Exploring Methods of Targeting Histone Methyltransferases and Their Applications in Cancer Therapeutics

Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2

(2021) Zhihao Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

CARM1 Inhibition Enables Immunotherapy of Resistant Tumors by Dual Action on Tumor cells and T cells

(2021) Sushil Kumar et al.   Cancer Discovery

Synthesis and Biological Activity of a Cytostatic Inhibitor of MLLr Leukemia Targeting the DOT1L Protein

(2021) Corentin Bon et al.   MOLECULES

A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models

(2021) Xufen Yu et al.   Science Translational Medicine

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

Tazemetostat: First Approval

(2020) Sheridan M. Hoy   DRUGS

Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor

(2020) Yudao Shen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response

(2020) Magdalena M. Szewczyk et al.   Nature Communications

Novel Inhibitors of the Histone-Methyltransferase DOT1L Show Potent Antileukemic Activity in Patient-derived Xenografts.

(2020) Florian Perner et al.   BLOOD

Discovery of First-in-class Protein Arginine Methyltransferase 5 (PRMT5) Degraders

(2020) Yudao Shen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tazemetostat for patients with relapsed or refractory follicular lymphoma: an open-label, single-arm, multicentre, phase 2 trial

(2020) Franck Morschhauser et al.   LANCET ONCOLOGY

Covalent inhibition of NSD1 histone methyltransferase

(2020) Huang Huang et al.   Nature Chemical Biology

The epigenetic regulator Mll1 is required for Wnt-driven intestinal tumorigenesis and cancer stemness

(2020) Johanna Grinat et al.   Nature Communications

BET and EZH2 Inhibitors: Novel Approaches for Targeting Cancer

(2019) Sofia Genta et al.   Current Oncology Reports

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

Covalent Inhibition in Drug Discovery

(2019) Avick Kumar Ghosh et al.   ChemMedChem

Nucleoside Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors

(2019) Hong Lin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Computer-Aided Discovery of Massonianoside B as a Novel Selective DOT1L Inhibitor

(2019) Jie Chen et al.   ACS Chemical Biology

Discovery of Potent and Selective Covalent Protein Arginine Methyl-transferase 5 (PRMT5) Inhibitors.

(2019) Hong Lin et al.   ACS Medicinal Chemistry Letters

LINC00665 Induces Acquired Resistance to Gefitinib through Recruiting EZH2 and Activating PI3K/AKT Pathway in NSCLC

(2019) Xinyin Liu et al.   Molecular Therapy-Nucleic Acids

The role and prospect of JMJD3 in stem cells and cancer

(2019) Xiaojiao Yin et al.   BIOMEDICINE & PHARMACOTHERAPY

Methyltransferase Inhibitors: Competing with, or Exploiting the Bound Cofactor

(2019) Renato Ferreira de Freitas et al.   MOLECULES

New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse

(2019) Frédéric Stauffer et al.   ACS Medicinal Chemistry Letters

The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia

(2018) Eytan M. Stein et al.   BLOOD

High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2

(2018) Nathan P Coussens et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study

(2018) Antoine Italiano et al.   LANCET ONCOLOGY

LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity

(2018) Zahid Q. Bonday et al.   ACS Medicinal Chemistry Letters

TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma

(2018) Kazuhide Nakayama et al.   Oncotarget

miR-137 mediates the functional link between c-Myc and EZH2 that regulates cisplatin resistance in ovarian cancer

(2018) Jing Sun et al.   ONCOGENE

PRMT7 contributes to the metastasis phenotype in human non-small-cell lung cancer cells possibly through the interaction with HSPA5 and EEF2

(2018) Dezhi Cheng et al.   OncoTargets and Therapy

COSMIC: the Catalogue Of Somatic Mutations In Cancer

(2018) John G Tate et al.   NUCLEIC ACIDS RESEARCH

The Histone H3 Lysine 4 Presenter WDR5 as an Oncogenic Protein and Novel Epigenetic Target in Cancer

