| Modulation of human estrogen receptor α activity by multivalent estradiol-peptidomimetic conjugates. | |
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MedLine Citation:
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PMID: 21218226 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Justin M Holub; Michael J Garabedian; Kent Kirshenbaum |
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Publication Detail:
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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:
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Title: Molecular bioSystems Volume: 7 ISSN: 1742-2051 ISO Abbreviation: Mol Biosyst Publication Date: 2011 Feb |
Date Detail:
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Created Date: 2011-01-19 Completed Date: 2011-05-24 Revised Date: 2011-05-26 |
Medline Journal Info:
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Nlm Unique ID: 101251620 Medline TA: Mol Biosyst Country: England |
Other Details:
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Languages: eng Pagination: 337-45 Citation Subset: IM |
Affiliation:
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Department of Chemistry, New York University, 100 Washington Square East, New York, New York 10003, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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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:
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C060RR-165720/RR/NCRR NIH HHS |
| Chemical | |
Reg. No./Substance:
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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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