2005
DOI: 10.1124/jpet.105.086082
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A Novel, Long-Acting Agonist of Glucose-Dependent Insulinotropic Polypeptide Suitable for Once-Daily Administration in Type 2 Diabetes

Abstract: Glucose-dependent insulinotropic polypeptide (GIP) is a gastrointestinal hormone with a potentially therapeutic role in type 2 diabetes. Rapid degradation by dipeptidylpeptidase IV has prompted the development of enzyme-resistant N-terminally modified analogs, but renal clearance still limits in vivo bioactivity. In this study, we report long-term antidiabetic effects of a novel, N-terminally protected, fatty acid-derivatized analog of GIP, N-AcGIP(LysPAL 37 ), in obese diabetic (ob/ob) mice. Oncedaily injecti… Show more

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Cited by 55 publications
(41 citation statements)
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“…However, circulating GIP is rapidly hydrolysed by the ubiquitous enzyme DPP-IV and efficiently cleared from the body through renal filtration [11]. The potential of C-16 fatty acid (PAL) conjugated GIP analogues has been explored recently with N-AcGIP(Lys 37 PAL) appearing to be the most promising analogue [15,16]. The present study examined further the effect of fatty acid chain length, with or without N-terminal acetylation, on biological efficacy through assessing in vitro and in vivo antihyperglycaemic and insulinotropic properties.…”
Section: Discussionmentioning
confidence: 99%
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“…However, circulating GIP is rapidly hydrolysed by the ubiquitous enzyme DPP-IV and efficiently cleared from the body through renal filtration [11]. The potential of C-16 fatty acid (PAL) conjugated GIP analogues has been explored recently with N-AcGIP(Lys 37 PAL) appearing to be the most promising analogue [15,16]. The present study examined further the effect of fatty acid chain length, with or without N-terminal acetylation, on biological efficacy through assessing in vitro and in vivo antihyperglycaemic and insulinotropic properties.…”
Section: Discussionmentioning
confidence: 99%
“…To date, only the biological efficacy of C-16 fatty acid derivatised GIP analogues have been reported [14][15][16][17][18]. Therefore, in the present study we characterised the effects of a range of fatty acid chain lengths (C-14, C-16 and C-18) with or without N-terminal acetylation on metabolic 51 stability and biological actions.…”
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confidence: 97%
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