A Naturally Occurring GIP Receptor Variant Undergoes Enhanced Agonist-Induced Desensitization, Which Impairs GIP Control of Adipose Insulin Sensitivity

Untitled work

Colman (2022) · doi:10.1073/pnas · Cited by 4,370 · see citing works

The biology of incretin hormones

Drucker, D. J. (2006) · Cell Metabolism · doi:10.1016/j.cmet.2006.01.004 · Cited by 2,210 · see citing works

Preserved incretin activity of glucagon-like peptide 1 [7-36 amide] but not of synthetic human gastric inhibitory polypeptide in patients with type-2 diabetes mellitus

Nauck, M. A., Heimesaat, M. M., Orskov, C., Holst, J. J., Ebert, R., & Creutzfeldt, W. (1993) · Journal of Clinical Investigation · doi:10.1172/jci116186 · Cited by 1,651 · see citing works

Turning off the signal: desensitization of β‐adrenergic receptor function

Hausdorff, W. P., Caron, M. G., & Lefkowitz, R. J. (1990) · The FASEB Journal · doi:10.1096/fasebj.4.11.2165947 · Cited by 1,259 · see citing works

The role of β-arrestins in the termination and transduction of G-protein-coupled receptor signals

Luttrell, L. M., & Lefkowitz, R. J. (2002) · Journal of Cell Science · doi:10.1242/jcs.115.3.455 · Cited by 1,123 · see citing works

Inhibition of gastric inhibitory polypeptide signaling prevents obesity

Miyawaki, K., Yamada, Y., Ban, N., Ihara, Y., Tsukiyama, K., Zhou, H., Fujimoto, S., Oku, A., Tsuda, K., Toyokuni, S., et al. (2002) · Nature Medicine · doi:10.1038/nm727 · Cited by 963 · see citing works

STIMULATION OF INSULIN SECRETION BY GASTRIC INHIBITORY POLYPEPTIDE IN MAN. ¹

Dupre, J., Ross, S. A., Watson, D., & Brown, J. C. (1973) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jcem-37-5-826 · Cited by 860 · see citing works

The role of incretins in glucose homeostasis and diabetes treatment

Kim, W., & Egan, J. M. (2008) · Pharmacological Reviews · doi:10.1124/pr.108.000604 · Cited by 824 · see citing works

Genetic variation in GIPR influences the glucose and insulin responses to an oral glucose challenge

Saxena, R., the MAGIC investigators, Hivert, M., Langenberg, C., Tanaka, T., Pankow, J. S., Vollenweider, P., Lyssenko, V., Bouatia‐Naji, N., Dupuis, J., et al. (2010) · Nature Genetics · doi:10.1038/ng.521 · Cited by 621 · see citing works

Defective amplification of the late phase insulin response to glucose by GIP in obese Type II diabetic patients

T., V., T., K., S., M., & J., H. (2002) · Diabetologia · doi:10.1007/s00125-002-0878-6 · Cited by 518 · see citing works

Fine-tuning of GPCR activity by receptor-interacting proteins

Ritter, S. L., & Hall, R. A. (2009) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm2803 · Cited by 479 · see citing works

Journal of Lipid Research

(2021) · Journal of Lipid Research · doi:10.1194/jlr · Cited by 435 · see citing works

Both GLP-1 and GIP are insulinotropic at basal and postprandial glucose levels and contribute nearly equally to the incretin effect of a meal in healthy subjects

Vilsbøll, T., Krarup, T., Madsbad, S., & Holst, J. J. (2003) · Regulatory Peptides · doi:10.1016/s0167-0115(03)00111-3 · Cited by 430 · see citing works

Agonist‐selective mechanisms of GPCR desensitization

Kelly, E., Bailey, C. P., & Henderson, G. (2007) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0707604 · Cited by 388 · see citing works

