rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
10
|
pubmed:dateCreated |
2006-4-3
|
pubmed:abstractText |
A novel series of achiral TNF-alpha converting enzyme (TACE) inhibitors has been discovered. These compounds exhibited activities from 0.35 to 11nM in a porcine TACE assay and inhibited TNF-alpha production in an LPS-stimulated whole blood assay with an IC(50) value of 23nM for the most potent one. They also have excellent selectivities over related metalloproteases including aggrecanases.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
May
|
pubmed:issn |
0960-894X
|
pubmed:author |
pubmed-author:CovingtonMaryanne BMB,
pubmed-author:DeciccoCarl PCP,
pubmed-author:DuanJames J-WJJ,
pubmed-author:GilmoreJohn LJL,
pubmed-author:HarrisCathyC,
pubmed-author:KingBryan WBW,
pubmed-author:LiuRui-QinRQ,
pubmed-author:MaduskuieThomasT,
pubmed-author:MercerStephen ESE,
pubmed-author:NewtonRobert CRC,
pubmed-author:QianMingxinM,
pubmed-author:RibadeneriaMaria DMD,
pubmed-author:TrzaskosJames MJM,
pubmed-author:VaddiKrishnaK
|
pubmed:issnType |
Print
|
pubmed:day |
15
|
pubmed:volume |
16
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
2699-704
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
|
pubmed:year |
2006
|
pubmed:articleTitle |
Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors.
|
pubmed:affiliation |
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. john.gilmore@bms.com
|
pubmed:publicationType |
Journal Article
|