3b92: Difference between revisions

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[[Image:3b92.jpg|left|200px]]
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[[Image:3b92.png|left|200px]]


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{{STRUCTURE_3b92|  PDB=3b92  |  SCENE=  }}  
{{STRUCTURE_3b92|  PDB=3b92  |  SCENE=  }}  


'''Novel thio-based TACE inhibitors Part 2: Rational design, synthesis and SAR of thiol-contaning aryl sufones'''
===Novel thio-based TACE inhibitors Part 2: Rational design, synthesis and SAR of thiol-contaning aryl sufones===




==Overview==
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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.
The line below this paragraph, {{ABSTRACT_PUBMED_18054488}}, adds the Publication Abstract to the page
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{{ABSTRACT_PUBMED_18054488}}


==About this Structure==
==About this Structure==
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[[Category: Zinc]]
[[Category: Zinc]]
[[Category: Zymogen]]
[[Category: Zymogen]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Apr 30 13:36:51 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 11:24:52 2008''

Revision as of 08:24, 28 July 2008

File:3b92.png

Template:STRUCTURE 3b92

Novel thio-based TACE inhibitors Part 2: Rational design, synthesis and SAR of thiol-contaning aryl sufones

Template:ABSTRACT PUBMED 18054488

About this Structure

3B92 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

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. 2008 Jan 1;18(1):44-8. Epub 2007 Nov 13. PMID:18054488

Page seeded by OCA on Mon Jul 28 11:24:52 2008

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