Mutation Information
Mutation Site
|
E138K |
Mutation Type
|
Amino acid level |
Gene/Protein/Region Type
|
RT |
Relevant Drug
|
NNRTIs |
Literature Information
PubMed PMID
|
32712537
|
Published Year
|
2020 |
Journal
|
European journal of medicinal chemistry |
Title
|
Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
Author
|
Chen X,Ding L,Tao Y,Pannecouque C,De Clercq E,Zhuang C,Chen FE |
Evidence
|
Among all the chiral derivatives, (S)-(-)-12a showed the best potency with the antiviral activities against wild-type (WT) and single mutant strains (L100I, K103 N, Y181C, E138K;especially Y188L), and RT enzyme in the low nanomolar concentration range.
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