Recent progress and future options in the development of GLP-1 receptor agonists for the treatment of diabesity.

[1]  R. Becker,et al.  Effects of lixisenatide once daily on gastric emptying in type 2 diabetes — Relationship to postprandial glycemia , 2013, Regulatory Peptides.

[2]  S. Woods,et al.  Fibroblast Growth Factor 21 Mediates Specific Glucagon Actions , 2013, Diabetes.

[3]  D. Raccah Efficacy and safety of lixisenatide in the treatment of Type 2 diabetes mellitus: a review of Phase III clinical data , 2013, Expert review of endocrinology & metabolism.

[4]  D. Urošević,et al.  Efficacy and tolerability of taspoglutide versus pioglitazone in subjects with type 2 diabetes uncontrolled with sulphonylurea or sulphonylurea‐metformin therapy: a randomized, double‐blind study (T‐emerge 6) , 2013, Diabetes, obesity & metabolism.

[5]  S. Inzucchi,et al.  Erratum to: Management of hyperglycaemia in type 2 diabetes: a patient-centered approach. Position statement of the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD) , 2013, Diabetologia.

[6]  J. Rosenstock,et al.  The Fate of Taspoglutide, a Weekly GLP-1 Receptor Agonist, Versus Twice-Daily Exenatide for Type 2 Diabetes , 2013, Diabetes Care.

[7]  W. Sheu,et al.  Exenatide once weekly versus liraglutide once daily in patients with type 2 diabetes (DURATION-6): a randomised, open-label study , 2013, The Lancet.

[8]  M. Christensen,et al.  GLP-1 agonists for type 2 diabetes: pharmacokinetic and toxicological considerations , 2013, Expert opinion on drug metabolism & toxicology.

[9]  B. Zinman,et al.  Weight change with liraglutide and comparator therapies: an analysis of seven phase 3 trials from the liraglutide diabetes development programme , 2013, Diabetes, obesity & metabolism.

[10]  M. Andjelkovic,et al.  Taspoglutide, a once‐weekly glucagon‐like peptide 1 analogue, vs. insulin glargine titrated to target in patients with Type 2 diabetes: an open‐label randomized trial , 2013, Diabetic Medicine.

[11]  J. Meier GLP-1 receptor agonists for individualized treatment of type 2 diabetes mellitus , 2012, Nature Reviews Endocrinology.

[12]  R. Bergenstal,et al.  Efficacy and Safety of Taspoglutide Versus Sitagliptin for Type 2 Diabetes Mellitus (T-Emerge 4 Trial) , 2012, Diabetes Therapy.

[13]  H. Santos,et al.  Oral Delivery of Glucagon-like Peptide-1 and Analogs: Alternatives for Diabetes Control? , 2012, Journal of diabetes science and technology.

[14]  G. Grunberger,et al.  Monotherapy with the once‐weekly GLP‐1 analogue dulaglutide for 12 weeks in patients with Type 2 diabetes: dose‐dependent effects on glycaemic control in a randomized, double‐blind, placebo‐controlled study , 2012, Diabetic medicine : a journal of the British Diabetic Association.

[15]  B. Hoogwerf,et al.  Efficacy of GLP-1 receptor agonists and DPP-4 inhibitors: meta-analysis and systematic review. , 2012, Clinical therapeutics.

[16]  D. Matthews,et al.  Management of Hyperglycemia in Type 2 Diabetes: A Patient-Centered Approach , 2012, Diabetes Care.

[17]  S. Mudaliar,et al.  Efficacy and safety of taspoglutide in patients with type 2 diabetes inadequately controlled with metformin plus pioglitazone over 24 weeks: T-Emerge 3 trial. , 2012, The Journal of clinical endocrinology and metabolism.

[18]  V. Fonseca,et al.  Efficacy and Safety of Taspoglutide Monotherapy in Drug-Naive Type 2 Diabetic Patients After 24 Weeks of Treatment , 2012, Diabetes Care.

[19]  D. Drucker,et al.  Cardiovascular biology of the incretin system. , 2012, Endocrine reviews.

[20]  M. Christensen,et al.  Effects of glucagon-like peptide-1 receptor agonists on weight loss: systematic review and meta-analyses of randomised controlled trials , 2012, BMJ : British Medical Journal.

[21]  K Khunti,et al.  An update on exenatide, a novel therapeutic option for patients with type 2 diabetes. , 2011, Drugs of today.

[22]  K. Khunti,et al.  Impact of weight gain on outcomes in type 2 diabetes , 2011, Current medical research and opinion.

