Glucagon receptor antibody completely suppresses type 1 diabetes phenotype without insulin by disrupting a novel diabetogenic pathway

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Structure, function and drug discovery of GPCR signaling

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Insulin and Glucagon: Partners for Life

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Role of Glucagon and Its Receptor in the Pathogenesis of Diabetes

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Glycemia Regulation: From Feedback Loops to Organizational Closure

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Berberine promotes glucose uptake and inhibits gluconeogenesis by inhibiting deacetylase SIRT3

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Antagonistic Glucagon Receptor Antibody Promotes α-Cell Proliferation and Increases β-Cell Mass in Diabetic Mice

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Acute disruption of glucagon secretion or action does not improve glucose tolerance in an insulin-deficient mouse model of diabetes

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A cullin 4B-RING E3 ligase complex fine-tunes pancreatic δ cell paracrine interactions

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Hypoglycemic Effect of Combined Ghrelin and Glucagon Receptor Blockade

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Diabetes News

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Lipid nanoparticle delivery of glucagon receptor siRNA improves glucose homeostasis in mouse models of diabetes

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Dapagliflozin suppresses glucagon signaling in rodent models of diabetes

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Chronic fractalkine administration improves glucose tolerance and pancreatic endocrine function

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Glucagon receptor gene deletion in insulin knockout mice modestly reduces blood glucose and ketones but does not promote survival

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Glucagon Receptor Antagonism Ameliorates Progression of Heart Failure

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Neutrophils Release Metalloproteinases during Adhesion in the Presence of Insulin, but Cathepsin G in the Presence of Glucagon

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Intercellular Communication in the Islet of Langerhans in Health and Disease

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Glucagon therapeutics: Dawn of a new era for diabetes care

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Oligofructose as an adjunct in treatment of diabetes in NOD mice

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Pharmacological Actions of Glucagon-Like Peptide-1, Gastric Inhibitory Polypeptide, and Glucagon

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Neutrophils as a source of branched-chain, aromatic and positively charged free amino acids

Galkina, S. I., Fedorova, N. V., Ksenofontov, A. L., Stadnichuk, V. I., Baratova, L. A., & Sud’ina, G. F. (2018) · Cell Adhesion & Migration · doi:10.1080/19336918.2018.1540903 · Cited by 24 · see citing works

Regulated and adaptive in vivo insulin secretion from islets only containing β-cells

Perez-Frances, M., Bru-Tari, E., Cohrs, C., Abate, M., van Gurp, L., Furuyama, K., Speier, S., Thorel, F., & Herrera, P. (2024) · Nature Metabolism · doi:10.1038/s42255-024-01114-8 · Cited by 25 · see citing works

Deletion of the glucagon receptor gene before and after experimental diabetes reveals differential protection from hyperglycemia

Rivero‐Gutiérrez, B., Haller, A. M., Holland, J., Yates, E., Khrisna, R., Habegger, K. M., DiMarchi, R. D., D’Alessio, D. A., & Pérez–Tilve, D. (2018) · Molecular Metabolism · doi:10.1016/j.molmet.2018.07.012 · Cited by 23 · see citing works

High-fat diet impacts more changes in beta-cell compared to alpha-cell transcriptome

Dusaulcy, R., Handgraaf, S., Visentin, F., Howald, C., Dermitzakis, E. T., Philippé, J., & Gosmain, Y. (2019) · PLoS ONE · doi:10.1371/journal.pone.0213299 · Cited by 23 · see citing works

Glucagon receptor antagonism increases mouse pancreatic δ-cell mass through cell proliferation and duct-derived neogenesis

Gu, L., Cui, X., Lang, S., Wang, H., Hong, T., & Wei, R. (2019) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2019.03.148 · Cited by 22 · see citing works

Optimization of Truncated Glucagon Peptides to Achieve Selective, High Potency, Full Antagonists

Yang, B. S., Gelfanov, V. M., Pérez–Tilve, D., DUBOIS, B. N., Rohlfs, R., Levy, J. J., Douros, J. D., Finan, B., Mayer, J. P., & DiMarchi, R. D. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c02069 · Cited by 21 · see citing works

