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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2002-9-18
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pubmed:abstractText |
The main objective of this study was to investigate the safety, tolerability and pharmacodynamics of the novel proteasome inhibitor PS-519 in young male volunteers. Many pro-inflammatory mediators such as cytokines and cell adhesion molecules that are responsible for the development of the cerebral infarct are under the control of the transcription factor Nuclear Factor kappa-B (NF-kappaB). The activity of NF-kappaB is itself tightly regulated through the multicatalytic enzyme known as the proteasome. PS-519 is a novel and highly selective small molecule that inhibits the proteasome. An ex vivo assay of 20S proteasome activity allows monitoring of the drug effect in blood. PS-519 is protective in multiple animal models of cerebral ischaemia over a range of doses that achieve 20S inhibition of 40%-80%.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-10093058,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-10452747,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-10548686,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-10602462,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-10724123,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-10756082,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-10794750,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-10884474,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-11739997,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-7538441,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-8011280,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-8087845,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-8622934,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-8717528,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12236847-8864118
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0306-5251
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
54
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
269-76
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:12236847-Acetylcysteine,
pubmed-meshheading:12236847-Bilirubin,
pubmed-meshheading:12236847-Blood Pressure,
pubmed-meshheading:12236847-Cysteine Endopeptidases,
pubmed-meshheading:12236847-Double-Blind Method,
pubmed-meshheading:12236847-Electrocardiography,
pubmed-meshheading:12236847-Heart Rate,
pubmed-meshheading:12236847-Humans,
pubmed-meshheading:12236847-Leukocyte Count,
pubmed-meshheading:12236847-Male,
pubmed-meshheading:12236847-Multienzyme Complexes,
pubmed-meshheading:12236847-Neutrophils,
pubmed-meshheading:12236847-Proteasome Endopeptidase Complex
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pubmed:year |
2002
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pubmed:articleTitle |
Early clinical experience with the novel proteasome inhibitor PS-519.
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pubmed:affiliation |
University Department of Medicine & Therapeutics, Western Infirmary, Glasgow, UK. I.M.Shah@clinmed.gla.ac.uk
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pubmed:publicationType |
Journal Article,
Clinical Trial,
Randomized Controlled Trial,
Research Support, Non-U.S. Gov't,
Clinical Trial, Phase I
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