Linked Life Data

8063618

Source:http://linkedlifedata.com/resource/pubmed/id/8063618

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
1994-9-21
pubmed:abstractText
The binding sites, other than the estrogen receptor (ER), of the antiestrogens droloxifene (DROL, (E)-a-[p-[2-(dimethylamino)ethoxy]-phenyl]-a'-ethyl-3-stilbenol) and tamoxifen (TAM), and estradiol-17 beta (E2) in the cytosol of 7,12-dimethylbenz[a]anthracene-induced rat mammary ER-positive tumor cells were studied using a high-performance liquid chromatography (HPLC) gel filtration assay. The cytosol was incubated with 3H-labeled drug with or without unlabeled drug, and separated by HPLC gel filtration. 3H-E2 produced two major peaks of radioactivity at fractions No. 40 and No. 70. The peak at fraction No. 70 was identified as the ER in an ER-enzyme-immuno assay. This peak was dose-dependently inhibited by unlabeled DROL or TAM, DROL being a more potent inhibitor than TAM. The peak at fraction No. 40 was also inhibited by co-incubation with unlabeled DROL or TAM. 3H-DROL or 3H-TAM provided only one peak at fraction No. 43. This peak was thought to be an antiestrogen binding site (AEBS), because it was inhibited by unlabeled antiestrogen but not by E2. The results suggest that the antiestrogens DROL and TAM have a higher affinity for the AEBS than for the ER in the absence of E2, while in the presence of E2 both have an affinity for the ER and inhibit E2 binding to the ER.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0910-5050
pubmed:author
pubmed:issnType
Print
pubmed:volume
85
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
639-44
pubmed:dateRevised
2003-11-14
pubmed:meshHeading
pubmed:year
1994
pubmed:articleTitle
Binding sites of droloxifene in the cytosol of 7,12-dimethylbenz[a]anthracene-induced rat mammary tumor cells.
pubmed:affiliation
Pharmacological Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka.
pubmed:publicationType
Journal Article