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The role of 2',3'-unsaturation on the antiviral activity of anti-HIV nucleosides against 3TC-resistant mutant (M184V).
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2003 Jun 16; Vol. 13 (12), pp. 1993-6. - Publication Year :
- 2003
-
Abstract
- Molecular modeling studies show that the 2',3'-double bond of the sugar moiety of various 2',3'-unsaturated nucleosides interacts with the aromatic moiety of Tyr115 of HIV-1 reverse transcriptase (RT) by hydrophobic pi-pi interaction. In 3TC-resistant mutant (M184V) RT, 2'-fluoro-2',3'-unsaturated nucleosides with a bulky 4'-substituent experience significant steric hindrance with the side chain of Val184.
- Subjects :
- Amino Acid Substitution
Drug Resistance, Viral
HIV Reverse Transcriptase chemistry
HIV Reverse Transcriptase genetics
HIV Reverse Transcriptase metabolism
HIV-1 enzymology
HIV-1 genetics
Lamivudine pharmacology
Models, Molecular
Molecular Conformation
Mutation
Nucleosides metabolism
Reverse Transcriptase Inhibitors chemistry
Reverse Transcriptase Inhibitors pharmacology
Structure-Activity Relationship
Tyrosine chemistry
Tyrosine metabolism
Anti-HIV Agents chemistry
Anti-HIV Agents pharmacology
HIV Reverse Transcriptase antagonists & inhibitors
HIV-1 drug effects
Nucleosides chemistry
Nucleosides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 13
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 12781181
- Full Text :
- https://doi.org/10.1016/s0960-894x(03)00330-5