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dc.contributor.author
Gray, William T.
dc.contributor.author
Frey, Kathleen M.
dc.contributor.author
Laskey, Sarah B.
dc.contributor.author
Mislak, Andrea C.
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Spasov, Krasimir A.
dc.contributor.author
Lee, Won Gil
dc.contributor.author
Bollini, Mariela
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dc.contributor.author
Siliciano, Robert F.
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Jorgensen, William L.
dc.contributor.author
Anderson, Karen S.
dc.date.available
2017-05-03T19:48:36Z
dc.date.issued
2015-09
dc.identifier.citation
Gray, William T.; Frey, Kathleen M.; Laskey, Sarah B.; Mislak, Andrea C.; Spasov, Krasimir A.; et al.; Potent inhibitors active against HIV reverse transcriptase with K101P, a mutation conferring rilpivirine resistance; American Chemical Society; ACS Medicinal Chemistry Letters; 6; 10; 9-2015; 1075-1079
dc.identifier.uri
http://hdl.handle.net/11336/15923
dc.description.abstract
Catechol diether compounds have nanomolar antiviral and enzymatic activity against HIV with reverse transcriptase (RT) variants containing K101P, a mutation that confers high-level resistance to FDA-approved non-nucleoside inhibitors efavirenz and rilpivirine. Kinetic data suggests that RT (K101P) variants are as catalytically fit as wild-type and thus can potentially increase in the viral population as more antiviral regimens include efavirenz or rilpivirine. Comparison of wild-type structures and a new crystal structure of RT (K101P) in complex with a leading compound confirms that the K101P mutation is not a liability for the catechol diethers while suggesting that key interactions are lost with efavirenz and rilpivirine.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
American Chemical Society
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dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
Hiv
dc.subject
Rreverse Transcriptase
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Non-Nucleoside Reverse Transcriptase Inhibitors
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Resistance
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Mutations
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Otras Ciencias Químicas
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dc.subject.classification
Ciencias Químicas
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dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
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dc.title
Potent inhibitors active against HIV reverse transcriptase with K101P, a mutation conferring rilpivirine resistance
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2017-04-28T17:10:06Z
dc.identifier.eissn
1948-5875
dc.journal.volume
6
dc.journal.number
10
dc.journal.pagination
1075-1079
dc.journal.pais
Estados Unidos
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dc.journal.ciudad
Washington
dc.description.fil
Fil: Gray, William T.. University of Yale; Estados Unidos
dc.description.fil
Fil: Frey, Kathleen M.. University of Yale; Estados Unidos
dc.description.fil
Fil: Laskey, Sarah B.. University Johns Hopkins; Estados Unidos
dc.description.fil
Fil: Mislak, Andrea C.. University of Yale; Estados Unidos
dc.description.fil
Fil: Spasov, Krasimir A.. University of Yale; Estados Unidos
dc.description.fil
Fil: Lee, Won Gil. University of Yale; Estados Unidos
dc.description.fil
Fil: Bollini, Mariela. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. University of Yale; Estados Unidos
dc.description.fil
Fil: Siliciano, Robert F.. University Johns Hopkins; Estados Unidos. Howard Hughes Medial Institute; Estados Unidos
dc.description.fil
Fil: Jorgensen, William L.. University of Yale; Estados Unidos
dc.description.fil
Fil: Anderson, Karen S.. University of Yale; Estados Unidos
dc.journal.title
ACS Medicinal Chemistry Letters
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1021/acsmedchemlett.5b00254
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://pubs.acs.org/doi/10.1021/acsmedchemlett.5b00254
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4601059/
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