Author/Authors :
Guohua Zhao، نويسنده , , Prakash C. Taunk، نويسنده , , David R. Magnin، نويسنده , , Ligaya M. Simpkins، نويسنده , , Jeffrey A. Robl، نويسنده , , Aiying Wang، نويسنده , , James G. Robertson، نويسنده , , Jovita Marcinkeviciene، نويسنده , , Doree F. Sitkoff، نويسنده , , Rex A. Parker، نويسنده , , Mark S. Kirby، نويسنده , , Lawrence G. Hamann، نويسنده ,
Abstract :
Dipeptidyl peptidase IV (DPP4) is a multifunctional type II transmembrane serine peptidase which regulates various physiological processes, most notably plasma glucose homeostasis by cleaving peptide hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide. Inhibition of DPP4 is a potentially valuable therapy for type 2 diabetes. Synthesis and structure–activity relationships of a series of substituted diprolyl nitriles are described, leading to the identification of compound 1 with a measured DPP4 Ki of 3.6 nM.
