Document Detail


Modulation of human estrogen receptor α activity by multivalent estradiol-peptidomimetic conjugates.
MedLine Citation:
PMID:  21218226     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Estradiol-peptidomimetic conjugates (EPCs) are linear, sequence-specific peptoid oligomers that site-specifically display multiple copies of 17β-estradiol (E2), a ligand for the human estrogen receptor α (hERα). We evaluate the ability of multivalent EPCs to activate hERα-mediated transcription. EPCs activated the hERα in both a length- and valence-dependent manner, with the highest levels of activation generated by divalent peptoid 6-mers, divalent 18-mers, and trivalent 9-mers. Hexavalent EPCs did not activate hERα, but instead blocked E2-mediated hERα activation. The physicochemical features of EPCs can be precisely tuned, which may allow the generation of a library of chemical tools for modulating specific effects of estrogens.
Authors:
Justin M Holub; Michael J Garabedian; Kent Kirshenbaum
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, Non-P.H.S.     Date:  2011-01-07
Journal Detail:
Title:  Molecular bioSystems     Volume:  7     ISSN:  1742-2051     ISO Abbreviation:  Mol Biosyst     Publication Date:  2011 Feb 
Date Detail:
Created Date:  2011-01-19     Completed Date:  2011-05-24     Revised Date:  2011-05-26    
Medline Journal Info:
Nlm Unique ID:  101251620     Medline TA:  Mol Biosyst     Country:  England    
Other Details:
Languages:  eng     Pagination:  337-45     Citation Subset:  IM    
Affiliation:
Department of Chemistry, New York University, 100 Washington Square East, New York, New York 10003, USA.
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MeSH Terms
Descriptor/Qualifier:
Cell Line
Cell Membrane Permeability
Estradiol / chemistry,  pharmacology*
Estrogen Receptor alpha / drug effects*,  metabolism,  physiology
Fluorescent Dyes / chemical synthesis
Humans
Hydrolysis
Molecular Mimicry*
Peptides / chemistry,  pharmacology*
Transcription, Genetic / physiology
Grant Support
ID/Acronym/Agency:
C060RR-165720/RR/NCRR NIH HHS
Chemical
Reg. No./Substance:
0/Estrogen Receptor alpha; 0/Fluorescent Dyes; 0/Peptides; 50-28-2/Estradiol

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


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