2ONC

Crystal structure of human DPP-4

Summary for 2ONC

• Entry DOI: 10.2210/pdb2onc/pdb
• Descriptor: Dipeptidyl peptidase 4, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... (5 entities in total)
• Functional Keywords: dpp4 protein-inhibitor complex, hydrolase
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 4
• Total formula weight: 346989.81

Authors

Feng, J.,Zhang, Z.,Wallace, M.B.,Stafford, J.A.,Kaldor, S.W.,Kassel, D.B.,Navre, M.,Shi, L.,Skene, R.J.,Asakawa, T.,Takeuchi, K.,Xu, R.,Webb, D.R.,Gwaltney, S.L. (deposition date: 2007-01-23, release date: 2008-03-04, Last modification date: 2023-12-27)

Primary citation

Feng, J.,Zhang, Z.,Wallace, M.B.,Stafford, J.A.,Kaldor, S.W.,Kassel, D.B.,Navre, M.,Shi, L.,Skene, R.J.,Asakawa, T.,Takeuchi, K.,Xu, R.,Webb, D.R.,Gwaltney, S.L.
Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.
J.Med.Chem., 50:2297-2300, 2007

PubMed 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.

PubMed: 17441705
DOI: 10.1021/jm070104l

Experimental method

X-RAY DIFFRACTION (2.55 Å)