Mutation Information
Mutation Site
|
E138K |
Mutation Type
|
Amino acid level |
Gene/Protein/Region Type
|
RT |
Relevant Drug
|
NNRTIs |
Literature Information
PubMed PMID
|
32528834
|
Published Year
|
2020 |
Journal
|
Acta pharmaceutica Sinica. B |
Title
|
Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs. |
Author
|
Kang D,Feng D,Ginex T,Zou J,Wei F,Zhao T,Huang B,Sun Y,Desta S,De Clercq E,Pannecouque C,Zhan P,Liu X |
Evidence
|
Especially, compound 26 exhibited the most potent activity against wild-type and a panel of single mutations (L100I, K103N, Y181C, Y188L and E138K) with an EC50 ranging from 6.02 to 23.9 nmol/L, which were comparable to those of etravirine (ETR).
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