Victor A Gault

Summary

Affiliation: University of Ulster
Country: UK

Publications

  1. ncbi Glucose-dependent insulinotropic polypeptide (GIP): anti-diabetic and anti-obesity potential?
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine, Northern Ireland, BT52 1SA, UK
    Neuropeptides 37:253-63. 2003
  2. ncbi C-terminal mini-PEGylation of glucose-dependent insulinotropic polypeptide exhibits metabolic stability and improved glucose homeostasis in dietary-induced diabetes
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine BT52 1SA, Northern Ireland, United Kingdom
    Biochem Pharmacol 75:2325-33. 2008
  3. ncbi Chemical ablation of gastric inhibitory polypeptide receptor action by daily (Pro3)GIP administration improves glucose tolerance and ameliorates insulin resistance and abnormalities of islet structure in obesity-related diabetes
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland BT52 1SA, UK
    Diabetes 54:2436-46. 2005
  4. ncbi Actions of exendin-4 therapy on cognitive function and hippocampal synaptic plasticity in mice fed a high-fat diet
    V A Gault
    The SAAD Centre for Pharmacy and Diabetes, School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, UK
    Int J Obes (Lond) 34:1341-4. 2010
  5. ncbi Effects of subchronic treatment with the long-acting glucose-dependent insulinotropic polypeptide receptor agonist, N-AcGIP, on glucose homeostasis in streptozotocin-induced diabetes
    Victor A Gault
    Diabetes Research Group, School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, UK
    Pancreas 35:73-9. 2007
  6. ncbi Glucose-dependent insulinotropic polypeptide analogues and their therapeutic potential for the treatment of obesity-diabetes
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine BT52 1SA, Northern Ireland, UK
    Biochem Biophys Res Commun 308:207-13. 2003
  7. ncbi Characterisation and glucoregulatory actions of a novel acylated form of the (Pro3)GIP receptor antagonist in type 2 diabetes
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Biol Chem 388:173-9. 2007
  8. ncbi DPP IV resistance and insulin releasing activity of a novel di-substituted analogue of glucose-dependent insulinotropic polypeptide, (Ser2-Asp13)GIP
    V A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Cell Biol Int 27:41-6. 2003
  9. ncbi Cyclic AMP production and insulin releasing activity of synthetic fragment peptides of glucose-dependent insulinotropic polypeptide
    V A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, BT52 ISA, UK
    Biosci Rep 22:523-8. 2002
  10. ncbi Administration of an acylated GLP-1 and GIP preparation provides added beneficial glucose-lowering and insulinotropic actions over single incretins in mice with Type 2 diabetes and obesity
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Clin Sci (Lond) 121:107-17. 2011

Collaborators

Detail Information

Publications70

  1. ncbi Glucose-dependent insulinotropic polypeptide (GIP): anti-diabetic and anti-obesity potential?
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine, Northern Ireland, BT52 1SA, UK
    Neuropeptides 37:253-63. 2003
    ..The present review aims to highlight the rapidly emerging potential therapeutic applications of GIP, and especially, enzyme-resistant GIP analogues...
  2. ncbi C-terminal mini-PEGylation of glucose-dependent insulinotropic polypeptide exhibits metabolic stability and improved glucose homeostasis in dietary-induced diabetes
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine BT52 1SA, Northern Ireland, United Kingdom
    Biochem Pharmacol 75:2325-33. 2008
    ..In summary, these data demonstrate that C-terminal mini-PEGylation of GIP is a useful strategy to prolong metabolic stability and improve biological action thus representing a novel therapeutic option for type 2 diabetes...
  3. ncbi Chemical ablation of gastric inhibitory polypeptide receptor action by daily (Pro3)GIP administration improves glucose tolerance and ameliorates insulin resistance and abnormalities of islet structure in obesity-related diabetes
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland BT52 1SA, UK
    Diabetes 54:2436-46. 2005
    ..These studies highlight a role for GIP in obesity-related glucose intolerance and emphasize the potential of specific GIP-R antagonists as a new class of drugs for the alleviation of insulin resistance and treatment of type 2 diabetes...