Intestinal Factors in the Control of Insulin Secretion

McIntyre, N. R., Holdsworth, C. D., & Turner, D. S. (1965) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jcem-25-10-1317 · Cited by 387 · see citing works

Regulation of GPCR activity, trafficking and localization by GPCR‐interacting proteins

Magalhães, A. C., Dunn, H. A., & Ferguson, S. S. G. (2011) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2011.01552.x · Cited by 352 · see citing works

G-protein-coupled receptor regulation: role of G-protein-coupled receptor kinases and arrestins

Ferguson, S. S. G., Barak, L. S., Zhang, J., & Caron, M. G. (1996) · Canadian Journal of Physiology and Pharmacology · doi:10.1139/cjpp-74-10-1095 · Cited by 330 · see citing works

Location, location, location…site-specific GPCR phosphorylation offers a mechanism for cell-type-specific signalling

Tobin, A. B., Butcher, A. J., & Kong, K. C. (2008) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2008.05.006 · Cited by 309 · see citing works

The insulinotropic actions of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (7–37) in normal and diabetic subjects

Elahi, D., McAloon-Dyke, M., Fukagawa, N. K., Meneilly, G. S., Sclater, A. L., Minaker, K. L., Habener, J. F., & Andersen, D. K. (1994) · Regulatory Peptides · doi:10.1016/0167-0115(94)90136-8 · Cited by 308 · see citing works

G-protein-coupled receptor regulation: role of G-protein-coupled receptor kinases and arrestins

Ferguson, S. S. G., Barak, L. S., Zhang, J., & Caron, M. G. (1996) · Canadian Journal of Physiology and Pharmacology · doi:10.1139/y96-124 · Cited by 294 · see citing works

Molecular mechanism of desensitization of the chemokine receptor CCR‐5: receptor signaling and internalization are dissociable from its role as an HIV‐1 co‐receptor

Aramori, I., Zhang, J., Ferguson, S. S. G., et al. (1997) · The EMBO Journal · doi:10.1093/emboj/16.15.4606 · Cited by 251 · see citing works

Functional GIP Receptors Are Present on Adipocytes

Yip, R. G.-C., Boylan, M. O., Kieffer, T. J., & Wolfe, M. M. (1998) · Endocrinology · doi:10.1210/endo.139.9.6288 · Cited by 237 · see citing works

Insulin Stimulation of GLUT4 Exocytosis, but Not Its Inhibition of Endocytosis, Is Dependent on RabGAP AS160

Zeigerer, A., McBrayer, M. K., & McGraw, T. E. (2004) · Molecular Biology of the Cell · doi:10.1091/mbc.e04-04-0333 · Cited by 226 · see citing works

Regulation of G Protein-Coupled Receptor Kinases

Penn, R. B. (2000) · Trends in Cardiovascular Medicine · doi:10.1016/s1050-1738(00)00053-0 · Cited by 211 · see citing works

Differential G-protein-coupled Receptor Phosphorylation Provides Evidence for a Signaling Bar Code

Butcher, A. J., Prihandoko, R., Kong, K. C., McWilliams, P., Edwards, J. M., Bottrill, A. R., Mistry, S. C., & Tobin, A. B. (2010) · Journal of Biological Chemistry · doi:10.1074/jbc.m110.154526 · Cited by 203 · see citing works

Glucose-dependent insulinotropic polypeptide may enhance fatty acid re-esterification in subcutaneous abdominal adipose tissue in lean humans

Asmar, M., Simonsen, L., Madsbad, S., Stallknecht, B., Holst, J. J., & Bülow, J. (2010) · Diabetes · doi:10.2337/db10-0098 · Cited by 184 · see citing works

GLUT4 Is Retained by an Intracellular Cycle of Vesicle Formation and Fusion with Endosomes

Karylowski, O., Zeigerer, A., Cohen, A., & McGraw, T. E. (2003) · Molecular Biology of the Cell · doi:10.1091/mbc.e03-07-0517 · Cited by 182 · see citing works

