Mutation Information
Mutation Site
|
Y181C |
Mutation Type
|
Amino acid level |
Gene/Protein/Region Type
|
RT |
Literature Information
PubMed PMID
|
32883642
|
Published Year
|
2020 |
Journal
|
European journal of medicinal chemistry |
Title
|
New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
Author
|
Nalli M,Armijos Rivera JI,Masci D,Coluccia A,Badia R,Riveira-Muñoz E,Brambilla A,Cinquina E,Turriziani O,Falasca F,Catalano M,Limatola C,Esté JA,Maga G,Silvestri R,Crespan E,La Regina G |
Evidence
|
Among these, IAS 12 exhibited a remarkable antiviral activity against single and double mutants (K103N EC50 = <0.7 nM;Y181C EC50 = <0.7 nM;Y188L EC50 = 21.3 nM;K103N-Y181C EC50 = 6.2 nM), resulting equally or more active than previuosly reported IAS 6 and some approved anti-HIV-1 drugs.
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