Document Detail


A diphenylmethane derivative selective for the anti-estrogen binding site may help define its biological role.
MedLine Citation:
PMID:  6548626     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
By employing as a probe the new compound, N,N-diethyl-2-[(4-phenyl-methyl)-phenoxy]-ethanamine X HC1 (N,N-DPPE), which preferentially binds the anti-estrogen binding site, it is demonstrated that this site appears to contribute to the growth inhibitory action of tamoxifen on MCF-7 human breast cancer cells, even at lower concentrations of this anti-estrogen (1 X 10(-7) M to 1 X 10(-6) M) at which the major effect is clearly mediated via estrogen receptor. The combination of N,N-DPPE and tamoxifen is additive and this effect is not abolished by 17 beta-estradiol. This suggests that the anti-estrogen binding site is not simply a passive reservoir for binding tamoxifen, but may itself mediate the cytotoxic effects of specific ligands.
Authors:
L J Brandes
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Biochemical and biophysical research communications     Volume:  124     ISSN:  0006-291X     ISO Abbreviation:  Biochem. Biophys. Res. Commun.     Publication Date:  1984 Oct 
Date Detail:
Created Date:  1984-12-05     Completed Date:  1984-12-05     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0372516     Medline TA:  Biochem Biophys Res Commun     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  244-9     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Breast Neoplasms / metabolism*,  pathology
Cell Division / drug effects
Cell Line
Female
Humans
Kinetics
Phenyl Ethers / pharmacology*
Receptors, Drug*
Receptors, Estrogen / metabolism*
Tamoxifen / metabolism*,  pharmacology
Chemical
Reg. No./Substance:
0/Phenyl Ethers; 0/Receptors, Drug; 0/Receptors, Estrogen; 10540-29-1/Tamoxifen; 98774-23-3/N,N-diethyl-2-((4-phenylmethyl)phenoxy)ethanamine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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