  4. ncbi Actions of exendin-4 therapy on cognitive function and hippocampal synaptic plasticity in mice fed a high-fat diet
    V A Gault
    The SAAD Centre for Pharmacy and Diabetes, School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, UK
    Int J Obes (Lond) 34:1341-4. 2010
    ..This study shows that exendin-4 therapy improves cognitive function and ameliorates impaired hippocampal synaptic plasticity in dietary-induced obesity...
  5. ncbi Effects of subchronic treatment with the long-acting glucose-dependent insulinotropic polypeptide receptor agonist, N-AcGIP, on glucose homeostasis in streptozotocin-induced diabetes
    Victor A Gault
    Diabetes Research Group, School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, UK
    Pancreas 35:73-9. 2007
    ..The present study investigated the effects of subchronic treatment with N-AcGIP on glucose homeostasis in a type 1 model, namely, streptozotocin (STZ)-induced diabetic mice...
  6. ncbi Glucose-dependent insulinotropic polypeptide analogues and their therapeutic potential for the treatment of obesity-diabetes
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine BT52 1SA, Northern Ireland, UK
    Biochem Biophys Res Commun 308:207-13. 2003
    ..The purpose of this article was to provide an overview of the biological effects of several GIP modifications and to highlight the potential of such analogues in the treatment of type 2 diabetes and obesity...
  7. ncbi Characterisation and glucoregulatory actions of a novel acylated form of the (Pro3)GIP receptor antagonist in type 2 diabetes
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Biol Chem 388:173-9. 2007
    ..05) in the (Pro3)GIPLys16PAL-treated mice. These data demonstrate that acylation of Lys16 with palmitic acid in (Pro3)GIP does not improve its biological effectiveness as a GIP receptor antagonist...
  8. ncbi DPP IV resistance and insulin releasing activity of a novel di-substituted analogue of glucose-dependent insulinotropic polypeptide, (Ser2-Asp13)GIP
    V A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Cell Biol Int 27:41-6. 2003
    ....
  9. ncbi Cyclic AMP production and insulin releasing activity of synthetic fragment peptides of glucose-dependent insulinotropic polypeptide
    V A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, BT52 ISA, UK
    Biosci Rep 22:523-8. 2002
    ..05 and 11 +/- 3%, respectively). These data demonstrate the critical role of the N-terminus and the involvement of regions of the C-terminal domain in generating full biological potency of GIP...
  10. ncbi Administration of an acylated GLP-1 and GIP preparation provides added beneficial glucose-lowering and insulinotropic actions over single incretins in mice with Type 2 diabetes and obesity
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Clin Sci (Lond) 121:107-17. 2011
    ....
  11. ncbi Evidence that the major degradation product of glucose-dependent insulinotropic polypeptide, GIP(3-42), is a GIP receptor antagonist in vivo
    V A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine, N Ireland BT52 1SA, UK
    J Endocrinol 175:525-33. 2002
    ..4-fold; P<0.001) induced by a conjoint glucose load. These data indicate that the N-terminally truncated GIP(3-42) fragment acts as a GIP receptor antagonist, moderating the insulin secreting and metabolic actions of GIP in vivo...
  12. ncbi Improved biological activity of Gly2- and Ser2-substituted analogues of glucose-dependent insulinotrophic polypeptide
    V A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, UK
    J Endocrinol 176:133-41. 2003
    ....
  13. ncbi Antagonistic effects of two novel GIP analogs, (Hyp3)GIP and (Hyp3)GIPLys16PAL, on the biological actions of GIP and longer-term effects in diabetic ob/ob mice
    Finbarr P M O'Harte
    School of Biomedical Sciences, University of Ulster, Coleraine, BT52 1SA, Northern Ireland
    Am J Physiol Endocrinol Metab 292:E1674-82. 2007
    ..Acylation of (Hyp(3))GIP to extend bioactivity does not appear to be of any additional benefit...
