Novel GLP-1 fusion chimera as potent long acting GLP-1 receptor agonist

PLoS ONE

Volumn 5, Issue 9, 2010, Pages 1-9

  Wang, Qinghua ^a,b   Chen, Kui ^a   Liu, Rui ^a   Zhao, Fang ^a   Gupta, Sandeep ^a   Zhang, Nina ^a   Prud'homme, Gerald J ^c  

^a ST MICHAEL'S HOSPITAL   (Canada)

^b UNIVERSITY OF TORONTO   (Canada)

^c ST MICHAEL'S HOSPITAL   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIDIABETIC AGENT; DYNAMIN; GLUCAGON LIKE PEPTIDE 1; GLUCAGON LIKE PEPTIDE 1 RECEPTOR; GLUCOSE; IMMUNOGLOBULIN G2; INSULIN; STREPTOZOCIN; GLUCAGON RECEPTOR; GLUCAGON-LIKE PEPTIDE-1 RECEPTOR; HYBRID PROTEIN; IMMUNOGLOBULIN G;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; BIOLOGICAL ACTIVITY; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG MECHANISM; DRUG RECEPTOR BINDING; GLUCOSE METABOLISM; GLUCOSE TOLERANCE TEST; GLYCEMIC CONTROL; INSULIN DEPENDENT DIABETES MELLITUS; INSULIN RELEASE; INTERNALIZATION; MALE; MOUSE; NONHUMAN; RAT; SINGLE DRUG DOSE; ANIMAL; CHEMISTRY; DIABETES MELLITUS; DISEASE MODEL; DRUG POTENTIATION; GENETICS; HUMAN; KINETICS; METABOLISM; PROTEIN BINDING; TUMOR CELL LINE;

MUS;

ANIMALS; CELL LINE, TUMOR; DIABETES MELLITUS; DISEASE MODELS, ANIMAL; GLUCAGON-LIKE PEPTIDE 1; HUMANS; HYPOGLYCEMIC AGENTS; IMMUNOGLOBULIN G; INSULIN; KINETICS; MALE; MICE; PROTEIN BINDING; RATS; RECEPTORS, GLUCAGON; RECOMBINANT FUSION PROTEINS;

EID: 77958603882     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0012734     Document Type: Article

References (46)

