köester, A., Ford, A. M., Coşkun, T., et al. (2013) · PLoS ONE · doi:10.1371/journal.pone.0058575 · Cited by 168

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

Hecht, R. I., Li, Y., Sun, J., Belouski, E., Hall, M. P., Hager, T., Yie, J., Wang, W., Winters, D., Smith, S. H., et al. (2012) · PLoS ONE · doi:10.1371/journal.pone.0049345 · Cited by 166

Fibroblast growth factor 21 is induced by endoplasmic reticulum stress

Schaap, F. G., Kremer, A. E., Lamers, W. H., Jansen, P. L. M., & Gaemers, I. C. (2012) · Biochimie · doi:10.1016/j.biochi.2012.10.019 · Cited by 164

FGF21 Analogs of Sustained Action Enabled by Orthogonal Biosynthesis Demonstrate Enhanced Antidiabetic Pharmacology in Rodents

Mu, J., Pinkstaff, J. K., Li, Z., Skidmore, L. K., Li, N., Myler, H. A., Dallas-Yang, Q., Hays, A. A., Yao, J., Bussell, S., et al. (2011) · Diabetes · doi:10.2337/db11-0838 · Cited by 162

Restoration of leptin responsiveness in diet‐induced obese mice using an optimized leptin analog in combination with exendin‐4 or FGF21

Müller, T. D., Sullivan, L. M., Habegger, K., Yi, C., Kabra, D., Grant, E., Ottaway, N., Krishna, R., Holland, J., Hembree, J., et al. (2012) · Journal of Peptide Science · doi:10.1002/psc.2408 · Cited by 156

Circulating Fibroblast Growth Factor 21 Is Induced by Peroxisome Proliferator-Activated Receptor Agonists But Not Ketosis in Man

Christodoulides, C., Dyson, P., Sprecher, D., Tsintzas, K., & Karpe, F. (2009) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jc.2009-0111 · Cited by 153

FGF21 N‐ and C‐termini play different roles in receptor interaction and activation

Yie, J., Hecht, R., Patel, J., Stevens, J., Wang, W., Hawkins, N., Steavenson, S., Smith, S., Winters, D., Fisher, S., et al. (2009) · FEBS Letters · doi:10.1016/j.febslet.2008.11.023 · Cited by 149

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

Véniant, M. M., Komorowski, R., Chen, P., Stanislaus, S., Winters, K., Hager, T., Zhou, L., Wada, R., Hecht, R. I., & Xu, J. (2012) · Endocrinology · doi:10.1210/en.2012-1211 · Cited by 148

Relevant use of Klotho in FGF19 subfamily signaling system in vivo

Tomiyama, K.-I., Maeda, R., Urakawa, I., Yamazaki, Y., Tanaka, T., Ito, S., Nabeshima, Y., Tomita, T., Odori, S., Hosoda, K., et al. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0913986107 · Cited by 144

Fibroblast Growth Factor 21 (FGF21) in Human Cerebrospinal Fluid

Tan, B. K., Hallschmid, M., Adya, R., Kern, W., Lehnert, H., & Randeva, H. S. (2011) · Diabetes · doi:10.2337/db11-0672 · Cited by 129

Fibroblast Growth Factor 21 Predicts the Metabolic Syndrome and Type 2 Diabetes in Caucasians

Bobbert, T., Schwarz, F., Fischer‐Rosinsky, A., Pfeiffer, A. F. H., Möhlig, M., Mai, K., & Spranger, J. (2012) · Diabetes Care · doi:10.2337/dc12-0703 · Cited by 125

Development of a Novel Long-Acting Antidiabetic FGF21 Mimetic by Targeted Conjugation to a Scaffold Antibody

Huang, J., Ishino, T., Chen, G., Rolzin, P., Osothprarop, T. F., Retting, K., Li, L., Jin, P., Matin, M. J., Huyghe, B., et al. (2013) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.113.204420 · Cited by 121

Distinct Changes in Serum Fibroblast Growth Factor 21 Levels in Different Subtypes of Diabetes

