1zxc: Difference between revisions
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New page: left|200px<br /> <applet load="1zxc" size="450" color="white" frame="true" align="right" spinBox="true" caption="1zxc, resolution 2.28Å" /> '''Crystal structure o... |
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[[Image:1zxc.gif|left|200px]]<br /> | [[Image:1zxc.gif|left|200px]]<br /><applet load="1zxc" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="1zxc" size=" | |||
caption="1zxc, resolution 2.28Å" /> | caption="1zxc, resolution 2.28Å" /> | ||
'''Crystal structure of catalytic domain of TNF-alpha converting enzyme (TACE) with inhibitor'''<br /> | '''Crystal structure of catalytic domain of TNF-alpha converting enzyme (TACE) with inhibitor'''<br /> | ||
==Overview== | ==Overview== | ||
The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors | The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing a butynyloxy P1' group was explored. In particular, compound 5k has excellent in vitro potency against TACE enzyme and in cells, and oral activity in an in vivo model of TNF-alpha production and a collagen-induced arthritis model. | ||
==About this Structure== | ==About this Structure== | ||
1ZXC 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 ZN and IH6 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/ADAM_17_endopeptidase ADAM 17 endopeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.86 3.4.24.86] Full crystallographic information is available from [http:// | 1ZXC 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=ZN:'>ZN</scene> and <scene name='pdbligand=IH6:'>IH6</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/ADAM_17_endopeptidase ADAM 17 endopeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.86 3.4.24.86] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1ZXC OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Barone, D.]] | [[Category: Barone, D.]] | ||
[[Category: Chen, J | [[Category: Chen, J M.]] | ||
[[Category: Cowling, R.]] | [[Category: Cowling, R.]] | ||
[[Category: Cummons, T.]] | [[Category: Cummons, T.]] | ||
[[Category: Du, M.]] | [[Category: Du, M.]] | ||
[[Category: Jin, G.]] | [[Category: Jin, G.]] | ||
[[Category: Laakso, L | [[Category: Laakso, L M.]] | ||
[[Category: Levin, J | [[Category: Levin, J I.]] | ||
[[Category: Schmid, J.]] | [[Category: Schmid, J.]] | ||
[[Category: Skotnicki, J | [[Category: Skotnicki, J S.]] | ||
[[Category: Xu, J.]] | [[Category: Xu, J.]] | ||
[[Category: Xu, W.]] | [[Category: Xu, W.]] | ||
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[[Category: zn-endopeptidase]] | [[Category: zn-endopeptidase]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:20:00 2008'' | ||
