Emerging role of G9a in cancer stemness and promises as a therapeutic target

G9a controls pluripotent-like identity and tumor-initiating function in human colorectal cancer

(2021) Christopher J. Bergin et al.   ONCOGENE

Dual EZH2 and G9a inhibition suppresses multiple myeloma cell proliferation by regulating the interferon signal and IRF4-MYC axis

(2021) Kazuya Ishiguro et al.   Cell Death Discovery

G9a Inhibition Enhances Checkpoint Inhibitor Blockade Response in Melanoma

(2021) Gregory M. Kelly et al.   CLINICAL CANCER RESEARCH

The roles of Polycomb repressive complexes in mammalian development and cancer

(2021) Andrea Piunti et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Targeting protein lysine methyltransferase G9A impairs self-renewal of chronic myelogenous leukemia stem cells via upregulation of SOX6

(2021) Min Zhou et al.   ONCOGENE

High throughput screening identifies SOX2 as a super pioneer factor that inhibits DNA methylation maintenance at its binding sites

(2021) Ludovica Vanzan et al.   Nature Communications

Complete loss of H3K9 methylation dissolves mouse heterochromatin organization

(2021) Thomas Montavon et al.   Nature Communications

Epigenetics of colorectal cancer: biomarker and therapeutic potential

(2020) Gerhard Jung et al.   Nature Reviews Gastroenterology & Hepatology

Selective targeting of TET catalytic domain promotes somatic cell reprogramming

(2020) Anup Kumar Singh et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Quantifying Hematopoietic Stem Cell Clonal Diversity by Selecting Informative Amplicon Barcodes

(2020) Emily M. Teets et al.   Scientific Reports

SETDB1-Mediated Cell Fate Transition between 2C-Like and Pluripotent States

(2020) Kaixin Wu et al.   Cell Reports

Gain-of-function genetic alterations of G9a drive oncogenesis

(2020) Shinichiro Kato et al.   Cancer Discovery

BMI1 Inhibition Eliminates Residual Cancer Stem Cells after PD1 Blockade and Activates Antitumor Immunity to Prevent Metastasis and Relapse

(2020) Lingfei Jia et al.   Cell Stem Cell

Histone-writer cancer drugs enter center stage

(2020) Ken Garber   NATURE BIOTECHNOLOGY

G9a regulates tumorigenicity and stemness through genome-wide DNA methylation reprogramming in non-small cell lung cancer

(2020) Rajendra P. Pangeni et al.   Clinical Epigenetics

Frequent upregulation of G9a promotes RelB-dependent proliferation and survival in multiple myeloma

(2020) Xi Yun Zhang et al.   Experimental Hematology & Oncology

Concepts of extracellular matrix remodelling in tumour progression and metastasis

(2020) Juliane Winkler et al.   Nature Communications

Context-Dependent Requirement of Euchromatic Histone Methyltransferase Activity during Reprogramming to Pluripotency

(2020) Simon E. Vidal et al.   Stem Cell Reports

Insight into the multi-faceted role of the SUV family of H3K9 methyltransferases in carcinogenesis and cancer progression

(2020) Nirmalya Saha et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

Discovery of DS79932728: A Potent, Orally Available G9a/GLP Inhibitor for Treating β-Thalassemia and Sickle Cell Disease

(2020) Katsushi Katayama et al.   ACS Medicinal Chemistry Letters

Cancer Stem Cells: The Architects of the Tumor Ecosystem

(2019) Briana C. Prager et al.   Cell Stem Cell

Targeting bivalency de-represses Indian Hedgehog and inhibits self-renewal of colorectal cancer-initiating cells

(2019) Evelyne Lima-Fernandes et al.   Nature Communications

Insights for the design of protein lysine methyltransferase G9a inhibitors

(2019) Mariasoosai Ramya Chandar Charles et al.   Future Medicinal Chemistry

Cancer stemness, intratumoral heterogeneity, and immune response across cancers

(2019) Alex Miranda et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Short-term 3D culture systems of various complexity for treatment optimization of colorectal carcinoma

(2019) Marloes Zoetemelk et al.   Scientific Reports

Inhibition of a G9a/DNMT network triggers immune-mediated bladder cancer regression

(2019) Cristina Segovia et al.   NATURE MEDICINE

A marker-independent lineage-tracing system to quantify clonal dynamics and stem cell functionality in cancer tissue

(2019) Kristiaan J. Lenos et al.   Nature Protocols

Improving drug discovery using image-based multiparametric analysis of the epigenetic landscape

(2019) Chen Farhy et al.   eLife

Machine Learning Identifies Stemness Features Associated with Oncogenic Dedifferentiation

(2018) Tathiane M. Malta et al.   CELL

Liver-specific knockout of histone methyltransferase G9a impairs liver maturation and dysregulates inflammatory, cytoprotective, and drug-processing genes

