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Novel Compounds Targeting the RNA-Binding Protein HuR. Structure-Based Design, Synthesis, and Interaction Studies.
Della Volpe, Serena Nasti, Rita Queirolo, Michele Unver, M Yagiz Jumde, Varsha K Dömling, Alexander Vasile, Francesca Potenza, Donatella Ambrosio, Francesca Alessandra Costa, Giosué
Della Volpe, Serena
Nasti, Rita
Queirolo, Michele
Unver, M Yagiz
Jumde, Varsha K
Dömling, Alexander
Vasile, Francesca
Potenza, Donatella
Ambrosio, Francesca Alessandra
Costa, Giosué
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2019-01-21
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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.
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ACS Med Chem Lett. 2019;10(4):615-620. Published 2019 Jan 21. doi:10.1021/acsmedchemlett.8b00600.
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PMC6466816
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Article
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en
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1948-5875
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Attribution-NonCommercial-ShareAlike 4.0 International