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

FGF-21 as a novel metabolic regulator

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Cellular signaling by fibroblast growth factor receptors

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Klotho converts canonical FGF receptor into a specific receptor for FGF23

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Receptor Specificity of the Fibroblast Growth Factor Family

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

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Structural basis for fibroblast growth factor receptor activation

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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

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Definition of a novel growth factor-dependent signal cascade for the suppression of bile acid biosynthesisPreprint

Holt, J. A., Luo, G., Billin, A. N., Bisi, J., McNeill, Y. Y., Kozarsky, K., Donahee, M. H., Wang, D. Y., Mansfield, T. A., Kliewer, S. A., et al. (2003) · Genes & Development · doi:10.1101/gad.1083503 · Cited by 714

FAP finds FGF21 easy to digest

Gillum, M. P., & Potthoff, M. J. (2016) · Biochemical Journal · doi:10.1042/bcj20160004 · Cited by 14

Engineered extracellular vesicles with surface FGF21 and enclosed miR-223 for treating metabolic dysfunction-associated steatohepatitis

Cho, H., Ju, H., Ahn, Y., Jang, J., Cho, J. L., Park, E., Kang, S.-M., Lee, J., Seo, D., Baek, M., et al. (2025) · Biomaterials · doi:10.1016/j.biomaterials.2025.123321 · Cited by 15

Metabolic Syndrome in Youth: Current Insights and Novel Serum Biomarkers

Santoro, N., & Weiss, R. (2012) · Biomarkers in Medicine · doi:10.2217/bmm.12.85 · Cited by 13

FGF21 inhibits apolipoprotein(a) expression in HepG2 cells via the FGFR1-ERK1/2-Elk-1 pathway

Lin, X., Li, G., He, X., Ma, X., Zhang, K., Zhang, H., Zeng, G., & Wang, Z. (2014) · Molecular and Cellular Biochemistry · doi:10.1007/s11010-014-2044-0 · Cited by 13

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

Xu, P., Zhang, Y., Song, L., Khoso, M. H., Li, J., Jiang, X., He, J., Li, J., Ma, X., Ren, G., et al. (2016) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2016.09.019 · Cited by 12

Mice with high FGF21 serum levels had a reduced preference for morphine and an attenuated development of acute antinociceptive tolerance and physical dependence

Dorval, L., Knapp, B. I., Majekodunmi, O. A., Eliseeva, S. I., & Bidlack, J. M. (2021) · Neuropharmacology · doi:10.1016/j.neuropharm.2021.108858 · Cited by 13

Development of Zalfermin, a Long-Acting Proteolytically Stabilized FGF21 Analog

Sass‐Ørum, K., Tagmose, T. M., Olsen, J., Sjölander, A., Wahlund, P., Han, D., Vegge, A., Reedtz‐Runge, S., Wang, Z., Gao, X., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c00391 · Cited by 11

Heating-mediated purification of active FGF21 and structure-based design of its variant with enhanced potency

Jung, Y., Lee, K. W., Cho, J. H., Bae, D., Jeong, B.-G., Jung, Y.-J., Park, S., An, Y. J., Kim, K., Lee, G. S., et al. (2023) · Scientific Reports · doi:10.1038/s41598-023-27717-x · Cited by 11

Two-hundred-liter scale fermentation, purification of recombinant human fibroblast growth factor-21, and its anti-diabetic effects on ob/ob mice

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Highly Selective and Sensitive Measurement of Active forms of FGF21 Using Novel Immunocapture Enrichment with LC–MS/MS

Zhao, Y., Liu, G., Kwok, S., Jones, B. R., Liu, J., Marchisin, D., Joyce, P., Peterson, J. E., & Shen, J. X. (2017) · Bioanalysis · doi:10.4155/bio-2017-0208 · Cited by 10

Circulating fibroblast growth factor 21 is reduced, whereas its production is increased in a fat depot-specific manner in cold-acclimated rats

Sepa-Kishi, D. M., & Ceddia, R. B. (2018) · Adipocyte · doi:10.1080/21623945.2018.1504591 · Cited by 10

FGF Pyramus Has a Transmembrane Domain and Cell-Autonomous Function in Polarity

Stepanik, V. A., Sun, J., & Stathopoulos, A. (2020) · Current Biology · doi:10.1016/j.cub.2020.06.006 · Cited by 10

Research progress on the role of FGF21 in insulin resistance

Zhang, H., Zhu, R., Sun, Q., & Du, L. (2025) · Frontiers in Endocrinology · doi:10.3389/fendo.2025.1619462 · Cited by 10

Preparation, characterization, and pharmacological study of a novel long-acting FGF21 with a potential therapeutic effect in obesity

Kim, D., Lee, J., Bae, I., Kim, M., Huh, Y., Choi, J., Bae, S., Choi, I. Y., Kim, H. H., & Kim, D. K. (2020) · Biologicals · doi:10.1016/j.biologicals.2020.11.005 · Cited by 9

Optimization of Peptide Inhibitors of β-Klotho as Antagonists of Fibroblast Growth Factors 19 and 21

