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Drug bioactivation, covalent binding to target proteins and toxicity relevance.

Author: ChanEli, ChenYu-Zong, DuanWei, HuangMin, ZhouShufeng

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Overview

Many therapeutic drugs undergo metabolic activation, producing reactive metabolites that can covalently bind to target proteins, leading to toxicity. This review discusses the mechanisms of drug bioactivation and protein adduct formation, focusing on the target proteins identified using mass spectrometry and proteomic approaches. It explores the potential consequences of drug bioactivation, including drug toxicity, organ toxicity, immune-mediated mechanisms, and drug-drug interactions. The clinical implications of drug bioactivation are complex and require further research to fully understand the structure-activity relationships of drug covalent binding to proteins and their clinical outcomes.
Paper Details　
Original Abstract of the Article :
A number of therapeutic drugs with different structures and mechanisms of action have been reported to undergo metabolic activation by Phase I or Phase II drug-metabolizing enzymes. The bioactivation gives rise to reactive metabolites/intermediates, which readily confer covalent binding to various t...See full text at original site
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引用元：
https://doi.org/10.1081/dmr-200028812

データ提供：米国国立医学図書館（NLM）

Drug Bioactivation: A Double-Edged Sword in the Desert of Drug Discovery

In the world of drug discovery, we are constantly seeking to create effective medications that can combat diseases without causing harm. This research explores the phenomenon of drug bioactivation, where some drugs undergo metabolic changes that can lead to the formation of reactive metabolites. These metabolites can bind to proteins in the body, sometimes leading to toxicity. It's like navigating a desert where unexpected storms can erupt from seemingly harmless mirages.

The Hidden Side of Drug Bioactivation

The authors provide a detailed overview of various drugs that undergo bioactivation, highlighting the potential for toxicity. They discuss the different mechanisms of bioactivation and the role of drug-metabolizing enzymes in this process. It's like mapping out the intricate pathways through which drugs can transform into their reactive forms, potentially causing harm.

Minimizing the Risk of Drug Toxicity

This research underscores the importance of understanding the potential for drug bioactivation and the need for careful evaluation of drug safety. It emphasizes the role of proteomic and genomic approaches in identifying potential targets for drug-induced toxicity. It's like using advanced tools to navigate the desert of drug discovery, avoiding the treacherous paths that can lead to toxic outcomes.

Dr.Camel's Conclusion

This research sheds light on the complex and sometimes unpredictable nature of drug bioactivation. It highlights the need for continued research to better understand the mechanisms of drug-induced toxicity and develop strategies for minimizing these risks. As we continue to explore the vast desert of drug discovery, we must remain vigilant and informed to ensure the safety and efficacy of our medications.
Date :
  1. Date Completed 2005-06-06
  2. Date Revised 2022-03-30
Further Info :

Pubmed ID

15747500

DOI: Digital Object Identifier

10.1081/dmr-200028812

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