Emerging Anti-Diabetic Drugs for Beta-Cell Protection in Type 1 Diabetes

Ajmal, N., Bogart, M. C., Khan, P., Max-Harry, I. M., & Nunemaker, C. S. (2023) · Cells · doi:10.3390/cells12111472 · Cited by 20 · see citing works

Hyperglucagonaemia in diabetes: altered amino acid metabolism triggers mTORC1 activation, which drives glucagon production

Riahi, Y., Kogot‐Levin, A., Kadosh, L., Agranovich, B., Malka, A., Assa, M., Piran, R., Avrahami, D., Gläser, B., Gottlieb, E., et al. (2023) · Diabetologia · doi:10.1007/s00125-023-05967-8 · Cited by 19 · see citing works

Angptl4 does not control hyperglucagonemia or α-cell hyperplasia following glucagon receptor inhibition

Okamoto, H., Cavino, K., Na, E., Krumm, E. A., Kim, S. B., Stevis, P. E., Harp, J. B., Murphy, A. J., Yancopoulos, G. D., & Gromada, J. (2017) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1620989114 · Cited by 20 · see citing works

Glucagon receptor antagonism promotes the production of gut proglucagon-derived peptides in diabetic mice

Lang, S., Wei, R., Wei, T., Gu, L., Feng, J. B., Yan, H., Yang, J., & Hong, T. (2020) · Peptides · doi:10.1016/j.peptides.2020.170349 · Cited by 19 · see citing works

Regulation of Hepatic Lipid and Glucose Metabolism by INSP3R1

Perry, R. J. (2022) · Diabetes · doi:10.2337/dbi22-0003 · Cited by 19 · see citing works

Inhibition of prolyl hydroxylases increases hepatic insulin and decreases glucagon sensitivity by an HIF-2α-dependent mechanism

Riopel, M., Moon, J.-S., Bandyopadhyay, G. K., You, S.-H., Lam, K., Liu, X., Kisseleva, T., Brenner, D. A., & Lee, Y. S. (2020) · Molecular Metabolism · doi:10.1016/j.molmet.2020.101039 · Cited by 19 · see citing works

Coordination of Functional Oligonucleotides Yields a Versatile Nanocomposite Microneedle Patch to Facilitate Local Wound Microenvironment Remodeling via Systemic Hyperglycemia Regulation

Qian, Y., Zhang, B., Xu, Y., Liang, J., Yang, X., Gu, Y., Fan, Z., Li, D., & Hu, Y. M. (2025) · Advanced Functional Materials · doi:10.1002/adfm.202423012 · Cited by 18 · see citing works

MTORC1 inhibition drives crinophagic degradation of glucagon

Rajak, S., Xie, S. Y., Tewari, A., Raza, S., Wu, Y., Bay, B., Yen, P. M., & Sinha, R. A. (2021) · Molecular Metabolism · doi:10.1016/j.molmet.2021.101286 · Cited by 16 · see citing works

The Role of Glucagon in Glycemic Variability in Type 1 Diabetes: A Narrative Review

Guo, K., Tian, Q., Yang, L., & Zhou, Z. (2021) · Diabetes Metabolic Syndrome and Obesity · doi:10.2147/dmso.s343514 · Cited by 17 · see citing works

Single-molecule analysis reveals that a glucagon-bound extracellular domain of the glucagon receptor is dynamic

Liu, T., Khanal, S., Hertslet, G. D., & Lamichhane, R. (2023) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2023.105160 · Cited by 13 · see citing works

Disease-modifying pharmacological treatments of type 1 diabetes: Molecular mechanisms, target checkpoints, and possible combinatorial treatments

Kosheleva, L., Koshelev, D., Lagunas‐Rangel, F. A., Levit, S., Rabinovitch, A., & Schiöth, H. B. (2025) · Pharmacological Reviews · doi:10.1016/j.pharmr.2025.100044 · Cited by 12 · see citing works

