Licochalcone A is a natural selective inhibitor of arginine methyltransferase 6

Gong, Shuai; Maegawa, Satoru; Yang, Yanwen; Gopalakrishnan, Vidya; Zheng, Guangrong; Cheng, Donghang

doi:10.1042/bcj20200411

Cited by 13 publications

(6 citation statements)

References 73 publications

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“…Licochalcone A showed cytotoxicity to human MCF-7 breast cancer cells but no cytotoxicity to MCF-10A breast epithelial cells by up-regulating p53 expression, blocking G2/M cell cycle progression, and then inhibiting apoptosis. These results also indicate that licochalcone A, one of the main flavonoids extracted from licorice root, is the first natural inhibitor of PRMT6 with higher specificity (136). There is also a study identified a bisubstrate inhibitor called 6'-methyleneamine sinefungin (GMS), which is an analog of sinefungin, and its inhibitory activity is stronger than other cofactor competitive inhibitors.…”

Section: Prmt6 Inhibitorsmentioning

confidence: 75%

The Emerging Role of PRMT6 in Cancer

et al. 2022

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Protein arginine methyltransferase 6 (PRMT6) is a type I PRMT that is involved in epigenetic regulation of gene expression through methylating histone or non-histone proteins, and other processes such as alternative splicing, DNA repair, cell proliferation and senescence, and cell signaling. In addition, PRMT6 also plays different roles in various cancers via influencing cell growth, migration, invasion, apoptosis, and drug resistant, which make PRMT6 an anti-tumor therapeutic target for a variety of cancers. As a result, many PRMT6 inhibitors are being utilized to explore their efficacy as potential drugs for various cancers. In this review, we summarize the current knowledge on the function and structure of PRMT6. At the same time, we highlight the role of PRMT6 in different cancers, including the differentiation of its promotive or inhibitory effects and the underlying mechanisms. Apart from the above, current research progress and the potential mechanisms of PRMT6 behind them were also summarized.

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Section: Prmt6 Inhibitorsmentioning

confidence: 75%

The Emerging Role of PRMT6 in Cancer

et al. 2022

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“…By reducing the expression of cyclin D1 and increasing the expression of p21, LA (5–50 μM) led to cell cycle arrest of MCF-7 cells at the G0/G1 phase ( Huang et al, 2019 ). The overexpression of PRMT6 in human breast cancer is related to tumorigenesis ( Cheng and Bedford, 2011 ), and LA (10–100 μM) caused the cell cycle arrest of MCF-7 cells at the G2/M phase by inhibiting PRMT6 expression and subsequently p53 expression ( Gong et al, 2020 ). By downregulating the expression levels of cyclin A, CDK2, and CDC25A and increasing the level of p21, LB (10–50 μM) induced the cell cycle arrest of MCF-7 cells at the S phase ( Yu et al, 2016 ).…”

Section: Anticancer Effects Of Licochalcones On Tumor Cellsmentioning

confidence: 99%

Anticancer effects of licochalcones: A review of the mechanisms

et al. 2023

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Cancer is a disease with a high fatality rate representing a serious threat to human health. Researchers have tried to identify effective anticancer drugs. Licorice is a widely used traditional Chinese medicine with various pharmacological properties, and licorice-derived flavonoids include licochalcones like licochalcone A, licochalcone B, licochalcone C, licochalcone D, licochalcone E, and licochalcone H. By regulating the expression in multiple signaling pathways such as the EGFR/ERK, PI3K/Akt/mTOR, p38/JNK, JAK2/STAT3, MEK/ERK, Wnt/β-catenin, and MKK4/JNK pathways, and their downstream proteins, licochalcones can activate the mitochondrial apoptosis pathway and death receptor pathway, promote autophagy-related protein expression, inhibit the expression of cell cycle proteins and angiogenesis factors, regulate autophagy and apoptosis, and inhibit the proliferation, migration, and invasion of cancer cells. Among the licochalcones, the largest number of studies examined licochalcone A, far more than other licochalcones. Licochalcone A not only has prominent anticancer effects but also can be used to inhibit the efflux of antineoplastic drugs from cancer cells. Moreover, derivatives of licochalcone A exhibit strong antitumor effects. Currently, most results of the anticancer effects of licochalcones are derived from cell experiments. Thus, more clinical studies are needed to confirm the antineoplastic effects of licochalcones.

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“…As PRMTs have been found to have the ability to regulate cell cycle, could be regarded as a novel potential research target for tumor therapy. PRMTs inhibitors like GMS, MS023, MS049 were found to inhibit some PRMTs ( Gong et al, 2020 ) unfortunately, there is no clinical data available about the role of these ones as therapeutic agents in PCa. Concomitant administration of CI-Amidine (a PADI2 inhibitor) with enzalutamide results in synergistic inhibition of cell proliferation and tumor progression under ADT condition.…”

Section: Prostate Cancer (Pca)mentioning

confidence: 99%

H3 histone methylation landscape in male urogenital cancers: from molecular mechanisms to epigenetic biomarkers and therapeutic targets

Burlibaşa

Nicu

Chifiriuc

et al. 2023

Front. Cell Dev. Biol.

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During the last decades, male urogenital cancers (including prostate, renal, bladder and testicular cancers) have become one of the most frequently encountered malignancies affecting all ages. While their great variety has promoted the development of various diagnosis, treatment and monitoring strategies, some aspects such as the common involvement of epigenetic mechanisms are still not elucidated. Epigenetic processes have come into the spotlight in the past years as important players in the initiation and progression of tumors, leading to a plethora of studies highlighting their potential as biomarkers for diagnosis, staging, prognosis, and even as therapeutic targets. Thus, fostering research on the various epigenetic mechanisms and their roles in cancer remains a priority for the scientific community. This review focuses on one of the main epigenetic mechanisms, namely, the methylation of the histone H3 at various sites and its involvement in male urogenital cancers. This histone modification presents a great interest due to its modulatory effect on gene expression, leading either to activation (e.g., H3K4me3, H3K36me3) or repression (e.g., H3K27me3, H3K9me3). In the last few years, growing evidence has demonstrated the aberrant expression of enzymes that methylate/demethylate histone H3 in cancer and inflammatory diseases, that might contribute to the initiation and progression of such disorders. We highlight how these particular epigenetic modifications are emerging as potential diagnostic and prognostic biomarkers or targets for the treatment of urogenital cancers.

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Licochalcone A is a natural selective inhibitor of arginine methyltransferase 6

Cited by 13 publications

References 73 publications

The Emerging Role of PRMT6 in Cancer

The Emerging Role of PRMT6 in Cancer

Anticancer effects of licochalcones: A review of the mechanisms

H3 histone methylation landscape in male urogenital cancers: from molecular mechanisms to epigenetic biomarkers and therapeutic targets

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