Metabolism of Nucleosides and Nucleotides Prodrugs
Coralie De Schutter1, Maryam Ehteshami1, Emily T Hammond1
1Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta,United States.
Background:
Modified nucleoside and nucleotide analogs are now the cornerstone of antiviral and anticancer chemotherapies. However, these compounds are not active on their own and need, after entering the cell, to be metabolized to their active 5'-triphosphate form.
Methods:
Limitations of these metabolic processes led to development of nucleoside/nucleotide prodrugs in which nucleosides are masked with different groups that can be intracellularly cleaved either chemically or enzymatically.
Results:
Several prodrug approaches have been successfully developed in order to increase the efficacy, bioavailability, penetration in target organ, and selectivity of nucleoside/nucleotide analogs.
Conclusion:
The concept of nucleoside/nucleotide prodrug is now a well-established approach that led to the approval of numerous drugs for the treatment of HIV, HBV, HCV, HSV and cancer.
More Related Videos
Related Concept Videos
Drug Metabolism: Phase II Reactions
Prodrugs
Prodrugs help overcome...
Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase
Drug Biotransformation: Overview
Drug Biotransformation: Overview
Biosynthesis of Nucleic Acids


