Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors

P Jaikhan, B Buranrat, Y Itoh, J Chotitumnavee… - Bioorganic & Medicinal …, 2019 - Elsevier
Abstract Fe (II)/α-ketoglutarate-dependent lysine demethylases (KDMs) are attractive drug
targets for several diseases including cancer. In this study, we designed and screened ortho …

Strategies of polypharmacology

Z Wang, B Yang - Polypharmacology: Principles and Methodologies, 2022 - Springer
In Chap. 1, we have learned that the modern pharmacological therapy of human disease
and new drug discovery are based primarily on four major strategies/modality: the STD …

[HTML][HTML] 组蛋白甲基转移酶SUV4-20H 的研究进展

赵丹洋, 姜红, 姜红堃 - 中国医科大学学报, 2020 - html.rhhz.net
组蛋白甲基转移酶SUV4-20H 为哺乳动物组蛋白H4 第20 位赖氨酸(H4K20)
的特异性甲基转移酶, 在人体组织中广泛表达. SUV4-20H 蛋白本身及其介导的H4K20 …

Modulation of DNA/RNA Methylation by Small-Molecule Modulators and Their Implications in Cancer

A Verma, A Sinha, D Datta - Metabolism and Epigenetic Regulation …, 2022 - Springer
Chromatin is an organized complex of DNA, histone proteins, and RNA. Chromatin
modifications include DNA methylation, RNA methylation, and histone acetylation and …

Epigenetic control using small molecules in cancer

T Kozako, Y Itoh, S Honda, T Suzuki - Approaching Complex Diseases …, 2020 - Springer
Epigenetics is defined as heritable alterations in gene expression that are not caused by
changes in DNA sequence. Such normal alterations are vital for appropriate differentiation …

[PDF][PDF] Mitochondria and Cancer Pathogenesis–The role of Reactive Oxygen Species (ROS) Production, Apoptosis, and Epigenetics: A Review

NA Chrysanthakopoulos, E Vryzaki - 2022 - researchgate.net
■ Abstract Mitochondria are metabolic organelles responsible for cellular functions such as
development, division, energy metabolism by oxidative phosphorylation (OXPHOS) …

[PDF][PDF] Modulatoren epigenetischer Regulationsmechanismen: Medizinische Chemie neuer KDM4-Inhibitoren und Methodenentwicklung zur SFC-MS-Analytik von …

GM Fassauer - 2018 - epub.ub.uni-greifswald.de
Die Zusammenhänge zwischen der Aktivität Epigenetik-assoziierter Enzyme und
Krankheitsgeschehen neoplastischer Art konnten nicht nur experimentell bestätigt, sondern …

Modus operandi of COMPASS/MLL epigenetic writers in the mammalian genome

D Bayarsaihan - Epigenomics, 2018 - Taylor & Francis
The COMPASS/MLL family of H3K4 methyltransferases is highly conserved throughout the
eukaryotic kingdom [1]. MLL4 (KMT2D) is a main H3K4 methyltransferase responsible for …

[PDF][PDF] Structural view on the role of TRD loop in regulating DNMT3A activity: a molecular dynamics study

Z Wang, Y Kang - researchgate.net
DNA methyltransferase 3A (DNMT3A) has been regarded as a potential epigenetic target for
the development of cancer therapeutics. A number of DNMT3A inhibitors have been …

[HTML][HTML] Mimicking the Nucleosomal Context in Peptide-Based Binders of a H3K36me Reader Increases Binding Affinity While Altering the Binding Mode

V Horn, SAK Jongkees, H van Ingen - Molecules, 2020 - mdpi.com
Targeting of proteins in the histone modification machinery has emerged as a promising
new direction to fight disease. The search for compounds that inhibit proteins that readout …