1. Meier JJ, Nauck MA (2005) Glucagon-like peptide 1(GLP-1) in biology and pathology. Diabetes Metab Res Rev 21: 91-117.
2. Holst JJ, Gromada J (2004) Role of incretin hormones in the regulation of insulin secretion in diabetic and nondiabetic humans. Am J Physiol Endocrinol Metab 287: E199-E206.
3. Todd JF, Wilding JP, Edwards CM, Khan FA, Ghatei MA, et al. (1997) Glucagon-like peptide-1 (GLP-1): a trial of treatment in non-insulin-dependent diabetes mellitus. Eur J Clin Invest 27: 533-536.
4. Wang Q, Brubaker PL (2002) Glucagon-like peptide-1 treatment delays the onset of diabetes in 8 week-old db/db mice. Diabetologia 45: 1263-1273.
5. Perfetti R, Zhou J, Doyle ME, Egan JM (2000) Glucagon-like peptide-1 induces cell proliferation and pancreatic-duodenum homeobox-1 expression and increases endocrine cell mass in the pancreas of old, glucose-intolerant rats. Endocrinology 141: 4600-4605.
6. Li Y, Hansotia T, Yusta B, Ris F, Halban PA, et al. (2003) Glucagon-like peptide-1 receptor signaling modulates beta cell apoptosis. J Biol Chem 278: 471-478.
7. Patti ME, McMahon G, Mun EC, et al. (2005) Severe hypoglycaemia postgastric bypass requiring partial pancreatectomy: evidence for inappropriate insulin secretion and pancreatic islet hyperplasia. Diabetologia 48: 2236-2240.
8. Drucker DJ (2006) The biology of incretin hormones. Cell Metab 3: 153-165.
9. Scrocchi LA, Brown TJ, MaClusky N, Brubaker PL, Auerbach AB, et al. (1996) Glucose intolerance but normal satiety in mice with a null mutation in the glucagon-like peptide 1 receptor gene. Nat Med 2: 1254-1258.
10. Kieffer TJ, McIntosh CH, Pederson RA (1995) Degradation of glucosedependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV. Endocrinology 136: 3585-3596.
11. Lovshin JA, Drucker DJ (2009) Incretin-based therapies for type 2 diabetes mellitus. Nat Rev Endocrinol 5: 262-269.
12. Soltani N, Kumar M, Glinka Y, Prud'homme GJ, Wang Q (2007) In vivo expression of GLP-1/IgG-Fc fusion protein enhances beta-cell mass and protects against streptozotocin-induced diabetes. Gene Ther 14: 981-988.
13. Kumar M, Hunag Y, Glinka Y, Prud'homme GJ, Wang Q (2007) Gene therapy of diabetes using a novel GLP-1/IgG1-Fc fusion construct normalizes glucose levels in db/db mice. Gene Ther 14: 162-172.
14. Woof JM, Burton DR (2004) Human antibody-Fc receptor interactions illuminated by crystal structures. Nat Rev Immunol 4: 89-99.
15. Syme CA, Zhang L, Bisello A (2006) Caveolin-1 regulates cellular trafficking and function of the glucagon-like Peptide 1 receptor. Mol Endocrinol 20: 3400-3411.
16. Mentlein R, Gallwitz B, Schmidt WE (1993) Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7-36)amide, peptide histidine methionine and is responsible for their degradation in human serum. Eur J Biochem 214: 829-835.
17. Ruiz-Grande C, Pintado J, Alarcon C, Castilla C, Valverde I, et al. (1990) Renal catabolism of human glucagon-like peptides 1 and 2. Can J Physiol Pharmacol 68: 1568-1573.
18. Weir AN, Nesbitt A, Chapman AP, Popplewell AG, Antoniw P, et al. (2002) Formatting antibody fragments to mediate specific therapeutic functions. Biochem Soc Trans 30: 512-516.
19. Larrick JW, Fry KE (1991) Recombinant antibodies. Hum Antibodies Hybridomas 2: 172-189.
20. Dumont JA, Low SC, Peters RT, Bitonti AJ (2006) Monomeric Fc fusions: impact on pharmacokinetic and biological activity of protein therapeutics. BioDrugs 20: 151-160.
21. Huang C (2009) Receptor-Fc fusion therapeutics, traps, and MIMETIBODY technology. Curr Opin Biotechnol 20: 692-699.
22. Hupe-Sodmann K, McGregor GP, Bridenbaugh R, et al. (1995) Characterisation of the processing by human neutral endopeptidase 24.11 of GLP-1(7-36) amide and comparison of the substrate specificity of the enzyme for other glucagon-like peptides. Regul Pept 58: 149-156.
23. Irwin DM, Satkunarajah M, Wen Y, Brubaker PL, Pederson RA, et al. (1997) The Xenopus proglucagon gene encodes novel GLP-1-like peptides with insulinotropic properties. Proc Natl Acad Sci U S A 94: 7915-7920.
24. Picha KM, Cunningham MR, Drucker DJ, Mathur A, Ort T, et al. (2008) Protein engineering strategies for sustained glucagon-like peptide-1 receptordependent control of glucose homeostasis. Diabetes 57: 1926-1934.
