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| [[Image:1d7x.jpg|left|200px]] | | {{Seed}} |
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| {{STRUCTURE_1d7x| PDB=1d7x | SCENE= }} | | {{STRUCTURE_1d7x| PDB=1d7x | SCENE= }} |
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| '''CRYSTAL STRUCTURE OF MMP3 COMPLEXED WITH A MODIFIED PROLINE SCAFFOLD BASED INHIBITOR.'''
| | ===CRYSTAL STRUCTURE OF MMP3 COMPLEXED WITH A MODIFIED PROLINE SCAFFOLD BASED INHIBITOR.=== |
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| ==Overview==
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| The synthesis and structure-activity relationship (SAR) studies of a series of proline-based matrix metalloproteinase inhibitors are described. The data reveal a remarkable potency enhancement in those compounds that contain an sp(2) center at the C-4 carbon of the ring relative to similar, saturated compounds. This effect was noted in compounds that contained a functionalized oxime moiety or an exomethylene at C-4, and the potencies were typically <10 nM for MMP-3 and <100 nM for MMP-1. Comparisons were then made against compounds with similar functionality where the C-4 carbon was reduced to sp(3) hybridization and the effect was typically an order of magnitude loss in potency. A comparison of compounds 14 and 34 exemplifies this observation. An X-ray structure was obtained for a stromelysin-inhibitor complex which provided insights into the SAR and selectivity trends observed within the series. In vitro intestinal permeability data for many compounds was also accumulated.
| | The line below this paragraph, {{ABSTRACT_PUBMED_10639284}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 10639284 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_10639284}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Mixed alpha beta structure]] | | [[Category: Mixed alpha beta structure]] |
| [[Category: Zinc protease]] | | [[Category: Zinc protease]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 13:33:00 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 22:38:53 2008'' |