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Compounds Interfering with Embryonic Lethal Abnormal Vision (ELAV) Protein–RNA Complexes: An Avenue for Discovering New Drugs
journal contribution
posted on 2017-06-06, 00:00 authored by Rita Nasti, Daniela Rossi, Marialaura Amadio, Alessia Pascale, M. Yagiz Unver, Anna K. H. Hirsch, Simona CollinaRNA-binding proteins play a key role
in post-transcriptional processes. Among these proteins, embryonic
lethal abnormal vision (ELAV) proteins are among the best described.
ELAV proteins predominantly act as positive regulators of gene expression,
and their dysregulation is involved in several pathologies, such as
cancer, inflammation, and neurodegenerative diseases. Only a few structurally
unrelated compounds interfering with ELAV protein–mRNA
complexes have been identified by applying high-throughput screening
approaches. Considering the structural diversity of the compounds
discovered so far and the different techniques employed for screening
their ability to interfere with ELAV protein–mRNA complexes,
drawing conclusions from structure–activity relationships remains
a challenge. We performed docking studies to understand the interactions
of compounds reported over the past decade to be inhibitors of ELAV
proteins and to evaluate the potential of computer-aided drug design
to target this family of proteins for further drug discovery.