2i3z
From Proteopedia
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|SITE= | |SITE= | ||
|LIGAND= <scene name='pdbligand=LIR:2-[(3S)-3-AMINOPIPERIDIN-1-YL]-1-(2-CYANOBENZYL)-5-METHYL-4,6-DIOXO-3,4,5,6-TETRAHYDROPYRROLO[3,4-D]IMIDAZOL-1-IUM'>LIR</scene> | |LIGAND= <scene name='pdbligand=LIR:2-[(3S)-3-AMINOPIPERIDIN-1-YL]-1-(2-CYANOBENZYL)-5-METHYL-4,6-DIOXO-3,4,5,6-TETRAHYDROPYRROLO[3,4-D]IMIDAZOL-1-IUM'>LIR</scene> | ||
| - | |ACTIVITY= [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] | + | |ACTIVITY= <span class='plainlinks'>[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] </span> |
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[2gbi|2GBI]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2i3z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2i3z OCA], [http://www.ebi.ac.uk/pdbsum/2i3z PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2i3z RCSB]</span> | ||
}} | }} | ||
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[[Category: VonGeldern, T W.]] | [[Category: VonGeldern, T W.]] | ||
[[Category: Winn, M.]] | [[Category: Winn, M.]] | ||
| - | [[Category: LIR]] | ||
[[Category: enzyme]] | [[Category: enzyme]] | ||
[[Category: inhibitor]] | [[Category: inhibitor]] | ||
[[Category: peptidase]] | [[Category: peptidase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:39:21 2008'' |
Revision as of 00:39, 31 March 2008
| |||||||
| , resolution 2.900Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Activity: | Dipeptidyl-peptidase IV, with EC number 3.4.14.5 | ||||||
| Related: | 2GBI
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
rat DPP-IV with xanthine mimetic inhibitor #7
Overview
A series of xanthine mimetics containing 5,5 and 5,6 heterocycle fused imidazoles were synthesized as dipeptidyl peptidase IV inhibitors. Compound 7 is potent (h-DPPIV K(i)=2nM) and exhibits excellent selectivity and no species specificity against rat and human enzymes. The X-ray structure confirms that the binding mode of 7 to rat DPPIV is similar to the parent xanthines.
About this Structure
2I3Z is a Single protein structure of sequence from Rattus norvegicus. Full crystallographic information is available from OCA.
Reference
Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors., Kurukulasuriya R, Rohde JJ, Szczepankiewicz BG, Basha F, Lai C, Jae HS, Winn M, Stewart KD, Longenecker KL, Lubben TW, Ballaron SJ, Sham HL, von Geldern TW, Bioorg Med Chem Lett. 2006 Dec 15;16(24):6226-30. Epub 2006 Sep 28. PMID:17010607
Page seeded by OCA on Mon Mar 31 03:39:21 2008
