Source:http://linkedlifedata.com/resource/pubmed/id/18605714
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
15
|
pubmed:dateCreated |
2008-8-7
|
pubmed:abstractText |
We report a series of inhibitors of secreted phospholipases A2 (sPLA2s) based on substituted indoles, 6,7-benzoindoles, and indolizines derived from LY315920, a well-known indole-based sPLA2 inhibitor. Using the human group X sPLA2 crystal structure, we prepared a highly potent and selective indole-based inhibitor of this enzyme. Also, we report human and mouse group IIA and IIE specific inhibitors and a substituted 6,7-benzoindole that inhibits nearly all human and mouse sPLA2s in the low nanomolar range.
|
pubmed:grant | |
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Aug
|
pubmed:issn |
1520-4804
|
pubmed:author | |
pubmed:issnType |
Electronic
|
pubmed:day |
14
|
pubmed:volume |
51
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
4708-14
|
pubmed:dateRevised |
2010-12-3
|
pubmed:meshHeading |
pubmed-meshheading:18605714-Animals,
pubmed-meshheading:18605714-Enzyme Inhibitors,
pubmed-meshheading:18605714-Humans,
pubmed-meshheading:18605714-Indoles,
pubmed-meshheading:18605714-Indolizidines,
pubmed-meshheading:18605714-Mice,
pubmed-meshheading:18605714-Models, Molecular,
pubmed-meshheading:18605714-Molecular Structure,
pubmed-meshheading:18605714-Phospholipases A2, Secretory,
pubmed-meshheading:18605714-Sensitivity and Specificity,
pubmed-meshheading:18605714-Structure-Activity Relationship
|
pubmed:year |
2008
|
pubmed:articleTitle |
Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
|
pubmed:affiliation |
Departments of Chemistry and Biochemistry, University of Washington, Seattle, Washington 98195, USA.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
|