Developing protein arginine methyltransferase 1 (PRMT1) inhibitor TC-E-5003 as an antitumor drug using INEI drug delivery systems

Zhang, Pengcheng; He, Tong‐Chuan; Yu, Liyang; Zhou, Lixiao; Zhu, Chenggang

doi:10.1080/10717544.2020.1745327

Cited by 23 publications

(6 citation statements)

References 26 publications

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“…Furthermore, by utilizing the INEI drug delivery system to deliver TC-E-5003-loaded INEI (40% NBCA) in an animal model, the average growth inhibition rate of xenografted human lung cancer cells was 68.23%, surpassing the inhibition rate achieved by TC-E-5003 alone (31.76%). This study further confirms the potential of the inhibitor TC-E-5003 as an anti-tumor drug and highlights INEI as an effective technique for enhancing anti-tumor effects [ 132 ].…”

Section: Selective Prmt1 Inhibitorssupporting

confidence: 74%

PRMT1 in human neoplasm: cancer biology and potential therapeutic target

Shen,

Zhou,

Xiao

et al. 2024

Cell Commun Signal

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Protein arginine methyltransferase 1 (PRMT1), the predominant type I protein arginine methyltransferase, plays a crucial role in normal biological functions by catalyzing the methylation of arginine side chains, specifically monomethylarginine (MMA) and asymmetric dimethylarginine (ADMA), within proteins. Recent investigations have unveiled an association between dysregulated PRMT1 expression and the initiation and progression of tumors, significantly impacting patient prognosis, attributed to PRMT1’s involvement in regulating various facets of tumor cell biology, including DNA damage repair, transcriptional and translational regulation, as well as signal transduction. In this review, we present an overview of recent advancements in PRMT1 research across different tumor types, with a specific focus on its contributions to tumor cell proliferation, metastasis, invasion, and drug resistance. Additionally, we expound on the dynamic functions of PRMT1 during distinct stages of cancer progression, elucidating its unique regulatory mechanisms within the same signaling pathway and distinguishing between its promotive and inhibitory effects. Importantly, we sought to provide a comprehensive summary and analysis of recent research progress on PRMT1 in tumors, contributing to a deeper understanding of its role in tumorigenesis, development, and potential treatment strategies.

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Section: Selective Prmt1 Inhibitorssupporting

confidence: 74%

PRMT1 in human neoplasm: cancer biology and potential therapeutic target

Shen,

Zhou,

Xiao

et al. 2024

Cell Commun Signal

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“…In our effort to establish if PRMT1 regulates HIV-1 protein synthesis, the impact of N , N ′-(Sulfonyldi-4,1-phenylene)bis(2-chloroacetamide) (TC-E 5003) ( 64 ), a selective PRMT1 inhibitor (IC 50 = 1.5 μM) on HIV-1 gene expression was evaluated. For this, HEK293T cells were transfected with pNL4.3-RLuc (200 ng) and treated or not (vehicle alone) with TC-E 5003 (0.125-2 μM).…”

Section: Resultsmentioning

confidence: 99%

Heterogeneous nuclear ribonucleoprotein K promotes cap-independent translation initiation of retroviral mRNAs

Fuentes,

Olguín,

López-Ulloa

et al. 2024

Nucleic Acids Research

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Translation initiation of the human immunodeficiency virus-type 1 (HIV-1) genomic mRNA (vRNA) is cap-dependent or mediated by an internal ribosome entry site (IRES). The HIV-1 IRES requires IRES-transacting factors (ITAFs) for function. In this study, we evaluated the role of the heterogeneous nuclear ribonucleoprotein K (hnRNPK) as a potential ITAF for the HIV-1 IRES. In HIV-1-expressing cells, the depletion of hnRNPK reduced HIV-1 vRNA translation. Furthermore, both the depletion and overexpression of hnRNPK modulated HIV-1 IRES activity. Phosphorylations and protein arginine methyltransferase 1 (PRMT1)-induced asymmetrical dimethylation (aDMA) of hnRNPK strongly impacted the protein's ability to promote the activity of the HIV-1 IRES. We also show that hnRNPK acts as an ITAF for the human T cell lymphotropic virus-type 1 (HTLV-1) IRES, present in the 5′UTR of the viral sense mRNA, but not for the IRES present in the antisense spliced transcript encoding the HTLV-1 basic leucine zipper protein (sHBZ). This study provides evidence for a novel role of the host hnRNPK as an ITAF that stimulates IRES-mediated translation initiation for the retroviruses HIV-1 and HTLV-1.

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“…TC-E 5003, a protein arginine methyltransferase 1 (PRMT1) inhibitor, was also very active against KAIMRC1 spheroids. It has previously been used as an antitumor agent (Zhang et al, 2020) and implicated in oxidative stress, inflammation, and NF-KB translocation to the nucleus (Bissinger et al, 2011). Both the compounds are inhibitors of NF-KB translocation, which reduces the expression of ICAM-1 adhesion molecules and consequently disintegrates and inhibits cell growth in spheroids.…”

Section: Discussionmentioning

confidence: 99%

New Born Calf Serum Can Induce Spheroid Formation in Breast Cancer KAIMRC1 Cell Line

Ali

Huwaizi

Alhallaj

et al. 2021

Front. Mol. Biosci.

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Three-dimensional (3D) cell culture systems have become very popular in the field of drug screening and discovery. There is an immense demand for highly efficient and easy methods to produce 3D spheroids in any cell format. We have developed a novel and easy method to produce spheroids from the newly isolated KAIMRC1 cell line in vitro. It can be used as a 3D model to study proliferation, differentiation, cell death, and drug response of cancer cells. Our procedure requires growth media supplemented with 10% new born calf serum (NBCS) and regular cell culture plates to generate KAIMRC1 spheroids without the need for any specialized 3D cell culture system. This procedure generates multiple spheroids within a 12–24-h culture. KAIMRC1 spheroids are compact, homogeneous in size and morphology with a mean size of 55.8 µm (±3.5). High content imaging (HCI) of KAIMRC1 spheroids treated with a panel of 240 compounds resulted in the identification of several highly specific compounds towards spheroids. Immunophenotyping of KAIMRC1 spheroids revealed phosphorylation of FAK, cJUN, and E-cadherin, which suggests the involvement of JNK/JUN pathway in the KAIMRC1 spheroids formation. Gene expression analysis showed upregulation of cell junction genes, GJB3, DSC1, CLDN5, CLDN8, and PLAU. Furthermore, co-culture of KAIMRC1 cells with primary cancer-associated-fibroblasts (CAFs) showcased the potential of these cells in drug discovery application.

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Developing protein arginine methyltransferase 1 (PRMT1) inhibitor TC-E-5003 as an antitumor drug using INEI drug delivery systems

Cited by 23 publications

References 26 publications

PRMT1 in human neoplasm: cancer biology and potential therapeutic target

PRMT1 in human neoplasm: cancer biology and potential therapeutic target

Heterogeneous nuclear ribonucleoprotein K promotes cap-independent translation initiation of retroviral mRNAs

New Born Calf Serum Can Induce Spheroid Formation in Breast Cancer KAIMRC1 Cell Line

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