3g0c
Crystal structure of dipeptidyl peptidase IV in complex with a pyrimidinedione inhibitor 1Crystal structure of dipeptidyl peptidase IV in complex with a pyrimidinedione inhibitor 1
Structural highlights
Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMedThe discovery of two classes of heterocyclic dipeptidyl peptidase IV (DPP-4) inhibitors, pyrimidinones and pyrimidinediones, is described. After a single oral dose, these potent, selective, and noncovalent inhibitors provide sustained reduction of plasma DPP-4 activity and lowering of blood glucose in animal models of diabetes. Compounds 13a, 27b, and 27j were selected for development. Design and Synthesis of Pyrimidinone and Pyrimidinedione Inhibitors of Dipeptidyl Peptidase IV.,Zhang Z, Wallace MB, Feng J, Stafford JA, Skene RJ, Shi L, Lee B, Aertgeerts K, Jennings A, Xu R, Kassel DB, Kaldor SW, Navre M, Webb DR, Gwaltney SL J Med Chem. 2010 Dec 27. PMID:21186796[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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OCA- Dipeptidyl-peptidase IV
- Homo sapiens
- Aertgeerts, K.
- Feng, J.
- Gwaltney, S L.
- Jennings, A.
- Kaldor, S W.
- Kassel, D.
- Lee, B.
- Shi, L.
- Skene, R J.
- Stafford, J A.
- Wallace, M B.
- Webb, D R.
- Xu, R.
- Zhang, Z.
- Aminopeptidase
- Cell membrane
- Dpp4
- Glycoprotein
- Hydrolase
- Hydrolase-hydrolase inhibitor complex
- Membrane
- Protease
- Pyrimidindione
- Pyrimidinone
- Secreted
- Serine protease
- Signal-anchor
- Transmembrane