2ole
From Proteopedia
(New page: 200px<br /><applet load="2ole" size="350" color="white" frame="true" align="right" spinBox="true" caption="2ole, resolution 2.4Å" /> '''Crystal Structure Of ...) |
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==Overview== | ==Overview== | ||
| - | Inhibitors of dipeptidyl peptidase IV (DPP-IV) have been shown to be | + | 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. |
==About this Structure== | ==About this Structure== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Ahn, J | + | [[Category: Ahn, J H.]] |
| - | [[Category: Kim, S | + | [[Category: Kim, S S.]] |
| - | [[Category: Lee, J | + | [[Category: Lee, J O.]] |
[[Category: KR2]] | [[Category: KR2]] | ||
[[Category: cyclic hydrazine]] | [[Category: cyclic hydrazine]] | ||
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[[Category: hydrolase]] | [[Category: hydrolase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:19:50 2008'' |
Revision as of 16:19, 21 February 2008
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Crystal Structure Of Human Dipeptidyl Peptidase IV (DPPIV) Complex With Cyclic Hydrazine Derivatives
Overview
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.
About this Structure
2OLE is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 Full crystallographic information is available from OCA.
Reference
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
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