|
Mutation Information
|
Mutation Site
|
K103N |
|
Mutation Type
|
Amino acid level |
|
Gene/Protein/Region Type
|
RT |
Literature Information
|
PubMed PMID
|
33279288
|
|
Published Year
|
2021 |
|
Journal
|
European journal of medicinal chemistry |
|
Title
|
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. |
|
Author
|
Jiang X,Huang B,Olotu FA,Li J,Kang D,Wang Z,De Clercq E,Soliman MES,Pannecouque C,Liu X,Zhan P |
|
Evidence
|
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).
|
|
|
HIV Mutation Detail Information