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In Silico Screening of Drugs That Target Different Forms of E Protein for Potential Treatment of COVID-19.
Ramírez Salinas, Gema Lizbeth; López Rincón, Alejandro; García Machorro, Jazmín; Correa Basurto, José; Martínez Archundia, Marlet.
Afiliação
  • Ramírez Salinas GL; Laboratorio de Diseño y Desarrollo de Nuevos Fármacos e Innovación Biotecnológica (Laboratory for the Design and Development of New Drugs and Biotechnological Innovation), Escuela Superior de Medicina, Instituto Politécnico Nacional, México City 11340, Mexico.
  • López Rincón A; Utrecht Institute for Pharmaceutical Sciences, Division Pharmacology, Utrecht University, 3553 Utrecht, The Netherlands.
  • García Machorro J; Julius Center for Health Sciences and Primary Care, Department of Data Science, University Medical Center Utrecht, 3553 Utrecht, The Netherlands.
  • Correa Basurto J; Laboratorio de Medicina de Conservación, Escuela Superior de Medicina, Instituto Politécnico Nacional, México City 11340, Mexico.
  • Martínez Archundia M; Laboratorio de Diseño y Desarrollo de Nuevos Fármacos e Innovación Biotecnológica (Laboratory for the Design and Development of New Drugs and Biotechnological Innovation), Escuela Superior de Medicina, Instituto Politécnico Nacional, México City 11340, Mexico.
Pharmaceuticals (Basel) ; 16(2)2023 Feb 14.
Article em En | MEDLINE | ID: mdl-37259437
Recently the E protein of SARS-CoV-2 has become a very important target in the potential treatment of COVID-19 since it is known to regulate different stages of the viral cycle. There is biochemical evidence that E protein exists in two forms, as monomer and homopentamer. An in silico screening analysis was carried out employing 5852 ligands (from Zinc databases), and performing an ADMET analysis, remaining a set of 2155 compounds. Furthermore, docking analysis was performed on specific sites and different forms of the E protein. From this study we could identify that the following ligands showed the highest binding affinity: nilotinib, dutasteride, irinotecan, saquinavir and alectinib. We carried out some molecular dynamics simulations and free energy MM-PBSA calculations of the protein-ligand complexes (with the mentioned ligands). Of worthy interest is that saquinavir, nilotinib and alectinib are also considered as a promising multitarget ligand because it seems to inhibit three targets, which play an important role in the viral cycle. On the other side, saquinavir was shown to be able to bind to E protein both in its monomeric as well as pentameric forms. Finally, further experimental assays are needed to probe our hypothesis derived from in silico studies.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Tipo de estudo: Diagnostic_studies / Screening_studies Idioma: En Ano de publicação: 2023 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Tipo de estudo: Diagnostic_studies / Screening_studies Idioma: En Ano de publicação: 2023 Tipo de documento: Article