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    
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.
L J Brandes
Related Documents :
3524806 - Quality control requirements in estrogen receptor determination.
19074846 - Microsomal antiestrogen-binding site ligands induce growth control and differentiation ...
16533016 - Phip carcinogenicity in breast cancer: computational and experimental evidence for comp...
3882696 - Electrophoretic characterization of purified bovine, porcine, murine, rat, and human ut...
11052796 - Radioiodinated n-(2-diethylaminoethyl)benzamide derivatives with high melanoma uptake: ...
7929326 - Influence of monovalent cations on the ultraviolet-visible spectrum of tryptophan trypt...
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    
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Breast Neoplasms / metabolism*,  pathology
Cell Division / drug effects
Cell Line
Phenyl Ethers / pharmacology*
Receptors, Drug*
Receptors, Estrogen / metabolism*
Tamoxifen / metabolism*,  pharmacology
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

Previous Document:  Fructose 2,6-bisphosphate in rat skeletal muscle during contraction.
Next Document:  Preparation and biological activity of taxol acetates.