GLUT4 Retention in Adipocytes Requires Two Intracellular Insulin-regulated Transport Steps

Zeigerer, A., Lampson, M. A., Karylowski, O., Sabatini, D. D., Adesnik, M., Ren, M., & McGraw, T. E. (2002) · Molecular Biology of the Cell · doi:10.1091/mbc.e02-02-0071 · Cited by 180 · see citing works

Postprandial stimulation of insulin release by glucose-dependent insulinotropic polypeptide (GIP). Effect of a specific glucose-dependent insulinotropic polypeptide receptor antagonist in the rat.

Tseng, C., Kieffer, T. J., Jarboe, L. A., Usdin, T. B., & Wolfe, M. M. (1996) · Journal of Clinical Investigation · doi:10.1172/jci119060 · Cited by 149 · see citing works

Imaging of receptor trafficking by using α-bungarotoxin-binding-site-tagged receptors

Sekine‐Aizawa, Y., & Huganir, R. L. (2004) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0407563101 · Cited by 147 · see citing works

Glucose-dependent insulinotropic polypeptide modulates adipocyte lipolysis and reesterification

Getty‐Kaushik, L., Song, D. H., Boylan, M. O., Corkey, B. E., & Wolfe, M. M. (2006) · Obesity · doi:10.1038/oby.2006.129 · Cited by 134 · see citing works

GIP increases human adipocyte LPL expression through CREB and TORC2-mediated trans-activation of the LPL gene

Kim, S.-J., Nian, C., & McIntosh, C. H. S. (2010) · Journal of Lipid Research · doi:10.1194/jlr.m006841 · Cited by 133 · see citing works

Insulin-regulated Release from the Endosomal Recycling Compartment Is Regulated by Budding of Specialized Vesicles

Lampson, M. A., Schmoranzer, J., Zeigerer, A., Simon, S. M., & McGraw, T. E. (2001) · Molecular Biology of the Cell · doi:10.1091/mbc.12.11.3489 · Cited by 128 · see citing works

Effects of Ingestion of Triglyceride or Galactose on Secretion of Gastric Inhibitory Polypeptide and on Responses to Intravenous Glucose in Normal and Diabetic Subjects

Ross, S. A., & Dupré, J. (1978) · Diabetes · doi:10.2337/diab.27.3.327 · Cited by 110 · see citing works

Demonstration of insulin-responsive trafficking of GLUT4 and vpTR in fibroblasts

Lampson, M. A., Racz, A., Cushman, S. W., & McGraw, T. E. (2000) · Journal of Cell Science · doi:10.1242/jcs.113.22.4065 · Cited by 109 · see citing works

Hormones, Receptors, and Cyclic AMP: Their Role in Target Cell Refractoriness

Lefkowitz, R. J., Wessels, M. R., & Stadel, J. M. (1980) · Current topics in cellular regulation · doi:10.1016/b978-0-12-152817-1.50011-0 · Cited by 108 · see citing works

Pleiotropic Effects of GIP on Islet Function Involve Osteopontin

Lyssenko, V., Eliasson, L., Kotova, O., Pilgaard, K. A., Wierup, N., Salehi, A. A., Wendt, A., Jonsson, A. E., Marinis, Y. Z. D., Berglund, L. M., et al. (2011) · Diabetes · doi:10.2337/db10-1532 · Cited by 97 · see citing works

Variants from GIPR, TCF7L2, DGKB, MADD, CRY2, GLIS3, PROX1, SLC30A8 and IGF1 Are Associated with Glucose Metabolism in the Chinese

Hu, C., Zhang, R., Wang, C., Wang, J., Ma, X., Hou, X., Lu, J., Yu, W., Jiang, F., Bao, Y., et al. (2010) · PLoS ONE · doi:10.1371/journal.pone.0015542 · Cited by 96 · see citing works