Xiao, Y., Xu, A., Law, L. S., Chen, C., Li, H., Li, X., Yang, L., Liu, S., Zhou, Z., & Lam, K. S. L. (2011) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jc.2011-1930 · Cited by 102

Understanding the Physical Interactions in the FGF21/FGFR/β‐Klotho Complex: Structural Requirements and Implications in FGF21 Signaling

Yie, J., Wang, W., Deng, L., Tam, L., Stevens, J., Chen, M. M., Li, Y., Xu, J., Lindberg, R., Hecht, R., et al. (2012) · Chemical Biology & Drug Design · doi:10.1111/j.1747-0285.2012.01325.x · Cited by 99

FGF-21, a novel metabolic regulator, has a robust neuroprotective role and is markedly elevated in neurons by mood stabilizers

Leng, Y., Wang, Z., Tsai, L.-K., Leeds, P. R., Fessler, E. B., Wang, J., & Chuang, D. M. (2014) · Molecular Psychiatry · doi:10.1038/mp.2013.192 · Cited by 96

Fibroblast Growth Factor 21 (FGF21) Inhibits Chondrocyte Function and Growth Hormone Action Directly at the Growth Plate

Wu, S., Levenson, A. E., Kharitonenkov, A., & Luca, F. D. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.m112.343707 · Cited by 94

Glucagon increases circulating fibroblast growth factor 21 independently of endogenous insulin levels: a novel mechanism of glucagon-stimulated lipolysis?

Arafat, A. M., Kaczmarek, P., Skrzypski, M., Pruszyńska‐Oszmałek, E., Kolodziejski, P. A., Szczepankiewicz, D., Sassek, M., Wojciechowicz, T., Wiedenmann, B. J., Pfeiffer, A. F. H., et al. (2012) · Diabetologia · doi:10.1007/s00125-012-2803-y · Cited by 90

Fine tuning of hepcidin expression by positive and negative regulators

Muckenthaler, M. U. (2008) · Cell Metabolism · doi:10.1016/j.cmet.2008.06.009 · Cited by 83

Fibroblast growth factor 21 is not required for the antidiabetic actions of the thiazoladinediones

Adams, A. C., Coşkun, T., Cheng, C., O’Farrell, L. S., DuBois, S. L., & Kharitonenkov, A. (2013) · Molecular Metabolism · doi:10.1016/j.molmet.2013.05.005 · Cited by 75

Plasma FGF21 displays a circadian rhythm during a 72‐h fast in healthy female volunteers

Andersen, B., Beck‐Nielsen, H., & Højlund, K. (2011) · Clinical Endocrinology · doi:10.1111/j.1365-2265.2011.04084.x · Cited by 74

Differential Enzyme-Linked Immunosorbent Assay and Ligand-Binding Mass Spectrometry for Analysis of Biotransformation of Protein Therapeutics: Application to Various FGF21 Modalities

Hager, T., Spahr, C. S., Xu, J., Salimi-Moosavi, H., & Hall, M. P. (2013) · Analytical Chemistry · doi:10.1021/ac303203y · Cited by 62

Polyethylene Glycol Modified FGF21 Engineered to Maximize Potency and Minimize Vacuole Formation

Xu, J., Bussiere, J. L., Yie, J., Sickmier, E. A., An, P., Belouski, E., Stanislaus, S., & Walker, K. W. (2013) · Bioconjugate Chemistry · doi:10.1021/bc300603k · Cited by 61

FGF21 Can Be Mimicked In Vitro and In Vivo by a Novel Anti-FGFR1c/β-Klotho Bispecific Protein

Smith, R. J., Duguay, A. N., Bakker, A., Li, P., Weiszmann, J., Thomas, M. R., Alba, B. M., Wu, X., Gupte, J., Li, Y., et al. (2013) · PLoS ONE · doi:10.1371/journal.pone.0061432 · Cited by 59

Physiological modulation of circulating FGF21: relevance of free fatty acids and insulin

Mai, K., Bobbert, T., Groth, C., Aßmann, A., Meinus, S., Kraatz, J., Andres, J., Arafat, A. M., Pfeiffer, A. F. H., Möhlig, M., et al. (2010) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.00020.2010 · Cited by 58

Downstream Signaling Pathways in Mouse Adipose Tissues Following Acute In Vivo Administration of Fibroblast Growth Factor 21

Muise, E. S., Souza, S., Chi, A., Tan, Y., Zhao, X., Liu, F., Dallas-yang, Q., Wu, M., Sarr, T., Zhu, L., et al. (2013) · PLoS ONE · doi:10.1371/journal.pone.0073011 · Cited by 57

Fibroblast growth factor 21 (FGF21) and bone: is there a relationship in humans?

