Article
A single conservative amino acid substitution in the reverse transcriptase of human immunodeficiency virus-1 confers resistance to (+)-(5S)-4,5,6,7-tetrahydro-5-methyl-6-(3-methyl-2-butenyl)imidazo[4,5, 1- jk][1,4]benzodiazepin-2(1H)-thione (TIBO R82150).
Molecular pharmacology - 1 Jan 1993
Mellors J W, Im G J, Tramontano E, Winkler S R, Medina D J, Dutschman G E, Bazmi H Z, Piras G, Gonzalez C J, Cheng Y C
Abstract excerpt
Tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione (TIBO) derivatives (e.g., R82150) are potent, human immunodeficiency virus-1 (HIV-1)-specific, inhibitors of reverse transcriptase (RT) that are undergoing initial evaluation in clinical trials. Because HIV-1 has become resistant...
Topics
- Antiviral Agents
- Base Sequence
- Benzodiazepines
- Drug Resistance
- HIV Reverse Transcriptase
- HIV-1
- Humans
- Imidazoles
- Molecular Sequence Data
- Mutation
- Phenotype
- Proviruses
- RNA-Directed DNA Polymerase