  14. ncbi Metabolic stability, receptor binding, cAMP generation, insulin secretion and antihyperglycaemic activity of novel N-terminal Glu9-substituted analogues of glucagon-like peptide-1
    Brian D Green
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Biol Chem 384:1543-51. 2003
    ..These observations indicate the importance of Glu9 for the biological activity of GLP-1 and susceptibility to DPP IV-mediated degradation...
  15. ncbi Degradation, receptor binding, insulin secreting and antihyperglycaemic actions of palmitate-derivatised native and Ala8-substituted GLP-1 analogues
    Brian D Green
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Biol Chem 385:169-77. 2004
    ..These studies support the potential usefulness of fatty acid linked analogues of GLP-1 but indicate the importance of chain length for peptide kinetics and bioavailability...
  16. ncbi GIP(Lys16PAL) and GIP(Lys37PAL): novel long-acting acylated analogues of glucose-dependent insulinotropic polypeptide with improved antidiabetic potential
    Nigel Irwin
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, U K
    J Med Chem 49:1047-54. 2006
    ..These data demonstrate that fatty acid derivatized GIP peptides represent a novel class of long-acting stable GIP analogues for therapy of type 2 diabetes...
  17. ncbi Degradation, insulin secretion, and antihyperglycemic actions of two palmitate-derivitized N-terminal pyroglutamyl analogues of glucose-dependent insulinotropic polypeptide
    Nigel Irwin
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, UK
    J Med Chem 48:1244-50. 2005
    ..These data indicate that palmitate-derivitized analogues of N-terminal pyroglutamyl GIP represent a novel class of stable, long-acting, and effective GIP analogues for potential type 2 diabetes therapy...
  18. ncbi GIP receptor antagonism reverses obesity, insulin resistance, and associated metabolic disturbances induced in mice by prolonged consumption of high-fat diet
    Paula L McClean
    School of Biomedical Sciences, Univ of Ulster, Coleraine, Northern Ireland, BT52 1SA, United Kingdom
    Am J Physiol Endocrinol Metab 293:E1746-55. 2007
    ..These data indicate that GIP receptor antagonism using (Pro(3))GIP provides an effective means of countering obesity and related diabetes induced by consumption of a high-fat, energy-rich diet...
  19. ncbi Metabolic effects of sub-chronic ablation of the incretin receptors by daily administration of (Pro3)GIP and exendin(9-39)amide in obese diabetic (ob/ob) mice
    Jeremy C Parker
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Biol Chem 388:221-6. 2007
    ..These studies highlight an important role for GIP in obesity-related forms of diabetes, suggesting the possible involvement of GLP-1 in the beneficial actions of GIP receptor antagonism...
  20. ncbi Comparison of the anti-diabetic effects of GIP- and GLP-1-receptor activation in obese diabetic (ob/ob) mice: studies with DPP IV resistant N-AcGIP and exendin(1-39)amide
    Nigel Irwin
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, UK
    Diabetes Metab Res Rev 23:572-9. 2007
    ....
  21. ncbi Biological activity and antidiabetic potential of synthetic fragment peptides of glucose-dependent insulinotropic polypeptide, GIP(1-16) and (Pro3)GIP(1-16)
    Nigel Irwin
    Diabetes Research Group, School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Regul Pept 135:45-53. 2006
    ..These data demonstrate that C-terminal truncation of GIP or (Pro3)GIP yields small molecular weight GIP molecules with significantly reduced biological activity that precludes therapeutic utility...
  22. ncbi Fatty acid derivatised analogues of glucose-dependent insulinotropic polypeptide with improved antihyperglycaemic and insulinotropic properties
    Barry D Kerr
    The SAAD Centre for Pharmacy and Diabetes, School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine BT52 1SA, Northern Ireland, UK
    Biochem Pharmacol 78:1008-16. 2009
    ..These data demonstrate that C-terminal acylation particularly with myristic acid provides a class of stable, longer-acting forms of GIP for further evaluation in diabetes therapy...
  23. ncbi A novel, long-acting agonist of glucose-dependent insulinotropic polypeptide suitable for once-daily administration in type 2 diabetes
    Nigel Irwin
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, UK
    J Pharmacol Exp Ther 314:1187-94. 2005
    ....
