3b92: Difference between revisions
New page: left|200px<br /><applet load="3b92" size="350" color="white" frame="true" align="right" spinBox="true" caption="3b92, resolution 2.00Å" /> '''Novel thio-based TAC... |
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==Overview== | ==Overview== | ||
A series of potent thiol-containing aryl sulfone TACE inhibitors were | A series of potent thiol-containing aryl sulfone TACE inhibitors were designed and synthesized. The SAR and MMP selectivity of the series were investigated. In particular, compound 8b showed excellent in vitro potency against the isolated enzyme and good selectivity over MMP-2, -7, -8, -9, and -13. The X-ray structure of 8b in complex with TACE was also obtained. | ||
==About this Structure== | ==About this Structure== | ||
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==Reference== | ==Reference== | ||
Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones., Bandarage UK, Wang T, Come JH, Perola E, Wei Y, Rao BG, Bioorg Med Chem Lett. 2007 Nov 13 | Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones., Bandarage UK, Wang T, Come JH, Perola E, Wei Y, Rao BG, Bioorg Med Chem Lett. 2008 Jan 1;18(1):44-8. Epub 2007 Nov 13. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=18054488 18054488] | ||
[[Category: ADAM 17 endopeptidase]] | [[Category: ADAM 17 endopeptidase]] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
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[[Category: zymogen]] | [[Category: zymogen]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 19:04:16 2008'' | ||
Revision as of 20:04, 21 February 2008
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Novel thio-based TACE inhibitors Part 2: Rational design, synthesis and SAR of thiol-contaning aryl sufones
OverviewOverview
A series of potent thiol-containing aryl sulfone TACE inhibitors were designed and synthesized. The SAR and MMP selectivity of the series were investigated. In particular, compound 8b showed excellent in vitro potency against the isolated enzyme and good selectivity over MMP-2, -7, -8, -9, and -13. The X-ray structure of 8b in complex with TACE was also obtained.
About this StructureAbout this Structure
3B92 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.
ReferenceReference
Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones., Bandarage UK, Wang T, Come JH, Perola E, Wei Y, Rao BG, Bioorg Med Chem Lett. 2008 Jan 1;18(1):44-8. Epub 2007 Nov 13. PMID:18054488
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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
- ADAM 17 endopeptidase
- Homo sapiens
- Single protein
- Wei, Y.
- 440
- ZN
- Alternative splicing
- Aryl-sulfonamide
- Cleavage on pair of basic residues
- Glycoprotein
- Hydrolase
- Membrane
- Metal-binding
- Metalloprotease
- Notch signaling pathway
- Phosphorylation
- Protease
- Sh3-binding
- Tace inhibitors
- Tnf-alpha converting enzyme
- Transmembrane
- Zinc
- Zymogen