2i3z: Difference between revisions
No edit summary |
No edit summary |
||
| Line 1: | Line 1: | ||
[[Image:2i3z.jpg|left|200px]] | [[Image:2i3z.jpg|left|200px]] | ||
'''rat DPP-IV with xanthine mimetic inhibitor #7''' | {{Structure | ||
|PDB= 2i3z |SIZE=350|CAPTION= <scene name='initialview01'>2i3z</scene>, resolution 2.900Å | |||
|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> | |||
|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] | |||
|GENE= | |||
}} | |||
'''rat DPP-IV with xanthine mimetic inhibitor #7''' | |||
==Overview== | ==Overview== | ||
| Line 7: | Line 16: | ||
==About this Structure== | ==About this Structure== | ||
2I3Z is a [ | 2I3Z is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2I3Z OCA]. | ||
==Reference== | ==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:[http:// | 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:[http://www.ncbi.nlm.nih.gov/pubmed/17010607 17010607] | ||
[[Category: Dipeptidyl-peptidase IV]] | [[Category: Dipeptidyl-peptidase IV]] | ||
[[Category: Rattus norvegicus]] | [[Category: Rattus norvegicus]] | ||
| Line 31: | Line 40: | ||
[[Category: peptidase]] | [[Category: peptidase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:25:08 2008'' | ||
Revision as of 15:25, 20 March 2008
| |||||||||||||
| 2i3z, resolution 2.900Å | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Ligands: | LIR | ||||||||||||
| Activity: | Dipeptidyl-peptidase IV, with EC number 3.4.14.5 | ||||||||||||
| 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 Thu Mar 20 17:25:08 2008