  24. ncbi Characterisation and biological activity of Glu3 amino acid substituted GIP receptor antagonists
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine BT52 1SA, Northern Ireland, UK
    Arch Biochem Biophys 461:263-74. 2007
    ..These data demonstrate that position 3 amino acid substitution of GIP with (Ala(3)), (Phe(3)), (Tyr(3)) or (Pro(3)) provides a new class of functional GIP receptor antagonists...
  25. ncbi Evaluation of the antidiabetic activity of DPP IV resistant N-terminally modified versus mid-chain acylated analogues of glucose-dependent insulinotropic polypeptide
    Nigel Irwin
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, UK
    Biochem Pharmacol 72:719-28. 2006
    ..These data demonstrate the therapeutic potential of once daily injection of enzyme resistant GIP analogues and indicate that N-AcGIP is equally as effective as related palmitate derivatised analogues of GIP...
  26. ncbi Soluble beta-amyloid[25-35] reversibly impairs hippocampal synaptic plasticity and spatial learning
    Christian Holscher
    School of Biomed Sci, Ulster University, Coleraine, UK
    Eur J Pharmacol 561:85-90. 2007
    ..These results suggest that treatment at very early stages of Alzheimer's disease could prevent later irreversible neuronal degeneration...
  27. ncbi Long-term administration of PACAP receptor antagonist, PACAP(6-27), impairs glucose tolerance and insulin sensitivity in obese diabetic ob/ob mice
    Brian D Green
    School of Biomedical Sciences, University of Ulster, Coleraine, BT52 1SA, Northern Ireland, United Kingdom
    Peptides 27:2343-9. 2006
    ..Plasma glucagon and lipids were unchanged. These observations indicate a role of endogenous PACAP for normal glucose homeostasis, but indicate a minor involvement in the regulation of insulin secretion in ob/ob mice...
  28. ncbi Degradation, cyclic adenosine monophosphate production, insulin secretion, and glycemic effects of two novel N-terminal Ala2-substituted analogs of glucose-dependent insulinotropic polypeptide with preserved biological activity in vivo
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine, N. Ireland, UK
    Metabolism 52:679-87. 2003
    ....
  29. ncbi Prolonged GIP receptor activation improves cognitive function, hippocampal synaptic plasticity and glucose homeostasis in high-fat fed mice
    David W Porter
    SAAD Centre for Pharmacy and Diabetes, University of Ulster, Cromore Road, Coleraine BT52 1SA, Northern Ireland, UK
    Eur J Pharmacol 650:688-93. 2011
    ....
  30. ncbi Effects of short-term chemical ablation of the GIP receptor on insulin secretion, islet morphology and glucose homeostasis in mice
    Nigel Irwin
    Diabetes Research Group, School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Biol Chem 385:845-52. 2004
    ..These data indicate that ablation of GIP signaling causes a readily reversible glucose intolerance without appreciable change of insulin secretion...
  31. ncbi Characterization of the cellular and metabolic effects of a novel enzyme-resistant antagonist of glucose-dependent insulinotropic polypeptide
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, BT52 1SA, United Kingdom
    Biochem Biophys Res Commun 290:1420-6. 2002
    ....
  32. ncbi Lys9 for Glu9 substitution in glucagon-like peptide-1(7-36)amide confers dipeptidylpeptidase IV resistance with cellular and metabolic actions similar to those of established antagonists glucagon-like peptide-1(9-36)amide and exendin (9-39)
    B D Green
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern, Ireland
    Metabolism 53:252-9. 2004
    ..We investigated the in vivo antagonistic actions of (Lys(9))GLP-1 in comparison with GLP-1(9-36)amide and exendin (9-39) and revealed that this novel analogue may serve as a functional antagonist of the GLP-1 receptor...
  33. ncbi Sub-chronic administration of the 11beta-HSD1 inhibitor, carbenoxolone, improves glucose tolerance and insulin sensitivity in mice with diet-induced obesity
    Ashley Taylor
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Biol Chem 389:441-5. 2008
    ....
