Development of a C-terminal site-specific PEGylated analog of GLP-1 with improved anti-diabetic effects in diabetic mice

Drug Development Research

Volumn 74, Issue 3, 2013, Pages 186-193

  Gao, Mingming ^a   Tong, Yue ^a   Gao, Xiangdong ^a   Yao, Wenbing ^a  

^a CHINA PHARMACEUTICAL UNIVERSITY   (China)

Author keywords

diabetes; glucagon like peptide 1; PEGylation

Indexed keywords

GLUCAGON LIKE PEPTIDE 1; GLUCOSE; INSULIN; MACROGOL;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIDIABETIC ACTIVITY; ARTICLE; BODY WEIGHT; CHROMATOGRAPHY; CONTROLLED STUDY; DRUG CONFORMATION; DRUG CONJUGATION; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; GLUCOSE HOMEOSTASIS; HISTOCHEMISTRY; MALE; MOUSE; NONHUMAN; ORAL GLUCOSE TOLERANCE TEST; PANCREAS; STOMACH EMPTYING; STREPTOZOCIN DIABETES; STRUCTURE ACTIVITY RELATION; TISSUE INJURY; WEIGHT GAIN;

EID: 84876156529     PISSN: 02724391     EISSN: 10982299     Source Type: Journal    
DOI: 10.1002/ddr.21059     Document Type: Article

References (21)

1. Adelhorst K, Hedegaard BB, Knudsen LB, Kirk O,. 1994. Structure-activity studies of glucagon-like peptide-1. J Biol Chem 269: 6275-6278.
2. Deacon CF, Knudsen LB, Madsen K, Wiberg FC, Jacobsen O, Holst JJ,. 1998. Dipeptidyl peptidase IV resistant analogues of glucagon-like peptide-1 which have extended metabolic stability and improved biological activity. Diabetologia 41: 271-278.
3. Drucker DJ, Nauck MA,. 2006. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 368: 1696-1705.
4. Eppens MC, Craig ME, Cusumano J, Hing S, Chan AK, Howard NJ, Silink M, Donaghue KC,. 2006. Prevalence of diabetes complications in adolescents with type 2 compared with type 1 diabetes. Diabetes Care 29: 1300-1306.
5. Foser S, Schacher A, Weyer KA, Brugger D, Dietel E, Marti S, Schreitmuller T,. 2003. Isolation, structural characterization, and antiviral activity of positional isomers of monopegylated interferon alpha-2a (PEGASYS). Protein Expr Purif 30: 78-87.
6. Gao M, Tian H, Ma C, Gao X, Guo W, Yao W,. 2010a. Expression, purification, and C-terminal site-specific PEGylation of cysteine-mutated glucagon-like peptide-1. Appl Biochem Biotechnol 162: 155-165.
7. Gao M, Ma C, Liu W, Zhu J, Tian H, Gao X, Yao W,. 2010b. Production and purification of an analog of glucagon-like peptide-1 by auto-induction and on-column cleavage in Escherichia coli. World J Microb Biot 26: 1675-1682.
8. Gao M, Jin Y, Tong Y, Tian H, Gao X, Yao W,. 2012. A site-specific PEGylated analog of exendin-4 with improved pharmacokinetics and pharmacodynamics in vivo. J Pharm Pharmacol 64: 1646-1653.
9. Harris JM, Chess RB,. 2003. Effect of pegylation on pharmaceuticals. Nat Rev Drug Discov 2: 214-221.
10. Holst JJ,. 2007. The physiology of glucagon-like peptide 1. Physiol Rev 87: 1409-1439.
11. Kaiser N, Leibowitz G, Nesher R,. 2003. Glucotoxicity and beta-cell failure in type 2 diabetes mellitus. J Pediatr Endocrinol Metab 16: 5-22.
12. Li W, Gao M, Liu W, Kong Y, Tian H, Yao W, Gao X,. 2012. Optimized soluble expression and purification of an aggregation-prone protein by fusion tag systems and on-column cleavage in Escherichia coli. Protein Pept Lett 19: 1324-1329.
13. Ma C, Gao M, Liu W, Zhu J, Tian H, Gao X, Yao W,. 2010. Intein-mediated expression and purification of an analog of glucagon-like peptide-1 in Escherichia coli. Protein Pept Lett 17: 1245-1250.
14. Nalysnyk L, Hernandez-Medina M, Krishnarajah G,. 2010. Glycaemic variability and complications in patients with diabetes mellitus: evidence from a systematic review of the literature. Diabetes Obes Metab 12: 288-298.
15. Nathan DM, Davidson MB, DeFronzo RA, Heine RJ, Henry RR, Pratley R, Zinman B,. 2007. Impaired fasting glucose and impaired glucose tolerance: implications for care. Diabetes Care 30: 753-759.
16. Nissen SE, Wolski K,. 2007. Effect of rosiglitazone on the risk of myocardial infarction and death from cardiovascular causes. N Engl J Med 356: 2457-2471.
17. Schagger H,. 2006. Tricine-SDS-PAGE. Nat Protoc 1: 16-22.
18. Stoffers DA,. 2004. The development of beta-cell mass: recent progress and potential role of GLP-1. Horm Metab Res 36: 811-821.
19. Underwood CR, Garibay P, Knudsen LB, Hastrup S, Peters GH, Rudolph R, Reedtz-Runge S,. 2010. Crystal structure of glucagon-like peptide-1 in complex with the extracellular domain of the glucagon-like peptide-1 receptor. J Biol Chem 285: 723-730.
20. Veronese FM, Pasut G,. 2005. PEGylation, successful approach to drug delivery. Drug Discov Today 10: 1451-1458.
21. Xu G, Stoffers DA, Habener JF, Bonner-Weir S,. 1999. Exendin-4 stimulates both beta-cell replication and neogenesis, resulting in increased beta-cell mass and improved glucose tolerance in diabetic rats. Diabetes 48: 2270-2276.