标题
Unravelling KDM4 histone demethylase inhibitors for cancer therapy
作者
关键词
KDM4 inhibitors, Epigenetics, Histone demethylation, Cancer, JmjC domain
出版物
DRUG DISCOVERY TODAY
Volume 26, Issue 8, Pages 1841-1856
出版商
Elsevier BV
发表日期
2021-05-26
DOI
10.1016/j.drudis.2021.05.015
参考文献
相关参考文献
注意:仅列出部分参考文献,下载原文获取全部文献信息。- Quantitative MS‐Based Proteomics: Comparing the MCF‐7 Cellular Response to Hypoxia and a 2‐Oxoglutarate Analogue
- (2020) Jacob T. Bush et al. CHEMBIOCHEM
- A New Family of Jumonji C Domain-Containing KDM Inhibitors Inspired by Natural Product Purpurogallin
- (2020) José A. Souto et al. Frontiers in Chemistry
- C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays
- (2019) Yann-Vaï Le Bihan et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Structure‐based screening of tetrazolylhydrazide inhibitors vs. KDM4 histone demethylases
- (2019) Piotr H Malecki et al. ChemMedChem
- Benzo[b]tellurophenes as a Potential Histone H3 Lysine 9 Demethylase (KDM4) Inhibitor
- (2019) Yoon-Jung Kim et al. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
- Rational design, synthesis and biological profiling of new KDM4C inhibitors
- (2019) Vatroslav Letfus et al. BIOORGANIC & MEDICINAL CHEMISTRY
- Inhibition of the Histone Demethylase KDM4B Leads to Activation of KDM1A, Attenuates Bacterial-Induced Pro-Inflammatory Cytokine Release, and Reduces Osteoclastogenesis
- (2018) Joy E. Kirkpatrick et al. Epigenetics
- The JmjN domain as a dimerization interface and a targeted inhibitor of KDM4 demethylase activity
- (2018) May Levin et al. Oncotarget
- Synthesis and Biological Evaluation of Tripartin, a Putative KDM4 Natural Product Inhibitor, and 1-Dichloromethylinden-1-ol Analogues
- (2018) Lucía Guillade et al. ChemMedChem
- Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models
- (2017) Young K. Chen et al. ACS Medicinal Chemistry Letters
- Highly selective inhibition of histone demethylases by de novo macrocyclic peptides
- (2017) Akane Kawamura et al. Nature Communications
- Interrogating the Druggability of the 2-Oxoglutarate-Dependent Dioxygenase Target Class by Chemical Proteomics
- (2016) Gérard Joberty et al. ACS Chemical Biology
- 4-Biphenylalanine- and 3-Phenyltyrosine-Derived Hydroxamic Acids as Inhibitors of the JumonjiC-Domain-Containing Histone Demethylase KDM4A
- (2016) Ludovica Morera et al. ChemMedChem
- Identification and characterization of PKF118-310 as a KDM4A inhibitor
- (2016) Gianluigi Franci et al. Epigenetics
- Substituted 2-(2-aminopyrimidin-4-yl)pyridine-4-carboxylates as potent inhibitors of JumonjiC domain-containing histone demethylases
- (2016) Martin Roatsch et al. Future Medicinal Chemistry
- Selective silencing of α-globin by the histone demethylase inhibitor IOX1: a potentially new pathway for treatment of β-thalassemia
- (2016) Sachith Mettananda et al. HAEMATOLOGICA
- 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors
- (2016) Vassilios Bavetsias et al. JOURNAL OF MEDICINAL CHEMISTRY
- Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives
- (2016) Susan M. Westaway et al. JOURNAL OF MEDICINAL CHEMISTRY
- Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives
- (2016) Susan M. Westaway et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structure Property Relationships of Carboxylic Acid Isosteres
- (2016) Pierrik Lassalas et al. JOURNAL OF MEDICINAL CHEMISTRY
- Histone Modifications and Cancer
- (2016) James E. Audia et al. Cold Spring Harbor Perspectives in Biology