  34. ncbi Effects of antidiabetic drugs on dipeptidyl peptidase IV activity: nateglinide is an inhibitor of DPP IV and augments the antidiabetic activity of glucagon-like peptide-1
    Nicola A Duffy
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, UK
    Eur J Pharmacol 568:278-86. 2007
    ..These data indicate that the use of nateglinide as a prandial insulin-releasing agent may partly rely on inhibition of GLP-1 degradation as well as beta-cell K(ATP) channel inhibition...
  35. ncbi Comparison of sub-chronic metabolic effects of stable forms of naturally occurring GIP(1-30) and GIP(1-42) in high-fat fed mice
    Victor A Gault
    School of Biomedical Sciences, SAAD Centre for Pharmacy and Diabetes, University of Ulster, Coleraine BT52 1SA, UK
    J Endocrinol 208:265-71. 2011
    ..However, no differences were discernable between the biological actions of the enzyme-resistant analogues of the naturally occurring forms, GIP(1-30) and GIP(1-42)...
  36. ncbi Stable agonist of glucose-dependent insulinotropic polypeptide (GIP) restores pancreatic beta cell glucose responsiveness but not glucose intolerance in aging mice
    Nigel Irwin
    Diabetes Research Group, School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Exp Gerontol 41:151-6. 2006
    ..Native GIP had a similar overall effect in younger and older mice. These data indicate that N-AcGIP(LysPAL37) is able to counter the age-related deterioration of pancreatic beta cell glucose sensitivity and insulin secretion...
  37. ncbi Effects on glucose homeostasis and insulin secretion of long term activation of the glucose-dependent insulinotropic polypeptide (GIP) receptor by N-AcGIP(LysPAL37) in normal mice
    Nigel Irwin
    Diabetes Research Group, School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Peptides 27:893-900. 2006
    ..These data indicate that long term activation of the GIP receptor by daily treatment with N-AcGIP(LysPAL37) improved glucose tolerance due to enhancement of pancreatic beta cell glucose responsiveness and insulin secretion...
  38. ncbi Enhanced cAMP generation and insulin-releasing potency of two novel Tyr1-modified enzyme-resistant forms of glucose-dependent insulinotropic polypeptide is associated with significant antihyperglycaemic activity in spontaneous obesity-diabetes
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine BT52 1SA, Northern Ireland, UK
    Biochem J 367:913-20. 2002
    ....
  39. ncbi Antidiabetic potential of two novel fatty acid derivatised, N-terminally modified analogues of glucose-dependent insulinotropic polypeptide (GIP): N-AcGIP(LysPAL16) and N-AcGIP(LysPAL37)
    Nigel Irwin
    School of Biomedical Sciences, University of Ulster, Coleraine, BT52 1SA, N Ireland, UK
    Biol Chem 386:679-87. 2005
    ..These data demonstrate that novel fatty acid-derivatised analogues of N-terminally modified AcGIP function as long-acting GIP-receptor agonists, with significant antidiabetic potential...
  40. ncbi Prolonged GIP receptor activation using stable mini-PEGylated GIP improves glucose homeostasis and beta-cell function in age-related glucose intolerance
    Barry D Kerr
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine, Northern Ireland BT52 1SA, UK
    Peptides 30:219-25. 2009
    ..These data indicate that prolonged activation of the GIP receptor with GIP[mPEG] counters aspects of impaired beta-cell function and age-related glucose intolerance...
  41. ncbi GLP-1 agonists facilitate hippocampal LTP and reverse the impairment of LTP induced by beta-amyloid
    Victor A Gault
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine, BT52 1SA, Northern Ireland, United Kingdom
    Eur J Pharmacol 587:112-7. 2008
    ..Therefore, longer-acting GLP-1 agonists show great potential as a novel treatment for preventing neurodegenerative processes in neurodegenerative disorders...
