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Journal articles on the topic 'GLP-1 analogues'

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Published: 4 June 2021

Last updated: 31 January 2023

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Macaulay, D. "Are GLP-1 analogues affordable?" BMJ 342, mar08 3 (2011): d1482. http://dx.doi.org/10.1136/bmj.d1482.

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Korbut, Anton Ivanovich, and Vadim Valerievich Klimontov. "Incretin-based therapy: renal effects." Diabetes mellitus 19, no. 1 (2016): 53–63. http://dx.doi.org/10.14341/dm7727.

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Glucagon like peptide-1 (GLP-1) analogues and dipeptidyl peptidase-4 (DPP-4) inhibitors are new classes of hypoglycemic agents with numerous pleiotropic effects. The review summarises data about the influence of GLP-1 analogues and DPP-4 inhibitors on structural and functional changes in diabetic kidneys. Growing evidence indicates that the kidney is one of the loci of the effects and degradation of GLP-1. The potency of the effects of GLP-1 in diabetic kidneys can be reduced by decrease in GLP-1 receptor expression or enhancement of GLP-1 degradation. In experimental models of diabetic nephropathy and non-diabetic renal injury, GLP-1 analogues and DPP-4 inhibitors slow the development of kidney fibrosis and prevent the decline of kidney function. The mechanisms of protective effect include hyperglycaemia reduction, enhancement of sodium excretion, suppression of inflammatory and fibrogenic signalling pathways, reduction of oxidative stress and apoptosis in the kidneys. In clinical studies, the urinary albumin excretion reduction rate while using the GLP-1 analogue and DPP-4 inhibitor treatment was demonstrated in patients with type 2 diabetes. Long-term impact of these agents on renal function in diabetes needs further investigations.

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Dharmaraj, B. "A brief review on newer Glucagon like Peptide-1 analogues." International Journal of Preclinical and Clinical Research 1, no. 1 (2020): 26–34. http://dx.doi.org/10.51131/ijpccr/v1i1.7.

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GLP-1 (Glucagon like Peptide-1) receptor agonists have been shown to be effective in the treatment of type 2 diabetes mellitus (T2DM). Although the first GLP-1 receptor agonist, Exenatide, was approved in the year 2000, other agents with a longer duration of action that do not require twice-daily dosing are now being developed. Indeed, Liraglutide, a once-daily GLP-1 receptor agonist, was approved in 2010, a once-weekly extended-release formulation of Exenatide (Exenatide ER) was approved in 2011 and now more recently Semaglutide, an oral GLP 1 receptor agonist was approved for medical use in the United States in September 2019 and in the European Union in April 2020. The importance of GLP-1 itself and the use of GLP-1 receptor agonists in T2DM are discussed. An overview of the clinical development of the GLP-1 receptor agonists (Exenatide ER, Liraglutide, Lixisenatide, Albiglutide, Taspoglutide and Semaglutide) is provided and their mechanism of action, efficacy in terms of glycaemic control, weight loss and tolerability are reviewed. Keywords: GLP1 receptor agonist; Liraglutide; Exenatide ER; Lixisenatide; Semaglutide

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Green, BD, VA Gault, MH Mooney, et al. "Novel dipeptidyl peptidase IV resistant analogues of glucagon-like peptide-1(7-36)amide have preserved biological activities in vitro conferring improved glucose-lowering action in vivo." Journal of Molecular Endocrinology 31, no. 3 (2003): 529–40. http://dx.doi.org/10.1677/jme.0.0310529.

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Although the incretin hormone glucagon-like peptide-1 (GLP-1) is a potent stimulator of insulin release, its rapid degradation in vivo by the enzyme dipeptidyl peptidase IV (DPP IV) greatly limits its potential for treatment of type 2 diabetes. Here, we report two novel Ala(8)-substituted analogues of GLP-1, (Abu(8))GLP-1 and (Val(8))GLP-1 which were completely resistant to inactivation by DPP IV or human plasma. (Abu(8))GLP-1 and (Val(8))GLP-1 exhibited moderate affinities (IC(50): 4.76 and 81.1 nM, respectively) for the human GLP-1 receptor compared with native GLP-1 (IC(50): 0.37 nM). (Abu(8))GLP-1 and (Val(8))GLP-1 dose-dependently stimulated cAMP in insulin-secreting BRIN BD11 cells with reduced potency compared with native GLP-1 (1.5- and 3.5-fold, respectively). Consistent with other mechanisms of action, the analogues showed similar, or in the case of (Val(8))GLP-1 slightly impaired insulin releasing activity in BRIN BD11 cells. Using adult obese (ob/ob) mice, (Abu(8))GLP-1 had similar glucose-lowering potency to native GLP-1 whereas the action of (Val(8))GLP-1 was enhanced by 37%. The in vivo insulin-releasing activities were similar. These data indicate that substitution of Ala(8) in GLP-1 with Abu or Val confers resistance to DPP IV inactivation and that (Val(8))GLP-1 is a particularly potent N-terminally modified GLP-1 analogue of possible use in type 2 diabetes.

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Green, BD, MH Mooney, VA Gault, et al. "N-terminal His(7)-modification of glucagon-like peptide-1(7-36) amide generates dipeptidyl peptidase IV-stable analogues with potent antihyperglycaemic activity." Journal of Endocrinology 180, no. 3 (2004): 379–88. http://dx.doi.org/10.1677/joe.0.1800379.

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Glucagon-like peptide-1(7-36)amide (GLP-1) possesses several unique and beneficial effects for the potential treatment of type 2 diabetes. However, the rapid inactivation of GLP-1 by dipeptidyl peptidase IV (DPP IV) results in a short half-life in vivo (less than 2 min) hindering therapeutic development. In the present study, a novel His(7)-modified analogue of GLP-1, N-pyroglutamyl-GLP-1, as well as N-acetyl-GLP-1 were synthesised and tested for DPP IV stability and biological activity. Incubation of GLP-1 with either DPP IV or human plasma resulted in rapid degradation of native GLP-1 to GLP-1(9-36)amide, while N-acetyl-GLP-1 and N-pyroglutamyl-GLP-1 were completely resistant to degradation. N-acetyl-GLP-1 and N-pyroglutamyl-GLP-1 bound to the GLP-1 receptor but had reduced affinities (IC(50) values 32.9 and 6.7 nM, respectively) compared with native GLP-1 (IC(50) 0.37 nM). Similarly, both analogues stimulated cAMP production with EC(50) values of 16.3 and 27 nM respectively compared with GLP-1 (EC(50) 4.7 nM). However, N-acetyl-GLP-1 and N-pyroglutamyl-GLP-1 exhibited potent insulinotropic activity in vitro at 5.6 mM glucose (P<0.05 to P<0.001) similar to native GLP-1. Both analogues (25 nM/kg body weight) lowered plasma glucose and increased plasma insulin levels when administered in conjunction with glucose (18 nM/kg body weight) to adult obese diabetic (ob/ob) mice. N-pyroglutamyl-GLP-1 was substantially better at lowering plasma glucose compared with the native peptide, while N-acetyl-GLP-1 was significantly more potent at stimulating insulin secretion. These studies indicate that N-terminal modification of GLP-1 results in DPP IV-resistant and biologically potent forms of GLP-1. The particularly powerful antihyperglycaemic action of N-pyroglutamyl-GLP-1 shows potential for the treatment of type 2 diabetes.

