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Modulation of human estrogen receptor α activity by multivalent estradiol-peptidomimetic conjugates.

Identifieur interne : 001F11 ( PubMed/Corpus ); précédent : 001F10; suivant : 001F12

Modulation of human estrogen receptor α activity by multivalent estradiol-peptidomimetic conjugates.

Auteurs : Justin M. Holub ; Michael J. Garabedian ; Kent Kirshenbaum

Source :

Molecular bioSystems [ 1742-2051 ] ; 2011.

RBID : pubmed:21218226

English descriptors

KwdEn :
- Cell Line, Cell Membrane Permeability, Estradiol (chemistry), Estradiol (pharmacology), Estrogen Receptor alpha (drug effects), Estrogen Receptor alpha (metabolism), Estrogen Receptor alpha (physiology), Fluorescent Dyes (chemical synthesis), Humans, Hydrolysis, Molecular Mimicry, Peptides (chemistry), Peptides (pharmacology), Transcription, Genetic (physiology).
MESH :
- chemical , chemical synthesis : Fluorescent Dyes.
- chemical , chemistry : Estradiol, Peptides.
- chemical , drug effects : Estrogen Receptor alpha.
- chemical , metabolism : Estrogen Receptor alpha.
- chemical , pharmacology : Estradiol, Peptides.
- chemical , physiology : Estrogen Receptor alpha.
- physiology : Transcription, Genetic.
- Cell Line, Cell Membrane Permeability, Humans, Hydrolysis, Molecular Mimicry.

Abstract

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.

DOI: 10.1039/c0mb00189a
PubMed: 21218226

Links to Exploration step

pubmed:21218226

Le document en format XML

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<author><name sortKey="Holub, Justin M" sort="Holub, Justin M" uniqKey="Holub J" first="Justin M" last="Holub">Justin M. Holub</name>
<affiliation><nlm:affiliation>Department of Chemistry, New York University, 100 Washington Square East, New York, New York 10003, USA.</nlm:affiliation>
</affiliation>
</author>
<author><name sortKey="Garabedian, Michael J" sort="Garabedian, Michael J" uniqKey="Garabedian M" first="Michael J" last="Garabedian">Michael J. Garabedian</name>
</author>
<author><name sortKey="Kirshenbaum, Kent" sort="Kirshenbaum, Kent" uniqKey="Kirshenbaum K" first="Kent" last="Kirshenbaum">Kent Kirshenbaum</name>
</author>
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<sourceDesc><biblStruct><analytic><title xml:lang="en">Modulation of human estrogen receptor α activity by multivalent estradiol-peptidomimetic conjugates.</title>
<author><name sortKey="Holub, Justin M" sort="Holub, Justin M" uniqKey="Holub J" first="Justin M" last="Holub">Justin M. Holub</name>
<affiliation><nlm:affiliation>Department of Chemistry, New York University, 100 Washington Square East, New York, New York 10003, USA.</nlm:affiliation>
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<author><name sortKey="Garabedian, Michael J" sort="Garabedian, Michael J" uniqKey="Garabedian M" first="Michael J" last="Garabedian">Michael J. Garabedian</name>
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<author><name sortKey="Kirshenbaum, Kent" sort="Kirshenbaum, Kent" uniqKey="Kirshenbaum K" first="Kent" last="Kirshenbaum">Kent Kirshenbaum</name>
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<series><title level="j">Molecular bioSystems</title>
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<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Cell Line</term>
<term>Cell Membrane Permeability</term>
<term>Estradiol (chemistry)</term>
<term>Estradiol (pharmacology)</term>
<term>Estrogen Receptor alpha (drug effects)</term>
<term>Estrogen Receptor alpha (metabolism)</term>
<term>Estrogen Receptor alpha (physiology)</term>
<term>Fluorescent Dyes (chemical synthesis)</term>
<term>Humans</term>
<term>Hydrolysis</term>
<term>Molecular Mimicry</term>
<term>Peptides (chemistry)</term>
<term>Peptides (pharmacology)</term>
<term>Transcription, Genetic (physiology)</term>
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<keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Fluorescent Dyes</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Estradiol</term>
<term>Peptides</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="drug effects" xml:lang="en"><term>Estrogen Receptor alpha</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Estrogen Receptor alpha</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Estradiol</term>
<term>Peptides</term>
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<keywords scheme="MESH" type="chemical" qualifier="physiology" xml:lang="en"><term>Estrogen Receptor alpha</term>
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<keywords scheme="MESH" qualifier="physiology" xml:lang="en"><term>Transcription, Genetic</term>
</keywords>
<keywords scheme="MESH" xml:lang="en"><term>Cell Line</term>
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<front><div type="abstract" xml:lang="en">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.</div>
</front>
</TEI>
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<Month>05</Month>
<Day>24</Day>
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<DateRevised><Year>2013</Year>
<Month>11</Month>
<Day>21</Day>
</DateRevised>
<Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1742-2051</ISSN>
<JournalIssue CitedMedium="Internet"><Volume>7</Volume>
<Issue>2</Issue>
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<Month>Feb</Month>
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<Title>Molecular bioSystems</Title>
<ISOAbbreviation>Mol Biosyst</ISOAbbreviation>
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<ArticleTitle>Modulation of human estrogen receptor α activity by multivalent estradiol-peptidomimetic conjugates.</ArticleTitle>
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<Abstract><AbstractText>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.</AbstractText>
</Abstract>
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<ForeName>Justin M</ForeName>
<Initials>JM</Initials>
<AffiliationInfo><Affiliation>Department of Chemistry, New York University, 100 Washington Square East, New York, New York 10003, USA.</Affiliation>
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<Language>eng</Language>
<GrantList CompleteYN="Y"><Grant><GrantID>C060RR-165720</GrantID>
<Acronym>RR</Acronym>
<Agency>NCRR NIH HHS</Agency>
<Country>United States</Country>
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<MeshHeading><DescriptorName UI="D004958" MajorTopicYN="N">Estradiol</DescriptorName>
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<MeshHeading><DescriptorName UI="D006868" MajorTopicYN="N">Hydrolysis</DescriptorName>
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<MeshHeading><DescriptorName UI="D018716" MajorTopicYN="Y">Molecular Mimicry</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D010455" MajorTopicYN="N">Peptides</DescriptorName>
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<QualifierName UI="Q000494" MajorTopicYN="Y">pharmacology</QualifierName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D014158" MajorTopicYN="N">Transcription, Genetic</DescriptorName>
<QualifierName UI="Q000502" MajorTopicYN="N">physiology</QualifierName>
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Modulation of human estrogen receptor α activity by multivalent estradiol-peptidomimetic conjugates.

Modulation of human estrogen receptor α activity by multivalent estradiol-peptidomimetic conjugates.

Source :

English descriptors

Abstract

Links to Exploration step

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri

Pour générer des pages wiki