2hha
From Proteopedia
(New page: 200px<br /> <applet load="2hha" size="450" color="white" frame="true" align="right" spinBox="true" caption="2hha, resolution 2.350Å" /> '''The structure of D...) |
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| - | [[Image:2hha.gif|left|200px]]<br /> | + | [[Image:2hha.gif|left|200px]]<br /><applet load="2hha" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2hha" size=" | + | |
caption="2hha, resolution 2.350Å" /> | caption="2hha, resolution 2.350Å" /> | ||
'''The structure of DPP4 in complex with an oxadiazole inhibitor'''<br /> | '''The structure of DPP4 in complex with an oxadiazole inhibitor'''<br /> | ||
==Overview== | ==Overview== | ||
| - | A novel series of oxadiazole based amides have been shown to be potent | + | A novel series of oxadiazole based amides have been shown to be potent DPP-4 inhibitors. The optimized compound 43 exhibited excellent selectivity over a variety of DPP-4 homologs. |
==About this Structure== | ==About this Structure== | ||
| - | 2HHA is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with NAG, NA and 3TP as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Dipeptidyl-peptidase_IV Dipeptidyl-peptidase IV], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.14.5 3.4.14.5] Full crystallographic information is available from [http:// | + | 2HHA is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=NAG:'>NAG</scene>, <scene name='pdbligand=NA:'>NA</scene> and <scene name='pdbligand=3TP:'>3TP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Dipeptidyl-peptidase_IV Dipeptidyl-peptidase IV], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.14.5 3.4.14.5] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2HHA OCA]. |
==Reference== | ==Reference== | ||
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[[Category: hydrolase]] | [[Category: hydrolase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:41:52 2008'' |
Revision as of 15:41, 21 February 2008
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The structure of DPP4 in complex with an oxadiazole inhibitor
Overview
A novel series of oxadiazole based amides have been shown to be potent DPP-4 inhibitors. The optimized compound 43 exhibited excellent selectivity over a variety of DPP-4 homologs.
About this Structure
2HHA is a Single protein structure of sequence from Homo sapiens with , and as ligands. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 Full crystallographic information is available from OCA.
Reference
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors., Xu J, Wei L, Mathvink RJ, Edmondson SD, Eiermann GJ, He H, Leone JF, Leiting B, Lyons KA, Marsilio F, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE, Bioorg Med Chem Lett. 2006 Oct 15;16(20):5373-7. Epub 2006 Aug 17. PMID:16919457
Page seeded by OCA on Thu Feb 21 17:41:52 2008
Categories: Dipeptidyl-peptidase IV | Homo sapiens | Single protein | Scapin, G. | 3TP | NA | NAG | Alpha/beta | Beta-propeller | Dimer | Hydrolase
