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Mutation Information
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Mutation Site
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E138K |
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Mutation Type
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Amino acid level |
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Gene/Protein/Region Type
|
RT |
Literature Information
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PubMed PMID
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33279288
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Published Year
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2021 |
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Journal
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European journal of medicinal chemistry |
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Title
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Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp3 values and favorable drug-like properties. |
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Author
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Jiang X,Huang B,Olotu FA,Li J,Kang D,Wang Z,De Clercq E,Soliman MES,Pannecouque C,Liu X,Zhan P |
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Evidence
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The most active inhibitor 10c exhibited outstanding antiviral activity against most of the viral panel, being about 2-fold (wild-type, EC50 = 0.0021 μM), 1.7-fold (K103N, EC50 = 0.0019 μM), and slightly more potent (E138K, EC50 = 0.0075 μM) than the NNRTI drug etravirine (ETR).
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HIV Mutation Detail Information