(2018) Kebin Lu et al.   Frontiers in Oncology

SHARPIN-mediated regulation of protein arginine methyltransferase 5 controls melanoma growth

(2017) Hironari Tamiya et al.   JOURNAL OF CLINICAL INVESTIGATION

The EED protein–protein interaction inhibitor A-395 inactivates the PRC2 complex

(2017) Yupeng He et al.   Nature Chemical Biology

The Role of Nuclear Receptor–Binding SET Domain Family Histone Lysine Methyltransferases in Cancer

(2017) Richard L. Bennett et al.   Cold Spring Harbor Perspectives in Medicine

Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma

(2017) Allison E. Drew et al.   Scientific Reports

Biological function and regulation of histone and non-histone lysine methylation in response to DNA damage

(2016) Yongcan Chen et al.   ACTA BIOCHIMICA ET BIOPHYSICA SINICA

MLL1 is essential for the senescence-associated secretory phenotype

(2016) Brian C. Capell et al.   GENES & DEVELOPMENT

Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6

(2016) Yudao Shen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase

(2016) Kyle V. Butler et al.   JOURNAL OF MEDICINAL CHEMISTRY

Complementary activities of DOT1L and Menin inhibitors in MLL-rearranged leukemia

(2016) C Dafflon et al.   LEUKEMIA

Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach

(2016) Chao Chen et al.   ACS Medicinal Chemistry Letters

Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase

(2015) David S. Rogawski et al.   BIOCHEMISTRY

The dual epigenetic role of PRMT5 in acute myeloid leukemia: gene activation and repression via histone arginine methylation

(2015) S S Tarighat et al.   LEUKEMIA

Epigenetic silencing of TH1-type chemokines shapes tumour immunity and immunotherapy

(2015) Dongjun Peng et al.   NATURE

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models

(2015) Elayne Chan-Penebre et al.   Nature Chemical Biology

Targeting the MLL complex in castration-resistant prostate cancer

(2015) Rohit Malik et al.   NATURE MEDICINE

Targeting histone lysine methylation in cancer

(2015) John McGrath et al.   PHARMACOLOGY & THERAPEUTICS

Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound

(2015) Lorna H. Mitchell et al.   ACS Medicinal Chemistry Letters

Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666

(2015) Kenneth W. Duncan et al.   ACS Medicinal Chemistry Letters

Structural biology and chemistry of protein arginine methyltransferases

(2014) Matthieu Schapira et al.   MedChemComm

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

Allostery in Disease and in Drug Discovery

(2013) Ruth Nussinov et al.   CELL

Histone Methyltransferase Inhibitors: Novel Epigenetic Agents for Cancer Treatment

(2013) C. Zagni et al.   CURRENT MEDICINAL CHEMISTRY

Protein arginine methyltransferase 5 is essential for growth of lung cancer cells

(2012) Zhongping Gu et al.   BIOCHEMICAL JOURNAL

Understanding the language of Lys36 methylation at histone H3

(2012) Eric J. Wagner et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

(2012) Wenyu Yu et al.   Nature Communications

EZH2 Is Required for Breast and Pancreatic Cancer Stem Cell Maintenance and Can Be Used as a Functional Cancer Stem Cell Reporter

(2012) Lilian E. van Vlerken et al.   Stem Cells Translational Medicine

Structural Chemistry of the Histone Methyltransferases Cofactor Binding Site

(2011) Valérie Campagna-Slater et al.   Journal of Chemical Information and Modeling

The Language of Histone Crosstalk

(2010) Jung-Shin Lee et al.   CELL

Structural Biology of Human H3K9 Methyltransferases

(2010) Hong Wu et al.   PLoS One

Protein Arginine Methylation in Mammals: Who, What, and Why

(2009) Mark T. Bedford et al.   MOLECULAR CELL