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DC Field | Value | Language |
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dc.citation.endPage | 10335 | - |
dc.citation.number | 32 | - |
dc.citation.startPage | 10326 | - |
dc.citation.title | JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | - |
dc.citation.volume | 137 | - |
dc.contributor.author | Kim, Sung Hoon | - |
dc.contributor.author | Madak-Erdogan, Zeynep | - |
dc.contributor.author | Bae, Sung Chul | - |
dc.contributor.author | Carlson, Kathryn E. | - |
dc.contributor.author | Mayne, Christopher G. | - |
dc.contributor.author | Granick, Steve | - |
dc.contributor.author | Katzenellenbogen, Benita S. | - |
dc.contributor.author | Katzenellenbogen, John, A. | - |
dc.date.accessioned | 2023-12-22T00:48:26Z | - |
dc.date.available | 2023-12-22T00:48:26Z | - |
dc.date.created | 2016-11-16 | - |
dc.date.issued | 2015-08 | - |
dc.description.abstract | Estrogen 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.identifier.bibliographicCitation | JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, v.137, no.32, pp.10326 - 10335 | - |
dc.identifier.doi | 10.1021/jacs.5b05952 | - |
dc.identifier.issn | 0002-7863 | - |
dc.identifier.scopusid | 2-s2.0-84939865433 | - |
dc.identifier.uri | https://scholarworks.unist.ac.kr/handle/201301/20740 | - |
dc.identifier.url | http://pubs.acs.org/doi/abs/10.1021/jacs.5b05952 | - |
dc.identifier.wosid | 000359962000054 | - |
dc.language | 영어 | - |
dc.publisher | AMER CHEMICAL SOC | - |
dc.title | Ligand Accessibility and Bioactivity of a Hormone-Dendrimer Conjugate Depend on pH and pH History | - |
dc.type | Article | - |
dc.description.isOpenAccess | FALSE | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Multidisciplinary | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.subject.keywordPlus | BREAST-CANCER CELLS | - |
dc.subject.keywordPlus | RESPONSIVE CONFORMATIONAL-CHANGES | - |
dc.subject.keywordPlus | CARBONIC-ANHYDRASE-IX | - |
dc.subject.keywordPlus | ESTROGEN-RECEPTOR | - |
dc.subject.keywordPlus | PAMAM DENDRIMERS | - |
dc.subject.keywordPlus | GENE-EXPRESSION | - |
dc.subject.keywordPlus | DRUG-DELIVERY | - |
dc.subject.keywordPlus | IN-VITRO | - |
dc.subject.keywordPlus | EXTRANUCLEAR | - |
dc.subject.keywordPlus | DYNAMICS | - |
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