Pan, J. B., Parlee, S. D., Brunel, F. M., Li, P., Lu, W., Pérez–Tilve, D., Liu, F., Finan, B., Kharitonenkov, A., & DiMarchi, R. D. (2020) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.0c00100 · Cited by 9

Targeting an Acid Labile Aspartyl–Prolyl Amide Bond as A Viable Alternative to Trypsin Digestion to Generate A Surrogate Peptide for LC–MS/MS Analysis

Fung, E. N., Zambito, F., Haulenbeek, J. R., Piccoli, S. P., Zhang, Y., Desilva, B. S., Arnold, M. E., & Kozhich, A. T. (2014) · Bioanalysis · doi:10.4155/bio.14.182 · Cited by 8

Localization of FGF21 Protein and Lipid Metabolism-Related Genes in Camels

Gao, Y., Zhao, S., Zhang, W., Tang, H., Yan, M., Yong, F., Bai, X., Wu, X., Zhang, Y., & Zhang, Q. (2023) · Life · doi:10.3390/life13020432 · Cited by 7

The emerging role of fibroblast growth factor 21 in diabetic nephropathy

Mao, S., Ren, X., & Zhang, J. (2016) · Journal of Receptors and Signal Transduction · doi:10.3109/10799893.2016.1147582 · Cited by 7

Noncompetitive immunoassay optimized for pharmacokinetic assessments of biologically active efruxifermin

Kinne, A. S., Tillman, E. J., Abdeen, S. J., Johnson, D. E., Parmer, E. S., Hurst, J. P., de Temple, B., Rinker, S. D., Rolph, T., & Bowsher, R. R. (2023) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2023.115402 · Cited by 6

Field-Flow Fractionation for Assessing Biomolecular Interactions in Solution

Chou, R., Pollastrini, J., Dillon, T. M., Bondarenko, P. V., Tam, L. T., Miller, J. M., Moxness, M. S., & Cao, S. (2011) · Springer eBooks · doi:10.1007/978-3-7091-0154-4_8 · Cited by 5

Insights into the role of FGF21 in coronary heart disease

Zhang, Q.-Y., & Liu, H. (2024) · International Journal of Biological Macromolecules · doi:10.1016/j.ijbiomac.2024.136911 · Cited by 4

Animal Models for Manipulation of Thermogenesis

Fuller‐Jackson, J., Clarke, I. J., & Henry, B. A. (2017) · Elsevier eBooks · doi:10.1016/b978-0-12-809468-6.00012-7 · Cited by 4

Stability and Glucose Regulation of FGF21 After Modified With Arginines*

Kun, H. E., Zhang, Y., Ye, X., Wang, W., Chen, R., Liu, M., Feng, M., Xu, J., & Li, D. (2012) · PROGRESS IN BIOCHEMISTRY AND BIOPHYSICS · doi:10.3724/sp.j.1206.2012.00007 · Cited by 4

Enhanced bioactivity and stability of a long-acting FGF21: A novel variant for the treatment of NASH

Ji, Y. R., Lu, Q., Duan, Y., Xuan, C., Zhang, Y., Yao, W., Yin, J., & Gao, X. (2024) · Biochimie · doi:10.1016/j.biochi.2024.05.013 · Cited by 3

Therapeutic effect of long-acting FGF21 with controlled site-specific modification on nonalcoholic steatohepatitis

Qi, J., Guo, Z., Zhu, S., Jiang, X. J., Wu, Y., Chen, Y., Hu, F., Xiong, J., Wu, Y., Ye, X., et al. (2024) · International Journal of Biological Macromolecules · doi:10.1016/j.ijbiomac.2024.129797 · Cited by 3

Fibroblast Growth Factor 21 is a Regulator of Energy Metabolism in the Liver and Adipose Tissue

Matikainen, N. (2014) · Elsevier eBooks · doi:10.1016/b978-0-12-407869-7.00039-8 · Cited by 3

Fibroblast Growth Factor 21 as a Regulator of Energy Metabolism in the Liver and Adipose Tissue

Matikainen, N., & Söderlund, S. (2019) · Elsevier eBooks · doi:10.1016/b978-0-12-816093-0.00013-6 · Cited by 2

Fibroblast growth factor-21: A link for glucose homeostasis

Naderali, E. K., Wong, C., & Hussain, M. (2009) · Diabetes & Metabolic Syndrome Clinical Research & Reviews · doi:10.1016/j.dsx.2009.07.002 · Cited by 2

Glucose and lipopolysaccharide differentially regulate fibroblast growth factor 21 in healthy male human volunteers – A prospective cross‐over trial

Pohlhammer, J., Heinzl, M. W., Klammer, C., Feldbauer, R., Rosenberger, K., Resl, M., Wagner, T., Obendorf, F., Egger-Salmhofer, M., Dieplinger, B., et al. (2022) · Journal of Cellular and Molecular Medicine · doi:10.1111/jcmm.17614 · Cited by 1

Animal Models for Manipulation of Thermogenesis

Henry, B. A., & Clarke, I. J. (2013) · Elsevier eBooks · doi:10.1016/b978-0-12-415894-8.00014-2 · Cited by 2

