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Mutation Information
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Mutation Site
|
F227L |
|
Mutation Type
|
Amino acid level |
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Gene/Protein/Region Type
|
RT |
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Combined Mutation
|
rt.V106A+rt.F227L |
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Relevant Drug
|
NNRTIs |
Literature Information
|
PubMed PMID
|
32712537
|
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Published Year
|
2020 |
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Journal
|
European journal of medicinal chemistry |
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Title
|
Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
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Author
|
Chen X,Ding L,Tao Y,Pannecouque C,De Clercq E,Zhuang C,Chen FE |
|
Evidence
|
Toward double mutant virus strains (F227L + V106A, RES056), (S)-(−)-12a possessed submicromolar antiviral activities. In addition, (S)-(−)-12a showed a high cell-based selectivity index (SI WT = 5822) and no apparent toxicity was observed in the in vivo acute toxicity assay and electrocardiogram.
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HIV Mutation Detail Information