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Liu, Hongbin, Anthony E. Dear, Lotte B. Knudsen, and Richard W. Simpson. "A long-acting glucagon-like peptide-1 analogue attenuates induction of plasminogen activator inhibitor type-1 and vascular adhesion molecules." Journal of Endocrinology 201, no. 1 (2009): 59–66. http://dx.doi.org/10.1677/joe-08-0468.

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Glucagon-like peptide-1 (GLP-1) administration attenuates endothelial cell dysfunction in diabetic patients and inhibits tumour necrosis factor α (TNF)-mediated plasminogen activator inhibitor type-1 (PAI-1) induction in human vascular endothelial cells. The short half-life of GLP-1 mediated via degradation by the enzyme dipeptidyl peptidase 4 mandates the clinical use of long-acting GLP-1 analogues. The effects of a long-acting GLP-1 analogue on PAI-1 and vascular adhesion molecule expression in vascular endothelial cells are unknown. In this report, we demonstrate for the first time that the treatment with liraglutide, a long-acting GLP-1 analogue, inhibited TNF or hyperglycaemia-mediated induction of PAI-1, intercellular adhesion molecule-1 and vascular cell adhesion molecule-1 mRNA and protein expression in a human vascular endothelial cell line. In addition, treatment attenuated TNF- or hyperglycaemia-mediated induction of the orphan nuclear receptor Nur77 mRNA expression. Taken together, these observations indicate that liraglutide inhibits TNF- or glucose-mediated induction of PAI-1 and vascular adhesion molecule expression, and this effect may involve the modulation of NUR77. These effects suggest that liraglutide may potentially improve the endothelial cell dysfunction associated with premature atherosclerosis identified in type 2 diabetic patients.

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Carydias, Elisabeth, Andoneta Tasho, Chara Kani, Flora Bacopoulou, Charikleia Stefanaki, and Sophia L. Markantonis. "Systematic Review and Meta-Analysis of the Efficacy and Safety of Metformin and GLP-1 Analogues in Children and Adolescents with Diabetes Mellitus Type 2." Children 9, no. 10 (2022): 1572. http://dx.doi.org/10.3390/children9101572.

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Diabetes mellitus type 2 (DMT2) is one of the most frequent glucose metabolism disorders, in which serum glucose concentrations are increased. In most cases, changes in lifestyle and diet are considered as the first step in addressing its therapy. If changes in lifestyle and diet fail, drugs, such as metformin, must be added. Lately, apart from metformin or insulin, the FDA has approved the use of glucagon-like peptide-1 (GLP-1) analogues for children and adolescents. Little is known about their efficacy and safety at this young age. The main aim of this systematic review/meta-analysis was to assess the safety and efficacy of metformin and GLP-1 analogues, exenatide and liraglutide, compared with placebos or other antidiabetic drugs used for DMT2 in children and adolescents. Metformin did not seem to demonstrate pharmacologic superiority, while GLP-1 analogues were found superior to placebos. GLP-1 analogues may be considered a useful alternative for the treatment of DMT2 in children and adolescents.

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Yudkin, J. S., R. Lehman, and H. M. Krumholz. "Use of GLP-1 analogues needs great caution." BMJ 342, mar08 3 (2011): d1478. http://dx.doi.org/10.1136/bmj.d1478.

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Brom, Maarten, Lieke Joosten, Wim J. G. Oyen, Martin Gotthardt, and Otto C. Boerman. "Radiolabelled GLP-1 analogues forin vivotargeting of insulinomas." Contrast Media & Molecular Imaging 7, no. 2 (2012): 160–66. http://dx.doi.org/10.1002/cmmi.475.

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Su, Yunfang, Zijuan Zhang, Hao Li, et al. "A GLP-2 Analogue Protects SH-SY5Y and Neuro-2a Cells Against Mitochondrial Damage, Autophagy Impairments and Apoptosis in a Parkinson Model." Drug Research 71, no. 01 (2020): 43–50. http://dx.doi.org/10.1055/a-1266-3263.

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AbstractGlucagon-like peptide-2 (GLP-2) is a peptide hormone that belongs to the glucagon-derived peptide family. We have previously shown that analogues of the sister hormone Glucagon-like peptide-1 (GLP-1) showed neuroprotective effects. Here we investigated the effect of a GLP-2 agonist in a cell model of Parkinsonʼs disease (PD) created by treating SH-SY5Y or Neuro-2a cells with 1-Methyl-4-phenyl-pyridine ion (MPP+). Cell viability and cell cytotoxicity was detected by MTT and LDH assays, respectively. The protein expression levels of mitochondrial, autophagy and apoptotic biomarkers including PGC-1α, Mfn2, IRE1, ATG7, LC3B, Beclin1 and Bcl-2 were detected by western blot. Mitochondrial superoxide was detected by MitoSOX Red. In addition, mitochondrial morphology, autophagosome and apoptotic corpuscles were observed by transmission electron microscope (TEM). We found that the GLP-1 and the GLP-2 agonists both protect cells against mitochondrial damage, autophagy impairments and apoptosis induced by MPP+both in SH-SY5Y and Neuro-2a cells. Cell signaling for mitogenesis was enhanced, and oxidative stress levels much reduced by the drugs. This demonstrates for the first time the neuroprotective effects of a GLP-2 analogue in PD cellular models, in which oxidative stress, autophagy and apoptosis play crucial roles. The protective effects were comparable to those seen with the GLP-1 analogue liraglutide. The results suggest that not only GLP-1, but also GLP-2 has neuroprotective properties and may be useful as a novel treatment of PD.

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Chun, Hyun-Ji, and Hyuk-Sang Kwon. "Clinical Efficacy of Glucagon Like Peptide-1 (GLP-1) Analogues." Journal of Korean Diabetes 14, no. 3 (2013): 125. http://dx.doi.org/10.4093/jkd.2013.14.3.125.

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Juul Holst, Jens. "Glucagon-like Peptide-1, A Gastrointestinal Hormone with a Pharmaceutical Potential." Current Medicinal Chemistry 6, no. 11 (1999): 1005–17. http://dx.doi.org/10.2174/092986730611220401163238.

