3b92: Difference between revisions
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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'' | ||
