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- Title
Therapeutic Target Identification and Drug Discovery Driven by Chemical Proteomics.
- Authors
Zou, Mingjie; Zhou, Haiyuan; Gu, Letian; Zhang, Jingzi; Fang, Lei
- Abstract
Simple Summary: Human beings are always associated with small molecules throughout their lives. Chemical proteomics, which selectively identifies small-molecule targets, is an emerging approach for unraveling the mechanism of action of small molecules for therapeutic target identification and drug discovery. This review attempts to introduce representative techniques of chemical proteomics and summarizes examples of identifying small-molecule targets. Throughout the human lifespan, from conception to the end of life, small molecules have an intrinsic relationship with numerous physiological processes. The investigation into small-molecule targets holds significant implications for pharmacological discovery. The determination of the action sites of small molecules provide clarity into the pharmacodynamics and toxicological mechanisms of small-molecule drugs, assisting in the elucidation of drug off-target effects and resistance mechanisms. Consequently, innovative methods to study small-molecule targets have proliferated in recent years, with chemical proteomics standing out as a vanguard development in chemical biology in the post-genomic age. Chemical proteomics can non-selectively identify unknown targets of compounds within complex biological matrices, with both probe and non-probe modalities enabling effective target identification. This review attempts to summarize methods and illustrative examples of small-molecule target identification via chemical proteomics. It delves deeply into the interactions between small molecules and human biology to provide pivotal directions and strategies for the discovery and comprehension of novel pharmaceuticals, as well as to improve the evaluation of drug safety.
- Subjects
DRUG discovery; SMALL molecules; CHEMICAL biology; HUMAN biology; DEVELOPMENTAL biology
- Publication
Biology (2079-7737), 2024, Vol 13, Issue 8, p555
- ISSN
2079-7737
- Publication type
Article
- DOI
10.3390/biology13080555