Regulation of α‐cell glucagon secretion: The role of second messengers

Acreman, S., & Zhang, Q. (2021) · Chronic Diseases and Translational Medicine · doi:10.1016/j.cdtm.2021.06.001 · Cited by 9 · see citing works

Misrouting of glucagon and stathmin-2 towards lysosomal system of α-cells in glucagon hypersecretion of diabetes

Asadi, F., & Dhanvantari, S. (2021) · Islets · doi:10.1080/19382014.2021.2011550 · Cited by 13 · see citing works

Reduced islet function contributes to impaired glucose homeostasis in fructose-fed mice

Shyr, Z. A., Cusumano, A., Yan, Z., Remedi, M. S., & Moley, K. H. (2016) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.00279.2016 · Cited by 12 · see citing works

Global Transcriptomic Analysis of Zebrafish Glucagon Receptor Mutant Reveals Its Regulated Metabolic Network

Kang, Q., Hu, M., Jia, J., Bai, X., Liu, C., Wu, Z., Chen, W., & Li, M. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21030724 · Cited by 12 · see citing works

A famsin-glucagon axis mediates glucose homeostasis

Long, A., Wang, Y., Guo, Y., Hong, J., Ning, G., Meng, Z., Wang, Y., & Wang, Y. (2024) · Cell Metabolism · doi:10.1016/j.cmet.2024.11.008 · Cited by 11 · see citing works

Glucagon receptor blockage inhibits β-cell dedifferentiation through FoxO1

Wang, K., Cui, X., Li, F., Li, X., Wei, T., Liu, J., Fu, W., Yang, J., Hong, T., & Wei, R. (2022) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.00101.2022 · Cited by 11 · see citing works

Tumor promoting effects of glucagon receptor: a promising biomarker of papillary thyroid carcinoma via regulating EMT and P38/ERK pathways

Jiang, H.-C., Chen, X., Sun, H., & Nie, Y.-W. (2019) · Human Cell · doi:10.1007/s13577-019-00284-y · Cited by 11 · see citing works

Intercellular Communication in the Islet of Langerhans in Health and Disease

Ng, X.-W., Yong, H.-C., & Piston, D. W. (2021) · Comprehensive Physiology · doi:10.1002/j.2040-4603.2021.tb00177.x · Cited by 27 · see citing works

Protein kinase C-δ signaling regulates glucagon secretion from pancreatic islets

Yamamoto, K., Mizuguchi, H., Tokashiki, N., Kobayashi, M., Tamaki, M., Sato, Y., Fukui, H., & Yamauchi, A. (2017) · The Journal of Medical Investigation · doi:10.2152/jmi.64.122 · Cited by 10 · see citing works

Plasticity in the Glucagon Interactome Reveals Novel Proteins That Regulate Glucagon Secretion in α-TC1-6 Cells

Asadi, F., & Dhanvantari, S. (2019) · Frontiers in Endocrinology · doi:10.3389/fendo.2018.00792 · Cited by 9 · see citing works

Insulin and Sugars

Litwack, G. (2017) · Elsevier eBooks · doi:10.1016/b978-0-12-383864-3.00006-5 · Cited by 9 · see citing works

Inhibition of Cellular Adhesion by Immunological Targeting of Osteopontin Neoepitopes Generated through Matrix Metalloproteinase and Thrombin Cleavage

Jürets, A., Bras, M. L., Staffler, G., Stein, G., Leitner, L., Neuhofer, A., Tardelli, M., Turkof, E., Zeyda, M., & Stulnig, T. M. (2016) · PLoS ONE · doi:10.1371/journal.pone.0148333 · Cited by 9 · see citing works

Glucagon antagonism in islet cell proliferation

Dean, E. D., Unger, R. H., & Holland, W. L. (2017) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1700468114 · Cited by 9 · see citing works

Combination of GLP-1 Receptor Activation and Glucagon Blockage Promotes Pancreatic β-Cell Regeneration In Situ in Type 1 Diabetic Mice

Gu, L., Wang, D., Cui, X., Wei, T., Yang, K., Yang, J., Wei, R., & Hong, T. (2021) · Journal of Diabetes Research · doi:10.1155/2021/7765623 · Cited by 8 · see citing works

