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Selectivity for strand-transfer over 3′-processing and susceptibility to clinical resistance of HIV-1 integrase inhibitors are driven by key enzyme–DNA interactions in the active site

Integrase strand transfer inhibitors (INSTIs) are highly effective against HIV infections. Co-crystal structures of the prototype foamy virus intasome have shown that all three FDA-approved drugs, raltegravir (RAL), elvitegravir and dolutegravir (DTG), act as interfacial inhibitors during the strand...

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Detalles Bibliográficos
Autores principales: Métifiot, Mathieu, Johnson, Barry C., Kiselev, Evgeny, Marler, Laura, Zhao, Xue Zhi, Burke, Terrence R., Marchand, Christophe, Hughes, Stephen H., Pommier, Yves
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Oxford University Press 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5001616/
https://www.ncbi.nlm.nih.gov/pubmed/27369381
http://dx.doi.org/10.1093/nar/gkw592