1d8m: Difference between revisions
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New page: left|200px<br /> <applet load="1d8m" size="450" color="white" frame="true" align="right" spinBox="true" caption="1d8m, resolution 2.44Å" /> '''CRYSTAL STRUCTURE O... |
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[[Image:1d8m.gif|left|200px]]<br /> | [[Image:1d8m.gif|left|200px]]<br /><applet load="1d8m" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="1d8m" size=" | |||
caption="1d8m, resolution 2.44Å" /> | caption="1d8m, resolution 2.44Å" /> | ||
'''CRYSTAL STRUCTURE OF MMP3 COMPLEXED WITH A HETEROCYCLE-BASED INHIBITOR'''<br /> | '''CRYSTAL STRUCTURE OF MMP3 COMPLEXED WITH A HETEROCYCLE-BASED INHIBITOR'''<br /> | ||
==Overview== | ==Overview== | ||
Potent and selective inhibition of matrix metalloproteinases was | Potent and selective inhibition of matrix metalloproteinases was demonstrated for a series of sulfonamide-based hydroxamic acids. The design of the heterocyclic sulfonamides incorporates a six- or seven-member central ring with a P2' substituent that can be modified. Binding interactions of this substituent at the S2' site are believed to contribute to high inhibitory potency against stromelysin, collagenase-3 and gelatinases A and B, and to provide selectivity against collagenase-1 and matrilysin. An X-ray structure of a stromelysin inhibitor complex was obtained to provide insights into the SAR and selectivity trends observed for the series. | ||
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
1D8M 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, CA and BBH as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Stromelysin_1 Stromelysin 1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.17 3.4.24.17] Full crystallographic information is available from [http:// | 1D8M 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>, <scene name='pdbligand=CA:'>CA</scene> and <scene name='pdbligand=BBH:'>BBH</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Stromelysin_1 Stromelysin 1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.17 3.4.24.17] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1D8M OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Stromelysin 1]] | [[Category: Stromelysin 1]] | ||
[[Category: Almstead, N | [[Category: Almstead, N G.]] | ||
[[Category: De, B.]] | [[Category: De, B.]] | ||
[[Category: Dunham, K | [[Category: Dunham, K M.]] | ||
[[Category: Gu, F.]] | [[Category: Gu, F.]] | ||
[[Category: Hsieh, L | [[Category: Hsieh, L C.]] | ||
[[Category: Hynd, B | [[Category: Hynd, B A.]] | ||
[[Category: Janusz, M | [[Category: Janusz, M J.]] | ||
[[Category: Mieling, G | [[Category: Mieling, G E.]] | ||
[[Category: Natchus, M | [[Category: Natchus, M G.]] | ||
[[Category: Pikul, S.]] | [[Category: Pikul, S.]] | ||
[[Category: Taiwo, Y | [[Category: Taiwo, Y O.]] | ||
[[Category: Williams, L | [[Category: Williams, L E.]] | ||
[[Category: BBH]] | [[Category: BBH]] | ||
[[Category: CA]] | [[Category: CA]] | ||
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[[Category: zinc protease]] | [[Category: zinc protease]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:14:08 2008'' | ||
