1zxc
From Proteopedia
(New page: 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'' |
Revision as of 14:20, 21 February 2008
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Crystal structure of catalytic domain of TNF-alpha converting enzyme (TACE) with inhibitor
Overview
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
1ZXC is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as ADAM 17 endopeptidase, with EC number 3.4.24.86 Full crystallographic information is available from OCA.
Reference
Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates., Levin JI, Chen JM, Laakso LM, Du M, Du X, Venkatesan AM, Sandanayaka V, Zask A, Xu J, Xu W, Zhang Y, Skotnicki JS, Bioorg Med Chem Lett. 2005 Oct 1;15(19):4345-9. PMID:16084720
Page seeded by OCA on Thu Feb 21 16:20:00 2008
Categories: ADAM 17 endopeptidase | Homo sapiens | Single protein | Barone, D. | Chen, J M. | Cowling, R. | Cummons, T. | Du, M. | Jin, G. | Laakso, L M. | Levin, J I. | Schmid, J. | Skotnicki, J S. | Xu, J. | Xu, W. | Zhang, Y. | IH6 | ZN | Tace-inhibitor complex | Tace/adam-17 | Zn-endopeptidase
