| Title : Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV - Feng_2007_J.Med.Chem_50_2297 |
| Author(s) : Feng J , Zhang Z , Wallace MB , Stafford JA , Kaldor SW , Kassel DB , Navre M , Shi L , Skene RJ , Asakawa T , Takeuchi K , Xu R , Webb DR , Gwaltney SL, 2nd |
| Ref : Journal of Medicinal Chemistry , 50 :2297 , 2007 |
|
Abstract :
Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4). Herein, we describe the structure-based design and optimization of alogliptin and related quinazolinone-based DPP-4 inhibitors. Following an oral dose, these noncovalent inhibitors provide sustained reduction of plasma DPP-4 activity and a lowering of blood glucose in animal models of diabetes. Alogliptin is currently undergoing phase III trials in patients with type 2 diabetes. |
| PubMedSearch : Feng_2007_J.Med.Chem_50_2297 |
| PubMedID: 17441705 |
| Gene_locus related to this paper: human-DPP4 |
| Inhibitor | Alogliptin |
| Gene_locus | human-DPP4 |
| Structure | 2ONC |
Feng J, Zhang Z, Wallace MB, Stafford JA, Kaldor SW, Kassel DB, Navre M, Shi L, Skene RJ, Asakawa T, Takeuchi K, Xu R, Webb DR, Gwaltney SL, 2nd (2007)
Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV
Journal of Medicinal Chemistry
50 :2297
Feng J, Zhang Z, Wallace MB, Stafford JA, Kaldor SW, Kassel DB, Navre M, Shi L, Skene RJ, Asakawa T, Takeuchi K, Xu R, Webb DR, Gwaltney SL, 2nd (2007)
Journal of Medicinal Chemistry
50 :2297