Abstract

In recent years, biologically active natural products have gradually become important agents in the field of drug research and development because of their wide availability and variety. However, the target sites of many natural products are yet to be identified, which is a setback in the pharmaceutical industry and has seriously hindered the translation of research findings of these natural products as viable candidates for new drug exploitation. This review systematically describes the commonly used strategies for target identification via the application of probe and non-probe approaches. The merits and demerits of each method were summarized using recent examples, with the goal of comparing currently available methods and selecting the optimum techniques for identifying the targets of bioactive natural products.

Highlights

  • Natural products (NPs) are a group of diverse and naturally-occurring chemical compounds or substances with a wide range of biological activities

  • CCCP, compound-lefted chemical proteomics; Activity-based protein profiling (ABPP), activity-based protein profiling; DARTS, drug affinity responsive target stability; SPROX, stability of proteins from rates of oxidation; SILAC, stable isotope labeling with amino acids in cell culture; isobaric tags for relative and absolute quantification (iTRAQ), isobaric tags for relative and absolute quantitation; CETSA, cellular thermal shift assay; TPP, thermal proteome profiling

  • Kong’s team employed a combination of iTRAQ, twodimensional LC, and MS/MS to investigate the effect of artesunate (ART) on S. japonicum proteome in susceptible mice

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Summary

INTRODUCTION

Natural products (NPs) are a group of diverse and naturally-occurring chemical compounds or substances with a wide range of biological activities. Identifying the targets of bioactive NPs is essential for elucidating their mechanisms of action and optimizing existing drugs for hastening the process of new drug development (Lo et al, 2015; ElWakil et al, 2017). It is very common for drugs to combine with multiple targets (Klessig et al, 2016; Peon et al, 2017; Majumder et al, 2018), which can significantly interfere with target identification and isolation. This offers novel opportunities and possibilities for the discovery of new targets.

45 Kongensin 46 Gambogic acid
61 Vioprolide A
Biophysical Methods
PROSPECTS AND CONCLUSIONS

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