1wxz
From Proteopedia
(New page: 200px<br /><applet load="1wxz" size="450" color="white" frame="true" align="right" spinBox="true" caption="1wxz, resolution 2.80Å" /> '''Crystal structure of...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:1wxz.gif|left|200px]]<br /><applet load="1wxz" size=" | + | [[Image:1wxz.gif|left|200px]]<br /><applet load="1wxz" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1wxz, resolution 2.80Å" /> | caption="1wxz, resolution 2.80Å" /> | ||
'''Crystal structure of adenosine deaminase ligated with a potent inhibitor'''<br /> | '''Crystal structure of adenosine deaminase ligated with a potent inhibitor'''<br /> | ||
==Overview== | ==Overview== | ||
| - | From metabolic considerations and prediction of an inhibitor-induced | + | From metabolic considerations and prediction of an inhibitor-induced conformational change, novel adenosine deaminase (ADA) inhibitors with improved activities and oral bioavailability have been developed on the basis of our originally designed non-nucleoside ADA inhibitors. They demonstrated in vivo efficacy in models of inflammation and lymphoma. Furthermore, X-ray crystal structure analysis has revealed a novel induced fit to ADA. |
==About this Structure== | ==About this Structure== | ||
| - | 1WXZ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] with ZN and FRL as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Adenosine_deaminase Adenosine deaminase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.5.4.4 3.5.4.4] Full crystallographic information is available from [http:// | + | 1WXZ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] with <scene name='pdbligand=ZN:'>ZN</scene> and <scene name='pdbligand=FRL:'>FRL</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Adenosine_deaminase Adenosine deaminase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.5.4.4 3.5.4.4] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1WXZ OCA]. |
==Reference== | ==Reference== | ||
| Line 19: | Line 19: | ||
[[Category: beta barel]] | [[Category: beta barel]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:49:17 2008'' |
Revision as of 13:49, 21 February 2008
|
Crystal structure of adenosine deaminase ligated with a potent inhibitor
Overview
From metabolic considerations and prediction of an inhibitor-induced conformational change, novel adenosine deaminase (ADA) inhibitors with improved activities and oral bioavailability have been developed on the basis of our originally designed non-nucleoside ADA inhibitors. They demonstrated in vivo efficacy in models of inflammation and lymphoma. Furthermore, X-ray crystal structure analysis has revealed a novel induced fit to ADA.
About this Structure
1WXZ is a Single protein structure of sequence from Bos taurus with and as ligands. Active as Adenosine deaminase, with EC number 3.5.4.4 Full crystallographic information is available from OCA.
Reference
Rational design of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors: predicting enzyme conformational change and metabolism., Terasaka T, Tsuji K, Kato T, Nakanishi I, Kinoshita T, Kato Y, Kuno M, Inoue T, Tanaka K, Nakamura K, J Med Chem. 2005 Jul 28;48(15):4750-3. PMID:16033254
Page seeded by OCA on Thu Feb 21 15:49:17 2008
