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Screening of small molecules to fight SARS-CoV-2 by combining novel approaches and sustainability

Project description

A novel drug discovery sensor against SARS-CoV-2

The SARS-CoV-2 pandemic has emphasised the need for antiviral drugs capable of inhibiting the pathogenicity of the virus. The proposed approach of the EU-funded SPOTLESS project relies on targeting the viral glycoprotein S known for its central role in virus attachment, fusion and entry into the host cell. To exert its function, the S glycoprotein must first be modified and activated by host cell proprotein convertases (PCs). To improve the drug screening process against PCs, the project proposes to develop novel sensors of cleavage having "cell-death" as readout in HTS settings. Implementation of the SPOTLESS strategy will simplify and expedite the drug discovery pipeline using a novel sustainable approach.

Objective

The novel SARS-CoV-2 is a lethal human pathogen with no FDA approved vaccines or drugs. An important step of the virus life-cycle is the viral glycoprotein S activation by Proprotein Convertases (PCs) which are proteases with a broad spectrum of cellular substrates. Inhibition of the processing step locks the virus into a form which eventually is no more pathogenic. Therefore, PCs represent attractive drug targets to fight against SARS-CoV-2. To date, there are no PCs inhibitors available for the in vivo use. Here, I propose three approaches to look for small molecule inhibitors of PCs, exploiting the virus cleavage site. Beside the classical in vitro screening, I aim to exploit novel PCs sensor platforms based on innovative ideas to ameliorate and simplify the readout. One attempt will see the use of luciferase reporters on the blueprint of sensors that I have recently published; following a second method, I will take advantage of the cellular death machinery as an on/off cleavage signal. In turn, these virtuous assays will contribute to a sustainable research approach. Novel PCs inhibitors are of great value against Covid-19 infections. Importantly, the inhibitors can be re-purposed against novel emerging pathogens, if necessary. Indeed, PCs dependence is becoming a distinctive mark of severe pathogenicity.

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Topic(s)

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MSCA-IF - Marie Skłodowska-Curie Individual Fellowships (IF)

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Call for proposal

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(opens in new window) H2020-MSCA-IF-2020

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Coordinator

UNIVERSITA DEGLI STUDI DI PADOVA
Net EU contribution

Net EU financial contribution. The sum of money that the participant receives, deducted by the EU contribution to its linked third party. It considers the distribution of the EU financial contribution between direct beneficiaries of the project and other types of participants, like third-party participants.

€ 257 209,92
Address
VIA 8 FEBBRAIO 2
35122 PADOVA
Italy

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Region
Nord-Est Veneto Padova
Activity type
Higher or Secondary Education Establishments
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Total cost

The total costs incurred by this organisation to participate in the project, including direct and indirect costs. This amount is a subset of the overall project budget.

€ 257 209,92
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