A comparative study of the binding properties, dipeptidyl peptidase‐4 (DPP‐4) inhibitory activity and glucose‐lowering efficacy of the DPP‐4 inhibitors alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin in mice
Endocrinology Diabetes & Metabolism2017Vol. 1(1), pp. e00002–e00002
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Joel P. Berger, Ranabir SinhaRoy, Alessandro Pocai, Theresa M. Kelly, Giovanna Scapin, Ying‐Duo Gao, Kelly Ann D. Pryor, Joseph K. Wu, George J. Eiermann, Shiyao Xu, Xiaoping Zhang, Daniel Tatosian, Ann E. Weber, Nancy A. Thornberry, Richard D. Carr
Abstract
The common binding site utilized by different DPP-4 inhibitors enables similar competitive inhibition of the cleavage of the endogenous DPP-4 substrates. Furthermore, despite chemical diversity and a range of binding potencies observed amongst the DPP-4 inhibitors, a direct relationship between enzyme inhibition in the plasma and glucose lowering is evident in mice for each member of the classes studied.
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