dc.creator | Xu, Jimin | es |
dc.creator | Berastegui-Cabrera, Judith | es |
dc.creator | Carretero Ledesma, Marta Claudia | es |
dc.creator | Chen, Haiying | es |
dc.creator | Xue, Yu | es |
dc.creator | Wold, Eric A. | es |
dc.creator | Pachón Díaz, Jerónimo | es |
dc.creator | Sánchez Céspedes, Javier | es |
dc.date.accessioned | 2021-05-21T10:47:57Z | |
dc.date.available | 2021-05-21T10:47:57Z | |
dc.date.issued | 2021-02-05 | |
dc.identifier.citation | Xu, J., Berastegui-Cabrera, J., Carretero Ledesma, M.C., Chen, H., Xue, Y., Wold, E.A.,...,Sánchez Céspedes, J. (2021). Discovery of a small molecule inhibitor of human adenovirus capable of preventing escape from the endosome. International journal of molecular sciences, 22 (4) | |
dc.identifier.issn | 1661-6596 | es |
dc.identifier.issn | 1422-0067(electrónico) | es |
dc.identifier.uri | https://hdl.handle.net/11441/109188 | |
dc.description.abstract | Human adenoviruses (HAdVs) display a wide range of tissue tropism and can cause an
array of symptoms from mild respiratory illnesses to disseminated and life-threatening infections
in immunocompromised individuals. However, no antiviral drug has been approved specifically
for the treatment of HAdV infections. Herein, we report our continued efforts to optimize salicylamide derivatives and discover compound 16 (JMX0493) as a potent inhibitor of HAdV infection.
Compound 16 displays submicromolar IC50 values, a higher selectivity index (SI > 100) and 2.5-fold
virus yield reduction compared to our hit compound niclosamide. Moreover, unlike niclosamide,
our mechanistic studies suggest that the antiviral activity of compound 16 against HAdV is achieved
through the inhibition of viral particle escape from the endosome, which bars subsequent uncoating
and the presentation of lytic protein VI. | es |
dc.description.sponsorship | Programa de Comercialización de Tecnología UTMB,John D. Stobo, M. D. Distinguished Chair Endowment Fund (para JZ) y John Sealy Memorial. Fondo de Dotación en UTMB, Plan Nacional de I + D + i 2013–2016 | es |
dc.description.sponsorship | Instituto de Salud Carlos III,Subdirección General de Redes y Centros de Investigación Cooperativa, Ministerio de Economía, Industria y Competitividad, Red Española de Investigación en Enfermedades Infecciosas REIPI RD16 / 0016/0009 | es |
dc.description.sponsorship | Cofinanciado por el Fondo Regional de Desarrollo Europeo “Una manera de lograr Europa”, Operativo programa Crecimiento Inteligente 20142020, el Instituto de Salud Carlos III, Proyectos de Investigación en Salud PI15 / 00489 y Proyectos de Desarrollo Tecnológico en Salud DTS17 / 00130 | es |
dc.description.sponsorship | Servicio Andaluz de Salud, Junta de Andalucía C-0059-2018 | es |
dc.format | application/pdf | es |
dc.format.extent | 21 p. | es |
dc.language.iso | eng | es |
dc.publisher | MDPI | es |
dc.relation.ispartof | International journal of molecular sciences, 22 (4) | |
dc.rights | Attribution-NonCommercial-NoDerivatives 4.0 Internacional | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | * |
dc.subject | Antiviral agent | es |
dc.subject | Adenovirus | es |
dc.subject | Salicylamide derivatives | es |
dc.subject | Entry inhibition | es |
dc.title | Discovery of a small molecule inhibitor of human adenovirus capable of preventing escape from the endosome | es |
dc.type | info:eu-repo/semantics/article | es |
dcterms.identifier | https://ror.org/03yxnpp24 | |
dc.type.version | info:eu-repo/semantics/publishedVersion | es |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | es |
dc.contributor.affiliation | Universidad de Sevilla. Departamento de Medicina | es |
dc.relation.projectID | I + D + i 2013–2016 | es |
dc.relation.projectID | REIPI RD16 / 0016/0009 | es |
dc.relation.projectID | PI15 / 00489 | es |
dc.relation.projectID | DTS17 / 00130 | es |
dc.relation.publisherversion | https://doi.org/10.3390/ijms22041617 | es |
dc.identifier.doi | 10.3390/ijms22041617 | es |
dc.journaltitle | International journal of molecular sciences | es |
dc.publication.volumen | 22 | es |
dc.publication.issue | 4 | es |