[23]  J. Holst,et al.  An overview of once‐weekly glucagon‐like peptide‐1 receptor agonists—available efficacy and safety data and perspectives for the future , 2011, Diabetes, obesity & metabolism.

[24]  A. Pocai,et al.  DPP‐IV‐resistant, long‐acting oxyntomodulin derivatives , 2011, Journal of peptide science : an official publication of the European Peptide Society.

[25]  R. Perugini,et al.  Remission of type 2 diabetes mellitus following bariatric surgery: review of mechanisms and presentation of the concept of ‘reversibility’ , 2011, Current opinion in endocrinology, diabetes, and obesity.

[26]  C. Kapitza,et al.  The once-daily human glucagon-like peptide-1 (GLP-1) analog liraglutide improves postprandial glucose levels in type 2 diabetes patients , 2011, Advances in therapy.

[27]  N. Tsomaia,et al.  Discovery and characterization of taspoglutide, a novel analogue of human glucagon‐like peptide‐1, engineered for sustained therapeutic activity in type 2 diabetes , 2011, Diabetes, obesity & metabolism.

[28]  M. Tschöp,et al.  The metabolic actions of glucagon revisited , 2010, Nature Reviews Endocrinology.

[29]  M. Christensen,et al.  Dulaglutide, a long-acting GLP-1 analog fused with an Fc antibody fragment for the potential treatment of type 2 diabetes. , 2010, Current opinion in molecular therapeutics.

[30]  J. Rosenstock,et al.  Dose-dependent effects of the once-daily GLP-1 receptor agonist lixisenatide in patients with Type 2 diabetes inadequately controlled with metformin: a randomized, double-blind, placebo-controlled trial , 2010, Diabetic medicine : a journal of the British Diabetic Association.

[31]  S. Bloom,et al.  Subcutaneous oxyntomodulin analogue administration reduces body weight in lean and obese rodents , 2010, International Journal of Obesity.

[32]  M. Nauck,et al.  Is the Diminished Incretin Effect in Type 2 Diabetes Just an Epi-Phenomenon of Impaired β-Cell Function? , 2010, Diabetes.

[33]  Shannon A. Miller,et al.  Albiglutide: a new GLP-1 analog for the treatment of type 2 diabetes , 2010, Expert opinion on biological therapy.

[34]  S. Kashyap,et al.  Improved Pancreatic β-Cell Function in Type 2 Diabetic Patients After Lifestyle-Induced Weight Loss Is Related to Glucose-Dependent Insulinotropic Polypeptide , 2010, Diabetes Care.

[35]  Willem P C Stemmer,et al.  A recombinant polypeptide extends the in vivo half-life of peptides and proteins in a tunable manner , 2009, Nature Biotechnology.

[36]  A. Astrup,et al.  Effects of liraglutide in the treatment of obesity: a randomised, double-blind, placebo-controlled study , 2009, The Lancet.

[37]  Lotte Bjerre Knudsen,et al.  Crystal Structure of Glucagon-like Peptide-1 in Complex with the Extracellular Domain of the Glucagon-like Peptide-1 Receptor* , 2009, The Journal of Biological Chemistry.

[38]  S. Woods,et al.  A new glucagon and GLP-1 co-agonist eliminates obesity in rodents. , 2009, Nature chemical biology.

[39]  Michael E. Lassman,et al.  Glucagon-Like Peptide 1/Glucagon Receptor Dual Agonism Reverses Obesity in Mice , 2009, Diabetes.

[40]  J. Rosenstock,et al.  Liraglutide once a day versus exenatide twice a day for type 2 diabetes: a 26-week randomised, parallel-group, multinational, open-label trial (LEAD-6) , 2009, The Lancet.

[41]  M. Jensen,et al.  Weight and type 2 diabetes after bariatric surgery: systematic review and meta-analysis. , 2009, The American journal of medicine.

[42]  T. Vilsbøll,et al.  Four weeks of near-normalisation of blood glucose improves the insulin response to glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide in patients with type 2 diabetes , 2009, Diabetologia.

[43]  M. Horowitz,et al.  Effect of exenatide on gastric emptying and relationship to postprandial glycemia in type 2 diabetes , 2008, Regulatory Peptides.

[44]  Philip J Larsen Mechanisms behind GLP-1 induced weight loss , 2008 .

[45]  D. Drucker,et al.  Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority study , 2008, The Lancet.

[46]  Kjeld Madsen,et al.  Crystal Structure of the Ligand-bound Glucagon-like Peptide-1 Receptor Extracellular Domain* , 2008, Journal of Biological Chemistry.

