Probe-based target fishing technologies for identifying molecular targets of triptolide and celastrol from Tripterygium wilfordii: recent advances and perspectives
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Updated: Oct 31, 2026

Network Pharmacology Prediction and Experimental Validation of Trichosanthes-Fritillaria thunbergii Action Mechanism Against Lung Adenocarcinoma
Published on: March 3, 2023
Jun Xiao1, Long Mu1, Ying-Da Zang1
1State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
Abstract:
Bioactive constituents of Tripterygium wilfordii Hook. f. possess potent pharmacological activities but are constrained by a narrow therapeutic window and prominent toxicities. Triptolide and celastrol are representative constituents for which direct target identification is essential to clarify efficacy-toxicity mechanisms. Probe-based target fishing and chemical proteomics enable direct profiling of protein engagement in complex biological systems. This review summarizes the principles and applications of these technologies in identifying therapeutic and toxicity-related targets of triptolide and celastrol, critically evaluates current methodological limitations, and highlights future directions for target validation, toxicity reduction, efficacy optimization, and mechanism-based drug development.
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