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Glucagon-like peptide-1 (GLP-1) is an insulinotropic hormone secreted from endocrine cells in the gut mucosa in response to meal ingestion. It is an important incretin hormone; mice with a null mutation in the GLP-1 receptor gene develop glucose intolerance. In addition, it inhibits gastrointestinal secretion and motility and is thought to be part of the "ileal brake" mechanism. Perhaps because of the latter actions it inhibits food intake, but intracerebral injection of GLP-1 also inhibits food intake. The insu linotropic effect is preserved in patients with type 2 diabetes mellitus, in whom also glucagon secretion is inhibited. Thus upon iv GLP-1 infusion blood glucose may be completely normalised. Because its actions are glucose-dependent hypoglycaemia does not develop. However, GLP-1 is metabolised extremely rapidly in vivo, initially by a mechanism that involves the enzyme dipeptidyl peptidase-IV. It is currently being investigated how GLP-1 or analogues thereof can be employed in practical diabetes therapy. Promising solutions include the development of stable analogues and inhibitors of the degrading enzyme.

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Holst, Jens Juul. "Pharmacology of GLP-1-based therapies." British Journal of Diabetes & Vascular Disease 8, no. 2_suppl (2008): S10—S18. http://dx.doi.org/10.1177/1474651408100523.

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Glucagon-like peptide-1 GLP-1 is a naturally occurring 30-amino acid peptide synthesised in intestinal endocrine L cells. GLP-1 mediates glucose homeostasis through stimulation of glucose-dependent insulin secretion, biosynthesis of insulin and inhibition of glucagon secretion. These effects have potential clinical value in type 2 diabetes. However, because native GLP-1 is rapidly degraded to its inactive form by dipeptidyl peptidase-4 (DPP-4), it has a short half-life in vivo . Strategies to overcome this therapeutic limitation include developing GLP-1 mimetics and analogues with longer half-lives and to inhibit DPP-4. Exenatide (exendin-4) is a 39-amino acid peptide originally derived from the venom of the Gila monster lizard, and shares a 53% sequence identity with human GLP-1. Exenatide has a longer circulating half-life, reflecting relative resistance to DPP-4 degradation, and is administered twice daily. Liraglutide is a once-daily human GLP-1 analogue with high (97%) sequence identity. The specific structural modifications that characterise liraglutide result in increased self-association (allowing slow absorption from the subcutaneous depot), promote albumin binding and reduce susceptibility to DPP-4, giving liraglutide a half-life of 13 hours after once-daily administration. Preliminary studies of exenatide and liraglutide show clinically relevant reductions in glycosylated haemoglobin A1c (HbA1c) compared with placebo, without hypoglycaemia and with weight loss of up to 3 kg. DPP-4 inhibitors, such as vildagliptin (not available in the USA) and sitagliptin can help stabilise postprandial GLP-1 levels and thus produce desirable effects on insulin and glucagon production. The potential for weight reduction with DPP-4 inhibitors appears limited, perhaps reflecting the limited increase in GLP-1 levels achieved with these agents.Br J Diabetes Vasc Dis, 2008;8 (Suppl 2) : S10—S18

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Subaran, Sharmila C., Matthew A. Sauder, Weidong Chai, et al. "GLP-1 at physiological concentrations recruits skeletal and cardiac muscle microvasculature in healthy humans." Clinical Science 127, no. 3 (2014): 163–70. http://dx.doi.org/10.1042/cs20130708.

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GLP-1 increases microvascular perfusion in both skeletal and cardiac muscle, and brachial artery diameter and blood flow in humans. These vascular actions may contribute to the beneficial actions of the GLP-1 receptor analogues.

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Chi, Yushi, Huibin Zhang, Jinpei Zhou, Wenlong Huang, and Shuaijian Ni. "Microwave-Assisted Solid Phase Synthesis of GLP-1-Analogues." Letters in Organic Chemistry 5, no. 5 (2008): 399–402. http://dx.doi.org/10.2174/157017808784872061.

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Schmid, Thomas. "Analogues du GLP-1 : un traitement oral bientôt disponible ?" Revue Médicale Suisse 15, no. 666 (2019): 1840. http://dx.doi.org/10.53738/revmed.2019.15.666.1840.

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Nauck, Michael A., and Juris J. Meier. "GLP-1 analogues and insulin: sound the wedding bells?" Nature Reviews Endocrinology 7, no. 4 (2011): 193–95. http://dx.doi.org/10.1038/nrendo.2011.30.

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Holmes, David. "Concerns about long-term use of GLP-1 analogues." Nature Reviews Endocrinology 12, no. 4 (2016): 186. http://dx.doi.org/10.1038/nrendo.2016.33.

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Kluger, Aaron Y., and Peter A. McCullough. "Semaglutide and GLP-1 analogues as weight-loss agents." Lancet 392, no. 10148 (2018): 615–16. http://dx.doi.org/10.1016/s0140-6736(18)31826-9.

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Stephens, Jeffrey W., and Stephen C. Bain. "Safety and adverse effects associated with GLP-1 analogues." Expert Opinion on Drug Safety 6, no. 4 (2007): 417–22. http://dx.doi.org/10.1517/14740338.6.4.417.

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Metelska, Aleksandra, Jakub Metelski, Dominika Sereda, and Hubert Nieścior. "GLP-1 analogs in the treatment of obesity." Journal of Education, Health and Sport 12, no. 8 (2022): 334–42. http://dx.doi.org/10.12775/jehs.2022.12.08.034.

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Introduction and purpose Obesity is a chronic disease that causes the development of numerous complications such as cardiovascular disease, cancer and type 2 diabetes. The 2017 global nutrition report showed that 2 billion adults and 41 million children worldwide are overweight or obese. Due to the growing problem of obesity, pharmacotherapy is recommended in patients with BMI ≥30 kg / m2 or BMI> 27 kg / m2 with accompanying risk factors. The aim of the study is to discuss the role of GLP-1 analogues in the treatment of obesity. Description of the state of knowledge  GLP-1 receptor agonists that were initially related to the treatment of type 2 diabetes are now being used successfully in the treatment of obesity. The GLP-1 hormone is released from intestinal enteroendocrine cells in response to an increase in glucose levels. Due to the wide neuroanatomical distribution of GLP-1R within the structures of the reward system, it is possible to suppress the need for food intake, which translates into a reduction in the amount of food consumed and a decrease in body weight. The most common side effects associated with the use of GLP-1 analogues include gastrointestinal symptoms such as nausea, vomiting, diarrhea and constipation, which rarely lead to discontinuation of treatment. Summary Numerous studies have shown that chronic systemic delivery of GLP-1 agonists led to weight loss and helped to maintain a lower body weight. Reduction in food intake is reported as the main mechanism. Discontinuation of the drug was associated with weight gain.