  42. ncbi Effects of sub-chronic exposure to naturally occurring N-terminally truncated metabolites of glucose-dependent insulinotrophic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1), GIP(3-42) and GLP-1(9-36)amide, on insulin secretion and glucose homeosta
    J C Parker
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine BT52 1SA, Northern Ireland, UK
    J Endocrinol 191:93-100. 2006
    ..GIP(3-42) might exert an overall beneficial effect by improving insulin sensitivity through extrapancreatic action...
  43. ncbi Improved stability, insulin-releasing activity and antidiabetic potential of two novel N-terminal analogues of gastric inhibitory polypeptide: N-acetyl-GIP and pGlu-GIP
    F P M O'Harte
    School of Biomedical Sciences, University of Ulster, Coleraine, N Ireland, UK
    Diabetologia 45:1281-91. 2002
    ..This study examined the plasma stability, biological activity and antidiabetic potential of two novel N-terminally modified analogues of gastric inhibitory polypeptide (GIP)...
  44. ncbi Structurally modified analogues of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) as future antidiabetic agents
    Brian D Green
    School of Biomedical Sciences, University of Ulster, Coleraine, BT52 1SA, Northern Ireland, UK
    Curr Pharm Des 10:3651-62. 2004
    ..This approach is currently being pursued actively by the pharmaceutical industry...
  45. ncbi Protease-resistant glucose-dependent insulinotropic polypeptide agonists facilitate hippocampal LTP and reverse the impairment of LTP induced by beta-amyloid
    Victor A Gault
    School of Biomedical Schiences, University of Ulster, Coleraine, Northern Ireland
    J Neurophysiol 99:1590-5. 2008
    ..The use of enzyme-resistant analogues of GIP show great promise as a potential novel treatment for preventing neurodegenerative processes in AD and other related disorders...
  46. ncbi Glucagon-like peptide-1 analogues enhance synaptic plasticity in the brain: a link between diabetes and Alzheimer's disease
    Paula L McClean
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine BT52 1SA, Northern Ireland, UK
    Eur J Pharmacol 630:158-62. 2010
    ..Therefore, the drug effects seen here could potentially ameliorate the impairments in neuronal communication and cognitive processes observed in Alzheimer's disease...
  47. ncbi Effects of the novel (Pro3)GIP antagonist and exendin(9-39)amide on GIP- and GLP-1-induced cyclic AMP generation, insulin secretion and postprandial insulin release in obese diabetic (ob/ob) mice: evidence that GIP is the major physiological incretin
    V A Gault
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine, BT52 1SA Northern Ireland, United Kingdom
    Diabetologia 46:222-30. 2003
    ....
  48. ncbi Effect of RU486 on hepatic and adipocyte gene expression improves diabetes control in obesity-type 2 diabetes
    A I Taylor
    The SAAD Centre for Pharmacy and Diabetes, School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Horm Metab Res 41:899-904. 2009
    ..001). These data demonstrate wide-ranging effects of glucocorticoid receptor antagonism on gene expression and metabolism, illustrating the therapeutic potential of specific glucocorticoid receptor antagonists in obesity-related diabetes...
  49. ncbi Val(8)GLP-1 rescues synaptic plasticity and reduces dense core plaques in APP/PS1 mice
    Simon Gengler
    School of Biomedical Sciences, Ulster University, Coleraine, UK
    Neurobiol Aging 33:265-76. 2012
    ..In 18-month-old mice, however, the number of Congo red positive dense-core amyloid plaques was reduced. Treatment with Val(8)GLP-1 might prevent or delay neurodegenerative processes...
  50. ncbi (D-Ser2)Oxm[mPEG-PAL]: a novel chemically modified analogue of oxyntomodulin with antihyperglycaemic, insulinotropic and anorexigenic actions
    Barry D Kerr
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, United Kingdom
    Biochem Pharmacol 80:1727-35. 2010
    ..The ability of enzyme-resistant (d-Ser(2))Oxm[mPEG-PAL] to improve glucose homeostasis, insulin secretion, satiety, bodyweight and markers of fat metabolism suggests significant promise for Oxm-based therapies for obesity-diabetes...
