Document Detail

Binding sites of droloxifene in the cytosol of 7,12-dimethylbenz[a]anthracene-induced rat mammary tumor cells.
MedLine Citation:
PMID:  8063618     Owner:  NLM     Status:  MEDLINE    
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.
I Kawamura; E Lacey; Y Tanaka; F Nishigaki; T Manda; K Shimomura
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Japanese journal of cancer research : Gann     Volume:  85     ISSN:  0910-5050     ISO Abbreviation:  Jpn. J. Cancer Res.     Publication Date:  1994 Jun 
Date Detail:
Created Date:  1994-09-21     Completed Date:  1994-09-21     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  8509412     Medline TA:  Jpn J Cancer Res     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  639-44     Citation Subset:  IM    
Pharmacological Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka.
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MeSH Terms
Antineoplastic Agents / metabolism*
Binding Sites
Chromatography, High Pressure Liquid
Cytosol / metabolism
Estradiol / metabolism
Estrogen Antagonists / metabolism*
Mammary Neoplasms, Experimental / chemically induced,  metabolism*
Rats, Sprague-Dawley
Receptors, Estrogen / analysis,  metabolism
Tamoxifen / analogs & derivatives*,  metabolism
Tumor Cells, Cultured
Reg. No./Substance:
0/Antineoplastic Agents; 0/Estrogen Antagonists; 0/Receptors, Estrogen; 10028-17-8/Tritium; 10540-29-1/Tamoxifen; 50-28-2/Estradiol; 57-97-6/9,10-Dimethyl-1,2-benzanthracene; 82413-20-5/3-hydroxytamoxifen

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