DOT1L: a key target in normal chromatin remodelling and in mixed-lineage leukaemia treatment

The histone methyltransferase DOT1L is required for proper DNA damage response, DNA repair, and modulates chemotherapy responsiveness

(2019) Vijayalakshmi Kari et al.   Clinical Epigenetics

Inhibition of histone methyltransferase DOT1L silences ERα gene and blocks proliferation of antiestrogen-resistant breast cancer cells

(2019) Giovanni Nassa et al.   Science Advances

Structural Basis for Recognition of Ubiquitylated Nucleosome by Dot1L Methyltransferase

(2019) Cathy J. Anderson et al.   Cell Reports

The histone methyltransferase EZH2 primes the early differentiation of follicular helper T cells during acute viral infection

(2019) Xiangyu Chen et al.   Cellular & Molecular Immunology

Conserved crosstalk between histone deacetylation and H3K79 methylation generates DOT1L‐dose dependency in HDAC1‐deficient thymic lymphoma

(2019) Hanneke Vlaming et al.   EMBO JOURNAL

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

(2018) Eytan M. Stein et al.   BLOOD

Structural and functional analysis of the DOT1L–AF10 complex reveals mechanistic insights into MLL-AF10-associated leukemogenesis

(2018) Heng Zhang et al.   GENES & DEVELOPMENT

The protective role of DOT1L in UV-induced melanomagenesis

(2018) Bo Zhu et al.   Nature Communications

Lung Cancer Therapy Targeting Histone Methylation: Opportunities and Challenges

(2018) Yuchen Chen et al.   Computational and Structural Biotechnology Journal

Epigenetic tools (The Writers, The Readers and The Erasers) and their implications in cancer therapy

(2018) Subhankar Biswas et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Peptidomimetics for Targeting Protein–Protein Interactions between DOT1L and MLL Oncofusion Proteins AF9 and ENL

(2018) Lei Du et al.   ACS Medicinal Chemistry Letters

Cooperative gene activation by AF4 and DOT1L drives MLL-rearranged leukemia

(2017) Hiroshi Okuda et al.   JOURNAL OF CLINICAL INVESTIGATION

The MLL recombinome of acute leukemias in 2017

(2017) C Meyer et al.   LEUKEMIA

Mechanisms of Pinometostat (EPZ-5676) Treatment–Emergent Resistance in MLL -Rearranged Leukemia

(2017) Carly T. Campbell et al.   MOLECULAR CANCER THERAPEUTICS

The histone demethylase KDM3A regulates the transcriptional program of the androgen receptor in prostate cancer cells

(2017) Stephen Wilson et al.   Oncotarget

DOT1L as a therapeutic target for the treatment of DNMT3A -mutant acute myeloid leukemia

(2016) Rachel E. Rau et al.   BLOOD

Identification of Novel Disruptor of Telomeric Silencing 1-like (DOT1L) Inhibitors through Structure-Based Virtual Screening and Biological Assays

(2016) Shijie Chen et al.   Journal of Chemical Information and Modeling

Functional interdependence of BRD4 and DOT1L in MLL leukemia

(2016) Omer Gilan et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

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

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

‘Acute myeloid leukemia: a comprehensive review and 2016 update’

(2016) I De Kouchkovsky et al.   Blood Cancer Journal

Functional interdependence of BRD4 and DOT1L in MLL leukemia

(2016) Omer Gilan et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Targeting DOT1L and HOX gene expression in MLL-rearranged leukemia and beyond

(2015) Chun-Wei Chen et al.   EXPERIMENTAL HEMATOLOGY

Exploring drug delivery for the DOT1L inhibitor pinometostat (EPZ-5676): Subcutaneous administration as an alternative to continuous IV infusion, in the pursuit of an epigenetic target

(2015) Nigel J. Waters et al.   JOURNAL OF CONTROLLED RELEASE

Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor

(2014) Aravind Basavapathruni et al.   BIOPHARMACEUTICS & DRUG DISPOSITION

Functional characterisation of different MLL fusion proteins by using inducible Sleeping Beauty vectors

(2014) K. Wächter et al.   CANCER LETTERS

AF9 YEATS Domain Links Histone Acetylation to DOT1L-Mediated H3K79 Methylation

(2014) Yuanyuan Li et al.   CELL

DOT1L-HES6 fusion drives androgen independent growth in prostate cancer

(2014) M. Annala et al.   EMBO Molecular Medicine

Survival of Adults with Acute Lymphoblastic Leukemia in Germany and the United States

(2014) Dianne Pulte et al.   PLoS One

DOT1L Inhibition Sensitizes MLL-Rearranged AML to Chemotherapy

(2014) Wei Liu et al.   PLoS One

Direct interactions promote eviction of the Sir3 heterochromatin protein by the SWI/SNF chromatin remodeling enzyme

(2014) Benjamin J. Manning et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1

(2013) Kyle D. Konze et al.   ACS Chemical Biology

Bromo-deaza-SAH: A potent and selective DOT1L inhibitor

(2013) Wenyu Yu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

Chromatin Remodeling at DNA Double-Strand Breaks

(2013) Brendan D. Price et al.   CELL

Protein arginine methylation of non-histone proteins and its role in diseases

(2013) Han Wei et al.   CELL CYCLE

Promoter histone H3K27 methylation in the control of IGF2 imprinting in human tumor cell lines

(2013) Tao Li et al.   HUMAN MOLECULAR GENETICS

A Medicinal Chemistry Perspective for Targeting Histone H3 Lysine-79 Methyltransferase DOT1L

