Identification of BMI1 promoter inhibitors from Streptomyces sp. IFM-11958

Yokoyama, Yusuke; Arai, Midori A.; Hara, Yukio; Ishibashi, Masami

doi:10.1016/j.bmc.2019.05.002

Cited by 7 publications

(8 citation statements)

References 22 publications

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“…In summary, whether PRC1 plays an oncogenic or tumor-suppressive role is mainly related to its function in cell proliferation, cell cycle progression, metastasis, and invasion (References are shown in Table 1 ). Given the prominent oncogenic role that PRC1 plays, inhibitors targeting PRC1 for antitumor therapy have also attracted attention, and a subset of inhibitors have been reported [ 247 , 248 , 249 , 250 ]. However, the precise roles of the various subunits of PRC1 in cancer remain to be defined, and future work should further delineate the molecular implications of these components in depth and identify appropriate therapeutic approaches to rescue their dysregulation in different cancers.…”

Section: Polycomb Repressive Complexes In Cancermentioning

confidence: 99%

“…PcG components have been reported to be associated with the growth and survival of different tumors, considered as targets for cancer therapy, and extensively explored [ 270 , 271 ]. Several PRC1-related inhibitors including PRT4165, PTC-209, IFM-11958, and RB-3 have been reported to date, but no inhibitor has entered clinical trials ( Figure 6 ) [ 247 , 248 , 249 , 250 ]. PRT4165 was shown to inhibit the E3 enzymatic activity of PRC1, whereas PTC-209 and IFM-11958 were described as inhibitors of the BMI-1 expression.…”

Section: Polycomb Repressive Complexes In Cancermentioning

confidence: 99%

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Critical Roles of Polycomb Repressive Complexes in Transcription and Cancer

Dong

et al. 2022

IJMS

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Polycomp group (PcG) proteins are members of highly conserved multiprotein complexes, recognized as gene transcriptional repressors during development and shown to play a role in various physiological and pathological processes. PcG proteins consist of two Polycomb repressive complexes (PRCs) with different enzymatic activities: Polycomb repressive complexes 1 (PRC1), a ubiquitin ligase, and Polycomb repressive complexes 2 (PRC2), a histone methyltransferase. Traditionally, PRCs have been described to be associated with transcriptional repression of homeotic genes, as well as gene transcription activating effects. Particularly in cancer, PRCs have been found to misregulate gene expression, not only depending on the function of the whole PRCs, but also through their separate subunits. In this review, we focused especially on the recent findings in the transcriptional regulation of PRCs, the oncogenic and tumor-suppressive roles of PcG proteins, and the research progress of inhibitors targeting PRCs.

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Section: Polycomb Repressive Complexes In Cancermentioning

confidence: 99%

Section: Polycomb Repressive Complexes In Cancermentioning

confidence: 99%

Critical Roles of Polycomb Repressive Complexes in Transcription and Cancer

Dong

et al. 2022

IJMS

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“…Several studies have documented that BMI-1 overexpression is inversely correlated to the expression of tumor suppressor genes such as PTEN and p16 [ 30 ]. Gisler et al [ 31 ] have shown that upregulation of BMI-1 significantly induces cancer cells proliferation.…”

Section: Main Textmentioning

confidence: 99%

Comparative evaluation of BMI-1 proto-oncogene expression in normal tissue, adenoma and papillary carcinoma of human thyroid in pathology samples

2021

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Objective Papillary Thyroid carcinoma accounts for more than 60% of adult thyroid carcinomas. Finding a helpful marker is vital to determine the correct treatment approach. The present study was aimed to evaluate the expression of the B cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) gene in papillary carcinoma, adenoma, and adjacent healthy thyroid tissues. Pathology blocks of thyroid tissues at the pathology department of patients who have undergone thyroid surgery between 2015 and 2019 were examined; papillary carcinoma, adenoma, and healthy tissues were selected and sectioned. Total RNA was extracted, and the relative expression level of the BMI-1 gene was examined using the Real-Time qPCR method. Results In the papillary and adenoma tissues, BMI-1 was overexpressed (1.047-fold and 1.042-fold) in comparison to healthy tissues (p < 0.05 for both comparisons). However, no statistically significant differences were observed between adenoma and papillary carcinoma tissues regarding BMI-1 gene expression. This study demonstrated a new biomarker for thyroid malignancies and found that the mRNA levels of the BMI-1 gene were higher in tumor tissues compared with healthy tissues. Further studies are needed to evaluate the BMI1 gene expression in other thyroid cancers.

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“…11,12) In addition, elaiophyllin, 2-methylelaiophyllin, and nocardamin were isolated as BMI1 promoter inhibitors. 11,13,14) Here, we search for natural compounds showing BMI1 gene expression inhibitory effect from tropical plants.…”

Section: Introductionmentioning

confidence: 99%

Natural Compounds with BMI1 Promoter Inhibitory Activity from <i>Mammea siamensis</i> and <i>Andrographis paniculata</i>

Fujii

Hara

Arai

et al. 2022

CHEMICAL & PHARMACEUTICAL BULLETIN

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A new coumarin derivative (1) and 30 known compounds were isolated from Mammea siamensis and Andrographis paniculata, guided by B cell-specific Moloney murine leukemia virus insertion region 1 (BMI1) promoter inhibitory activity. Among the isolated compounds, 15 compounds showed BMI1 promoter inhibitory activity, and five compounds were found to be cytotoxic. 14-Deoxy-11,12-dehydroandrographolide (18) was highly cytotoxic to DU145 cells with an IC 50 value of 25.4 µM. Western blotting analysis of compound 18 in DU145 cells suggested that compound 18 suppresses BMI1 expression.

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Identification of BMI1 promoter inhibitors from Streptomyces sp. IFM-11958

Cited by 7 publications

References 22 publications

Critical Roles of Polycomb Repressive Complexes in Transcription and Cancer

Critical Roles of Polycomb Repressive Complexes in Transcription and Cancer

Comparative evaluation of BMI-1 proto-oncogene expression in normal tissue, adenoma and papillary carcinoma of human thyroid in pathology samples

Natural Compounds with BMI1 Promoter Inhibitory Activity from <i>Mammea siamensis</i> and <i>Andrographis paniculata</i>

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