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http://hdl.handle.net/2445/44407
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DC Field | Value | Language |
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dc.contributor.author | López-Senín, Paula | - |
dc.contributor.author | Gómez-Pinto, Irene | - |
dc.contributor.author | Grandas Sagarra, Anna | - |
dc.contributor.author | Marchán Sancho, Vicente | - |
dc.date.accessioned | 2013-06-25T08:38:59Z | - |
dc.date.available | 2020-11-01T06:10:17Z | - |
dc.date.issued | 2011 | - |
dc.identifier.issn | 0947-6539 | - |
dc.identifier.uri | http://hdl.handle.net/2445/44407 | - |
dc.description.abstract | We describe the use of dynamic combinatorial chemistry (DCC) to identify ligands for the stem-loop structure located at the exon 10-5'-intron junction of Tau pre-mRNA, which is involved in the onset of several tauopathies including frontotemporal dementia with Parkinsonism linked to chromosome 17 (FTDP-17). A series of ligands that combine the small aminoglycoside neamine and heteroaromatic moieties (azaquinolone and two acridines) have been identified by using DCC. These compounds effectively bind the stem-loop RNA target (the concentration required for 50% RNA response (EC(50)): 2-58 μM), as determined by fluorescence titration experiments. Importantly, most of them are able to stabilize both the wild-type and the +3 and +14 mutated sequences associated with the development of FTDP-17 without producing a significant change in the overall structure of the RNA (as analyzed by circular dichroism (CD) spectroscopy), which is a key factor for recognition by the splicing regulatory machinery. A good correlation has been found between the affinity of the ligands for the target and their ability to stabilize the RNA secondary structure. | - |
dc.format.extent | 14 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Wiley-VCH | - |
dc.relation.isformatof | Versió preprint del document publicat a: http://dx.doi.org/10.1002/chem.201002065 | - |
dc.relation.ispartof | Chemistry-A European Journal, 2011, vol. 17, num. 6, p. 1946-1953 | - |
dc.relation.uri | http://dx.doi.org/10.1002/chem.201002065 | - |
dc.rights | (c) Wiley-VCH, 2011 | - |
dc.source | Articles publicats en revistes (Química Inorgànica i Orgànica) | - |
dc.subject.classification | Química combinatòria | - |
dc.subject.classification | Bioquímica | - |
dc.subject.classification | RNA | - |
dc.subject.classification | Reconeixement molecular | - |
dc.subject.other | Combinatorial chemistry | - |
dc.subject.other | Biochemistry | - |
dc.subject.other | RNA | - |
dc.subject.other | Molecular recognition | - |
dc.title | Identification of Ligands for the Tau Exon 10 Splicing Regulatory Element RNA Using Dynamic Combinatorial Chemistry | eng |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/submittedVersion | - |
dc.identifier.idgrec | 586607 | - |
dc.date.updated | 2013-06-21T06:39:16Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
Appears in Collections: | Articles publicats en revistes (Química Inorgànica i Orgànica) |
Files in This Item:
File | Description | Size | Format | |
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586607.pdf | 180.1 kB | Adobe PDF | View/Open |
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