The merging of distinct computational approaches has become a powerful strategy for discovering new biologically active compounds. By using molecular modeling, significant efforts have recently resulted in the development of new molecules, demonstrating high efficiency in reducing the replication of severe acute respiratory coronavirus 2 (SARS-CoV-2), the agent responsible for the COVID-19 pandemic. We have focused our interest on non-structural protein Nsp13 (NTPase/helicase), as a crucial protein, embedded in the replication-transcription complex (RTC), that controls the virus life cycle. To assist in the identification of the most druggable surfaces of Nsps13, we applied a combination of four computational tools: FTMap, SiteMap, Fpocket and LigandScout. These software packages explored the binding sites for different three-dimensional structures of RTC complexes (PDB codes: 6XEZ, 7CXM, 7CXN), thus, detecting several hot spots, that were clustered to obtain ensemble consensus sites, through a combination of four different approaches. The comparison of data provided new insights about putative druggable sites that might be employed for further docking simulations on druggable surfaces of Nsps13, in a scenario of repurposing drugs.

In Silico Insights towards the Identification of SARS-CoV-2 NSP13 Helicase Druggable Pockets

Ricci, Federico;Gitto, Rosaria;Pitasi, Giovanna;De Luca, Laura
2022-01-01

Abstract

The merging of distinct computational approaches has become a powerful strategy for discovering new biologically active compounds. By using molecular modeling, significant efforts have recently resulted in the development of new molecules, demonstrating high efficiency in reducing the replication of severe acute respiratory coronavirus 2 (SARS-CoV-2), the agent responsible for the COVID-19 pandemic. We have focused our interest on non-structural protein Nsp13 (NTPase/helicase), as a crucial protein, embedded in the replication-transcription complex (RTC), that controls the virus life cycle. To assist in the identification of the most druggable surfaces of Nsps13, we applied a combination of four computational tools: FTMap, SiteMap, Fpocket and LigandScout. These software packages explored the binding sites for different three-dimensional structures of RTC complexes (PDB codes: 6XEZ, 7CXM, 7CXN), thus, detecting several hot spots, that were clustered to obtain ensemble consensus sites, through a combination of four different approaches. The comparison of data provided new insights about putative druggable sites that might be employed for further docking simulations on druggable surfaces of Nsps13, in a scenario of repurposing drugs.
2022
Inglese
ELETTRONICO
MDPI
12
4
482
493
12
10.3390/biom12040482
Internazionale
Esperti anonimi
COVID-19; FTMap; Fpocket; LigandScout software packages; Nsp13; SiteMap; binding site prediction; protein structure; Binding Sites; COVID-19; Humans; Pandemics; Antiviral Agents; RNA Helicases; SARS-CoV-2; Viral Nonstructural Proteins
info:eu-repo/semantics/article
Ricci, Federico; Gitto, Rosaria; Pitasi, Giovanna; De Luca, Laura
14.a Contributo in Rivista::14.a.1 Articolo su rivista
4
262
none
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11570/3237853
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