(2013) Justin L. Anglin et al.   JOURNAL OF MEDICINAL CHEMISTRY

The MLL recombinome of acute leukemias in 2013

(2013) C Meyer et al.   LEUKEMIA

Histone H4 Lysine 20 methylation: key player in epigenetic regulation of genomic integrity

(2013) S. Jorgensen et al.   NUCLEIC ACIDS RESEARCH

Structure of the Catalytic Domain of EZH2 Reveals Conformational Plasticity in Cofactor and Substrate Binding Sites and Explains Oncogenic Mutations

(2013) Hong Wu et al.   PLoS One

Epigenetics in Saccharomyces cerevisiae

(2013) M. Grunstein et al.   Cold Spring Harbor Perspectives in Biology

ATM Release at Resected Double-Strand Breaks Provides Heterochromatin Reconstitution to Facilitate Homologous Recombination

(2013) Verena Geuting et al.   PLoS Genetics

S-Adenosyl-Methionine-Dependent Methyltransferases: Highly Versatile Enzymes in Biocatalysis, Biosynthesis and Other Biotechnological Applications

(2012) Anna-Winona Struck et al.   CHEMBIOCHEM

Bat3 facilitates H3K79 dimethylation by DOT1L and promotes DNA damage-induced 53BP1 foci at G1/G2 cell-cycle phases

(2012) Timothy P Wakeman et al.   EMBO JOURNAL

The N676D and G697R mutations in the kinase domain of FLT3 confer resistance to the inhibitor AC220

(2012) D. Pauwels et al.   HAEMATOLOGICA

Mutations of FLT3/ITD confer resistance to multiple tyrosine kinase inhibitors

(2012) A B Williams et al.   LEUKEMIA

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

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

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

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

Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation

(2012) W. Qi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

(2012) Wenyu Yu et al.   Nature Communications

Requirement for Dot1l in murine postnatal hematopoiesis and leukemogenesis by MLL translocation

(2011) S. Y. Jo et al.   BLOOD

DOT1L, the H3K79 methyltransferase, is required for MLL-AF9-mediated leukemogenesis

(2011) A. T. Nguyen et al.   BLOOD

Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor

(2011) Scott R. Daigle et al.   CANCER CELL

Validation of the histone methyltransferase EZH2 as a therapeutic target for various types of human cancer and as a prognostic marker

(2011) Masashi Takawa et al.   CANCER SCIENCE

Essential role of DOT1L in maintaining normal adult hematopoiesis

(2011) Anh T Nguyen et al.   CELL RESEARCH

Deficiency of H3K79 Histone Methyltransferase Dot1-like Protein (DOT1L) Inhibits Cell Proliferation

(2011) Wootae Kim et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Histone Methyltransferase SETD3 Regulates Muscle Differentiation

(2011) Gwang Hyeon Eom et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Selective Inhibitors of Histone Methyltransferase DOT1L: Design, Synthesis, and Crystallographic Studies

(2011) Yuan Yao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The heterogeneity of pediatric MLL-rearranged acute myeloid leukemia

(2011) B V Balgobind et al.   LEUKEMIA

Dot1 and Histone H3K79 Methylation in Natural Telomeric and HM Silencing

(2011) Yoh-Hei Takahashi et al.   MOLECULAR CELL

A Common Telomeric Gene Silencing Assay Is Affected by Nucleotide Metabolism

(2011) Marlies P. Rossmann et al.   MOLECULAR CELL

Catalytic Mechanism Investigation of Lysine-Specific Demethylase 1 (LSD1): A Computational Study

(2011) Xiangqian Kong et al.   PLoS One

The AF4{middle dot}MLL fusion protein is capable of inducing ALL in mice without requirement of MLL{middle dot}AF4

(2010) A. Bursen et al.   BLOOD

MLL-AF9-Induced Leukemogenesis Requires Coexpression of the Wild-Type Mll Allele

(2010) Austin T. Thiel et al.   CANCER CELL

Outcome after relapse of acute lymphoblastic leukemia in adult patients included in four consecutive risk-adapted trials by the PETHEMA Study Group

(2010) A. Oriol et al.   HAEMATOLOGICA

Overexpression ofgrappaencoding a histone methyltransferase enhances stress resistance inDrosophila

(2009) Olivier List et al.   HEREDITAS

Molecular implementation and physiological roles for histone H3 lysine 4 (H3K4) methylation

(2008) Ali Shilatifard   CURRENT OPINION IN CELL BIOLOGY

Aberrant chromatin at genes encoding stem cell regulators in human mixed-lineage leukemia

(2008) M. G. Guenther et al.   GENES & DEVELOPMENT

DOT1L/KMT4 Recruitment and H3K79 Methylation Are Ubiquitously Coupled with Gene Transcription in Mammalian Cells

(2008) D. J. Steger et al.   MOLECULAR AND CELLULAR BIOLOGY

Chemically ubiquitylated histone H2B stimulates hDot1L-mediated intranucleosomal methylation

(2008) Robert K. McGinty et al.   NATURE

Nonprocessive methylation by Dot1 leads to functional redundancy of histone H3K79 methylation states

(2008) Floor Frederiks et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Genomic Loss of microRNA-101 Leads to Overexpression of Histone Methyltransferase EZH2 in Cancer

(2008) S. Varambally et al.   SCIENCE

The Histone H3K79 Methyltransferase Dot1L Is Essential for Mammalian Development and Heterochromatin Structure

(2008) Brendan Jones et al.   PLoS Genetics

Chronic Myeloid Leukemia Stem Cells

(2008) C. H. Jamieson   Hematology-American Society of Hematology Education Program