Lee, P., Linderman, J. D., Smith, S. M., Brychta, R. J., Perron, R., Idelson, C. R., Werner, C., Chen, K. Y., & Celi, F. S. (2013) · Osteoporosis International · doi:10.1007/s00198-013-2464-9 · Cited by 55

Characterization of a FGF19 Variant with Altered Receptor Specificity Revealed a Central Role for FGFR1c in the Regulation of Glucose Metabolism

Ge, H., Baribault, H., Vonderfecht, S. L., Lemon, B. D., Weiszmann, J., Gardner, J., Lee, K. J., Gupte, J., Mookherjee, P., Wang, M., et al. (2012) · PLoS ONE · doi:10.1371/journal.pone.0033603 · Cited by 43

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

Camacho, R. C., Zafian, P., Achanfuo-Yeboah, J., Manibusan, A., & Berger, J. P. (2013) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2013.06.023 · Cited by 38

Metabolically Protective Cytokines Adiponectin and Fibroblast Growth Factor-21 Are Increased by Acute Overfeeding in Healthy Humans

Heilbronn, L. K., Campbell, L. V., Xu, A., & Samocha‐Bonet, D. (2013) · PLoS ONE · doi:10.1371/journal.pone.0078864 · Cited by 36

Stress heats up the adipocyte

Fisher, F. M., & Maratos–Flier, E. (2013) · Nature Medicine · doi:10.1038/nm.3058 · Cited by 9

Mechanisms of Insulin Action and Insulin Resistance

Petersen, M. C., & Shulman, G. I. (2018) · Physiological Reviews · doi:10.1152/physrev.00063.2017 · Cited by 3,028

Understanding the Physiology of FGF21

Fisher, F. M., & Maratos-Flier, E. (2016) · Annual Review of Physiology · doi:10.1146/annurev-physiol-021115-105339 · Cited by 912

Targeting adipose tissue in the treatment of obesity-associated diabetes

Kusminski, C. M., Bickel, P. E., & Scherer, P. E. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.75 · Cited by 678

A long-acting FGF21 molecule, PF-05231023, decreases body weight and improves lipid profile in non-human primates and type 2 diabetic subjects

Talukdar, S., Zhou, Y., Li, D., Rossulek, M., Dong, J., Somayaji, V., Weng, Y., Clark, R., Lanba, A., Owen, B. M., et al. (2016) · Cell Metabolism · doi:10.1016/j.cmet.2016.02.001 · Cited by 496

Therapeutic potential of the endocrine fibroblast growth factors FGF19, FGF21 and FGF23

Degirolamo, C., Sabbà, C., & Moschetta, A. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2015.9 · Cited by 424

The potential function and clinical application of FGF21 in metabolic diseases

Chen, Z., Yang, L., Liu, Y., Huang, P., Song, H., & Zheng, P. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.1089214 · Cited by 73

Fibroblast growth factor 21: a novel metabolic regulator with potential therapeutic properties in obesity/type 2 diabetes mellitus

Dostálová, I., Haluzíková, D., & Haluzı́k, M. (2009) · Physiological Research · doi:10.33549/physiolres.931610 · Cited by 83

Metabolic actions of FGF21: molecular mechanisms and therapeutic implications

Ge, X., Wang, Y., Lam, K. S., & Xu, A. (2012) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2012.06.011 · Cited by 35

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

Geng, L., Lam, K. S. L., & Xu, A. (2020) · Nature Reviews Endocrinology · doi:10.1038/s41574-020-0386-0 · Cited by 607

FGF21: a novel prospect for the treatment of metabolic diseases.

Kharitonenkov, A., & Shanafelt, A. B. (2009) · PubMed · Cited by 91