2i3z: Difference between revisions
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New page: left|200px<br /><applet load="2i3z" size="450" color="white" frame="true" align="right" spinBox="true" caption="2i3z, resolution 2.900Å" /> '''rat DPP-IV with xan... |
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[[Image:2i3z.jpg|left|200px]]<br /><applet load="2i3z" size=" | [[Image:2i3z.jpg|left|200px]]<br /><applet load="2i3z" size="350" color="white" frame="true" align="right" spinBox="true" | ||
caption="2i3z, resolution 2.900Å" /> | caption="2i3z, resolution 2.900Å" /> | ||
'''rat DPP-IV with xanthine mimetic inhibitor #7'''<br /> | '''rat DPP-IV with xanthine mimetic inhibitor #7'''<br /> | ||
==Overview== | ==Overview== | ||
A series of xanthine mimetics containing 5,5 and 5,6 heterocycle fused | 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== | ==About this Structure== | ||
2I3Z is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with LIR as [http://en.wikipedia.org/wiki/ligand ligand]. 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:// | 2I3Z is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with <scene name='pdbligand=LIR:'>LIR</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. 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=2I3Z OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Rattus norvegicus]] | [[Category: Rattus norvegicus]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Ballaron, S | [[Category: Ballaron, S J.]] | ||
[[Category: Basha, F.]] | [[Category: Basha, F.]] | ||
[[Category: Kurukulasuriya, R.]] | [[Category: Kurukulasuriya, R.]] | ||
[[Category: Lai, C.]] | [[Category: Lai, C.]] | ||
[[Category: Longenecker, K | [[Category: Longenecker, K L.]] | ||
[[Category: Lubben, T | [[Category: Lubben, T W.]] | ||
[[Category: Rohde, J | [[Category: Rohde, J J.]] | ||
[[Category: Sham, H | [[Category: Sham, H L.]] | ||
[[Category: Stewart, K | [[Category: Stewart, K D.]] | ||
[[Category: Szczepankiewicz, B | [[Category: Szczepankiewicz, B G]] | ||
[[Category: VonGeldern, T | [[Category: VonGeldern, T W.]] | ||
[[Category: Winn, M.]] | [[Category: Winn, M.]] | ||
[[Category: LIR]] | [[Category: LIR]] | ||
| Line 31: | Line 31: | ||
[[Category: peptidase]] | [[Category: peptidase]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:48:50 2008'' | ||