- Selective silencing of α-globin by the histone demethylase inhibitor IOX1: a potentially new pathway for treatment of β-thalassemia
- (2016) Sachith Mettananda et al. HAEMATOLOGICA
- Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases
- (2015) C. C. Thinnes et al. CHEMICAL COMMUNICATIONS
- KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR and BMYB-Regulated Genes
- (2015) Lingling Duan et al. CHEMISTRY & BIOLOGY
- Tetrazolylhydrazides as Selective Fragment-Like Inhibitors of the JumonjiC-Domain-Containing Histone Demethylase KDM4A
- (2015) Nicole Rüger et al. ChemMedChem
- Novel 5-carboxy-8-HQ based histone demethylase JMJD2A inhibitors: Introduction of an additional carboxyl group at the C-2 position of quinoline
- (2015) Taotao Feng et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- IOX1, a JMJD2A inhibitor, suppresses the proliferation and migration of vascular smooth muscle cells induced by angiotensin II by regulating the expression of cell cycle-related proteins
- (2015) QI HU et al. INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE
- Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors
- (2015) Magdalena Korczynska et al. JOURNAL OF MEDICINAL CHEMISTRY
- An Iridium(III) Complex Inhibits JMJD2 Activities and Acts as a Potential Epigenetic Modulator
- (2015) Li-Juan Liu et al. JOURNAL OF MEDICINAL CHEMISTRY
- Substrate- and Cofactor-independent Inhibition of Histone Demethylase KDM4C
- (2014) Ulrike Leurs et al. ACS Chemical Biology
- A Cell-Permeable Ester Derivative of the JmjC Histone Demethylase Inhibitor IOX1
- (2014) Rachel Schiller et al. ChemMedChem
- KDM4B as a Target for Prostate Cancer: Structural Analysis and Selective Inhibition by a Novel Inhibitor
- (2014) Chia-Han Chu et al. JOURNAL OF MEDICINAL CHEMISTRY
- Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor
- (2014) Katherine S. England et al. MedChemComm
- Structural Investigations of the Nickel-Induced Inhibition of Truncated Constructs of the JMJD2 Family of Histone Demethylases Using X-ray Absorption Spectroscopy
- (2013) Nitai Charan Giri et al. BIOCHEMISTRY
- Mutant IDH1 Enhances the Production of 2-Hydroxyglutarate Due to Its Kinetic Mechanism
- (2013) Alan R. Rendina et al. BIOCHEMISTRY
- KDM4/JMJD2 Histone Demethylases: Epigenetic Regulators in Cancer Cells
- (2013) W. L. Berry et al. CANCER RESEARCH
- Pan-Histone Demethylase Inhibitors Simultaneously Targeting Jumonji C and Lysine-Specific Demethylases Display High Anticancer Activities
- (2013) Dante Rotili et al. JOURNAL OF MEDICINAL CHEMISTRY
- Tripartin, a Histone Demethylase Inhibitor from a Bacterium Associated with a Dung Beetle Larva
- (2013) Seong-Hwan Kim et al. ORGANIC LETTERS
- Targeting the JMJD2 Histone Demethylases to Epigenetically Control Herpesvirus Infection and Reactivation from Latency
- (2013) Y. Liang et al. Science Translational Medicine
- 5-Carboxy-8-hydroxyquinoline is a broad spectrum 2-oxoglutarate oxygenase inhibitor which causes iron translocation
- (2013) Richard J. Hopkinson et al. Chemical Science
- The Ugi four-component reaction enables expedient synthesis and comparison of photoaffinity probes
- (2013) Jacob T. Bush et al. Chemical Science
- A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth
- (2013) Lei Wang et al. Nature Communications
- Linking of 2-Oxoglutarate and Substrate Binding Sites Enables Potent and Highly Selective Inhibition of JmjC Histone Demethylases
- (2012) Esther C. Y. Woon et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C)
- (2012) Ulrike Leurs et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Plant Growth Regulator Daminozide Is a Selective Inhibitor of Human KDM2/7 Histone Demethylases
