RNA-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.

Compounds interfering with Embryonic Lethal Abnormal Vision (ELAV) protein–RNA complexes : an avenue for discovering new drugs / R. Nasti, D. Rossi, M. Amadio, A. Pascale, M.Y. Unver, A.K.H. Hirsch, S. Collina. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 60:2(2017 Oct 26), pp. 8257-8267. [10.1021/acs.jmedchem.6b01871]

Compounds interfering with Embryonic Lethal Abnormal Vision (ELAV) protein–RNA complexes : an avenue for discovering new drugs

R. Nasti;
2017-10-26

Abstract

RNA-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.
Settore CHIM/08 - Chimica Farmaceutica
JOURNAL OF MEDICINAL CHEMISTRY
Article (author)
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/679998
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