Results 41 to 50 of about 2,026 (156)

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

Canonical and Non-Canonical Functions of Histone H3K4 Methylation Modifiers in Cancer. [PDF]

Cancer Sci
Histone H3K4‐modifying enzymes regulate gene expression and cellular processes critical to cancer development. Beyond their canonical roles, these enzymes also exhibit non‐catalytic and non‐histone functions, offering new opportunities for therapeutic intervention. ABSTRACT Histone H3K4 modifications are altered in the regulation of gene expression and
Hoshii T.
europepmc   +2 more sources

Temporal Nasal Epithelial Gene Expression Patterns in Healthy Individuals Infected With Rhinovirus-16, and Its Modulation by Carrot Rhamnogalacturonan-I. [PDF]

J Med Virol
ABSTRACT Innate immune and interferon‐induced responses to in vivo nasal infection with rhinovirus (RV)16 in healthy subjects are accelerated by low‐dose dietary supplementation with carrot‐derived pectic polysaccharide rhamnogalacturonan‐I (cRG‐I), together with reduced duration and severity of symptoms.
Mol J, Volckmann R, Ravi A, Ravanetti L, Calame W, McKay S, Albers R, Koster J, Lutter R.   +8 more
europepmc   +2 more sources

Discovery of Irreversible Inhibitors Targeting Histone Methyltransferase, SMYD3 [PDF]

ACS Medicinal Chemistry Letters, 2019
SMYD3 is a histone methyltransferase that regulates gene transcription, and its overexpression is associated with multiple human cancers. A novel class of tetrahydroacridine compounds which inhibit SMYD3 through a covalent mechanism of action is identified. Optimization of these irreversible inhibitors resulted in the discovery of 4-chloroquinolines, a
Chuhui Huang, Si Si Liew, Grace R. Lin, Anders Poulsen, Melgious J. Y. Ang, Brian C. S. Chia, Sin Yin Chew, Zekui P. Kwek, John L. K. Wee, Esther H. Ong, Priya Retna, Nithya Baburajendran, Rong Li, Weixuan Yu, Xiaoying Koh-Stenta, Anna Ngo, Sravanthy Manesh, Justina Fulwood, Zhiyuan Ke, Hwa Hwa Chung, Sugunavathi Sepramaniam, Xin Hui Chew, Nurul Dinie, May Ann Lee, Yun Shan Chew, Choon Bing Low, Vishal Pendharkar, Vithya Manoharan, Susmitha Vuddagiri, Kanda Sangthongpitag, Joma Joy, Alex Matter, Jeffrey Hill, Thomas H. Keller, Klement Foo   +34 more
openaire   +2 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

SMYD3 (SET and MYND domain containing 3) [PDF]

Atlas of Genetics and Cytogenetics in Oncology and Haematology, 2011
Review on SMYD3 (SET and MYND domain containing 3), with data on DNA, on the protein encoded, and where the gene is implicated.
Luo, XG, Guo, S, Zhang, TC
openaire   +2 more sources

Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors

ACS Medicinal Chemistry Letters, 2019
We report herein the discovery of isoxazole amides as potent and selective SET and MYND Domain-Containing Protein 3 (SMYD3) inhibitors. Elucidation of the structure-activity relationship of the high-throughput screening (HTS) lead compound 1 provided potent and selective SMYD3 inhibitors.
Dai-Shi Su, Junya Qu, Mark Schulz, Chuck W. Blackledge, Hongyi Yu, Jenny Zeng, Joelle Burgess, Alexander Reif, Melissa Stern, Raman Nagarajan, Melissa Baker Pappalardi, Kristen Wong, Alan P. Graves, William Bonnette, Liping Wang, Patricia Elkins, Beth Knapp-Reed, Jeffrey D. Carson, Charles McHugh, Helai Mohammad, Ryan Kruger, Juan Luengo, Dirk A. Heerding, Caretha L. Creasy   +23 more
openaire   +3 more sources