(2018) Hong Lu et al.   XENOBIOTICA

Identification of Chemotherapy-Induced Leukemic-Regenerating Cells Reveals a Transient Vulnerability of Human AML Recurrence

(2018) Allison L. Boyd et al.   CANCER CELL

H3K9 methyltransferases and demethylases control lung tumor-propagating cells and lung cancer progression

(2018) S. P. Rowbotham et al.   Nature Communications

A distinct role for Lgr5+ stem cells in primary and metastatic colon cancer

(2017) Felipe de Sousa e Melo et al.   NATURE

Colonic organoids derived from human induced pluripotent stem cells for modeling colorectal cancer and drug testing

(2017) Miguel Crespo et al.   NATURE MEDICINE

G9a governs colon cancer stem cell phenotype and chemoradioresistance through PP2A-RPA axis-mediated DNA damage response

(2017) Chi-Wen Luo et al.   RADIOTHERAPY AND ONCOLOGY

Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies

(2017) Edurne San José-Enériz et al.   Nature Communications

Lineage-Specific Differentiation Is Influenced by State of Human Pluripotency

(2017) Jong-Hee Lee et al.   Cell Reports

G9a inhibition potentiates the anti-tumour activity of DNA double-strand break inducing agents by impairing DNA repair independent of p53 status

(2016) Pallavi Agarwal et al.   CANCER LETTERS

Inhibiting the SUMO Pathway Represses the Cancer Stem Cell Population in Breast and Colorectal Carcinomas

(2016) Maria V. Bogachek et al.   Stem Cell Reports

DNA-Demethylating Agents Target Colorectal Cancer Cells by Inducing Viral Mimicry by Endogenous Transcripts

(2015) David Roulois et al.   CELL

Prospective Derivation of a Living Organoid Biobank of Colorectal Cancer Patients

(2015) Marc van de Wetering et al.   CELL

The interplay of histone modifications - writers that read

(2015) T. Zhang et al.   EMBO REPORTS

Melanoma-intrinsic β-catenin signalling prevents anti-tumour immunity

(2015) Stefani Spranger et al.   NATURE

Ductal pancreatic cancer modeling and drug screening using human pluripotent stem cell– and patient-derived tumor organoids

(2015) Ling Huang et al.   NATURE MEDICINE

G9a is essential for EMT-mediated metastasis and maintenance of cancer stem cell-like characters in head and neck squamous cell carcinoma

(2015) Shuli Liu et al.   Oncotarget

Dual EZH2 and EHMT2 histone methyltransferase inhibition increases biological efficacy in breast cancer cells

(2015) Edward Curry et al.   Clinical Epigenetics

Chromatin dynamics and the role of G9a in gene regulation and enhancer silencing during early mouse development

(2015) Jan J Zylicz et al.   eLife

Progressive Chromatin Condensation and H3K9 Methylation Regulate the Differentiation of Embryonic and Hematopoietic Stem Cells

(2015) Fernando Ugarte et al.   Stem Cell Reports

Functional Role of G9a Histone Methyltransferase in Cancer

(2015) Francesco Casciello et al.   Frontiers in Immunology

The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia

(2015) William N. Pappano et al.   PLoS One

Premature Termination of Reprogramming In Vivo Leads to Cancer Development through Altered Epigenetic Regulation

(2014) Kotaro Ohnishi et al.   CELL

Reconstructing and Reprogramming the Tumor-Propagating Potential of Glioblastoma Stem-like Cells

(2014) Mario L. Suvà et al.   CELL

Evolution of the Cancer Stem Cell Model

(2014) Antonija Kreso et al.   Cell Stem Cell

Molecular Pathways: Epigenetic Modulation of Wnt-Glycogen Synthase Kinase-3 Signaling to Target Human Cancer Stem Cells

(2014) Y. D. Benoit et al.   CLINICAL CANCER RESEARCH

The methyltransferase G9a regulates HoxA9-dependent transcription in AML

(2014) B. Lehnertz et al.   GENES & DEVELOPMENT

The Histone H3 Lysine 9 Methyltransferases G9a and GLP Regulate Polycomb Repressive Complex 2-Mediated Gene Silencing

(2014) Chiara Mozzetta et al.   MOLECULAR CELL

Identification of pre-leukaemic haematopoietic stem cells in acute leukaemia

(2014) Liran I. Shlush et al.   NATURE

The Histone H3 Methyltransferase G9A Epigenetically Activates the Serine-Glycine Synthesis Pathway to Sustain Cancer Cell Survival and Proliferation

