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

ROSSI, DANIELA;AMADIO, MARIALAURA;PASCALE, ALESSIA ANGELA;COLLINA, SIMONA
2017-01-01

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.
2017
Chemistry & Analysis covers research on natural and laboratory syntheses, chemical structure, structure-function relationship, isolation and analyses of biologically significant molecules, medicinal and food chemistry. Technical material describing crucial chemical methods in biochemical analysis and research is also placed in this category. Resources covering general biochemistry and natural metabolic pathways are excluded.
Esperti anonimi
Inglese
Internazionale
STAMPA
60
20
8257
8267
11
AU-RICH ELEMENT; MESSENGER-RNA; BINDING PROTEINS; ALZHEIMERS-DISEASE; RECOGNITION MOTIF; NERVOUS-SYSTEM; HUR; CANCER; DROSOPHILA; IDENTIFICATION
7
info:eu-repo/semantics/article
262
Nasti, R; Rossi, Daniela; Amadio, Marialaura; Pascale, ALESSIA ANGELA; Unver M., Y.; Hirsch A. K., H.; Collina, Simona
1 Contributo su Rivista::1.1 Articolo in rivista
none
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11571/1202248
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