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Chemoproteomics reveals berberine directly binds to PKM2 to inhibit the progression of colorectal cancer.


ABSTRACT: Colorectal cancer is one of the most serious tumors and berberine can inhibit the recurrence and transformation of colorectal adenoma into colorectal cancer. However, the direct binding target proteins of berberine in inhibiting colorectal cancer remain unclear. In this study, the chemical proteomics method was used and demonstrated that berberine is directly bound to pyruvate kinase isozyme type M2 (PKM2) in colorectal cancer cells. The triangular N-O-O triangular structure of berberine contributed to hydrophobic interaction with I119 amino acid residues and π-π interaction with F244 amino acid residues of PKM2 protein. Moreover, berberine was shown to inhibit the reprogramming of glucose metabolism and the phosphorylation of STAT3, down regulate the expression of Bcl-2 and Cyclin D1 genes, ultimately inhibiting the progression of colorectal cancer. This study uncovered the direct binding target protein and mechanism of berberine to improve metabolic reprogramming in colorectal cancer, which is helpful to guide the optimization of berberine.

SUBMITTER: Yan SH 

PROVIDER: S-EPMC9386086 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature

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Chemoproteomics reveals berberine directly binds to PKM2 to inhibit the progression of colorectal cancer.

Yan Shi-Hai SH   Hu Li-Mu LM   Hao Xue-Hui XH   Liu Jiang J   Tan Xi-Ying XY   Geng Zhi-Rong ZR   Ma Jing J   Wang Zhi-Lin ZL  

iScience 20220720 8


Colorectal cancer is one of the most serious tumors and berberine can inhibit the recurrence and transformation of colorectal adenoma into colorectal cancer. However, the direct binding target proteins of berberine in inhibiting colorectal cancer remain unclear. In this study, the chemical proteomics method was used and demonstrated that berberine is directly bound to pyruvate kinase isozyme type M2 (PKM2) in colorectal cancer cells. The triangular N-<i>O</i>-O triangular structure of berberine  ...[more]

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