|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
8
|
|
pubmed:dateCreated |
2001-4-30
|
|
pubmed:abstractText |
Potent and selective inhibition of matrix metalloproteinases was demonstrated for a series of sulfonamide-based hydroxamic acids. The design of the heterocyclic sulfonamides incorporates a six- or seven-member central ring with a P2' substituent that can be modified. Binding interactions of this substituent at the S2' site are believed to contribute to high inhibitory potency against stromelysin, collagenase-3 and gelatinases A and B, and to provide selectivity against collagenase-1 and matrilysin. An X-ray structure of a stromelysin inhibitor complex was obtained to provide insights into the SAR and selectivity trends observed for the series.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Collagenases,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Heterocyclic Compounds, 1-Ring,
http://linkedlifedata.com/resource/pubmed/chemical/Macromolecular Substances,
http://linkedlifedata.com/resource/pubmed/chemical/Matrix Metalloproteinase 13,
http://linkedlifedata.com/resource/pubmed/chemical/Matrix Metalloproteinase 2,
http://linkedlifedata.com/resource/pubmed/chemical/Matrix Metalloproteinase 3,
http://linkedlifedata.com/resource/pubmed/chemical/Matrix Metalloproteinase 7,
http://linkedlifedata.com/resource/pubmed/chemical/Matrix Metalloproteinase 9,
http://linkedlifedata.com/resource/pubmed/chemical/Matrix Metalloproteinases,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfonamides,
http://linkedlifedata.com/resource/pubmed/chemical/collagenase 1
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Apr
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:AlmsteadN GNG,
pubmed-author:DunhamK MKM,
pubmed-author:EYWW,
pubmed-author:HsiehL CLC,
pubmed-author:HyndB ABA,
pubmed-author:JanuszM JMJ,
pubmed-author:KAON CNC,
pubmed-author:MielingG EGE,
pubmed-author:NatchusM GMG,
pubmed-author:PikusJJ,
pubmed-author:TaiwoY OYO,
pubmed-author:WilliamsL ELE
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
23
|
|
pubmed:volume |
11
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
1009-13
|
|
pubmed:dateRevised |
2006-11-15
|
|
pubmed:meshHeading |
pubmed-meshheading:11327577-Collagenases,
pubmed-meshheading:11327577-Crystallography, X-Ray,
pubmed-meshheading:11327577-Enzyme Inhibitors,
pubmed-meshheading:11327577-Heterocyclic Compounds, 1-Ring,
pubmed-meshheading:11327577-Inhibitory Concentration 50,
pubmed-meshheading:11327577-Macromolecular Substances,
pubmed-meshheading:11327577-Matrix Metalloproteinase 13,
pubmed-meshheading:11327577-Matrix Metalloproteinase 2,
pubmed-meshheading:11327577-Matrix Metalloproteinase 3,
pubmed-meshheading:11327577-Matrix Metalloproteinase 7,
pubmed-meshheading:11327577-Matrix Metalloproteinase 9,
pubmed-meshheading:11327577-Matrix Metalloproteinases,
pubmed-meshheading:11327577-Sensitivity and Specificity,
pubmed-meshheading:11327577-Structure-Activity Relationship,
pubmed-meshheading:11327577-Sulfonamides
|
|
pubmed:year |
2001
|
|
pubmed:articleTitle |
Heterocycle-based MMP inhibitors with P2' substituents.
|
|
pubmed:affiliation |
Procter and Gamble Pharmaceuticals, Health Care Research Center, Mason, OH 45040, USA. spikul@avalonrx.com
|
|
pubmed:publicationType |
Journal Article
|