Link between GIP and osteopontin in adipose tissue and insulin resistance

Ahlqvist, E., Osmark, P., Kuulasmaa, T., Pilgaard, K., Omar, B., Brøns, C., Kotova, O., Zetterqvist, A. V., Stančáková, A., Jonsson, A., et al. (2013) · Diabetes · doi:10.2337/db12-0976 · Cited by 96 · see citing works

GLUT4 Distribution between the Plasma Membrane and the Intracellular Compartments Is Maintained by an Insulin-modulated Bipartite Dynamic Mechanism

Martin, O. J., Lee, A. V., & McGraw, T. E. (2005) · Journal of Biological Chemistry · doi:10.1074/jbc.m505944200 · Cited by 92 · see citing works

The Chemokine Receptor CCR1 Is Constitutively Active, Which Leads to G Protein-independent, β-Arrestin-mediated Internalization

Gilliland, C. T., Salanga, C. L., Kawamura, T., Trejo, J., & Handel, T. M. (2013) · Journal of Biological Chemistry · doi:10.1074/jbc.m113.503797 · Cited by 90 · see citing works

Receptor downregulation and desensitization enhance the information processing ability of signalling receptors

Shankaran, H., Wiley, H. S., & Resat, H. (2007) · BMC Systems Biology · doi:10.1186/1752-0509-1-48 · Cited by 89 · see citing works

Pharmacological Characterization of Human Incretin Receptor Missense Variants

Fortin, J., Schroeder, J. C., Zhu, Y., Beinborn, M., & Kopin, A. S. (2009) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.109.160531 · Cited by 86 · see citing works

Cannabinoid receptor 2 undergoes Rab5-mediated internalization and recycles via a Rab11-dependent pathway

Grimsey, N. L., Goodfellow, C. E., Dragunow, M., & Glass, M. (2011) · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research · doi:10.1016/j.bbamcr.2011.05.010 · Cited by 83 · see citing works

Disease-associated GPR56 Mutations Cause Bilateral Frontoparietal Polymicrogyria via Multiple Mechanisms

Chiang, N., Hsiao, C., Huang, Y.-S., Chen, H.-Y., Hsieh, I.-J., Chang, G.-W., & Lin, H. (2011) · Journal of Biological Chemistry · doi:10.1074/jbc.m110.183830 · Cited by 82 · see citing works

Characterisation of beta-cell dysfunction of impaired glucose tolerance: Evidence for impairment of incretin-induced insulin secretion

Fritsche, A., Stefan, N., Hardt, E., Häring, H., & Stümvoll, M. (2000) · Diabetologia · doi:10.1007/s001250051461 · Cited by 76 · see citing works

Gastric inhibitory polypeptide modulates adiposity and fat oxidation under diminished insulin action

Zhou, H., Yamada, Y., Tsukiyama, K., Miyawaki, K., Hosokawa, M., Nagashima, K., Toyoda, K., Naitoh, R., Mizunoya, W., Fushiki, T., et al. (2005) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2005.07.164 · Cited by 76 · see citing works

Ubiquitination is involved in glucose-mediated downregulation of GIP receptors in islets

Zhou, J., Livak, M. F. A., Bernier, M., Muller, D. C., Carlson, O. D., Elahi, D., Maudsley, S. R., & Egan, J. M. (2007) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.00070.2007 · Cited by 72 · see citing works

Discovery of amino acid variants in the human glucose-dependent insulinotropic polypeptide (GIP) receptor: the impact on the pancreatic beta cell responses and functional expression studies in Chinese hamster fibroblast cells

Almind, K., Ambye, L., Urhammer, S. A., Hansen, T. F., Echwald, S. M., Holst, J. J., Gromada, J., Thorens, B., & Pedersen, O. B. (1998) · Diabetologia · doi:10.1007/s001250051051 · Cited by 68 · see citing works