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GÓRSKA, ALEKSANDRA, and MARCIN B. ARCISZEWSKI. "Distribution and function of glucagon-like peptide 1 (GLP-1) in the digestive tract of mammals and the clinical use of its analogues." Medycyna Weterynaryjna 76, no. 07 (2023): 6374–2023. http://dx.doi.org/10.21521/mw.6374.

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Recently, interest in glucagon-like peptide-1 (GLP-1) and other peptides derived from preproglucagon has increased significantly. GLP-1 is a 30-amino acid peptide hormone produced in L-type enteroendocrine cells as a response to food intake. GLP-1 is rapidly metabolized and inactivated by the dipeptidyl peptidase IV enzyme before the hormone leaves the intestine, which increases the likelihood that GLP-1 action is transmitted through sensory neurons in the intestine and liver through the GLP-1 receptor. The main actions of GLP-1 are to stimulate insulin secretion (i.e. act as incretin hormone) and inhibit glucagon secretion, thus contributing to the reduction of postprandial glucose spikes. GLP-1 also inhibits motility and gastrointestinal secretion, and therefore acts as part of the „small bowel brake” mechanism. GLP-1 also appears to be a physiological regulator of appetite and food intake. Because of these effects, GLP-1 or GLP-1 receptor agonists are now increasingly used to treat type 2 diabetes. Reduced GLP-1 secretion may contribute to the development of obesity, and excessive secretion may be responsible for postprandial reactive hypoglycemia. The use of GLP-1 agonists opens up new possibilities for the treatment of type 2 diabetes and other metabolic diseases. In the last two decades, many interesting studies covering both the physiological and pathophysiological role of GLP-1 have been published, and our understanding of GLP-1 has broadened significantly. In this review article, we have tried to describe our current understanding of how GLP-1 works as both a peripheral hormone and as a central neurotransmitter in health and disease. We focused on its biological effects on the body and the potential clinical application in relation to current research.

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Azad, Babak Behnam, Vanessa Rota, Lihai Yu, et al. "Synthesis and Evaluation of Optical and PET GLP-1 Peptide Analogues for GLP-1R Imaging." Molecular Imaging 14, no. 1 (2015): 1–16. http://dx.doi.org/10.2310/7290.2014.00057.

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Gariani, Karim. "Analogues du GLP-1 en 2019 : pour qui et comment ?" Revue Médicale Suisse 15, no. 653 (2019): 1117–23. http://dx.doi.org/10.53738/revmed.2019.15.653.1117.

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Sauvanet, J. P. "Les analogues du GLP- 1, au-delà du contrôle glycémique…" Médecine des Maladies Métaboliques 4, no. 3 (2010): 342. http://dx.doi.org/10.1016/s1957-2557(10)70073-0.

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Siegel, Erhard G., Baptist Gallwitz, Gritie Scharf, et al. "Biological activity of GLP-1-analogues with N-terminal modifications." Regulatory Peptides 79, no. 2-3 (1999): 93–102. http://dx.doi.org/10.1016/s0167-0115(98)00155-4.

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Banham, Stephen. "The incretin effect, GLP-1 analogues and DPP-4 inhibitors." Prescriber 22, no. 19 (2011): 73–74. http://dx.doi.org/10.1002/psb.817.

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Yellon, DerekM, MarynaV Basalay, and SeanM Davidson. "Can glucagon-like peptide-1 (GLP-1) analogues make neuroprotection a reality?" Neural Regeneration Research 15, no. 10 (2020): 1852. http://dx.doi.org/10.4103/1673-5374.280313.

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Basalay, Maryna V., Sean M. Davidson, and Derek M. Yellon. "Neuroprotection in Rats Following Ischaemia-Reperfusion Injury by GLP-1 Analogues—Liraglutide and Semaglutide." Cardiovascular Drugs and Therapy 33, no. 6 (2019): 661–67. http://dx.doi.org/10.1007/s10557-019-06915-8.

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Abstract Purpose A substantial number of ischaemic stroke patients who receive reperfusion therapy in the acute phase do not ever fully recover. This reveals the urgent need to develop new adjunctive neuroprotective treatment strategies alongside reperfusion therapy. Previous experimental studies demonstrated the potential of glucagon-like peptide-1 (GLP-1) to reduce acute ischaemic damage in the brain. Here, we examined the neuroprotective effects of two GLP-1 analogues, liraglutide and semaglutide. Methods A non-diabetic rat model of acute ischaemic stroke involved 90, 120 or 180 min of middle cerebral artery occlusion (MCAO). Liraglutide or semaglutide was administered either i.v. at the onset of reperfusion or s.c. 5 min before the onset of reperfusion. Infarct size and functional status were evaluated after 24 h or 72 h of reperfusion. Results Liraglutide, administered as a bolus at the onset of reperfusion, reduced infarct size by up to 90% and improved neuroscore at 24 h in a dose-dependent manner, following 90-min, but not 120-min or 180-min ischaemia. Semaglutide and liraglutide administered s.c. reduced infarct size by 63% and 48%, respectively, and improved neuroscore at 72 h following 90-min MCAO. Neuroprotection by semaglutide was abolished by GLP1-R antagonist exendin(9-39). Conclusion Infarct-limiting and functional neuroprotective effects of liraglutide are dose-dependent. Neuroprotection by semaglutide is at least as strong as by liraglutide and is mediated by GLP-1Rs.

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Gallwitz, Baptist. "Managing the β-cell with GLP-1 in type 2 diabetes". British Journal of Diabetes & Vascular Disease 8, № 2_suppl (2008): S19—S25. http://dx.doi.org/10.1177/1474651408100522.

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The clinical course of type 2 diabetes mellitus is characterised by a progressive decline in β -cell mass. The changing β-cell mass reflects a shifting balance between β-cell neogenesis, islet neogenesis and β-cell apoptosis. In persons with diabetes, administration of exogenous glucagon-like peptide-1 (GLP-1) improves glucose sensitivity and insulin synthesis and may help increase β cell mass. As the effects of GLP-1 on the β cell are becoming better understood at both the molecular and cellular levels, it has become possible to develop therapies with the potential to harness and sustain the positive effects of endogenous GLP-1 in patients with type 2 diabetes. Data from in vitro, preclinical and phase II studies show promising results with GLP-1 analogues in improving β-cell function in patients with type 2 diabetes. For example, in vitro models have shown the GLP-1 analogue liraglutide inhibits β-cell apoptosis in isolated neonatal rat islets. In vitro, animal models demonstrate increasing β-cell mass with liraglutide administration. Results from a recently completed phase II clinical trial with liraglutide in patients with type 2 diabetes demonstrate that daily treatment markedly improves β -cell function as shown by an increased first-phase insulin response and secretory capacity and a decreased proinsulin:insulin ratio. Now, phase III trials continue to bear out the potential for liraglutide for treatment of patients with type 2 diabetes.Br J Diabetes Vasc Dis 2008;8 (Suppl 2): S19-S25

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Zoicas, Flavius, Michael Droste, Bernhard Mayr, Michael Buchfelder, and Christof Schöfl. "GLP-1 analogues as a new treatment option for hypothalamic obesity in adults: report of nine cases." European Journal of Endocrinology 168, no. 5 (2013): 699–706. http://dx.doi.org/10.1530/eje-12-0997.

