Related Experiment Video
Updated: May 3, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Fluorinated mechanism-based inhibitors: common themes and recent developments
Christina Tysoe, Stephen G Withers1
1Department of Chemistry, University of British Columbia, 2036, Main Mall, Vancouver, British Columbia, V6T 1Z1, Canada. withers@chem.ubc.ca.
Abstract:
Mechanism-based inhibitors are relatively chemically inert compounds that become activated when processed by their target enzyme, leading to covalent enzyme inactivation. Fluorine substitution confers a number of properties that are beneficial to the chemistry of such inhibitors and to their potential use as pharmaceuticals, and indeed several fluorinated mechanism-based inhibitors have made it to clinical usage over the past 50 years. Well-known examples are the 5- fluorouracil metabolite, 5-fluoro-2'-deoxyuridine-5'-monophosphate, which is used in the treatment of cancer, and α- difluoromethylornithine for the treatment of African sleeping sickness. As the prevalence of fluorine in medicinal chemistry continues to rise, more and more medically relevant fluorinated mechanism-based inhibitors are being developed with a variety of interesting properties and uses.
Related Concept Videos
Inhibitors of Bacterial DNA Synthesis
Inhibitors of Viral Protein Synthesis
Anthelminthic Agents
Enzyme Inhibition
FISH - Fluorescent In-situ Hybridization
Gene Regulation in Microbial Communities: Quorum Sensing

