rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
17
|
pubmed:dateCreated |
1992-7-16
|
pubmed:abstractText |
Squalestatin 1 is a member of a novel family of fermentation products isolated from a previously unknown Phoma species (Coelomycetes). Squalestatin 1 is a potent, selective inhibitor of squalene synthase, a key enzyme in cholesterol biosynthesis; in vitro, 50% inhibition of enzyme activity is observed at a concentration of 12 +/- 5 nM (range of 4-22 nM). Squalestatin 1 inhibits cholesterol biosynthesis from [14C]acetate by isolated rat hepatocytes (50% inhibition at 39 nM) and by rat liver in vivo. In marmosets, a species with a lipoprotein profile similar to that of man, squalestatin 1 lowers serum cholesterol by up to 75%. This compound will allow further investigation of the control of the sterol biosynthesis pathway and could also lead to the development of new therapies for elevated serum cholesterol.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jun
|
pubmed:issn |
0021-9258
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
15
|
pubmed:volume |
267
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
N
|
pubmed:pagination |
11705-8
|
pubmed:dateRevised |
2005-11-17
|
pubmed:meshHeading |
pubmed-meshheading:1601846-Animals,
pubmed-meshheading:1601846-Apolipoprotein A-I,
pubmed-meshheading:1601846-Apolipoproteins B,
pubmed-meshheading:1601846-Bicyclo Compounds,
pubmed-meshheading:1601846-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:1601846-Callithrix,
pubmed-meshheading:1601846-Cells, Cultured,
pubmed-meshheading:1601846-Cholesterol,
pubmed-meshheading:1601846-Farnesyl-Diphosphate Farnesyltransferase,
pubmed-meshheading:1601846-Liver,
pubmed-meshheading:1601846-Male,
pubmed-meshheading:1601846-Rats,
pubmed-meshheading:1601846-Tricarboxylic Acids
|
pubmed:year |
1992
|
pubmed:articleTitle |
Squalestatin 1, a potent inhibitor of squalene synthase, which lowers serum cholesterol in vivo.
|
pubmed:affiliation |
Glaxo Group Research Ltd., Greenford, Middlesex, United Kingdom.
|
pubmed:publicationType |
Journal Article
|