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BackgroundPatients with hypothalamic pathology often develop morbid obesity, causing severe metabolic alterations resulting in increased morbidity and mortality. Glucagon-like peptide-1 (GLP-1) analogues improve glycaemic control in type 2 diabetic patients and cause weight loss in obese patients by yet unknown mechanisms. Here we tested whether GLP-1 analogues were also effective in the treatment of obesity and associated metabolic alterations in patients with hypothalamic disease.MethodsNine patients (eight with type 2 diabetes mellitus) with moderate to severe hypothalamic obesity were treated with GLP-1 analogues for up to 51 months. Body weight, homeostasis model assessment - insulin resistance (HOMA-IR), HbA1c and lipids were assessed.ResultsEight patients experienced substantial weight loss (−13.1±5.1 kg (range −9 to −22)). Insulin resistance (HOMA-IR −3.2±3.5 (range −9.1 to 0.8)) and HbA1c values (−1.3±1.4% (range −4.5 to 0.0)) improved under treatment (24.3±18.9 months (range 6 to 51)). Five patients reported increased satiation in response to the treatment. Two of the eight patients complained about nausea and vomiting and one of them abandoned therapy because of sustained gastrointestinal discomfort after 6 months. One patient suffered from intolerable nausea and vomiting and discontinued treatment within 2 weeks.ConclusionGLP-1 analogues can cause substantial and sustained weight loss in obese patients with hypothalamic disease. This offers a new approach for medical treatment of moderate to severe hypothalamic obesity and associated metabolic alterations.

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Sawamura, Toshitaka, Shigehiro Karashima, Ai Ohmori, et al. "Remitting Seronegative Symmetrical Synovitis with Pitting Edema Syndrome Worsen after the Administration of Dulaglutide." Medicina 58, no. 2 (2022): 289. http://dx.doi.org/10.3390/medicina58020289.

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Remitting seronegative symmetrical synovitis with pitting edema (RS3PE) syndrome is characterized by symmetrical polyarthritis and limb pitting edema. Although the detailed mechanisms of this syndrome have not been clearly understood, some agents including dipeptidyl peptidase-4 inhibitors have been reported to induce RS3PE syndrome. However, glucagon-like peptide-1 (GLP-1) analogues have not been reported to be associated with this syndrome. A 91-year-old woman was admitted to our hospital with complaints of severe polyarthritis and limb edema. She was diagnosed with RS3PE syndrome. Oral prednisolone improved her symptoms. However, her symptoms worsened after the administration of dulaglutide, with elevated serum inflammatory markers. Discontinuation of dulaglutide without additional treatment improved her symptoms and laboratory findings. This case might indicate the possibility of development and worsening of RS3PE syndrome caused after GLP-1 analogue.

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Nauck, Michael A. "Liraglutide, a once-daily human GLP-1 analogue." British Journal of Diabetes & Vascular Disease 8, no. 2_suppl (2008): S26—S33. http://dx.doi.org/10.1177/1474651408100524.

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Glucagon-like peptide-1 (GLP-1) is an incretin hormone physiologically playing a role in glucose homeostasis, together with the partner incretin, glucose dependent insulinotropic peptide (GIP). Active concentrations of this hormone are not maintained for long because of its very rapid degradation and elimination. The effects of the hormone are of potential therapeutic value in type 2 diabetes; therefore, analogues of GLP-1 have been developed that are characterised by a prolonged circulating half-life relative to the naturally occurring hormone. One such long-acting analogue is liraglutide. The effects of liraglutide are maintained over 24 h, allowing once-daily dosing. Liraglutide provides all of the beneficial actions of endogenous GLP-1: glucose-dependent stimulation of insulin secretion, glucagon suppression, deceleration of gastric emptying, appetite suppression/weight loss and, in animal models, inhibition of β-cell apoptosis and promotion of β-cell regeneration. Because liraglutide stimulates insulin secretion and suppresses glucagon secretion only when blood glucose levels are elevated, the risk of treatment-associated hypoglycaemia is low. In clinical studies, liraglutide substantially lowered fasting and postprandial glucose concentrations, with an overall reduction in haemoglobin A1c of up to 1-2%. In some studies, liraglutide has decreased several biomarkers of cardiovascular risk and lowered triglyceride levels significantly. Side effects most commonly are gastrointestinal symptoms; they are usually mild to moderate and resolve over time. Long-term clinical trials are needed to assess whether the effects of liraglutide on the β cell translate into a durable improvement in β-cell function and mass in patients with type 2 diabetes and, if so, whether this will slow or halt disease progression and help prevent complications.Br J Diabetes Vasc Dis, 2008; 8 (Suppl 2): S26—S33

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Welling, Mila Sofie, Cornelis J. de Groot, Lotte Kleinendorst, et al. "Effects of Glucagon-Like-Peptide-1 Analogue Treatment in Genetic Obesity." Journal of the Endocrine Society 5, Supplement_1 (2021): A33—A34. http://dx.doi.org/10.1210/jendso/bvab048.065.

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Abstract Introduction: Obesity is highly prevalent, comes with serious health burden and is difficult to treat. In a minority, there is a genetic cause for the obesity. In these patients, therapy-resistant obesity is often observed despite intensive lifestyle treatment. Moreover, it is still unclear whether bariatric surgery is less successful in genetic obesity. Liraglutide is a Glucagon-Like-Peptide-1 (GLP-1) receptor agonist or GLP-1 analogue, showing positive effects on metabolic parameters, satiety and weight loss in lifestyle-induced obesity. We present our experiences of GLP-1 analogue treatment in patients with genetic obesity disorders. Methods: Adults with overweight or severe obesity and a molecularly proven genetic cause were treated with liraglutide 3,0 mg daily, in addition to ongoing intensive supportive lifestyle treatment. Anthropometrics, metabolic parameters, resting energy expenditure (REE), side effects, and subjectively reported satiety and quality of life were assessed. Results: Two patients with a heterozygous pathogenic melanocortin 4 recepter variant and two patients with 16p11.2 deletion syndrome, ranging in age between 21 and 32 years and in BMI between 28.1 and 55.7 kg/m2 at baseline, were treated. At end of follow-up, ranging between 33 weeks and 12 years, a mean change in BMI and waist circumference was observed of -5.7 ± 3.8 kg/m2 and -15.2 ± 21.1 cm, respectively. All patients reported better quality of life, three of them also reported improved satiety. Moreover, improvement of metabolic parameters was seen. No clear effect on REE was observed. Two patients experienced mild side effects, e.g. nausea and stomach pain, for a brief period. Conclusion: We here show beneficial effects of GLP-1 analogues on weight, metabolic parameters, and quality of life in four patients with genetic obesity. Satiety improved in three of the four patients. All patient achieved at least the clinically relevant 5–10% weight loss. Our findings suggest that GLP-1 analogue treatment might be an effective treatment option, in addition to a healthy lifestyle, for patients with genetic obesity.