Disease-Associated Mutations Prevent GPR56-Collagen III Interaction

Luo, R., Jin, Z., Deng, Y., Strokes, N., & Piao, X. (2012) · PLoS ONE · doi:10.1371/journal.pone.0029818 · Cited by 65 · see citing works

Gastric inhibitory peptide controls adipose insulin sensitivity via activation of cAMP-response element-binding protein and p110β isoform of phosphatidylinositol 3-kinase

Mohammad, S., Ramos, L. S., Buck, J., Levin, L. R., Rubino, F., & McGraw, T. E. (2011) · Journal of Biological Chemistry · doi:10.1074/jbc.m111.289009 · Cited by 59 · see citing works

Constitutive Internalization of the Leucine-rich G Protein-coupled Receptor-5 (LGR5) to the Trans-Golgi Network

Snyder, J. C., Rochelle, L. K., Lyerly, H. K., Caron, M. G., & Barak, L. S. (2013) · Journal of Biological Chemistry · doi:10.1074/jbc.m112.447540 · Cited by 59 · see citing works

Obesity-Linked Variants of Melanocortin-4 Receptor Are Misfolded in the Endoplasmic Reticulum and Can Be Rescued to the Cell Surface by a Chemical Chaperone

Granell, S., Mohammad, S., Ramanagoudr‐Bhojappa, R., & Baldini, G. (2010) · Molecular Endocrinology · doi:10.1210/me.2010-0071 · Cited by 58 · see citing works

Glucose-dependent insulinotropic polypeptide has impaired effect on abdominal, subcutaneous adipose tissue metabolism in obese subjects

Asmar, M., Simonsen, L., Arngrim, N., Holst, J. J., Dela, F., & Bülow, J. (2013) · International Journal of Obesity · doi:10.1038/ijo.2013.73 · Cited by 57 · see citing works

Constitutive Traffic of Melanocortin-4 Receptor in Neuro2A Cells and Immortalized Hypothalamic Neurons

Mohammad, S., Baldini, G., Granell, S., Narducci, P., Martelli, A. M., & Baldini, G. (2006) · Journal of Biological Chemistry · doi:10.1074/jbc.m608283200 · Cited by 56 · see citing works

GIP increases insulin receptor affinity and cellular sensitivity in adipocytes

Starich, G. H., Bar, R. S., & Mazzaferri, E. L. (1985) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.1985.249.6.e603 · Cited by 56 · see citing works

Chronic desensitization of the glucose-dependent insulinotropic polypeptide receptor in diabetic rats

Tseng, C., Boylan, M. O., Jarboe, L. A., Usdin, T. B., & Wolfe, M. M. (1996) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.1996.270.4.e661 · Cited by 56 · see citing works

Pharmacological Characterization of 30 Human Melanocortin-4 Receptor Polymorphisms with the Endogenous Proopiomelanocortin-Derived Agonists, Synthetic Agonists, and the Endogenous Agouti-Related Protein Antagonist,

Xiang, Z., Proneth, B., Dirain, M. L. S., Litherland, S. A., & Haskell‐Luevano, C. (2010) · Biochemistry · doi:10.1021/bi100068u · Cited by 54 · see citing works

Atlantic white-sided dolphin (Lagenorhynchus acutus)

Reeves, R., Galatius, A., Kinze, C. C., et al. (2025) · Academic Press eBooks · doi:10.1016/b978 · Cited by 51 · see citing works

Role of G Protein-Coupled Receptor Kinases in Glucose-Dependent Insulinotropic Polypeptide Receptor Signaling

Tseng, C., & Zhang, X. (2000) · Endocrinology · doi:10.1210/endo.141.3.7365 · Cited by 50 · see citing works

Gastric inhibitory peptide (GIP), pancreatic glucagon and vasoactive intestinal peptide (VIP) are cAMP-inducing hormones in the human gastric cancer cell line HGT-1. Homologous desensitization of VIP receptor activity