25. Baggio LL, Huang Q, Brown TJ, Drucker DJ (2004) A recombinant human glucagon-like peptide (GLP)-1-albumin protein (albugon) mimics peptidergic activation of GLP-1 receptor-dependent pathways coupled with satiety, gastrointestinal motility, and glucose homeostasis. Diabetes 53: 2492-2500.
26. George SR, O'Dowd BF, Lee SP (2002) G-protein-coupled receptor oligomerization and its potential for drug discovery. Nat Rev Drug Discov 1: 808-820.
27. Jefferis R, Lund J (2002) Interaction sites on human IgG-Fc for FcgammaR: current models. Immunol Lett 82: 57-65.
28. Murphy K, Travers P, Walport M, eds. Janeway's Immunobiology 7th Edition, Garland Science, NY. 409-413. 2008. (GENERIC).
29. Kumpel BM, Beliard R, Brossard Y, et al. (2002) Section 1C: Assessment of the functional activity and IgG Fc receptor utilisation of 64 IgG Rh monoclonal antibodies. Coordinator's report. Transfus Clin Biol 9: 45-53.
30. Prislovsky A, Marathe B, Hosni A, Bolen AL, Nimmerjahn F, et al. (2008) Rapid platelet turnover in WASP(-) mice correlates with increased ex vivo phagocytosis of opsonized WASP(-) platelets. Exp Hematol 36: 609-623.
31. Lee AY, Chey WY, Choi J, Jeon JS (2002) Insulin-induced drug eruptions and reliability of skin tests. Acta Derm Venereol 82: 114-117.
32. Ahangari G, Ostadali MR, Rabani A, Rashidian J, Sanati MH, et al. (2004) Growth hormone antibodies formation in patients treated with recombinant human growth hormone. Int J Immunopathol Pharmacol 17: 33-38.
33. Takai T (2005) Fc receptors and their role in immune regulation and autoimmunity. J Clin Immunol 25: 1-18.
34. King LB, Monroe JG (2000) Immunobiology of the immature B cell: plasticity in the B-cell antigen receptor-induced response fine tunes negative selection. Immunol Rev 176: 86-104.: 86-104.
35. Melo ME, Qian J, El-Amine M, Agarwal RK, Soukhareva N, et al. (2002) Gene transfer of Ig-fusion proteins into B cells prevents and treats autoimmune diseases. J Immunol 168: 4788-4795.
36. Uray K, Medgyesi D, Hilbert A, Sarmay G, Gergely J, et al. (2004) Synthesis and receptor binding of IgG1 peptides derived from the IgG Fc region. J Mol Recognit 17: 95-105.
37. Thorens B, Waeber G (1993) Glucagon-like peptide-I and the control of insulin secretion in the normal state and in NIDDM. Diabetes 42: 1219-1225.
38. Jorgensen R, Martini L, Schwartz TW, Elling CE (2005) Characterization of glucagon-like peptide-1 receptor beta-arrestin 2 interaction: a high-affinity receptor phenotype. Mol Endocrinol 19: 812-823.
39. Wang Y, Perfetti R, Greig NH, Holloway HW, DeOre KA, et al. (1997) Glucagon-like peptide-1 can reverse the age-related decline in glucose tolerance in rats. J Clin Invest 99: 2883-2889.
40. Baggio LL, Kim JG, Drucker DJ (2004) Chronic exposure to GLP-1R agonists promotes homologous GLP-1 receptor desensitization in vitro but does not attenuate GLP-1R-dependent glucose homeostasis in vivo. Diabetes 53 Suppl 3: S205-14.: S205-S214.
41. Zander M, Madsbad S, Madsen JL, Holst JJ (2002) Effect of 6-week course of glucagon-like peptide 1 on glycaemic control, insulin sensitivity, and beta-cell function in type 2 diabetes: a parallel-group study. Lancet 359: 824-830.
42. Larsen J, Hylleberg B, Ng K, Damsbo P (2001) Glucagon-like peptide-1 infusion must be maintained for 24 h/day to obtain acceptable glycemia in type 2 diabetic patients who are poorly controlled on sulphonylurea treatment. Diabetes Care 24: 1416-1421.
43. Yu SS, Lefkowitz RJ, Hausdorff WP (1993) Beta-adrenergic receptor sequestration. A potential mechanism of receptor resensitization. J Biol Chem 268: 337-341.
44. Pippig S, Andexinger S, Lohse MJ (1995) Sequestration and recycling of beta 2-adrenergic receptors permit receptor resensitization. Mol Pharmacol 47: 666-676.
45. Widmann C, Dolci W, Thorens B (1997) Internalization and homologous desensitization of the GLP-1 receptor depend on phosphorylation of the receptor carboxyl tail at the same three sites. Mol Endocrinol 11: 1094-1102.
46. Barak LS, Tiberi M, Freedman NJ, Kwatra MM, Lefkowitz RJ, et al. (1994) A highly conserved tyrosine residue in G protein-coupled receptors is required for agonist-mediated beta 2-adrenergic receptor sequestration. J Biol Chem 269: 2790-2795.