Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors.

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Lam B, Zhang Z, Stafford JA, Skene RJ, Shi L, Gwaltney SL 2nd

Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors.

Bioorg Med Chem Lett. 2012 Nov 1;22(21):6628-31. doi: 10.1016/j.bmcl.2012.08.110. Epub 2012 Sep 7.

PubMed ID

23025999 [ View in PubMed

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Abstract

Dipeptidyl peptidase IV (DPP-4) inhibitors have been shown to enhance GLP-1 levels and thereby improve hyperglycemia in type II diabetes. From a small fragment hit, using structure-based design, we have discovered a new class of non-covalent, potent and selective DPP-4 inhibitors.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
1-biphenyl-2-ylmethanamine	Dipeptidyl peptidase 4	IC 50 (nM)	30000	N/A	N/A	Details