Results 41 to 50 of about 1,974 (156)

Targeting SMYD3 to Sensitize Homologous Recombination-Proficient Tumors to PARP-Mediated Synthetic Lethality

iScience, 2020
Summary: SMYD3 is frequently overexpressed in a wide variety of cancers. Indeed, its inactivation reduces tumor growth in preclinical in vivo animal models.
Paola Sanese, Candida Fasano, Giacomo Buscemi, Cinzia Bottino, Silvia Corbetta, Edoardo Fabini, Valentina Silvestri, Virginia Valentini, Vittoria Disciglio, Giovanna Forte, Martina Lepore Signorile, Katia De Marco, Stefania Bertora, Valentina Grossi, Ummu Guven, Natale Porta, Valeria Di Maio, Elisabetta Manoni, Gianluigi Giannelli, Manuela Bartolini, Alberto Del Rio, Giuseppina Caretti, Laura Ottini, Cristiano Simone   +23 more
doaj   +1 more source

Putting SMYD3 on the MAP [PDF]

Science-Business eXchange, 2014
Stanford and GlaxoSmithKline report that SMYD3 acts in the cytoplasm to regulate the MAPK pathway and not in the nucleus as previously thought. The discovery implies that inhibiting the enzyme can counter activating mutations in MAPK pathway components such as KRAS.
openaire   +1 more source

Targeting Smyd3 by next-generation antisense oligonucleotides suppresses liver tumor growth

iScience, 2021
Summary: The oncogenic function of suppressor of variegation, enhancer of zeste and MYeloid-Nervy-DEAF1-domain family methyltransferase Smyd3 has been implicated in various malignancies, including hepatocellular carcinoma (HCC).
Haroula Kontaki, Marina Koukaki, Maria Vasilarou, Antonis Giakountis, Elena Deligianni, Xiaolin Luo, Youngsoo Kim, Iannis Talianidis   +7 more
doaj   +1 more source

Unveiling the Biochemistry of the Epigenetic Regulator SMYD3

Biochemistry, 2019
SET and MYND domain-containing protein 3 (SMYD3) is a lysine methyltransferase that plays a central role in a variety of cancer diseases, exerting its pro-oncogenic activity by methylation of key proteins, of both nuclear and cytoplasmic nature. However, the role of SMYD3 in the initiation and progression of cancer is not yet fully understood and ...
Fabini E., Talibov V. O., Mihalic F., Naldi M., Bartolini M., Bertucci C., Del Rio A., Danielson U. H.   +7 more
openaire   +3 more sources

Novel insights into the oncogenic function of the SMYD3 lysine methyltransferase [PDF]

Translational Cancer Research, 2016
SMYD3 is a member of the SMYD family of lysine methyltransferases (KMTs). In humans, there are five SMYD members (SMYD1–5) that are characterized by the presence of a split catalytic SET domain interrupted by a MYND zinc finger domain. The MYND domain is thought to potentially mediate DNA or protein binding but a clear function is yet to be established.
Mazur, Pawel, Gozani, Or, Sage, Julien, Reynoird, Nicolas   +3 more
openaire   +4 more sources

Evaluation and Characterization of Isoxazole Amides as SMYD3 Inhibitors [PDF]

, 2022
Optimization of binding affinities for ligands to their target protein is a primary objective in rational drug discovery. Herein we report on a collaborative study that evaluates various compounds designed to bind to the SET and MYND domain-containing protein 3 (SMYD3). SMYD3 is a histone methyltransferase and plays an important role in transcriptional
Shunzhou Wan, Agastya Bhati, David Wright, Ian Wall, Alan Graves, Darren Green, Peter Coveney   +6 more
openaire   +1 more source

Structural Analysis of SMYD3 Lysine Methyltransferase for the Development of Competitive and Specific Enzyme Inhibitors

Diseases, 2021
Lysine methylation is among the key posttranslational modifications to histones that contribute to epigenetic regulation. SMYD3 is a lysine methyltransferase that is essential for the proliferation of a range of tumorigenic cells. The findings that SMYD3
Dillon K. Jarrell, Kelly N. Hassell, Ilham Alshiraihi, Debbie C. Crans, Mark A. Brown   +4 more
doaj   +1 more source

SMYD3 induces sorafenib resistance by activating SMAD2/3-mediated epithelial-mesenchymal transition in hepatocellular carcinoma

iScience, 2023
Summary: Drug resistance prominently hampers the effects of systemic therapy of sorafenib to hepatocellular carcinoma (HCC). Epigenetics have critical regulatory roles in drug resistance.
Shanshan Wang, Xin You, Xiaoshu Liu, Fengwei Zhang, Hongjuan Zhou, Xuechai Shang, Long Cai   +6 more
doaj   +1 more source

Discovery of an Allosteric Ligand Binding Site in SMYD3 Lysine Methyltransferase

ChemBioChem, 2021
AbstractSMYD3 is a multifunctional epigenetic enzyme with lysine methyltransferase activity and various interaction partners. It is implicated in the pathophysiology of cancers but with an unclear mechanism. To discover tool compounds for clarifying its biochemistry and potential as a therapeutic target, a set of drug‐like compounds was screened in a ...
Vladimir O. Talibov, Edoardo Fabini, Edward A. FitzGerald, Daniele Tedesco, Daniela Cederfelt, Martin J. Talu, Moira M. Rachman, Filip Mihalic, Elisabetta Manoni, Marina Naldi, Paola Sanese, Giovanna Forte, Martina Lepore Signorile, Xavier Barril, Cristiano Simone, Manuela Bartolini, Doreen Dobritzsch, Alberto Del Rio, U. Helena Danielson   +18 more
openaire   +7 more sources

A SMYD3 Small‐Molecule Inhibitor Impairing Cancer Cell Growth [PDF]

Journal of Cellular Physiology, 2015
SMYD3 is a histone lysine methyltransferase that plays an important role in transcriptional activation as a member of an RNA polymerase complex, and its oncogenic role has been described in different cancer types. We studied the expression and activity of SMYD3 in a preclinical model of colorectal cancer (CRC) and found that it is strongly upregulated ...
Peserico, Alessia, Germani, Aldo, Sanese, Paola, Barbosa, Armenio Jorge, di Virgilio, Valeria, Fittipaldi, Raffaella, Fabini, Edoardo, Bertucci, Carlo, Varchi, Greta, Moyer, Mary Pat, Caretti, Giuseppina, del Rio, Alberto, Simone, Cristiano   +25 more
openaire   +6 more sources