  51. ncbi N-acetyl-GLP-1: a DPP IV-resistant analogue of glucagon-like peptide-1 (GLP-1) with improved effects on pancreatic beta-cell-associated gene expression
    Hui-Kang Liu
    School of Biomedical Sciences, University of Ulster, Coleraine, BT52 1SA, Northern Ireland, UK
    Cell Biol Int 28:69-73. 2004
    ..Further investigation of the effects of stable GLP-1 analogues on beta-cell differentiation is required to assess their potential in diabetic therapy...
  52. ncbi (Pro(3))GIP[mPEG]: novel, long-acting, mPEGylated antagonist of gastric inhibitory polypeptide for obesity-diabetes (diabesity) therapy
    P L McClean
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, UK
    Br J Pharmacol 155:690-701. 2008
    ..This study has examined the ability of a novel and longer-acting form of (Pro(3))GIP, (Pro(3))GIP mini-polyethylene glycol ((Pro(3))GIP[mPEG]), to counter diet-induced diabesity in mice, using a daily and intermittent dosing regime...
  53. ncbi Chemical gastric inhibitory polypeptide receptor antagonism protects against obesity, insulin resistance, glucose intolerance and associated disturbances in mice fed high-fat and cafeteria diets
    V A Gault
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine, Northern Ireland, UK
    Diabetologia 50:1752-62. 2007
    ..This study examined the ability of (Pro(3))GIP to counter the development of obesity, insulin resistance and diabetes in mice fed high-fat and cafeteria diets...
  54. ncbi Characterization and biological actions of N-terminal truncated forms of glucose-dependent insulinotropic polypeptide
    Barry D Kerr
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, UK
    Biochem Biophys Res Commun 404:870-6. 2011
    ..These data confirm the importance of the N-terminal region of GIP in regulating bioactivity and reveal that sequential truncation of the peptide yields novel GIP receptor antagonists which may have functional significance...
  55. ncbi Evaluation of the degradation and metabolic effects of the gut peptide xenin on insulin secretion, glycaemic control and satiety
    Ashley I Taylor
    SAAD Centre for Pharmacy and Diabetes, School of Biomedical Sciences Research Institute, University of Ulster, Coleraine, UK
    J Endocrinol 207:87-93. 2010
    ..Overall, these data demonstrate that xenin may have significant metabolic effects on glucose control, which merit further study...
  56. ncbi Glucose-dependent insulinotropic polypeptide receptor knockout mice are impaired in learning, synaptic plasticity, and neurogenesis
    Emilie Faivre
    School of Biomedical Sciences, Ulster University, Coleraine, United Kingdom
    J Neurophysiol 105:1574-80. 2011
    ..Together the results suggest that GIP receptors play an important role in cognition, neurotransmission, and cell proliferation...
  57. ncbi Effects of gamma-glutamyl linker on DPP-IV resistance, duration of action and biological efficacy of acylated glucagon-like peptide-1
    Barry D Kerr
    The SAAD Centre for Pharmacy and Diabetes, School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine BT52 1SA, Northern Ireland, UK
    Biochem Pharmacol 80:396-401. 2010
    ..4-fold; p<0.05). Functional characteristics of Lira-gammaGlu and Liraglutide are almost indistinguishable, questioning necessity of gamma-glutamyl linker in acylation for generation of long-acting incretin mimetics...
  58. ncbi Daily administration of the GIP-R antagonist (Pro3)GIP in streptozotocin-induced diabetes suggests that insulin-dependent mechanisms are critical to anti-obesity-diabetes actions of (Pro3)GIP
    P L McClean
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, UK
    Diabetes Obes Metab 10:336-42. 2008
    ..The effect of GIP-R antagonism in a streptozotocin (STZ)-induced model of insulin deficiency has not been evaluated. The present study has investigated the effects of daily administration of (Pro(3))GIP to STZ-treated mice...
  59. ncbi Impairments of hippocampal synaptic plasticity induced by aggregated beta-amyloid (25-35) are dependent on stimulation-protocol and genetic background
    Simon Gengler
    School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine, BT52 1SA, Northern Ireland
    Exp Brain Res 179:621-30. 2007
    ....