(2013) Jane Ding et al.   Cell Metabolism

Phenotypic vs. Target-Based Drug Discovery for First-in-Class Medicines

(2013) D C Swinney   CLINICAL PHARMACOLOGY & THERAPEUTICS

Pharmacological inhibition of polycomb repressive complex-2 activity induces apoptosis in human colon cancer stem cells

(2013) Yannick D. Benoit et al.   EXPERIMENTAL CELL RESEARCH

Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP

(2013) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

AID stabilizes stem-cell phenotype by removing epigenetic memory of pluripotency genes

(2013) Ritu Kumar et al.   NATURE

Self-renewal as a therapeutic target in human colorectal cancer

(2013) Antonija Kreso et al.   NATURE MEDICINE

Genomic and Epigenomic Landscapes of Adult De Novo Acute Myeloid Leukemia

(2013)   NEW ENGLAND JOURNAL OF MEDICINE

Epigenetic Reprogramming in Cancer

(2013) M. L. Suva et al.   SCIENCE

Pluripotent Stem Cells Induced from Mouse Somatic Cells by Small-Molecule Compounds

(2013) P. Hou et al.   SCIENCE

Cancer Stem Cells: Impact, Heterogeneity, and Uncertainty

(2012) Jeffrey A. Magee et al.   CANCER CELL

Identification of Drugs Including a Dopamine Receptor Antagonist that Selectively Target Cancer Stem Cells

(2012) Eleftherios Sachlos et al.   CELL

Histone Lysine Methylation Dynamics: Establishment, Regulation, and Biological Impact

(2012) Joshua C. Black et al.   MOLECULAR CELL

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

(2012) Michael T. McCabe et al.   NATURE

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

(2012) Sarah K Knutson et al.   Nature Chemical Biology

Maintenance of gene silencing by the coordinate action of the H3K9 methyltransferase G9a/KMT1C and the H3K4 demethylase Jarid1a/KDM5A

(2012) C.-P. Chaturvedi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Regulation of chromatin by histone modifications

(2011) Andrew J Bannister et al.   CELL RESEARCH

Maintaining embryonic stem cell pluripotency with Wnt signaling

(2011) S. Y. Sokol   DEVELOPMENT

Global histone modification of histone H3 in colorectal cancer and its precursor lesions

(2011) Tadao Nakazawa et al.   HUMAN PATHOLOGY

A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells

(2011) Masoud Vedadi et al.   Nature Chemical Biology

Lysine methyltransferase G9a is required for de novo DNA methylation and the establishment, but not the maintenance, of proviral silencing

(2011) D. C. Leung et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

MPP8 mediates the interactions between DNA methyltransferase Dnmt3a and H3K9 methyltransferase GLP/G9a

(2011) Yanqi Chang et al.   Nature Communications

Revisiting Heterochromatin in Embryonic Stem Cells

(2011) Irina Stancheva   PLoS Genetics

Leukemic IDH1 and IDH2 Mutations Result in a Hypermethylation Phenotype, Disrupt TET2 Function, and Impair Hematopoietic Differentiation

(2010) Maria E. Figueroa et al.   CANCER CELL

A Myc Network Accounts for Similarities between Embryonic Stem and Cancer Cell Transcription Programs

(2010) Jonghwan Kim et al.   CELL

Polycomb Group Proteins Set the Stage for Early Lineage Commitment

(2010) Lauren E. Surface et al.   Cell Stem Cell

Methyl-H3K9-binding protein MPP8 mediates E-cadherin gene silencing and promotes tumour cell motility and invasion

(2010) Kenji Kokura et al.   EMBO JOURNAL

Activating and inhibitory functions for the histone lysine methyltransferase G9a in T helper cell differentiation and function

(2010) Bernhard Lehnertz et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Loss of miR-200 Inhibition of Suz12 Leads to Polycomb-Mediated Repression Required for the Formation and Maintenance of Cancer Stem Cells

(2010) Dimitrios Iliopoulos et al.   MOLECULAR CELL

Epigenetic memory in induced pluripotent stem cells

(2010) K. Kim et al.   NATURE

Wnt activity defines colon cancer stem cells and is regulated by the microenvironment

(2010) Louis Vermeulen et al.   NATURE CELL BIOLOGY

EZH2 Is Essential for Glioblastoma Cancer Stem Cell Maintenance

(2009) M.-L. Suva et al.   CANCER RESEARCH

Characterization of human embryonic stem cells with features of neoplastic progression

(2009) Tamra E Werbowetski-Ogilvie et al.   NATURE BIOTECHNOLOGY

An embryonic stem cell–like gene expression signature in poorly differentiated aggressive human tumors

(2008) Ittai Ben-Porath et al.   NATURE GENETICS

De novo DNA methylation promoted by G9a prevents reprogramming of embryonically silenced genes

(2008) Silvina Epsztejn-Litman et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY