|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
22
|
|
pubmed:dateCreated |
2005-10-27
|
|
pubmed:abstractText |
A series of oxamyl dipeptides were optimized for pan caspase inhibition, anti-apoptotic cellular activity and in vivo efficacy. This structure-activity relationship study focused on the P4 oxamides and warhead moieties. Primarily on the basis of in vitro data, inhibitors were selected for study in a murine model of alpha-Fas-induced liver injury. IDN-6556 (1) was further profiled in additional in vivo models and pharmacokinetic studies. This first-in-class caspase inhibitor is now the subject of two Phase II clinical trials, evaluating its safety and efficacy for use in liver disease.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/3-(2-(2-tert-butylphenylaminooxalyl)...,
http://linkedlifedata.com/resource/pubmed/chemical/Alanine Transaminase,
http://linkedlifedata.com/resource/pubmed/chemical/Aspartate Aminotransferases,
http://linkedlifedata.com/resource/pubmed/chemical/CASP3 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Casp3 protein, mouse,
http://linkedlifedata.com/resource/pubmed/chemical/Casp3 protein, rat,
http://linkedlifedata.com/resource/pubmed/chemical/Caspase 3,
http://linkedlifedata.com/resource/pubmed/chemical/Caspases,
http://linkedlifedata.com/resource/pubmed/chemical/Pentanoic Acids
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Nov
|
|
pubmed:issn |
0022-2623
|
|
pubmed:author |
pubmed-author:AjaTeresaT,
pubmed-author:ArmstrongRobert ARA,
pubmed-author:BaiXuX,
pubmed-author:ChenLong-ShiuhLS,
pubmed-author:ChenNingN,
pubmed-author:ChingBrettB,
pubmed-author:ContrerasPatriciaP,
pubmed-author:DiazJose-LuisJL,
pubmed-author:FisherCraig DCD,
pubmed-author:FritzLawrence CLC,
pubmed-author:GladstonePatriciaP,
pubmed-author:GroesslToddT,
pubmed-author:GuXinX,
pubmed-author:HerrmannJuliaJ,
pubmed-author:HirakawaBrad PBP,
pubmed-author:HoglenNiel CNC,
pubmed-author:JahangiriKathy GKG,
pubmed-author:KalishVincent JVJ,
pubmed-author:KaranewskyDonald SDS,
pubmed-author:KodandapaniLalithaL,
pubmed-author:KrebsJosephJ,
pubmed-author:LintonSteven DSD,
pubmed-author:McQuistonJeffJ,
pubmed-author:MedunaSteven PSP,
pubmed-author:NalleyKipK,
pubmed-author:RobinsonEdward DED,
pubmed-author:SayersRobert ORO,
pubmed-author:SebringKristenK,
pubmed-author:SpadaAlfred PAP,
pubmed-author:TernanskyRobert JRJ,
pubmed-author:TomaselliKevin JKJ,
pubmed-author:UllmanBrett RBR,
pubmed-author:ValentinoKaren LKL,
pubmed-author:WeeksSuzanneS,
pubmed-author:WinnDavidD,
pubmed-author:WuJoe CJC,
pubmed-author:YeoPaulineP,
pubmed-author:ZhangCheng-zhiCZ
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
3
|
|
pubmed:volume |
48
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
6779-82
|
|
pubmed:dateRevised |
2007-11-15
|
|
pubmed:meshHeading |
pubmed-meshheading:16250635-Adult,
pubmed-meshheading:16250635-Alanine Transaminase,
pubmed-meshheading:16250635-Animals,
pubmed-meshheading:16250635-Apoptosis,
pubmed-meshheading:16250635-Aspartate Aminotransferases,
pubmed-meshheading:16250635-Biological Availability,
pubmed-meshheading:16250635-Caspase 3,
pubmed-meshheading:16250635-Caspases,
pubmed-meshheading:16250635-Cholestasis,
pubmed-meshheading:16250635-Clinical Trials, Phase I as Topic,
pubmed-meshheading:16250635-Half-Life,
pubmed-meshheading:16250635-Hepatitis C, Chronic,
pubmed-meshheading:16250635-Hepatocytes,
pubmed-meshheading:16250635-Humans,
pubmed-meshheading:16250635-Jurkat Cells,
pubmed-meshheading:16250635-Liver,
pubmed-meshheading:16250635-Liver Diseases,
pubmed-meshheading:16250635-Mice,
pubmed-meshheading:16250635-Pentanoic Acids,
pubmed-meshheading:16250635-Rats,
pubmed-meshheading:16250635-Structure-Activity Relationship
|
|
pubmed:year |
2005
|
|
pubmed:articleTitle |
First-in-class pan caspase inhibitor developed for the treatment of liver disease.
|
|
pubmed:affiliation |
Idun Pharmaceuticals, 9380 Judicial Drive, San Diego, CA 92121, USA. slinton@idun.com
|
|
pubmed:publicationType |
Journal Article
|