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Ruyatkina, Lyudmila Alexandrovna, and Maxim Sorokin. "Combined insulin detemir and liraglutide therapy in type 2 diabetic patients: a base for an alliance." Diabetes mellitus 20, no. 2 (2017): 142–50. http://dx.doi.org/10.14341/7875.

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Combined glucose-lowering therapy, comprising of basal insulin with glucagon-like peptide-1 (GLP-1) analogues, has become central to the treatment of type 2 diabetes both at the start of insulin therapy, and as an alternative to basal-bolus insulin. The combination of insulin detemir (insulin analogue) with liraglutide (GLP-1 analogue) reduces fasting and postprandial glycaemia, lowers the risk of hypoglycaemia and does not have a negative impact on body weight. In this literature review, the pharmacodynamic and pharmacokinetic profiles, as well as the potential benefits of combined insulin detemir and liraglutide therapy on diabetic nephropathy and high cardiovascular disease risk were determined. Data from randomised clinical trials and the National Registry were used to assess the clinical efficacy of combined insulin detemir and liraglutide therapy. The different mechanistic actions of insulin detemir and liraglutide resulted in an additive glucose-lowering effect, which did not affect the pharmacodynamic and pharmacokinetic profiles of each therapeutic agent.

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Hager, Marlies V., Lisa M. Johnson, Denise Wootten, Patrick M. Sexton та Samuel H. Gellman. "β-Arrestin-Biased Agonists of the GLP-1 Receptor from β-Amino Acid Residue Incorporation into GLP-1 Analogues". Journal of the American Chemical Society 138, № 45 (2016): 14970–79. http://dx.doi.org/10.1021/jacs.6b08323.

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Ji, Chenhui, Guo-Fang Xue, Guanglai Li, Dongfang Li, and Christian Hölscher. "Neuroprotective effects of glucose-dependent insulinotropic polypeptide in Alzheimer’s disease." Reviews in the Neurosciences 27, no. 1 (2016): 61–70. http://dx.doi.org/10.1515/revneuro-2015-0021.

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AbstractGlucose-dependent insulinotropic polypeptide (GIP) is a member of the incretin hormones and growth factors. Neurons express the GIP receptor, and GIP and its agonists can pass through the blood brain barrier and show remarkable neuroprotective effects by protecting synapse function and numbers, promoting neuronal proliferation, reducing amyloid plaques in the cortex and reducing the chronic inflammation response of the nervous system. Long-acting analogues of GIP that are protease resistant had been developed as a treatment for type 2 diabetes. It has been found that such GIP analogues show good protective effects in animal models of Alzheimer’s disease. Novel dual agonist peptides that activate the GIP receptor and another incretin receptor, glucagon-like peptide -1 (GLP-1), are under development that show superior effects in diabetic patients compared to single GLP-1 agonists. The dual agonists also show great promise in treating neurodegenerative disorders, and there are currently several clinical trials ongoing, testing GLP-1 mimetics in people with Alzheimer’s or Parkinson’s disease.

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Iacobellis, Gianluca, Vladimir Camarena, David Sant, and Gaofeng Wang. "Human Epicardial Fat Expresses Glucagon-Like Peptide 1 and 2 Receptors Genes." Hormone and Metabolic Research 49, no. 08 (2017): 625–30. http://dx.doi.org/10.1055/s-0043-109563.

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AbstractEpicardial adipose tissue (EAT) is an easily measurable visceral fat of the heart with unique anatomy, functionality, and transcriptome. EAT can serve as a therapeutic target for pharmaceutical agents targeting the fat. Glucagon-like peptide-1 (GLP-1) and GLP-2 analogues are newer drugs showing beneficial cardiovascular and metabolic effects. Whether EAT expresses GLP- 1 and 2 receptors (GLP-1R and GLP-2R) is unknown. RNA-seq analysis and quantitative real-time polymerase chain reaction (qRT-PCR) were performed to evaluate the presence of GLP-1R and GLP-2R in EAT and subcutaneous fat (SAT) obtained from 8 subjects with coronary artery disease and type 2 diabetes mellitus undergoing elective cardiac surgery. Immunofluorescence was also performed on EAT and SAT samples using Mab3f52 against GLP-1R. Our RNA-sequencing (RNA-seq) analysis showed that EAT expresses both GLP-1R and GLP-2R genes. qRT-PCR analysis confirmed that GLP-1R expression was low but detected by 2 different sets of intron-spanning primers. GLP-2R expression was detected in all patients and was found to be 5-fold higher than GLP-1R. The combination of accurately spliced reads from RNA-seq and successful amplification using intron-spanning primers indicates that both GLP-1R and GLP-2R are expressed in EAT. Immunofluorescence clearly showed that GLP-1R is present and more abundant in EAT than SAT. This is the first time that human EAT is found to express both GLP-1R and GLP-2R genes. Pharmacologically targeting EAT may induce beneficial cardiovascular and metabolic effects.

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Kim, Ki-Suk, and Hyeung-Jin Jang. "Medicinal Plants Qua Glucagon-Like Peptide-1 Secretagogue via Intestinal Nutrient Sensors." Evidence-Based Complementary and Alternative Medicine 2015 (2015): 1–9. http://dx.doi.org/10.1155/2015/171742.

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Glucagon-like peptide-1 (GLP-1) participates in glucose homeostasis and feeding behavior. Because GLP-1 is rapidly inactivated by the enzymatic cleavage of dipeptidyl peptidase-4 (DPP4) long-acting GLP-1 analogues, for example, exenatide and DPP4 inhibitors, for example, liraglutide, have been developed as therapeutics for type 2 diabetes mellitus (T2DM). However, the inefficient clinical performance and the incidence of side effects reported on the existing therapeutics for T2DM have led to the development of a novel therapeutic strategy to stimulate endogenous GLP-1 secretion from enteroendocrine L cells. Since the GLP-1 secretion of enteroendocrine L cells depends on the luminal nutrient constituents, the intestinal nutrient sensors involved in GLP-1 secretion have been investigated. In particular, nutrient sensors for tastants, cannabinoids, and bile acids are able to recognize the nonnutritional chemical compounds, which are abundant in medicinal plants. These GLP-1 secretagogues derived from medicinal plants are easy to find in our surroundings, and their effectiveness has been demonstrated through traditional remedies. The finding of GLP-1 secretagogues is directly linked to understanding of the role of intestinal nutrient sensors and their recognizable nutrients. Concurrently, this study demonstrates the possibility of developing novel therapeutics for metabolic disorders such as T2DM and obesity using nutrients that are readily accessible in our surroundings.

