| Structural highlights
2ole is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: |
| | Gene: | chromosome 2 (Homo sapiens) |
| Activity: | Dipeptidyl-peptidase IV, with EC number 3.4.14.5 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
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 PubMed
Inhibitors of dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2 diabetes. A series of beta-aminoacyl-containing cyclic hydrazine derivatives were synthesized and evaluated as DPP-IV inhibitors. One member of this series, (R)-3-amino-1-(2-benzoyl-1,2-diazepan-1-yl)-4-(2,4,5-trifluorophenyl)butan -1-one (10f), showed potent in vitro activity, good selectivity and in vivo efficacy in mouse models. Also, the binding mode of compound 10f was determined by X-ray crystallography.
Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors.,Ahn JH, Shin MS, Jun MA, Jung SH, Kang SK, Kim KR, Rhee SD, Kang NS, Kim SY, Sohn SK, Kim SG, Jin MS, Lee JO, Cheon HG, Kim SS Bioorg Med Chem Lett. 2007 May 1;17(9):2622-8. Epub 2007 Feb 8. PMID:17331715[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Ahn JH, Shin MS, Jun MA, Jung SH, Kang SK, Kim KR, Rhee SD, Kang NS, Kim SY, Sohn SK, Kim SG, Jin MS, Lee JO, Cheon HG, Kim SS. Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors. Bioorg Med Chem Lett. 2007 May 1;17(9):2622-8. Epub 2007 Feb 8. PMID:17331715 doi:10.1016/j.bmcl.2007.01.111
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