Fibroblast Growth Factor 21 as a Novel Metabolic Regulator

Micanovic, R., Dunbar, J. D., & Kharitonenkov, A. (2011) · Wiley eBooks · doi:10.1002/9780470910016.ch14 · Cited by 2

The Role of The βklotho Gene, Fgf21 and Fgfr1 in Cancerogenesis

Wójcik‐Krowiranda, K., Szczepaniec, S., & Bieńkiewicz, A. (2018) · Women Health Care and Issues · doi:10.31579/2642-9756/003 · Cited by 1

GH replacement therapy in adults stimulates fibroblast activation protein-α activity

Bæk, A., Pedersen, A. K. N., Billeskov, T. B., Dollerup, O. L., Arlien-Søborg, M. C., Jessen, N., Bjerre, M., & Jørgensen, J. O. L. (2025) · European Journal of Endocrinology · doi:10.1093/ejendo/lvaf244 · Cited by 1

Serum fibroblast growth factor 21 is a novel biomarker of cachexia in chronic liver disease

Tanaka, T., Suda, G., Ohara, M., Maehara, O., Yoda, T., Fu, Q., Yang, Z., Yasuura, N., Meno, A., Sasaki, T., et al. (2026) · Frontiers in Nutrition · doi:10.3389/fnut.2026.1730695 · Cited by 1

Current therapeutic landscape and future treatment perspectives of MASH

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Fibroblast growth factor 21: a novel link in the development and treatment of metabolic disorders

Mikhailova, A. A., Sharypova, M. V., Симаненкова, А. В., Cheburkin, Y. V., Станиславовна, Ф. О., Тимкина, Н. В., Dyachuk, V. A., & Каронова, Т. Л. (2025) · Arterial’naya Gipertenziya (Arterial Hypertension) · doi:10.18705/1607-419x-2024-2455 · Cited by 1

FGF21

Cheng, T. W., & Leung, P. S. (2017) · Springer eBooks · doi:10.1007/978-3-319-67199-4_101992 · Cited by 1

The role of metabolic hormone Fibroblast Growth Factor 21 (FGF21) in mammalian hibernation using transgenic ground squirrels

Nelson, B. T. (2012) · University of Minnesota Digital Conservancy (University of Minnesota)

IN PARTIAL FULFILLMENT OF THE REQUIREMENTS FOR THE DEGREE OF DOCTOR OF PHILOSOPHY

Nelson, B. T. (2012)

Potensi Terapeutik Fibroblast Growth Factor 21 terhadap Resistensi Insulin

Kurniasari, K., & Arozal, W. (2015) · eJournal Kedokteran Indonesia · doi:10.23886/ejki.3.5049

Harnessing the Action of Fibroblast Growth Factor21 as a Therapeutic Agent

Brunetti, L., & Kagan, L. (2017) · Current Pharmacology Reports · doi:10.1007/s40495-017-0080-7

Molecular description of fibroblast growth factor and mechanisms by which fibroblast growth factor-21 mediating biological actions and acting as a biologic biomarker of cardiovascular diseases

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Temperature-responsive structural reversibility of FGF21 and structure-based design of its variant with enhanced potencyPreprint

Jung, Y., Lee, K. W., Cho, J., Bae, D., Jeong, B., Jung, Y.-J., An, Y.-J., Kim, K., Lee, G., Kang, L.-W., et al. (2021) · bioRxiv · doi:10.1101/2021.11.16.468794

FGF21

Cheng, T. W., & Leung, P. S. (2017) · Springer eBooks · doi:10.1007/978-1-4614-6438-9_101992-1

Bioreactor and engineering

Li, X. (2024) · Elsevier eBooks · doi:10.1016/b978-0-443-15793-6.00007-x

Endocrine fibroblast growth factors in domestic animals

Brinker, E. J., Hardcastle, M., Dittmer, K. E., & Graff, E. C. (2024) · Domestic Animal Endocrinology · doi:10.1016/j.domaniend.2024.106872

Fibroblast activation protein and down-stream effects on its substrates in metabolic dysfunction-associated steatotic liver disease

Hansson, S. F., Nasr, P., Knöchel, J., Miliotis, T., Andréasson, A., Hober, A., Nyström, A., Bergenholm, L., Karimi, M., Peng, X., et al. (2026) · Scandinavian Journal of Gastroenterology · doi:10.1080/00365521.2026.2679101

Peptide hormone-based combinational pharmacotherapies for chronic metabolic diseases

Chui, Z. S. W., Xue, Y., Wu, X., & Xu, A. (2026) · Pharmacological Reviews · doi:10.1016/j.pharmr.2026.100150

Terminus-specific antibody development and bioanalytical assay validation to quantify active DR10624 in pharmacokinetic studies

Zhou, Z., Cao, K., 姚高峰, Liu, Y., Duan, W., Yang, C., Sheng, S., & Huang, Y. (2026) · Frontiers in Pharmacology · doi:10.3389/fphar.2026.1863402

Different roles of N‐ and C‐ termini in the functional activity of FGF21

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Estradiol regulates renal klotho through estrogen receptor alpha

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

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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

The FGFR D3 Domain Determines Receptor Selectivity For Fibroblast Growth Factor 21

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