Gespach, C. P., Emami, S., & Rosselin, G. (1984) · Biochemical and Biophysical Research Communications · doi:10.1016/0006-291x(84)91304-4 · Cited by 46 · see citing works

Aberrant trafficking of human melanocortin 1 receptor variants associated with red hair and skin cancer: Steady‐state retention of mutant forms in the proximal golgi

Sánchez‐Laorden, B. L., Herráiz, C., Valencia, J. C., Hearing, V. J., Jiménez‐Cervantes, C., & García-Borrón, J. C. (2009) · Journal of Cellular Physiology · doi:10.1002/jcp.21804 · Cited by 45 · see citing works

Association analyses of GIP and GIPR polymorphisms with traits of the metabolic syndrome

Nitz, I., Fisher, E., Weikert, C., Burwinkel, B., Li, Y., Möhlig, M., Boeing, H., Schreiber, S., Schrezenmeir, J., & Döring, F. (2007) · Molecular Nutrition & Food Research · doi:10.1002/mnfr.200700048 · Cited by 44 · see citing works

Constitutive internalization and recycling of metabotropic glutamate receptor 5 (mGluR5)

Trivedi, R. R., & Bhattacharyya, S. (2012) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2012.09.040 · Cited by 39 · see citing works

Enhanced cAMP generation and insulin-releasing potency of two novel Tyr1-modified enzyme-resistant forms of glucose-dependent insulinotropic polypeptide is associated with significant antihyperglycaemic activity in spontaneous obesity-diabetes

Gault, V. A., Flatt, P. R., Bailey, C. J., Harriott, P., Greer, B., Mooney, M. H., & O'Harte, F. P. M. (2002) · Biochemical Journal · doi:10.1042/bj20020319 · Cited by 38 · see citing works

The Postendocytotic Trafficking of the Human Lutropin Receptor Is Mediated by a Transferable Motif Consisting of the C-Terminal Cysteine and an Upstream Leucine

Galet, C., Hirakawa, T., & Ascoli, M. (2003) · Molecular Endocrinology · doi:10.1210/me.2003-0293 · Cited by 36 · see citing works

-Aminobutyric Acid Type B (GABAB) Receptor Internalization Is Regulated by the R2 Subunit

Hannan, S. B., Wilkins, M. E., Dehghani-Tafti, E., et al. (2011) · Journal of Biological Chemistry · doi:10.1074/jbc.m110.220814 · Cited by 31 · see citing works

Association of variants in gastric inhibitory polypeptide receptor gene with impaired glucose homeostasis in obese children and adolescents from Berlin

Sauber, J., Grothe, J., Behm, M., Scherag, A., Grallert, H., Illig, T., Hinney, A., Hebebrand, J., Wiegand, S., Grüters, A., et al. (2010) · European Journal of Endocrinology · doi:10.1530/eje-10-0444 · Cited by 30 · see citing works

γ-Aminobutyric Acid Type B (GABAB) Receptor Internalization Is Regulated by the R2 Subunit

Hannan, S. B., Wilkins, M. E., Dehghani-Tafti, E., et al. (2011) · Journal of Biological Chemistry · doi:10.1074/jbc.m111.220814 · Cited by 24 · see citing works

Endocytosis and downregulation of G protein-coupled receptors

von Zastrow, M. (2001) · Parkinsonism & Related Disorders · doi:10.1016/s1353-8020(00)00069-9 · Cited by 23 · see citing works

Tracking Cell Surface Mobility of GPCRs Using α-Bungarotoxin-Linked Fluorophores

Hannan, S. B., Wilkins, M. E., Thomas, P., et al. (2013) · Methods in enzymology on CD-ROM/Methods in enzymology · doi:10.1016/b978-0-12-391862-8.00006-5 · Cited by 17 · see citing works

Molecular mechanisms of beta-adrenergic receptor desensitization.

