The transformative breakthroughs in GLP-1 research recognized by the 2024 Lasker~DeBakey award

References

[1] Butler J, Shah SJ, Petrie MC, Borlaug BA, Abildstrom SZ, Davies MJ, Hovingh GK, Kitzman DW, Moller DV, Verma S, et al.. Semaglutide versus placebo in people with obesity-related heart failure with preserved ejection fraction: a pooled analysis of the STEP-HFpEF and STEP-HFpEF DM randomised trials. Lancet, 2024, 403: 1635-1648

[2] Drucker DJ, Mojsov S, Habener JF. Cell-specific post-translational processing of preproglucagon expressed from a metallothionein-glucagon fusion gene. J Biol Chem, 1986, 261: 9637-9643

[3] Friedrichsen M, Breitschaft A, Tadayon S, Wizert A, Skovgaard D. The effect of semaglutide 2.4 mg once weekly on energy intake, appetite, control of eating, and gastric emptying in adults with obesity. Diabetes Obes Metab, 2021, 23: 754-762

[4] Holz Iv GG, Kiihtreiber WM, Habener JF. Pancreatic beta-cells are rendered glucose-competent by the insulinotropic hormone glucagon-like peptide-1(7–37). Nature, 1993, 361: 362-365

[5] Jastreboff AM, Aronne LJ, Ahmad NN, Wharton S, Connery L, Alves B, Kiyosue A, Zhang S, Liu B, Bunck MC, et al.. Tirzepatide once weekly for the treatment of obesity. N Engl J Med, 2022, 387: 205-216

[6] Knudsen LB, Nielsen PF, Huusfeldt PO, Johansen NL, Madsen K, Pedersen FZ, Thøgersen H, Wilken M, Agersø H. Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration. J Med Chem, 2000, 43: 1664-1669

[7] Knudsen LB, Calatayud D, Bardram L, Hvelplund A, Kaastrup P, Reedtz-Runge S, Ørskov C, Kirk RK, Heller RS, Pyke C. GLP-1 receptor localization in monkey and human tissue: novel distribution revealed with extensively validated monoclonal antibody. Endocrinology, 2014, 155: 1280-1290

[8] Marso SP, Daniels GH, Brown-Frandsen K, Kristensen P, Mann JFE, Nauck MA, Nissen SE, Pocock S, Poulter NR, Ravn LS, et al.. Liraglutide and cardiovascular outcomes in type 2 diabetes. N Engl J Med, 2016, 375: 311-322

[9] Mojsov S, Heinrich G, Wilson IB, Ravazzola M, Orci L, Habener JF. Preproglucagon gene expression in pancreas and intestine diversifies at the level of post-translational processing. J Biol Chem, 1986, 261: 11880-11889

[10] Mojsov S, Weir GC, Habener JF. Insulinotropin: glucagon-like peptide I (7–37) co-encoded in the glucagon gene is a potent stimulator of insulin release in the perfused rat pancreas. J Clin Invest, 1987, 79: 616-619

[11] Perkovic V, Tuttle KR, Rossing P, Mahaffey KW, Mann JFE, Bakris G, Baeres FMM, Idorn T, Bosch-Traberg H, Lausvig NL, et al.. Effects of semaglutide on chronic kidney disease in patients with type 2 diabetes. N Engl J Med, 2024, 391: 109-121

[12] Philippe J, Mojsov S, Drucker DJ, Habener JF. Proglucagon processing in a rat islet cell line resembles phenotype of intestine rather than pancreas. Endocrinology, 1986, 119: 2833-2839

[13] Pi-Sunyer X, Astrup A, Fujioka K, Greenway F, Halpern A, Krempf M, Lau DCW, le Roux CW, Violante Ortiz R, Jensen CB, et al.. A randomized, controlled trial of 3.0 mg of liraglutide in weight management. N Engl J Med, 2015, 373: 11-22

[14] Rakipovski G, Rolin B, Nøhr J, Klewe I, Frederiksen KS, Augustin R, Hecksher-Sørensen J, Ingvorsen C, Polex-Wolf J, Knudsen LB. The GLP-1 analogs liraglutide and semaglutide reduce atherosclerosis in ApoE(-/-) and LDLr(-/-) mice by a mechanism that includes inflammatory pathways. JACC Basic Transl Sci, 2018, 3: 844-857

[15] Rosenstock J, Frias J, Jastreboff AM, Du Y, Lou J, Gurbuz S, Thomas MK, Hartman ML, Haupt A, Milicevic Z, et al.. Retatrutide, a GIP, GLP-1 and glucagon receptor agonist, for people with type 2 diabetes: a randomised, double-blind, placebo and active-controlled, parallel-group, phase 2 trial conducted in the USA. Lancet, 2023, 402: 529-544

[16] Secher A, Jelsing J, Baquero AF, Hecksher-Sorensen J, Cowley MA, Dalboge LS, Hansen G, Grove KL, Pyke C, Raun K, et al.. The arcuate nucleus mediates GLP-1 receptor agonist liraglutide-dependent weight loss. J Clin Invest, 2014, 124: 4473-4488

[17] Turton MD, O'Shea D, Gunn I, Beak SA, Edwards CM, Meeran K, Choi SJ, Taylor GM, Heath MM, Lambert PD, et al.. A role for glucagon-like peptide-1 in the central regulation of feeding. Nature, 1996, 379: 69-72

[18] Wharton S, Blevins T, Connery L, Rosenstock J, Raha S, Liu R, Ma X, Mather KJ, Haupt A, Robins D, et al.. Daily oral GLP-1 receptor agonist orforglipron for adults with obesity. N Engl J Med, 2023, 389: 877-888

[19] Wilding JPH, Batterham RL, Calanna S, Davies M, Van Gaal LF, Lingvay I, McGowan BM, Rosenstock J, Tran MTD, Wadden TA, et al.. Once-weekly semaglutide in adults with overweight or obesity. N Engl J Med, 2021, 384: 989-1002

Funding

National Natural Science Foundation of China(81930019, 82341076)

RIGHTS & PERMISSIONS

The Author(s)