1utz: Difference between revisions
New page: left|200px<br /> <applet load="1utz" size="450" color="white" frame="true" align="right" spinBox="true" caption="1utz, resolution 2.5Å" /> '''CRYSTAL STRUCTURE OF... |
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==About this Structure== | ==About this Structure== | ||
1UTZ 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, PF3 and HAE as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.65 3.4.24.65]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1UTZ OCA]]. | 1UTZ 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, PF3 and HAE as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/Macrophage_elastase Macrophage elastase]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.65 3.4.24.65]]. Structure known Active Site: ZN2. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1UTZ OCA]]. | ||
==Reference== | ==Reference== | ||
Crystal structures of novel non-peptidic, non-zinc chelating inhibitors bound to MMP-12., Morales R, Perrier S, Florent JM, Beltra J, Dufour S, De Mendez I, Manceau P, Tertre A, Moreau F, Compere D, Dublanchet AC, O'Gara M, J Mol Biol. 2004 Aug 20;341(4):1063-76. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15289103 15289103] | Crystal structures of novel non-peptidic, non-zinc chelating inhibitors bound to MMP-12., Morales R, Perrier S, Florent JM, Beltra J, Dufour S, De Mendez I, Manceau P, Tertre A, Moreau F, Compere D, Dublanchet AC, O'Gara M, J Mol Biol. 2004 Aug 20;341(4):1063-76. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15289103 15289103] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Macrophage elastase]] | |||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Beltra, J.]] | [[Category: Beltra, J.]] | ||
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[[Category: non-zinc chelator]] | [[Category: non-zinc chelator]] | ||
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 11:16:42 2007'' | ||
Revision as of 12:11, 30 October 2007
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CRYSTAL STRUCTURE OF MMP-12 COMPLEXED TO (2R)-3-({[4-[(PYRI DIN-4-YL)PHENYL]-THIEN-2-YL}CARBOXAMIDO)(PHENYL)PROPANOIC ACID
OverviewOverview
Human macrophage elastase (MMP-12) plays an important role in inflammatory, processes and has been implicated in diseases such as emphysema and, chronic obstructive pulmonary disease (COPD). It is therefore an, attractive target for therapeutic agents. As part of a structure-based, drug design programme to find new inhibitors of MMP-12, the crystal, structures of the MMP-12 catalytic domain (residues 106-268) complexed to, three different non-peptidic small molecule inhibitors have been, determined. The structures reveal that all three ligands bind in the S1', pocket but show varying degrees of interaction with the Zn atom. The, structures of the complexes with inhibitors CP-271485 and PF-00356231, reveal that their central morpholinone and thiophene rings, respectively, sit over the Zn ... [(full description)]
About this StructureAbout this Structure
1UTZ is a [Single protein] structure of sequence from [Homo sapiens] with ZN, CA, PF3 and HAE as [ligands]. Active as [Macrophage elastase], with EC number [3.4.24.65]. Structure known Active Site: ZN2. Full crystallographic information is available from [OCA].
ReferenceReference
Crystal structures of novel non-peptidic, non-zinc chelating inhibitors bound to MMP-12., Morales R, Perrier S, Florent JM, Beltra J, Dufour S, De Mendez I, Manceau P, Tertre A, Moreau F, Compere D, Dublanchet AC, O'Gara M, J Mol Biol. 2004 Aug 20;341(4):1063-76. PMID:15289103
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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- Homo sapiens
- Macrophage elastase
- Single protein
- Beltra, J.
- Compere, D.
- Dublanchet, A.C.
- Dufour, S.
- Florent, J.M.
- Gara, M.O.
- Manceau, P.
- Mendez, I.De.
- Morales, R.
- Moreau, F.
- Perrier, S.
- Tertre, A.
- CA
- HAE
- PF3
- ZN
- Hydrolase
- Macrophage metalloelastase
- Metalloprotease
- Mmp inhibitor
- Mmp-12
- Non-zinc chelator