Results 51 to 60 of about 141,545 (201)

Targeting EZH2-mediated methylation of H3K27 inhibits proliferation and migration of Synovial Sarcoma in vitro. [PDF]

, 2016
Synovial sarcoma is an aggressive soft tissue sarcoma genetically defined by the fusion oncogene SS18-SSX. It is hypothesized that either SS18-SSX disrupts SWI/SNF complex inhibition of the polycomb complex 2 (PRC2) methyltransferase Enhancer of Zeste ...
Choy, Edwin, Cote, Gregory M, Duan, Zhenfeng, Gao, Yan, Hornicek, Francis J, Mankin, Henry J, Shen, Jacson K   +6 more
core   +2 more sources

DNA Methyltransferase Inhibitors with Novel Chemical Scaffolds [PDF]

, 2020
AbstractInhibitors 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.
K. Eurídice Juárez-Mercado, Fernando D. Prieto-Martínez, Norberto Sánchez-Cruz, Andrea Peña-Castillo, Diego Prada-Gracia, José L. Medina-Franco   +5 more
openaire   +1 more source

Structural insight into the DNMT1 reaction cycle by cryo-electron microscopy.

PLoS ONE
DNMT1 is an essential DNA methyltransferase that catalyzes the transfer of methyl groups to CpG islands in DNA and generates a prominent epigenetic mark.
Inessa De, Jonas Weidenhausen, Nestor Concha, Christoph W Müller   +3 more
doaj   +1 more source

METTL3 regulates WTAP protein homeostasis [PDF]

, 2018
The Wilms tumor 1 (WT1)-associated protein (WTAP) is upregulated in many tumors, including, acute myeloid leukemia (AML), where it plays an oncogenic role by interacting with different proteins involved in RNA processing and cell proliferation.
Capuano, Ernestina, Cruciani, Sonia, Fatica, Alessandro, Fazi, Francesco, Ginistrelli, Lavinia Ceci, Ianniello, Zaira, Larivera, Simone, Marchioni, Marcella, Sorci, Melissa   +8 more
core   +2 more sources

Targeted inhibition of the methyltransferase SETD8 synergizes with the Wee1 inhibitor adavosertib in restraining glioblastoma growth

Cell Death and Disease, 2023
Despite intense research efforts, glioblastoma remains an incurable brain tumor with a dismal median survival time of 15 months. Thus, identifying new therapeutic targets is an urgent need.
Rosa Della Monica, Michela Buonaiuto, Mariella Cuomo, Cristina Pagano, Federica Trio, Davide Costabile, Giulia de Riso, Francesca Sveva Cicala, Maddalena Raia, Raduan Ahmed Franca, Marialaura Del Basso De Caro, Domenico Sorrentino, Giovanna Navarra, Laura Coppola, Lorella Tripodi, Lucio Pastore, Juergen Hench, Stephan Frank, Claudio Schonauer, Giuseppe Catapano, Maurizio Bifulco, Lorenzo Chiariotti, Roberta Visconti   +22 more
doaj   +1 more source

Identification and Biological Evaluation of Secondary Metabolites from Marine Derived Fungi-Aspergillus sp. SCSIOW3, Cultivated in the Presence of Epigenetic Modifying Agents

Molecules, 2017
Chemical epigenetic manipulation was applied to a deep marine-derived fungus, Aspergillus sp. SCSIOW3, resulting in significant changes of the secondary metabolites.
Xiaofan Li, Zhenyao Xia, Jianqiang Tang, Jiahui Wu, Jing Tong, Mengjie Li, Jianhua Ju, Huirong Chen, Liyan Wang   +8 more
doaj   +1 more source

DNA methyltransferase inhibitor zebularine inhibits human hepatic carcinoma cells proliferation and induces apoptosis. [PDF]

PLoS ONE, 2013
Hepatocellular carcinoma is one of the most common cancers worldwide. During tumorigenesis, tumor suppressor and cancer-related genes are commonly silenced by aberrant DNA methylation in their promoter regions.
Kazuaki Nakamura, Kazuko Aizawa, Kazuhiko Nakabayashi, Natsuko Kato, Junji Yamauchi, Kenichiro Hata, Akito Tanoue   +6 more
doaj   +1 more source

Epigenetic and antitumor effects of platinum(IV)-octanoato conjugates [PDF]

, 2017
We present the anticancer properties of cis, cis, trans-[Pt(IV)(NH3)2Cl2(OA)2] [Pt(IV)diOA] (OA = octanoato), Pt(IV) derivative of cisplatin containing two OA units appended to the axial positions of a six-coordinate Pt(IV) center.
Brabec, Viktor, Gandin, Valentina, Gibson, Dan, Kasparkova, Jana, Marzano, Cristina, Novohradsky, Vojtech, Osella, Domenico, Pracharova, Jitka, Zanellato, Ilaria   +8 more
core   +1 more source

Ornithine decarboxylase antizyme induces hypomethylation of genome DNA and histone H3 lysine 9 dimethylation (H3K9me2) in human oral cancer cell line.

PLoS ONE, 2010
BackgroundMethylation of CpG islands of genome DNA and lysine residues of histone H3 and H4 tails regulates gene transcription. Inhibition of polyamine synthesis by ornithine decarboxylase antizyme-1 (OAZ) in human oral cancer cell line resulted in ...
Daisuke Yamamoto, Kaori Shima, Kou Matsuo, Takashi Nishioka, Chang Yan Chen, Guo-Fu Hu, Akira Sasaki, Takanori Tsuji   +7 more
doaj   +1 more source

Re-Expression of ERα and AR in Receptor Negative Endocrine Cancers via GSK3 Inhibition

Frontiers in Oncology, 2022
DNA methylation, catalyzed by DNA methyltransferase (DNMT), is a well-characterized epigenetic modification in cancer cells. In particular, promoter hypermethylation of AR and ESR1 results in loss of expression on Androgen Receptor (AR) and Estrogen ...
Vikas Sharma, Jayadev Joshi, I-Ju Yeh, YongQiu Doughman, Daniel Blankenberg, David Wald, Monica M. Montano   +6 more
doaj   +1 more source