Mutation Information
Mutation Site
|
T174I |
Mutation Type
|
Amino acid level |
Gene/Protein/Region Type
|
IN |
Literature Information
PubMed PMID
|
33316407
|
Published Year
|
2021 |
Journal
|
Bioorganic & medicinal chemistry letters |
Title
|
Discovery of novel HIV-1 integrase-LEDGF/p75 allosteric inhibitors based on a pyridine scaffold forming an intramolecular hydrogen bond. |
Author
|
Sugiyama S,Akiyama T,Taoda Y,Iwaki T,Matsuoka E,Akihisa E,Seki T,Yoshinaga T,Kawasuji T |
Evidence
|
Compound 34f exhibited better antiviral potency against WT and the T174I mutant (EC50 (WT) = 6.6 nM, EC50 (T174I) = 270 nM) than BI 224436 (EC50 (WT) = 22 nM, EC50 (T174I) > 5000 nM).
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