[47]  D. Drucker,et al.  An albumin-exendin-4 conjugate engages central and peripheral circuits regulating murine energy and glucose homeostasis. , 2008, Gastroenterology.

[48]  R. Pederson,et al.  Reversal of islet GIP receptor down-regulation and resistance to GIP by reducing hyperglycemia in the Zucker rat. , 2007, Biochemical and biophysical research communications.

[49]  L. B. Knudsen,et al.  Structure-activity and protraction relationship of long-acting glucagon-like peptide-1 derivatives: importance of fatty acid length, polarity, and bulkiness. , 2007, Journal of medicinal chemistry.

[50]  J. Holst The physiology of glucagon-like peptide 1. , 2007, Physiological reviews.

[51]  R. Rudolph,et al.  Crystal structure of the incretin-bound extracellular domain of a G protein-coupled receptor , 2007, Proceedings of the National Academy of Sciences.

[52]  G. Frost,et al.  Oxyntomodulin increases energy expenditure in addition to decreasing energy intake in overweight and obese humans: a randomised controlled trial , 2006, International Journal of Obesity.

[53]  P. J. Larsen,et al.  PYY(3-36) reduces food intake and body weight and improves insulin sensitivity in rodent models of diet-induced obesity. , 2006, American journal of physiology. Regulatory, integrative and comparative physiology.

[54]  Karim Meeran,et al.  Subcutaneous oxyntomodulin reduces body weight in overweight and obese subjects: a double-blind, randomized, controlled trial. , 2005, Diabetes.

[55]  R. Hansen,et al.  Antibody pharmacokinetics and pharmacodynamics. , 2004, Journal of pharmaceutical sciences.

[56]  Claude Colette,et al.  Contributions of fasting and postprandial plasma glucose increments to the overall diurnal hyperglycemia of type 2 diabetic patients: variations with increasing levels of HbA(1c). , 2003, Diabetes care.

[57]  D. Pearl,et al.  The Major Histocompatibility Complex–related Fc Receptor for IgG (FcRn) Binds Albumin and Prolongs Its Lifespan , 2003, The Journal of experimental medicine.

[58]  Rachel L. Batterham,et al.  Gut hormone PYY3-36 physiologically inhibits food intake , 2002, Nature.

[59]  J. W. Neidigh,et al.  Exendin-4 and glucagon-like-peptide-1: NMR structural comparisons in the solution and micelle-associated states. , 2001, Biochemistry.

[60]  L. B. Knudsen,et al.  Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration. , 2000, Journal of medicinal chemistry.

[61]  G. Ramadori,et al.  A synthetic glucagon-like peptide-1 analog with improved plasma stability. , 1998, The Journal of endocrinology.

[62]  J. Holst,et al.  Dipeptidyl peptidase IV resistant analogues of glucagon-like peptide-1 which have extended metabolic stability and improved biological activity , 1998, Diabetologia.

[63]  U. Ribel,et al.  Soluble, fatty acid acylated insulins bind to albumin and show protracted action in pigs , 1996, Diabetologia.

[64]  U. Ribel,et al.  Albumin binding of insulins acylated with fatty acids: characterization of the ligand-protein interaction and correlation between binding affinity and timing of the insulin effect in vivo. , 1995, The Biochemical journal.

[65]  J. Holst,et al.  Both Subcutaneously and Intravenously Administered Glucagon-Like Peptide I Are Rapidly Degraded From the NH2-Terminus in Type II Diabetic Patients and in Healthy Subjects , 1995, Diabetes.

[66]  M. Bryer-Ash,et al.  The Effect of Glyburide on β-Cell Sensitivity to Glucose-Dependent Insulinotropic Polypeptide , 1993, Diabetes Care.

[67]  R. Eaton,et al.  Incretin effects of increasing glucose loads in man calculated from venous insulin and C-peptide responses. , 1986, The Journal of clinical endocrinology and metabolism.

[68]  B. Meloun,et al.  Complete amino acid sequence of human serum albumin , 1975, FEBS letters.

[69]  M. M. G. Brao 48th Annual Meeting of the European Association for the Study of Diabetes (EASD), Berlin, Germany - October 1-5, 2012 , 2012 .

[70]  M. Erion,et al.  Optimization of co‐agonism at GLP‐1 and glucagon receptors to safely maximize weight reduction in DIO‐rodents , 2012, Biopolymers.

[71]  Y. Farag,et al.  Diabesity: an overview of a rising epidemic. , 2011, Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association.

[72]  J. Leahy Effects of Once-Weekly Dosing of a Long-Acting Release Formulation of Exenatide on Glucose Control and Body Weight in Subjects With Type 2 Diabetes , 2008 .