Related Experiment Video
Updated: Apr 25, 2026

Assembly and Purification of Prototype Foamy Virus Intasomes
Published on: March 19, 2018
Modular assembly of purine-like bisphosphonates as inhibitors of HIV-1 reverse transcriptase
Cyrus M Lacbay1, John Mancuso, Yih-Shyan Lin
1Department of Chemistry, McGill University , 801 Sherbrooke Street West, Montreal, Quebec H3A 0B8, Canada.
Abstract:
Bisphosphonates can mimic the pyrophosphate leaving group of the nucleotidyl transfer reaction and effectively inhibit RNA/DNA polymerases. In a search of HIV-1 reverse transcriptase (RT) inhibitors, a new chemotype of nonhydrolyzable purine diphosphate mimic was synthesized. A modular synthetic protocol was developed, utilizing 2-amino-6-(methylthio)-4-(trimethylsilyl)nicotinonitrile as the key synthon in the preparation of highly substituted 2-aminonicotinonitriles. These building blocks were subsequently elaborated to the pyrido[2,3-d]pyrimidine bisphosphonates (PYPY-BPs). Biochemical screening identified analogs of PYPY-BPs that inhibit HIV-1 RT-catalyzed DNA synthesis.
More Related Videos
10:29Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
07:22A High-throughput Cre-Lox Activated Viral Membrane Fusion Assay to Identify Inhibitors of HIV-1 Viral Membrane Fusion
Published on: August 14, 2018
Related Concept Videos
Inhibitors of Viral Protein Synthesis
Inhibitors of Bacterial DNA Synthesis
Inhibitors of Bacterial Protein Synthesis
Protein Complex Assembly
Many viruses self-assemble into a fully functional unit using the infected host cell to...
Retrovirus Life Cycles