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첨단연성물질연구단
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Ligand Accessibility and Bioactivity of a Hormone-Dendrimer Conjugate Depend on pH and pH History

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dc.contributor.authorKim, SH-
dc.contributor.authorMadak-Erdogan, Z-
dc.contributor.authorSung Chul Bae-
dc.contributor.authorCarlson, KE-
dc.contributor.authorMayne, CG-
dc.contributor.authorSteve Granick-
dc.contributor.authorKatzenellenbogen, BS-
dc.contributor.authorKatzenellenbogen, JA-
dc.date.available2016-01-07T09:11:24Z-
dc.date.created2015-09-21-
dc.date.issued2015-08-
dc.identifier.issn0002-7863-
dc.identifier.urihttps://pr.ibs.re.kr/handle/8788114/1915-
dc.description.abstractEstrogen conjugates with a polyamidoamine (PAMAM) dendrimer have shown remarkably selective regulation of the nongenomic actions of estrogens in target cells. In response to pH changes, however, these estrogen-dendrimer conjugates (EDCs) display a major morphological transition that alters the accessibility of the estrogen ligands that compromises the bioactivity of the EDC. A sharp break in dynamic behavior near pH 7 occurs for three different ligands on the surface of a PAMAM-G6 dendrimer: a fluorophore (tetramethylrhodamine [TMR]) and two estrogens (17 alpha-ethynylestradiol and diphenolic acid). Collisional quenching and time-resolved fluorescence anisotropy experiments with TMR-PAMAM revealed high ligand shielding above pH 7 and low shielding below pH 7. Furthermore, when the pH was cycled from 8.5 (conditions of ligand-PAMAM conjugation) to 4.5 (e.g., endosome/lysosome) and through 6.5 (e.g., hypoxic environment) back to pH 8.5, the 17 alpha-ethynylestradiol- and diphenolic acid-PAMAM conjugates experienced a draniatic, irreversible loss in cell stimulatory activity; dynamic NMR studies indicated that the hormonal ligands had become occluded within the more hydrophobic core of the PAMAM dendrimer. Thus, the active state of these estrogen-dendrimer conjugates appears to be metastable. This pH-dependent irreversible masking of activity is of considerable relevance to the design of drug conjugates with amine-bearing PAMAM dendrimers-
dc.description.uri1-
dc.language영어-
dc.publisherAMER CHEMICAL SOC-
dc.titleLigand Accessibility and Bioactivity of a Hormone-Dendrimer Conjugate Depend on pH and pH History-
dc.typeArticle-
dc.type.rimsART-
dc.identifier.wosid000359962000054-
dc.identifier.scopusid2-s2.0-84939865433-
dc.identifier.rimsid21025ko
dc.date.tcdate2018-10-01-
dc.contributor.affiliatedAuthorSung Chul Bae-
dc.contributor.affiliatedAuthorSteve Granick-
dc.identifier.doi10.1021/jacs.5b05952-
dc.identifier.bibliographicCitationJOURNAL OF THE AMERICAN CHEMICAL SOCIETY, v.137, no.32, pp.10326 - 10335-
dc.citation.titleJOURNAL OF THE AMERICAN CHEMICAL SOCIETY-
dc.citation.volume137-
dc.citation.number32-
dc.citation.startPage10326-
dc.citation.endPage10335-
dc.date.scptcdate2018-10-01-
dc.description.wostc8-
dc.description.scptc8-
dc.description.journalClass1-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.subject.keywordPlusBREAST-CANCER CELLS-
dc.subject.keywordPlusRESPONSIVE CONFORMATIONAL-CHANGES-
dc.subject.keywordPlusCARBONIC-ANHYDRASE-IX-
dc.subject.keywordPlusESTROGEN-RECEPTOR-
dc.subject.keywordPlusPAMAM DENDRIMERS-
dc.subject.keywordPlusGENE-EXPRESSION-
dc.subject.keywordPlusDRUG-DELIVERY-
dc.subject.keywordPlusIN-VITRO-
dc.subject.keywordPlusEXTRANUCLEAR-
dc.subject.keywordPlusDYNAMICS-
Appears in Collections:
Center for Soft and Living Matter(첨단연성물질 연구단) > 1. Journal Papers (저널논문)
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