In vivo-BRET drug discovery platform for the identification of protein-protein interaction inhibitors of biomedical interest

Settore ERC
LS1_1 - Molecular biology and interactions
LS7_3 - Pharmacology, pharmacogenomics, drug discovery and design, drug therapy
Montanini Barbara

Aree / Gruppi di ricerca

Partecipanti al progetto

Descrizione del progetto

The research and development of a new drug is a lengthy and costly process, which requires considerable investment by the pharmaceutical industries, with a very low success rate and a constant need for innovative approaches. The so-called “reverse approach” (or target-based drug discovery) is based on the screening of small molecule libraries, to identify "hit compounds" capable of interacting and modulating the biological activity of the target of interest. In recent years, protein-protein interactions (PPI) have emerged as promising new targets, especially considering their key role in most cellular processes, under both physiological and pathological conditions.

The aim of this project is the development of an in vivo high-throughput platform based on the BRET (Bioluminescence Resonance Energy Transfer) technology as a tool to monitor PPI and to screen compound libraries for the identification of new potential PPI inhibitors.

Risultati e pubblicazioni

Sartini, S, Levati, E, Maccesi, M, Guerra, M, Spadoni, G, Bach, S, Benincasa, M, Scocchi, M, Ottonello, S, Rivara, S, & Montanini, B. (2019) New Antimicrobials Targeting Bacterial RNA Polymerase Holoenzyme Assembly Identified with an in Vivo BRET-Based Discovery Platform, ACS Chemical Biology, 14, 1727-1736.

Corbel, C, Sartini, S, Levati, E, Colas, P, Maillet, L, Couturier, C, Montanini, B., & Bach, S. P. (2017) Screening for Protein-Protein Interaction Inhibitors Using a Bioluminescence Resonance Energy Transfer (BRET)-Based Assay in Yeast, Slas Discovery, 22, 751-759.

Caputo, A, Sartini, S, Levati, E, Minato, I, Elisi, G. M, Di Stasi, A, Guillou, C, Goekjian, P. G, Garcia, P, Gueyrard, D, Bach, S. P, Comte, A, Ottonello, S, Rivara, S, &Montanini, B. (2022) An Optimized Workflow for the Discovery of New Antimicrobial Compounds Targeting Bacterial RNA Polymerase Complex Formation, Antibiotics, 11.

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