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Novel Compounds Targeting the RNA-Binding Protein HuR. Structure-Based Design, Synthesis, and Interaction Studies

Della Volpe, S., Nasti, R., Queirolo, M., Unver, M. Y., Jumde, V. K., Dömling, A., Vasile, F., Potenza, D., Ambrosio, F. A., Costa, G., Alcaro, S., Zucal, C., Provenzani, A., Di Giacomo, M., Rossi, D., Hirsch, A. K. H. & Collina, S., 11-Apr-2019, In : Bioorganic & Medicinal Chemistry Letters. 10, 4, p. 615-620 6 p.

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  • Novel Compounds Targeting the RNA-Binding Protein HuR.Structure-Based Design, Synthesis, and Interaction Studies

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DOI

  • Serena Della Volpe
  • Rita Nasti
  • Michele Queirolo
  • M Yagiz Unver
  • Varsha K Jumde
  • Alexander Dömling
  • Francesca Vasile
  • Donatella Potenza
  • Francesca Alessandra Ambrosio
  • Giosué Costa
  • Stefano Alcaro
  • Chiara Zucal
  • Alessandro Provenzani
  • Marcello Di Giacomo
  • Daniela Rossi
  • Anna K H Hirsch
  • Simona Collina

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.

Original languageEnglish
Pages (from-to)615-620
Number of pages6
JournalBioorganic & Medicinal Chemistry Letters
Volume10
Issue number4
Publication statusPublished - 11-Apr-2019

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