Aiying Wang, Charles Dorso, Lisa Kopcho, Gregory Locke, Robert Langish, Eric Harstad, Petia Shipkova, Jovita Marcinkeviciene, Lawrence Hamann, Mark S Kirby
BACKGROUND: Dipeptidylpeptidase 4 (DPP4) inhibitors have clinical benefit in patients with type 2 diabetes mellitus by increasing levels of glucose-lowering incretin hormones, such as glucagon-like peptide -1 (GLP-1), a peptide with a short half life that is secreted for approximately 1 hour following a meal. Since drugs with prolonged binding to their target have been shown to maximize pharmacodynamic effects while minimizing drug levels, we developed a time-dependent inhibitor that has a half-life for dissociation from DPP4 close to the duration of the first phase of GLP-1 release...
April 4, 2012: BMC Pharmacology