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Yu, Ji Hee, So Young Park, Da Young Lee, Nan Hee Kim, and Ji A. Seo. "GLP-1 receptor agonists in diabetic kidney disease: current evidence and future directions." Kidney Research and Clinical Practice 41, no. 2 (2022): 136–49. http://dx.doi.org/10.23876/j.krcp.22.001.

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With the emergence of various classes of blood glucose-lowering agents, choosing the appropriate drug for each patient is emphasized in diabetes management. Among incretin-based drugs, glucagon-like peptide 1 (GLP-1) receptor agonists are a promising therapeutic option for patients with diabetic kidney disease (DKD). Several cardiovascular outcome trials have demonstrated that GLP-1 receptor agonists have beneficial effects on cardiorenal outcomes beyond their blood glucose-lowering effects in patients with type 2 diabetes mellitus (T2DM). The renal protective effects of GLP-1 receptor agonists likely result from their direct actions on the kidney, in addition to their indirect actions that improve conventional risk factors for DKD, such as reducing blood glucose levels, blood pressure, and body weight. Inhibition of oxidative stress and inflammation and induction of natriuresis are major renoprotective mechanisms of GLP-1 analogues. Early evidence from the development of dual and triple combination agents suggests that GLP-1 receptor agonists will probably become popular treatment options for patients with T2DM.

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Levine, Paul M., Timothy W. Craven, Xinting Li, et al. "Generation of Potent and Stable GLP-1 Analogues Via “Serine Ligation”." ACS Chemical Biology 17, no. 4 (2022): 804–9. http://dx.doi.org/10.1021/acschembio.2c00075.

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Farr, Olivia M., and Christos S. Mantzoros. "Treating prediabetes in the obese: are GLP-1 analogues the answer?" Lancet 389, no. 10077 (2017): 1371–72. http://dx.doi.org/10.1016/s0140-6736(17)30315-x.

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Miras, Isabel, Nieves Ramírez, Pablo Sánchez, Carlos Hernández, and Domingo Acosta. "Pneumoperitoneum by subcutaneous injections of GLP-1 analogues. A case report." Endocrinología, Diabetes y Nutrición (English ed.) 65, no. 9 (2018): 548–49. http://dx.doi.org/10.1016/j.endien.2018.06.001.

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Williams, David M., Matthew Staff, Stephen C. Bain, and Thinzar Min. "Glucagon-like Peptide-1 Receptor Analogues for the Treatment of Obesity." Endocrinology 18, no. 1 (2022): 43. http://dx.doi.org/10.17925/ee.2022.18.1.43.

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There is an increasing prevalence of obesity worldwide, associated with significant morbidity and mortality, which frequently reduces quality of life and life expectancy. Consequently, there is a substantial and growing personal and economic burden necessitating the development of more effective therapies for obesity. Glucagon-like peptide-1 receptor analogues (GLP-1RAs) are licensed for the treatment of type 2 diabetes (T2D), and there is substantial evidence that these drugs not only improve cardiovascular outcomes but also promote weight loss. More recent evidence supports the use of the GLP-1RAs liraglutide and semaglutide in people with obesity without T2D. This article discusses the results of the major cardiovascular outcome trials for GLP-1RAs in people with T2D, the SCALE Obesity and Prediabetes study (Effect of liraglutide on body weight in non-diabetic obese subjects or overweight subjects with co-morbidities: SCALE™ - Obesity and Pre-diabetes; ClinicalTrials.gov identifier: NCT01272219; investigating liraglutide) and the STEP studies (Semaglutide treatment effect in people with obesity; assorted studies; investigating subcutaneous semaglutide). We also highlight the importance of a cost-effective approach to obesity pharmacotherapy. Clinicians should consider the use of GLP-1RAs in people with obesity, especially those with T2D or other obesity-related diseases, such as hypertension and dyslipidaemia. Ongoing trials, as well as clinical and cost-effectiveness appraisals, are anticipated over the next 12 months, and their findings may change the current landscape of obesity pharmacotherapy.

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Qin, Kunhao, Shengting Zhang, Jie Wang, et al. "Screening GLP-1 Receptor Ligands from Natural Products in Herbs through High-Content Technique." Combinatorial Chemistry & High Throughput Screening 22, no. 7 (2019): 445–54. http://dx.doi.org/10.2174/1386207322666190919143735.

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Aim and Objective: Screening of active components from a natural product, especially from a crude extract, is a great challenge. To avoid potential activity interference of the N-terminus modification in the most common constructs based on GCPRs labeled with GFP technology, a Cterminus tGFP-labeled hGLP-1 receptor containing recombinant cell line hGLP-1R-tGFP was constructed and tried to be used in the screening of natural products from Chinese herb. Materials and Methods: The GLP1 receptor gene was amplified and the inserts pCMV6-AC-tGFP and tGFP were fused at the C-terminus of GLP1 receptor to construct a recombinant plasmid. The recombinant was transfected into U2OS cell and selected with antibiotics and flow cytometry. The constructed cell line was named as hGLP-1R-tGFP cell line. The expression levels of GLP-1R-tGFP protein were confirmed by western-blot. The fluorescence imaging of re-distribution from diffusing to aggregate spots inside the cells was quantitated and analyzed by High Content Screening (HCS) assay. Meanwhile, the specificity, stability and C-terminus function of hGLP-1R-tGFP cell line were characterized. In order to allow the recombinant cell line of hGLP-1R-tGFP to be suitable in highcontent system of Arrayscan-infinity-700 in screening mode, several conditions have also been optimized. In the end, a total of 100 crude extract samples provided by the Yunnan Institute of Materia Medica have been screened with this method. Results: Upon the activation of GLP-1 receptors by Exendin 4, fluorescent patches appeared on the cell membrane and subsequently internalized to form fluorescent aggregates inside the cells under fluorescent microscopy examination. The agonistic activity, sensitivity and specificity of the formation of fluorescent aggregate spot in hGLP-1R-tGFP cells have been confirmed by the activation of GLP-1R using the GLP-1analogues. The agonistic effects of GLP-1 analogues are blocked by a GLP-1R antagonist, Exendin9-39. The downstream of GLP-1 pathway, the activation of adenylate cyclase and the raising of cellular cAMP levels, remained intact in these tGFP modified C-terminus GLP-1 receptor cells. Meanwhile, a total of 100 crude extract samples from Chinese herbs have been screened by this method to find new active ingredients. Conclusion: Combined with High Content Screening image and data automatic acquisition processing, a new screening assay based on a recombinant U2OS cell line which GFP labeled at the C terminus of GLP1 receptor has been developed. GLP-1R agonist activity in extracts of Astragalus propinquus and Panax notoginseng from Chinese herbs has been determined by this method.