- (2012) Nathan R. Rose et al. JOURNAL OF MEDICINAL CHEMISTRY
- Histone methylation: a dynamic mark in health, disease and inheritance
- (2012) Eric L. Greer et al. NATURE REVIEWS GENETICS
- Targeting Histone Lysine Demethylases by Truncating the Histone 3 Tail to Obtain Selective Substrate-Based Inhibitors
- (2011) Brian Lohse et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Regulation of chromatin by histone modifications
- (2011) Andrew J Bannister et al. CELL RESEARCH
- A Photoreactive Small-Molecule Probe for 2-Oxoglutarate Oxygenases
- (2011) Dante Rotili et al. CHEMISTRY & BIOLOGY
- Inhibition of Histone Demethylases by 4-Carboxy-2,2′-Bipyridyl Compounds
- (2011) Kai-Hsuan Chang et al. ChemMedChem
- Structural and Evolutionary Basis for the Dual Substrate Selectivity of Human KDM4 Histone Demethylase Family
- (2011) Lars Hillringhaus et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- A Selective Inhibitor and Probe of the Cellular Functions of Jumonji C Domain-Containing Histone Demethylases
- (2011) Xuelai Luo et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Inhibition of prolyl hydroxylases by dimethyloxaloylglycine after stroke reduces ischemic brain injury and requires hypoxia inducible factor-1α
- (2011) Molly E. Ogle et al. NEUROBIOLOGY OF DISEASE
- Structural insights into histone lysine demethylation
- (2010) Haifeng Hou et al. CURRENT OPINION IN STRUCTURAL BIOLOGY
- Selective Inhibitors of the JMJD2 Histone Demethylases: Combined Nondenaturing Mass Spectrometric Screening and Crystallographic Approaches
- (2010) Nathan R. Rose et al. JOURNAL OF MEDICINAL CHEMISTRY
- Design, Synthesis, Enzyme-Inhibitory Activity, and Effect on Human Cancer Cells of a Novel Series of Jumonji Domain-Containing Protein 2 Histone Demethylase Inhibitors
- (2010) Shohei Hamada et al. JOURNAL OF MEDICINAL CHEMISTRY
- Small-Molecule-Based Inhibition of Histone Demethylation in Cells Assessed by Quantitative Mass Spectrometry
- (2010) Mukram M. Mackeen et al. JOURNAL OF PROTEOME RESEARCH
- Chromatin structure and the inheritance of epigenetic information
- (2010) Raphaël Margueron et al. NATURE REVIEWS GENETICS
- Inhibition of the histone demethylase JMJD2E by 3-substituted pyridine 2,4-dicarboxylates
- (2010) Armin Thalhammer et al. ORGANIC & BIOMOLECULAR CHEMISTRY
- Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors
- (2010) Oliver N. F. King et al. PLoS One
- Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors
- (2009) Shohei Hamada et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Inhibition of the histone lysine demethylase JMJD2A by ejection of structural Zn(ii)
- (2009) Rok Sekirnik et al. CHEMICAL COMMUNICATIONS
- Dynamic Histone H1 Isotype 4 Methylation and Demethylation by Histone Lysine Methyltransferase G9a/KMT1C and the Jumonji Domain-containing JMJD2/KDM4 Proteins
- (2009) Patrick Trojer et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- A miniaturized screen for inhibitors of Jumonji histone demethylases
- (2009) Masaaki Sakurai et al. Molecular BioSystems
- Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases⊥
- (2008) Nathan R. Rose et al. JOURNAL OF MEDICINAL CHEMISTRY
Find Funding. Review Successful Grants.
Explore over 25,000 new funding opportunities and over 6,000,000 successful grants.
ExploreAdd your recorded webinar
Do you already have a recorded webinar? Grow your audience and get more views by easily listing your recording on Peeref.
Upload Now