Modulation of human estrogen receptor α activity by multivalent estradiol-peptidomimetic conjugates.
Identifieur interne : 002452 ( Main/Exploration ); précédent : 002451; suivant : 002453Modulation of human estrogen receptor α activity by multivalent estradiol-peptidomimetic conjugates.
Auteurs : Justin M. Holub [États-Unis] ; Michael J. Garabedian ; Kent KirshenbaumSource :
- Molecular bioSystems [ 1742-2051 ] ; 2011.
Descripteurs français
- KwdFr :
- Colorants fluorescents (synthèse chimique), Humains, Hydrolyse, Lignée cellulaire, Mimétisme moléculaire, Oestradiol (), Oestradiol (pharmacologie), Peptides (), Peptides (pharmacologie), Perméabilité de la membrane cellulaire, Récepteur alpha des oestrogènes (), Récepteur alpha des oestrogènes (métabolisme), Récepteur alpha des oestrogènes (physiologie), Transcription génétique (physiologie).
- MESH :
- métabolisme : Récepteur alpha des oestrogènes.
- pharmacologie : Oestradiol, Peptides.
- physiologie : Récepteur alpha des oestrogènes, Transcription génétique.
- synthèse chimique : Colorants fluorescents.
- Humains, Hydrolyse, Lignée cellulaire, Mimétisme moléculaire, Oestradiol, Peptides, Perméabilité de la membrane cellulaire, Récepteur alpha des oestrogènes.
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
Affiliations:
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Le document en format XML
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Holub</name><affiliation wicri:level="1"><nlm:affiliation>Department of Chemistry, New York University, 100 Washington Square East, New York, New York 10003, USA.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Chemistry, New York University, 100 Washington Square East, New York, New York 10003</wicri:regionArea><wicri:noRegion>New York 10003</wicri:noRegion></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></analytic><series><title level="j">Molecular bioSystems</title><idno type="eISSN">1742-2051</idno><imprint><date when="2011" type="published">2011</date></imprint></series></biblStruct></sourceDesc></fileDesc><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></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Colorants fluorescents (synthèse chimique)</term><term>Humains</term><term>Hydrolyse</term><term>Lignée cellulaire</term><term>Mimétisme moléculaire</term><term>Oestradiol ()</term><term>Oestradiol (pharmacologie)</term><term>Peptides ()</term><term>Peptides (pharmacologie)</term><term>Perméabilité de la membrane cellulaire</term><term>Récepteur alpha des oestrogènes ()</term><term>Récepteur alpha des oestrogènes (métabolisme)</term><term>Récepteur alpha des oestrogènes (physiologie)</term><term>Transcription génétique (physiologie)</term></keywords><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></keywords><keywords scheme="MESH" type="chemical" qualifier="physiology" xml:lang="en"><term>Estrogen Receptor alpha</term></keywords><keywords scheme="MESH" qualifier="métabolisme" xml:lang="fr"><term>Récepteur alpha des oestrogènes</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Oestradiol</term><term>Peptides</term></keywords><keywords scheme="MESH" qualifier="physiologie" xml:lang="fr"><term>Récepteur alpha des oestrogènes</term><term>Transcription génétique</term></keywords><keywords scheme="MESH" qualifier="physiology" xml:lang="en"><term>Transcription, Genetic</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Colorants fluorescents</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Cell Line</term><term>Cell Membrane Permeability</term><term>Humans</term><term>Hydrolysis</term><term>Molecular Mimicry</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Humains</term><term>Hydrolyse</term><term>Lignée cellulaire</term><term>Mimétisme moléculaire</term><term>Oestradiol</term><term>Peptides</term><term>Perméabilité de la membrane cellulaire</term><term>Récepteur alpha des oestrogènes</term></keywords></textClass></profileDesc></teiHeader><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><affiliations><list><country><li>États-Unis</li></country></list><tree><noCountry><name sortKey="Garabedian, Michael J" sort="Garabedian, Michael J" uniqKey="Garabedian M" first="Michael J" last="Garabedian">Michael J. Garabedian</name><name sortKey="Kirshenbaum, Kent" sort="Kirshenbaum, Kent" uniqKey="Kirshenbaum K" first="Kent" last="Kirshenbaum">Kent Kirshenbaum</name></noCountry><country name="États-Unis"><noRegion><name sortKey="Holub, Justin M" sort="Holub, Justin M" uniqKey="Holub J" first="Justin M" last="Holub">Justin M. Holub</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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