Mutation Information
Mutation Site
|
N236T |
Mutation Type
|
Amino acid level |
Gene/Protein/Region Type
|
RT |
Immune Escape
|
Y |
Relevant Drug
|
adefovir (ADV);adefovir dipivoxil (ADV) |
Literature Information
PubMed PMID
|
32084506
|
Published Year
|
2020 |
Journal
|
Antiviral research |
Title
|
7-Deaza-7-fluoro modification confers on 4'-cyano-nucleosides potent activity against entecavir/adefovir-resistant HBV variants and favorable safety. |
Author
|
Hayashi S,Higashi-Kuwata N,Das D,Tomaya K,Yamada K,Murakami S,Venzon DJ,Hattori SI,Isogawa M,Sarafianos SG,Mitsuya H,Tanaka Y |
Evidence
|
Southern blot analysis using wild-type HBV (HBVWT)-encoding-plasmid-transfected HepG2 cells revealed that CdFA efficiently suppresses the production of HBVWT (IC50 = 153.7 nM), entecavir (ETV)-resistant HBV carrying L180M/S202G/M204V substitutions (HBVETV(R); IC50 = 373.2 nM), and adefovir dipivoxil (ADV)-resistant HBV carrying A181T/N236T substitutions (HBVADV(R); IC50=192.6 nM), whereas ETV and ADV were less potent against HBVETV(R) and HBVADV(R) (IC50: >1,000 and 4,022.5 nM, respectively).
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