Jm, S., & Lefkowitz, R. J. (1980) · PubMed · Cited by 5 · see citing works

Effect of Gastrin on Fasting and Postprandial Plasma GIP Release in Man

Jorde, R., Schulz, T. B., BURHOL, P. G., et al. (2009) · Digestion · doi:10.1159/000198815 · Cited by 1 · see citing works

Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist

Willard, F. S., Douros, J. D., Gabe, M. B. N., Showalter, A. D., Wainscott, D. B., Suter, T. M., Capozzi, M. E., van der Velden, W. J. C., Stutsman, C., Cardona, G. R., et al. (2020) · JCI Insight · doi:10.1172/jci.insight.140532 · Cited by 541 · see citing works

How May GIP Enhance the Therapeutic Efficacy of GLP-1?

Samms, R. J., Coghlan, M. P., & Sloop, K. W. (2020) · Trends in Endocrinology & Metabolism · doi:10.1016/j.tem.2020.02.006 · Cited by 419 · see citing works

What is the pipeline for future medications for obesity?

Melson, E., Ashraf, U., Papamargaritis, D., & Davies, M. J. (2025) · International Journal of Obesity · doi:10.1038/s41366-024-01473-y · Cited by 332 · see citing works

GIPR agonism mediates weight-independent insulin sensitization by tirzepatide in obese mice

Samms, R. J., Christe, M. E., Collins, K. A. L., Pirro, V., Droz, B. A., Holland, A. K., Friedrich, J. L., Wojnicki, S., Konkol, D. L., Cosgrove, R., et al. (2021) · Journal of Clinical Investigation · doi:10.1172/jci146353 · Cited by 256 · see citing works

Mechanisms of action and therapeutic applications of GLP-1 and dual GIP/GLP-1 receptor agonists

Liu, Q. K. (2024) · Frontiers in Endocrinology · doi:10.3389/fendo.2024.1431292 · Cited by 265 · see citing works

Anti-obesity effects of GIPR antagonists alone and in combination with GLP-1R agonists in preclinical models

Killion, E. A., Wang, J., Yie, J., Shi, S. D.-H., Bates, D., Min, X., Komorowski, R., Hager, T., Deng, L., Atangan, L., et al. (2018) · Science Translational Medicine · doi:10.1126/scitranslmed.aat3392 · Cited by 237 · see citing works

GIP as a Therapeutic Target in Diabetes and Obesity: Insight From Incretin Co-agonists

Holst, J. J., & Rosenkilde, M. M. (2020) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/clinem/dgaa327 · Cited by 207 · see citing works

Reappraisal of GIP Pharmacology for Metabolic Diseases

Finan, B., Müller, T. D., Clemmensen, C., Perez-Tilve, D., DiMarchi, R. D., & Tschöp, M. H. (2016) · Trends in Molecular Medicine · doi:10.1016/j.molmed.2016.03.005 · Cited by 180 · see citing works

Chronic glucose-dependent insulinotropic polypeptide receptor (GIPR) agonism desensitizes adipocyte GIPR activity mimicking functional GIPR antagonism

Killion, E. A., Chen, M., Falsey, J. R., Sivits, G., Hager, T., Atangan, L., Helmering, J., Lee, J., Li, H., Wu, B., et al. (2020) · Nature Communications · doi:10.1038/s41467-020-18751-8 · Cited by 151 · see citing works

Targeting the GIPR for obesity: To agonize or antagonize? Potential mechanisms

Campbell, J. E. (2021) · Molecular Metabolism · doi:10.1016/j.molmet.2020.101139 · Cited by 133 · see citing works

Glucose-dependent insulinotropic polypeptide receptor therapies for the treatment of obesity, do agonists=antagonists?

