Structure-Based Design and Characterization of the Highly Potent and Selective Covalent Inhibitors Targeting the Lysine Methyltransferases G9a/GLP

Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5

(2022) Deqin Rong et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of the First-in-Class G9a/GLP Covalent Inhibitors

(2022) Kwang-Su Park et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Epigenetic Regulators with Covalent Small-Molecule Inhibitors

(2021) Yi Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2021) Joshua R. Haebe et al.   Oncogenesis

The Histone Methyltransferase G9a Promotes Cholangiocarcinogenesis through Regulation of the Hippo Pathway Kinase LATS2 and YAP Signaling Pathway

(2020) Wenbo Ma et al.   HEPATOLOGY

Discovery of novel histone lysine methyltransferase G9a/GLP (EHMT2/1) inhibitors: Design, synthesis, and structure-activity relationships of 2,4-diamino-6-methylpyrimidines

(2020) Katsushi Katayama et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure

(2019) Ciro Milite et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of G9a by a small molecule inhibitor, UNC0642, induces apoptosis of human bladder cancer cells

(2019) Yue-peng Cao et al.   ACTA PHARMACOLOGICA SINICA

Insights for the design of protein lysine methyltransferase G9a inhibitors

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

Recent progress in histone methyltransferase (G9a) inhibitors as anticancer agents

(2019) Hao Cao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Histone lysine methyltransferases in biology and disease

(2019) Dylan Husmann et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Inhibition of the G9a/GLP histone methyltransferase complex modulates anxiety-related behavior in mice

(2018) Dong-yao Wang et al.   ACTA PHARMACOLOGICA SINICA

Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces

(2018) Obdulia Rabal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy

(2018) Obdulia Rabal et al.   JOURNAL OF MEDICINAL CHEMISTRY

G9A promotes gastric cancer metastasis by upregulating ITGB3 in a SET domain-independent manner

(2018) Lei Hu et al.   Cell Death & Disease

Novel pharmacological maps of protein lysine methyltransferases: key for target deorphanization

(2018) Obdulia Rabal et al.   Journal of Cheminformatics

Aminopyrazole Carboxamide Bruton’s Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning

(2018) Mark E. Schnute et al.   ACS Medicinal Chemistry Letters

Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase

(2017) Yan Xiong et al.   JOURNAL OF MEDICINAL CHEMISTRY

The winding path of protein methylation research: milestones and new frontiers

(2017) Jernej Murn et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-Plasmodium activity

(2017) Sandeep Sundriyal et al.   MedChemComm

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

Discovery of novel small molecule inhibitors of lysine methyltransferase G9a and their mechanism in leukemia cell lines

(2016) Shukkoor M. Kondengaden et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader–Willi syndrome

(2016) Yuna Kim et al.   NATURE MEDICINE

G9a-mediated methylation of ERα links the PHF20/MOF histone acetyltransferase complex to hormonal gene expression

(2016) Xi Zhang et al.   Nature Communications

Regulation of CD4 T-cell differentiation and inflammation by repressive histone methylation

(2015) Frann Antignano et al.   IMMUNOLOGY AND CELL BIOLOGY

The role of chromatin repressive marks in cognition and disease: A focus on the repressive complex GLP/G9a

(2015) Marco Benevento et al.   NEUROBIOLOGY OF LEARNING AND MEMORY

Functional Role of G9a Histone Methyltransferase in Cancer

(2015) Francesco Casciello et al.   Frontiers in Immunology

Chemical Probes of Histone Lysine Methyltransferases

(2014) H. Ümit Kaniskan et al.   ACS Chemical Biology

A Chemical Tool for In Vitro and In Vivo Precipitation of Lysine Methyltransferase G9a

(2014) Kyle D. Konze et al.   ChemMedChem

Functional Analysis of Histone Methyltransferase G9a in B and T Lymphocytes

(2014) L. R. Thomas et al.   JOURNAL OF IMMUNOLOGY

Selective Inhibitors of Protein Methyltransferases

(2014) H. Ümit Kaniskan et al.   JOURNAL OF MEDICINAL CHEMISTRY

The H3K9 methyltransferase G9a is a marker of aggressive ovarian cancer that promotes peritoneal metastasis

(2014) Kuo-Tai Hua et al.   Molecular Cancer

The cellular thermal shift assay for evaluating drug target interactions in cells

(2014) Rozbeh Jafari et al.   Nature Protocols

Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors

(2014) Nitipol Srimongkolpithak et al.   MedChemComm

Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a

(2014) Ramzi F. Sweis et al.   ACS Medicinal Chemistry Letters

Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2

(2014) Kanchan Devkota et al.   ACS Medicinal Chemistry Letters

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

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

A General Molecular Affinity Strategy for Global Detection and Proteomic Analysis of Lysine Methylation

(2013) Kaitlyn E. Moore et al.   MOLECULAR CELL

A Small-Molecule Probe of the Histone Methyltransferase G9a Induces Cellular Senescence in Pancreatic Adenocarcinoma

(2012) Yuan Yuan et al.   ACS Chemical Biology

Histone H3 Lysine 56 Methylation Regulates DNA Replication through Its Interaction with PCNA

(2012) Yongxin Yu et al.   MOLECULAR CELL

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

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

Histone methylation: a dynamic mark in health, disease and inheritance

(2012) Eric L. Greer et al.   NATURE REVIEWS GENETICS

Optimization of Cellular Activity of G9a Inhibitors 7-Aminoalkoxy-quinazolines

(2011) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

G9a and Glp Methylate Lysine 373 in the Tumor Suppressor p53

(2010) Jing Huang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines.

(2010) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Adding a Lysine Mimic in the Design of Potent Inhibitors of Histone Lysine Methyltransferases

(2010) Yanqi Chang et al.   JOURNAL OF MOLECULAR BIOLOGY

Histone H1 variant-specific lysine methylation by G9a/KMT1C and Glp1/KMT1D

(2010) Thomas Weiss et al.   Epigenetics & Chromatin

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

Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a

(2009) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294

(2009) Yanqi Chang et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Control of Cognition and Adaptive Behavior by the GLP/G9a Epigenetic Suppressor Complex

(2009) Anne Schaefer et al.   NEURON

Protein lysine methyltransferase G9a acts on non-histone targets

(2008) Philipp Rathert et al.   Nature Chemical Biology