An AlphaScreen Assay for the Discovery of Synthetic Chemical Inhibitors of Glucagon Production

Evans, M. R., Wei, S., Posner, B. A., Unger, R. H., & Roth, M. G. (2015) · SLAS DISCOVERY · doi:10.1177/1087057115622201 · Cited by 8 · see citing works

Disruption of the glucagon receptor increases glucagon expression beyond α-cell hyperplasia in zebrafish

Kang, Q., Zheng, J., Jia, J., Xü, Y., Bai, X., Chen, X., Zhang, X.-K., Wong, F. S., Zhang, C., & Li, M. (2022) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2022.102665 · Cited by 7 · see citing works

Central leptin action on euglycemia restoration in type 1 diabetes: Restraining responses normally induced by fasting?

Xu, Y., & Tong, Q. (2016) · The International Journal of Biochemistry & Cell Biology · doi:10.1016/j.biocel.2016.09.027 · Cited by 7 · see citing works

Mechano-sensor Piezo1 inhibits glucagon production in pancreatic α-cells

Guo, W., Gao, L., Mo, H., Deng, H., Zhao, Y., & Xu, G. (2024) · Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease · doi:10.1016/j.bbadis.2024.167185 · Cited by 5 · see citing works

Abnormal late postprandial glucagon response in type 1 diabetes is a function of differences in stimulated C-peptide concentrations

Zhang, L., Qin, Y., Huang, Y., Hu, Q., Wu, Q., Wang, X., & Zhang, M. (2024) · Frontiers in Endocrinology · doi:10.3389/fendo.2024.1419329 · Cited by 6 · see citing works

Efficacy and safety of the glucagon receptor antagonist volagidemab in type‐1 diabetes: A systematic review and meta‐analysis

Dutta, D., Kamrul-Hasan, A. B. M., Surana, V., Singla, R., Khandelwal, D., Aggarwal, S., Nagendra, L., & Bhattacharya, S. (2024) · Annals of the New York Academy of Sciences · doi:10.1111/nyas.15262 · Cited by 5 · see citing works

Glucagon receptor signaling is indispensable for the healthspan effects of caloric restriction in aging male mice

Bruner, K. R., Byington, I. R., Marx, T. J., Vasileva, A., Fletcher, T., Ghimire, S., Zappia, I. J., Shaju, Y., Zeng, J., Wachsmuth, H. R., et al. (2025) · GeroScience · doi:10.1007/s11357-025-01899-w · Cited by 7 · see citing works

An orally available compound suppresses glucagon hypersecretion and normalizes hyperglycemia in type 1 diabetes

Asadi, F., Gunawardana, S. C., Dolle, R. E., & Piston, D. W. (2024) · JCI Insight · doi:10.1172/jci.insight.172626 · Cited by 4 · see citing works

Design, synthesis, and effects of novel phenylpyrimidines as glucagon receptor antagonists

Choi, H., Lee, C., Park, E., Lee, K. M., Shin, D., & Jun, H. (2018) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2018.10.013 · Cited by 4 · see citing works

Glucagon receptor antagonists might stimulate β-cell expansion

de Celis, M. F. R., & Bonner‐Weir, S. (2022) · Nature Reviews Endocrinology · doi:10.1038/s41574-022-00735-x · Cited by 4 · see citing works

Flycodes enable simultaneous preclinical analysis for dozens of antibodies in single cassette–dosed mice

Walter, J. D., Beffinger, M., Egloff, P., Zimmermann, I., Hürlimann, L. M., Ackle, F., Seifert, M., Kobold, S., Berg, J. V., & Seeger, M. A. (2025) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2426481122 · Cited by 3 · see citing works

The Inferential Binding Sites of GCGR for Small Molecules Using Protein Dynamic Conformations and Crystal Structures

Wang, M., Fu, X., Du, L., Shi, F., Huang, Z., & Yang, L. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25158389 · Cited by 3 · see citing works