  60. ncbi N-terminal His(7)-modification of glucagon-like peptide-1(7-36) amide generates dipeptidyl peptidase IV-stable analogues with potent antihyperglycaemic activity
    B D Green
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, N Ireland, UK
    J Endocrinol 180:379-88. 2004
    ..The particularly powerful antihyperglycaemic action of N-pyroglutamyl-GLP-1 shows potential for the treatment of type 2 diabetes...
  61. ncbi Comparative effects of GLP-1 and GIP on cAMP production, insulin secretion, and in vivo antidiabetic actions following substitution of Ala8/Ala2 with 2-aminobutyric acid
    B D Green
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Arch Biochem Biophys 428:136-43. 2004
    ....
  62. ncbi Chronic treatment with exendin(9-39)amide indicates a minor role for endogenous glucagon-like peptide-1 in metabolic abnormalities of obesity-related diabetes in ob/ob mice
    B D Green
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, United Kingdom
    J Endocrinol 185:307-17. 2005
    ....
  63. ncbi A comparison of the cellular and biological properties of DPP-IV-resistant N-glucitol analogues of glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide
    B D Green
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, UK
    Diabetes Obes Metab 7:595-604. 2005
    ..This study directly compares the cellular and biological properties of GLP-1, GIP and their N-terminally modified counterparts, with glucitol extension at positions His7 and Tyr1 respectively, to confer DPP-IV resistance...
  64. ncbi Early administration of the glucose-dependent insulinotropic polypeptide receptor antagonist (Pro3)GIP prevents the development of diabetes and related metabolic abnormalities associated with genetically inherited obesity in ob/ob mice
    N Irwin
    School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, BT52 1SA, UK
    Diabetologia 50:1532-40. 2007
    ..The aim of this study was to use prediabetic ob/ob mice to examine whether 60 days of chemical GIP receptor ablation with (Pro(3))GIP is able to counter the development of genetic obesity-related diabetes...
  65. ncbi 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
    B D Green
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    J Mol Endocrinol 31:529-40. 2003
    ..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...
  66. ncbi Actions of incretin metabolites on locomotor activity, cognitive function and in vivo hippocampal synaptic plasticity in high fat fed mice
    David Porter
    The SAAD Centre for Pharmacy and Diabetes, School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, United Kingdom
    Peptides 35:1-8. 2012
    ..These data indicate that incretin metabolites do not influence locomotor activity, cognitive function and hippocampal synaptic plasticity when administered at pharmacological doses to mice fed a high-fat diet...
  67. ncbi Mass spectrometric characterisation and quantitation of selected low molecular mass compounds from the venom of Haplopelma lividum (Theraphosidae)
    Sara Moore
    The SAAD Centre for Pharmacy and Diabetes, Biomedical Sciences Research Institute, University of Ulster, Coleraine BT52 1SA, UK
    Rapid Commun Mass Spectrom 23:1747-55. 2009
    ..002%. The limits of detection and quantification were established for each of the identified components. The fragmentation profile for histamine has also been proposed...
  68. ncbi NMR structure of the glucose-dependent insulinotropic polypeptide fragment, GIP(1-30)amide
    Iñigo Alaña
    Department of Biochemistry, Centre for Synthesis and Chemical Biology, Conway Institute of Biomolecular and Biomedical Research, University College Dublin, Belfield, Dublin 4, Ireland
    Biochem Biophys Res Commun 325:281-6. 2004
    ..The structure is characterised by a full length alpha-helical conformation between residues F(6) and A(28). This structural information could play an important role in the design of therapeutic agents based upon GIP receptor agonists...
  69. ncbi Inhibition of dipeptidyl peptidase-IV activity by metformin enhances the antidiabetic effects of glucagon-like peptide-1
    Brian D Green
    School of Biological Sciences, Queens University Belfast, David Keir Building, Stranmillis Road, Belfast BT9 5AG, Northern Ireland
    Eur J Pharmacol 547:192-9. 2006
    ..These findings indicate that metformin decreases the plasma DPP IV activity, limiting the inactivation of exogenously administered GLP-1 and improving glycaemic control...