Drug design, development and therapy · 2026
Proteome Microarray-Guided Global View: Multiple Pharmacological Targets of Icariin.
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Gong Guichun, Tang Xianjin, Yuan Guanghun, Yang Xinxing, Wang Guoqing, Zhang Feng
Аннотация
BACKGROUND: Icariin (ICA) is a major bioactive compound extracted from the traditional Chinese medicinal herb Epimedium, demonstrated a broad spectrum of pharmacological properties. However, a comprehensive and up-to-date study exclusively focusing on ICA direct binding proteins has not yet been conducted.
METHODS: HuProt™ 20K human proteome microarray, the highest capacity human protein microarray, is suitable for the applications of small molecule targeting proteins. Here, we constructed an atlas of the ICA-binding proteins directly via proteome microarray.
RESULTS: We showed that a total of 246 proteins which directly interacted with ICA. Subsequent PPI network analysis organized these proteins into 4 functionally distinct clusters, revealing that ICA interacts with proteins central to fundamental cellular processes, including protein folding chaperone complexes, the ubiquitin-proteasome system, apoptotic and PI3K-Akt signaling pathways, and nucleotide metabolism.
CONCLUSION: This study constructed an atlas of the ICA-binding proteins directly via microarray, which spans protein folding, ubiquitin-proteasome, apoptosis and nucleotide metabolism, providing a theoretical basis for ICA treatment of diseases caused by dysregulation of these core pathways.
METHODS: HuProt™ 20K human proteome microarray, the highest capacity human protein microarray, is suitable for the applications of small molecule targeting proteins. Here, we constructed an atlas of the ICA-binding proteins directly via proteome microarray.
RESULTS: We showed that a total of 246 proteins which directly interacted with ICA. Subsequent PPI network analysis organized these proteins into 4 functionally distinct clusters, revealing that ICA interacts with proteins central to fundamental cellular processes, including protein folding chaperone complexes, the ubiquitin-proteasome system, apoptotic and PI3K-Akt signaling pathways, and nucleotide metabolism.
CONCLUSION: This study constructed an atlas of the ICA-binding proteins directly via microarray, which spans protein folding, ubiquitin-proteasome, apoptosis and nucleotide metabolism, providing a theoretical basis for ICA treatment of diseases caused by dysregulation of these core pathways.