Where are we now? Biased signalling of Class B G protein-coupled receptor-targeted therapeutics

Tasma, Z., Garelja, M. L., Jamaluddin, A., Alexander, T. I., & Rees, T. A. (2025) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2025.108846 · Cited by 2 · see citing works

Diabetes News

Regier, E. E., Gao, H. X., & Close, K. L. (2015) · Journal of Diabetes · doi:10.1111/1753-0407.12328 · Cited by 2 · see citing works

The impact of glucagon to support postabsorptive glucose flux and glycemia in healthy rats and its attenuation in male Zucker diabetic fatty rats

Estes, S. K., Shiota, C., O’Brien, T. P., Printz, R. L., & Shiota, M. (2024) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.00192.2023 · Cited by 1 · see citing works

Case-based learning: a case of maturity-onset diabetes of the young 5 (MODY5) due to 17q12 microdeletion with a diminished plasma glucagon level

Sugano, Y., Sekiya, M., Murayama, Y., Osaki, Y., Iwasaki, H., Suzuki, H., Fukushima, H., Suzuki, H., Noguchi, E., & Shimano, H. (2025) · Diabetology International · doi:10.1007/s13340-025-00804-2 · Cited by 1 · see citing works

Regulation of Type 1 Diabetes via Brown Adipocyte–Secreted Proteins and the Novel Glucagon Regulator Nidogen-2

Lee, J., Ustione, A., Wilkerson, E., Balakrishnan, R., Thurmond, D. C., Goldfarb, D., & Piston, D. W. (2025) · Diabetes · doi:10.2337/db24-1003 · Cited by 1 · see citing works

Contribution of systemic inflammation to permanence of KATP-induced neonatal diabetes in mice

Emfinger, C. H., Yan, Z., Welscher, A., Hung, P., McAllister, W., Hruz, P. W., Nichols, C. G., & Remedi, M. S. (2018) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.00137.2018 · Cited by 1 · see citing works

Small molecule glucagon release inhibitors with activity in human islets

Kalwat, M. A., Rodrigues-dos-Santos, K., Binns, D. D., Wei, S., Zhou, A., Evans, M. R., Posner, B. A., Roth, M. G., & Cobb, M. H. (2023) · Frontiers in Endocrinology · doi:10.3389/fendo.2023.1114799 · Cited by 1 · see citing works

Deletion of the glucagon receptor gene before and after experimental diabetes reveals differential protection from hyperglycemia

Rivero‐Gutiérrez, B., Haller, A. M., Holland, J., Yates, E., Khrisna, R., Habegger, K. M., DiMarchi, R. D., D’Alessio, D. A., & Pérez–Tilve, D. (2018) · Molecular Metabolism · doi:10.1016/j.molmet.2018.07.012 · Cited by 23 · see citing works

Glucagon receptor knockout prevents insulin-deficient type 1 diabetes in mice

Lee, Y., Wang, M.-Y., Du, X. Q., Charron, M. J., & Unger, R. H. (2011) · Diabetes · doi:10.2337/db10-0426 · Cited by 327 · see citing works

Hypoglycemic Effect of Combined Ghrelin and Glucagon Receptor Blockade

Mani, B. K., Uchida, A., Lee, Y., Osborne-Lawrence, S. L., Charron, M. J., Unger, R. H., Berglund, E. D., & Zigman, J. M. (2017) · Diabetes · doi:10.2337/db16-1303 · Cited by 34 · see citing works

New treatment approach for T1DM

Greenhill, C. (2015) · Nature Reviews Endocrinology · doi:10.1038/nrendo.2015.29

Long-Term Inhibition of the Glucagon Receptor with a Monoclonal Antibody in Mice Causes Sustained Improvement in Glycemic Control, with Reversible α-Cell Hyperplasia and Hyperglucagonemia

Gu, W., Yan, H., Winters, K. A., Komorowski, R., Vonderfecht, S. L., Atangan, L. I., Sivits, G. N., Hill, D., Yang, J., Bi, V., et al. (2009) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.109.157685 · Cited by 105 · see citing works