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McClenaghan, Neville H., Peter R. Flatt, and Andrew J. Ball. "Actions of glucagon-like peptide-1 on KATP channel-dependent and -independent effects of glucose, sulphonylureas and nateglinide." Journal of Endocrinology 190, no. 3 (2006): 889–96. http://dx.doi.org/10.1677/joe.1.06949.

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This study examined the effects of glucagon-like peptide-1 (GLP-1) on insulin secretion alone and in combination with sulphonylureas or nateglinide, with particular attention to KATP channel-independent insulin secretion. In depolarised cells, GLP-1 significantly augmented glucose-induced KATP channel-independent insulin secretion in a glucose concentration-dependent manner. GLP-1 similarly augmented the KATP channel-independent insulin-releasing effects of tolbutamide, glibenclamide or nateglinide. Downregulation of protein kinase A (PKA)- or protein kinase C (PKC)-signalling pathways in culture revealed that the KATP channel-independent effects of sulphonylureas or nateglinide were critically dependent upon intact PKA and PKC signalling. In contrast, GLP-1 exhibited a reduced but still significant insulin-releasing effect following PKA and PKC downregulation, indicating that GLP-1 can modulate KATP channel-independent insulin secretion by protein kinase-dependent and -independent mechanisms. The synergistic insulin-releasing effects of combinatorial GLP-1 and sulphonylurea/nateglinide were lost following PKA- or PKC-desensitisation, despite GLP-1 retaining an insulin-releasing effect, demonstrating that GLP-1 can induce insulin release under conditions where sulphonylureas and nateglinide are no longer effective. Our results provide new insights into the mechanisms of action of GLP-1, and further highlight the promise of GLP-1 or similarly acting analogues alone or in combination with sulphonylureas or meglitinide drugs in type 2 diabetes therapy.

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Luo, Shiqi, Harsharn Gill, Bryce Feltis, Andrew Hung, Linh Toan Nguyen, and George Binh Lenon. "The Effects of a Weight-Loss Herbal Formula RCM-107 and Its Eight Individual Ingredients on Glucagon-Like Peptide-1 Secretion—An In Vitro and In Silico Study." International Journal of Molecular Sciences 21, no. 8 (2020): 2854. http://dx.doi.org/10.3390/ijms21082854.

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Obesity is a multifactorial disease that can lead to other health issues. Glucagon-like peptide-1(GLP-1), as one of the satiety signal, has been linked with appetite suppression and weight loss. Due to the limitations of GLP-1 and its analogues, alternative treatments such as herbal therapies have become popular. The herbal formula RCM-107 has demonstrated its inhibitory effects on lipid and carbohydrate absorption in our previous work. However, no published data described its effects on GLP-1 secretion. Therefore, this study aimed to determine the effects of RCM-107 and its individual ingredients on GLP-1 secretion via enzyme-linked immunosorbent assay (ELISA). Furthermore, molecular docking was performed to predict the key chemical compounds that are likely to be GLP-1 receptor agonists. Gardeniae fructus, one of the ingredients in RCM-107, demonstrated significantly greater effects on inducing GLP-1 secretion than the positive control epigallocatechin gallate (EGCG). Two Gardeniae fructus ligands, 3-epioleanolic acid and crocin were predicted to bind to the active form of GLP-1 receptor at the binding pocket with residues known for the receptor activation, suggesting that they could potentially serve as receptor agonists. Overall, this study reported the effects of researched herbs on GLP-1 secretion and proposed two compounds that may be responsible for antiobesity via GLP-1 receptor activation.

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Wiberg, Sebastian, Jesper Kjaergaard, Rasmus Møgelvang, et al. "Efficacy of a glucagon-like peptide-1 agonist and restrictive versus liberal oxygen supply in patients undergoing coronary artery bypass grafting or aortic valve replacement: study protocol for a 2-by-2 factorial designed, randomised clinical trial." BMJ Open 11, no. 11 (2021): e052340. http://dx.doi.org/10.1136/bmjopen-2021-052340.

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IntroductionCoronary artery bypass grafting (CABG) and/or aortic valve replacement (AVR) are associated with risk of death, as well as brain, heart and kidney injury. Glucagon-like peptide-1 (GLP-1) analogues are approved for treatment of type 2 diabetes, and GLP-1 analogues have been suggested to have potential organ-protective and anti-inflammatory effects. During cardiopulmonary bypass (CPB), consensus on the optimal fraction of oxygen is lacking. The objective of this study is to determine the efficacy of the GLP-1-analogue exenatide versus placebo and restrictive oxygenation (50% fractional inspired oxygen, FiO2) versus liberal oxygenation (100% FiO2) in patients undergoing open heart surgery.Methods and analysisA randomised, placebo-controlled, double blind (for the exenatide intervention)/single blind (for the oxygenation strategy), 2×2 factorial designed single-centre trial on adult patients undergoing elective or subacute CABG and/or surgical AVR. Patients will be randomised in a 1:1 and 1:1 ratio to a 6-hour and 15 min infusion of 17.4 µg of exenatide or placebo during CPB and to a FiO2 of 50% or 100% during and after weaning from CPB. Patients will be followed until 12 months after inclusion of the last participant. The primary composite endpoint consists of time to first event of death, renal failure requiring renal replacement therapy, hospitalisation for stroke or heart failure. In addition, the trial will include predefined sub-studies applying more advanced measures of cardiac- and pulmonary dysfunction, renal dysfunction and cerebral dysfunction. The trial is event driven and aims at 323 primary endpoints with a projected inclusion of 1400 patients.Ethics and disseminationEligible patients will provide informed, written consent prior to randomisation. The trial is approved by the local ethics committee and is conducted in accordance with Danish legislation and the Declaration of Helsinki. The results will be presented in peer-reviewed journals.Trial registration numberNCT02673931.

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Sonne, David P., Thomas Engstrøm, and Marek Treiman. "Protective effects of GLP-1 analogues exendin-4 and GLP-1(9–36) amide against ischemia–reperfusion injury in rat heart." Regulatory Peptides 146, no. 1-3 (2008): 243–49. http://dx.doi.org/10.1016/j.regpep.2007.10.001.

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Zhou, Qing-Xia, Zi-Yu Wang, Hua-Feng Zhao, and Shan Wang. "The effects of GLP-1 analogues on pre-diabetes of the children." Experimental and Therapeutic Medicine 13, no. 4 (2017): 1426–30. http://dx.doi.org/10.3892/etm.2017.4129.

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