Killion, E. A., Lu, S.-C., Fort, M., Yamada, Y., Véniant, M. M., & Lloyd, D. J. (2020) · Endocrine Reviews · doi:10.1210/endrev/bnz002 · Cited by 94 · see citing works

Anti-Obesity Medications and Investigational Agents: An Obesity Medicine Association (OMA) Clinical Practice Statement (CPS) 2022

Bays, H. E., Fitch, A., Christensen, S., Burridge, K., & Tondt, J. (2022) · Obesity Pillars · doi:10.1016/j.obpill.2022.100018 · Cited by 68 · see citing works

Loss of Function Glucose-Dependent Insulinotropic Polypeptide Receptor Variants Are Associated With Alterations in BMI, Bone Strength and Cardiovascular Outcomes

Kizilkaya, H. S., Sørensen, K. V., Kibsgaard, C. J., Gasbjerg, L. S., Hauser, A. S., Sparre-Ulrich, A. H., Grarup, N., & Rosenkilde, M. M. (2021) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2021.749607 · Cited by 52 · see citing works

The promise of glucagon-like peptide 1 receptor agonists (GLP-1RA) for the treatment of obesity: a look at phase 2 and 3 pipelines

Madsbad, S., & Holst, J. J. (2025) · Expert Opinion on Investigational Drugs · doi:10.1080/13543784.2025.2472408 · Cited by 43 · see citing works

GIP receptor deletion in mice confers resistance to high-fat diet-induced obesity via alterations in energy expenditure and adipose tissue lipid metabolism

Boer, G. A., Keenan, S. N., Miotto, P. M., Holst, J. J., & Watt, M. J. (2021) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.00646.2020 · Cited by 38 · see citing works

Reagents and models for detecting endogenous GLP1R and GIPR

Ast, J., Broichhagen, J., & Hodson, D. J. (2021) · EBioMedicine · doi:10.1016/j.ebiom.2021.103739 · Cited by 40 · see citing works

Gut hormone GIP induces inflammation and insulin resistance in the hypothalamus

Fu, Y., Kaneko, K., Lin, H.-Y., Mo, Q., Xu, Y., Suganami, T., Ravn, P., & Fukuda, M. (2020) · Endocrinology · doi:10.1210/endocr/bqaa102 · Cited by 38 · see citing works

Naturally occurring mutations in G protein-coupled receptors associated with obesity and type 2 diabetes mellitus

Liu, T., Ji, R.-L., & Tao, Y.-X. (2022) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2021.108044 · Cited by 34 · see citing works

Effects on pancreatic Beta and other Islet cells of the glucose-dependent insulinotropic polypeptide

Khan, R., Tomas, A., & Rutter, G. A. (2020) · Peptides · doi:10.1016/j.peptides.2019.170201 · Cited by 24 · see citing works

Treatment of Type 2 Diabetes and Obesity on the Basis of the Incretin System: The 2021 Banting Medal for Scientific Achievement Award Lecture

Holst, J. J. (2021) · Diabetes · doi:10.2337/dbi21-0026 · Cited by 23 · see citing works

GLP-1 and GIP : hormones of the entero-insular axis.

Elliott, R. M. (1992) · Surrey Research Insight Open Access (The University of Surrey)

Gastric Inhibitory Polypeptide Analogues

Holst, J. J. (2002) · BioDrugs · doi:10.2165/00063030-200216030-00002 · Cited by 22 · see citing works

Secretion of the Incretin Hormones Glucagon-Like Peptide-1 and Gastric Inhibitory Polypeptide Correlates with Insulin Secretion in Normal Man Throughout the Day

Ørskov, C., Wettergren, A., & Holst, J. J. (1996) · Scandinavian Journal of Gastroenterology · doi:10.3109/00365529609009147 · Cited by 271 · see citing works

[Gastric inhibitory polypeptide (GIP), incretin and gastrointestinal diseases].

Levy, N., & Stermer, E. (1984) · PubMed

On the role of the incretin hormones GIP and GLP-1 in the pathogenesis of Type 2 diabetes mellitus.

Vilsbøll, T. (2004) · PubMed · Cited by 36 · see citing works