DNA Methyltransferase Inhibitors

2010 ◽  
pp. 416-416
Author(s):  
Nicola Simola ◽  
Micaela Morelli ◽  
Tooru Mizuno ◽  
Suzanne H. Mitchell ◽  
Harriet de Wit ◽  
...  
Keyword(s):  
Dna Methyltransferase ◽  
Dna Methyltransferase Inhibitors

DNA methyltransferase inhibitors modulate histone methylation: epigenetic crosstalk between H3K4me3 and DNA methylation during sperm differentiation

Zygote ◽  
2021 ◽  
pp. 1-6
Author(s):  
Liliana Burlibaşa ◽  
Alina-Teodora Nicu ◽  
Carmen Domnariu
Keyword(s):  
Dna Methylation ◽  
Histone Methylation ◽  
Dna Methyltransferase ◽  
Integrated Approach ◽  
Regulatory Mechanisms ◽  
Temporal Expression ◽  
Dna Methyltransferase Inhibitors ◽  
Expression Of Genes ◽  
Species Survival ◽  
Advanced Stages

Summary The process of cytodifferentiation in spermatogenesis is governed by a unique genetic and molecular programme. In this context, accurate ‘tuning’ of the regulatory mechanisms involved in germ cells differentiation is required, as any error could have dramatic consequences on species survival and maintenance. To study the processes that govern the spatial–temporal expression of genes, as well as analyse transmission of epigenetic information to descendants, an integrated approach of genetics, biochemistry and cytology data is necessary. As information in the literature on interplay between DNA methylation and histone H3 lysine 4 trimethylation (H3K4me3) in the advanced stages of murine spermatogenesis is still scarce, we investigated the effect of a DNA methyltransferase inhibitor, 5-aza-2′-deoxycytidine, at the cytological level using immunocytochemistry methodology. Our results revealed a particular distribution of H3K4me3 during sperm cell differentiation and highlighted an important role for regulation of DNA methylation in controlling histone methylation and chromatin remodelling during spermatogenesis.

scholarly journals Expanding the Structural Diversity of DNA Methyltransferase Inhibitors

2020 ◽  
Vol 14 (1) ◽  
pp. 17
Author(s):  
K. Eurídice Juárez-Mercado ◽  
Fernando D. Prieto-Martínez ◽  
Norberto Sánchez-Cruz ◽  
Andrea Peña-Castillo ◽  
Diego Prada-Gracia ◽  
...  
Keyword(s):  
Histone Deacetylases ◽  
Dna Methyltransferase ◽  
Structural Diversity ◽  
Dna Methyltransferases ◽  
Dna Methyltransferase Inhibitors ◽  
Epigenetic Drug ◽  
Ic50 Values ◽  
Dietary Component ◽  
Approved Drugs ◽  
Epigenetic Processes

Inhibitors of DNA methyltransferases (DNMTs) are attractive compounds for epigenetic drug discovery. They are also chemical tools to understand the biochemistry of epigenetic processes. Herein, we report five distinct inhibitors of DNMT1 characterized in enzymatic inhibition assays that did not show activity with DNMT3B. It was concluded that the dietary component theaflavin is an inhibitor of DNMT1. Two additional novel inhibitors of DNMT1 are the approved drugs glyburide and panobinostat. The DNMT1 enzymatic inhibitory activity of panobinostat, a known pan inhibitor of histone deacetylases, agrees with experimental reports of its ability to reduce DNMT1 activity in liver cancer cell lines. Molecular docking of the active compounds with DNMT1, and re-scoring with the recently developed extended connectivity interaction features approach, led to an excellent agreement between the experimental IC50 values and docking scores.

scholarly journals Targeting DNA methylation for treating triple-negative breast cancer

2019 ◽  
Vol 20 (16) ◽  
pp. 1151-1157 ◽  
Author(s):  
Jia Yu ◽  
Jacqueline Zayas ◽  
Bo Qin ◽  
Liewei Wang
Keyword(s):  
Breast Cancer ◽  
Dna Methylation ◽  
Tumor Suppressor ◽  
Triple Negative Breast Cancer ◽  
Targeted Therapies ◽  
Tumor Suppressor Genes ◽  
Dna Methyltransferase ◽  
Triple Negative ◽  
Suppressor Genes ◽  
Dna Methyltransferase Inhibitors

Triple-negative breast cancer (TNBC) accounts for 15–20% of all invasive breast cancers and tends to have aggressive histological features and poor clinical outcomes. Unlike, estrogen receptor- or HER2-positive diseases, TNBC patients currently lack the US FDA-approved targeted therapies. DNA methylation is a critical mechanism of epigenetic modification. It is well known that aberrant DNA methylation contributes to the malignant transformation of cells by silencing critical tumor suppressor genes. DNA methyltransferase inhibitors reactivate silenced tumor suppressor genes and result in tumor growth arrest, with therapeutic effects observed in patients with hematologic malignancies. The antitumor effect of these DNA methyltransferase inhibitors has also been explored in solid tumors, especially in TNBC that currently lacks targeted therapies.

scholarly journals DNA methyltransferase inhibitors upregulate CD38 protein expression and enhance daratumumab efficacy in multiple myeloma

Leukemia ◽  
2019 ◽  
Vol 34 (3) ◽  
pp. 938-941 ◽  
Author(s):  
Priya Choudhry ◽  
Margarette C. Mariano ◽  
Huimin Geng ◽  
Thomas G. Martin ◽  
Jeffrey L. Wolf ◽  
...  
Keyword(s):  
Multiple Myeloma ◽  
Protein Expression ◽  
Dna Methyltransferase ◽  
Dna Methyltransferase Inhibitors

scholarly journals The DNA methyltransferase inhibitors zebularine and decitabine induce mitochondria-mediated apoptosis and DNA damage in p53 mutant leukemic T cells

2011 ◽  
Vol 130 (5) ◽  
pp. 1195-1207 ◽  
Author(s):  
María J. Ruiz-Magaña ◽  
Jose M. Rodríguez-Vargas ◽  
Jorge C. Morales ◽  
Manuel A. Saldivia ◽  
Klaus Schulze-Osthoff ◽  
...  
Keyword(s):  
Dna Damage ◽  
T Cells ◽  
Dna Methyltransferase ◽  
Dna Methyltransferase Inhibitors

scholarly journals New Insights on the Mechanism of Quinoline-based DNA Methyltransferase Inhibitors

2014 ◽  
Vol 290 (10) ◽  
pp. 6293-6302 ◽  
Author(s):  
Christina Gros ◽  
Laurence Fleury ◽  
Virginie Nahoum ◽  
Céline Faux ◽  
Sergio Valente ◽  
...  
Keyword(s):  
Dna Methyltransferase ◽  
Dna Methyltransferase Inhibitors
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