PMID: 9658587Jul 11, 1998Paper

Molecular toxicology and the medicinal chemist

Il Farmaco
B Testa, J Mayer

Abstract

Drug metabolism has a number of pharmacodynamic and pharmacokinetic consequences which cannot be ignored even at the early stages of drug research. A number of aspects of drug metabolism are thus of interest to medicinal chemists, e.g. prodrug and soft drug design. This mini-review focuses mainly on toxication resulting from reactions of functionalization and conjugation. In the former case, oxidoreductases can reduce xenobiotics to nucleophilic radicals, or oxidize them to electrophilic and oxidizable metabolites. Conjugation reactions also play a role in toxication by generating lipophilic residues (e.g. hybrid triglycerides) or adduct-forming metabolites (e.g. some acylglucuronides), or by interfering with physiological pathways (e.g. Coenzyme A conjugates). Functional moieties undergoing such reactions are known as toxophoric groups. Because they are the biochemical endpoint of several toxication reactions, macromolecular adducts are now of special significance in molecular toxicology. But, as discussed in the conclusion, the substrate specificity of drug-metabolizing enzymes, the many biological factors that influence metabolism, and various repair and removal mechanisms all contribute to decrease toxicological risks and t...Continue Reading

References

May 1, 1996·Medicinal Research Reviews·B Testa, J Caldwell

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Citations

Jul 27, 2001·Mutation Research·G SelloE Benfenati
May 30, 2009·Chemistry & Biodiversity·Bernard Testa, Stefanie D Krämer
Jun 11, 2016·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Xiao SunYu-Feng Ding

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