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Titel: Novel Compounds Targeting the RNA-Binding Protein HuR. Structure-Based Design, Synthesis, and Interaction Studies
VerfasserIn: Della Volpe, Serena
Nasti, Rita
Queirolo, Michele
Unver, M. Yagiz
Jumde, Varsha K.
Dömling, Alexander
Vasile, Francesca
Potenza, Donatella
Ambrosio, Francesca Alessandra
Costa, Giosué
Alcaro, Stefano
Zucal, Chiara
Provenzani, Alessandro
Di Giacomo, Marcello
Rossi, Daniela
Hirsch, Anna K. H.
Collina, Simona
Sprache: Englisch
Titel: ACS Medicinal Chemistry Letters
Bandnummer: 10
Heft: 4
Seiten: 615-620
Verlag/Plattform: American Chemical Society
Erscheinungsjahr: 2019
Freie Schlagwörter: RNA-binding protein
HuR−RNA complexes
STD-NMR
virtual screening
multicomponent reactions
DDC-Sachgruppe: 500 Naturwissenschaften
Dokumenttyp: Journalartikel / Zeitschriftenartikel
Abstract: The key role of RNA-binding proteins (RBPs) in regulating post-transcriptional processes and their involvement in several pathologies (i.e., cancer and neurodegeneration) have highlighted their potential as therapeutic targets. In this scenario, Embryonic Lethal Abnormal Vision (ELAV) or Hu proteins and their complexes with target mRNAs have been gaining growing attention. Compounds able to modulate the complex stability could constitute an innovative pharmacological strategy for the treatment of numerous diseases. Nevertheless, medicinal-chemistry efforts aimed at developing such compounds are still at an early stage. As part of our ongoing research in this field, we hereby present the rational design and synthesis of structurally novel HuR ligands, potentially acting as HuR−RNA interferers. The following assessment of the structural features of their interaction with HuR, combining saturation-transfer difference NMR and in silico studies, provides a guide for further research on the development of new effective interfering compounds of the HuR−RNA complex
DOI der Erstveröffentlichung: 10.1021/acsmedchemlett.8b00600
URL der Erstveröffentlichung: https://pubs.acs.org/doi/10.1021/acsmedchemlett.8b00600
Link zu diesem Datensatz: urn:nbn:de:bsz:291--ds-390916
hdl:20.500.11880/35250
http://dx.doi.org/10.22028/D291-39091
ISSN: 1948-5875
Datum des Eintrags: 17-Feb-2023
Bezeichnung des in Beziehung stehenden Objekts: Supporting Information
In Beziehung stehendes Objekt: https://pubs.acs.org/doi/suppl/10.1021/acsmedchemlett.8b00600/suppl_file/ml8b00600_si_001.pdf
Fakultät: NT - Naturwissenschaftlich- Technische Fakultät
Fachrichtung: NT - Pharmazie
Professur: NT - Prof. Dr. Anna Hirsch
Sammlung:SciDok - Der Wissenschaftsserver der Universität des Saarlandes

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