Targeting human SET1/MLL family of proteins

Enhancer deregulation in cancer and other diseases

(2016) Hans-Martin Herz   BIOESSAYS

Design of a fluorescent ligand targeting the S-adenosylmethionine binding site of the histone methyltransferase MLL1

(2016) Yepeng Luan et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Loss of Mll3 Catalytic Function Promotes Aberrant Myelopoiesis

(2016) Kelly M. Arcipowski et al.   PLoS One

A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

(2015) H. Ümit Kaniskan et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Development and Use of Assay Conditions Suited to Screening for and Profiling of SET-Domain-Targeted Inhibitors of the MLL/SET1 Family of Lysine Methyltransferases

(2015) Joseph J. Ferry et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Kinetic characterization of human histone H3 lysine 36 methyltransferases, ASH1L and SETD2

(2015) Mohammad S. Eram et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Pharmacologic Inhibition of the Menin-MLL Interaction Blocks Progression of MLL Leukemia In Vivo

(2015) Dmitry Borkin et al.   CANCER CELL

Integrated Genomic Analysis Suggests MLL3 Is a Novel Candidate Susceptibility Gene for Familial Nasopharyngeal Carcinoma

(2015) M. M. Sasaki et al.   CANCER EPIDEMIOLOGY BIOMARKERS & PREVENTION

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

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

Biochemical Reconstitution and Phylogenetic Comparison of Human SET1 Family Core Complexes Involved in Histone Methylation

(2015) Stephen A. Shinsky et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Unique Role of the WD-40 Repeat Protein 5 (WDR5) Subunit within the Mixed Lineage Leukemia 3 (MLL3) Histone Methyltransferase Complex

(2015) Stephen A. Shinsky et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Gain-of-function p53 mutants co-opt chromatin pathways to drive cancer growth

(2015) Jiajun Zhu et al.   NATURE

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia

(2015) Florian Grebien et al.   Nature Chemical Biology

Evolving Catalytic Properties of the MLL Family SET Domain

(2015) Ying Zhang et al.   STRUCTURE

Clinical implications of genomic alterations in the tumour and circulation of pancreatic cancer patients

(2015) Mark Sausen et al.   Nature Communications

The cancer COMPASS: navigating the functions of MLL complexes in cancer

(2015) David J. Ford et al.   Cancer Genetics

Somatic cancer mutations in the MLL3-SET domain alter the catalytic properties of the enzyme

(2015) Sara Weirich et al.   Clinical Epigenetics

Roles of DPY30 in the Proliferation and Motility of Gastric Cancer Cells

(2015) Yong Joo Lee et al.   PLoS One

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

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

The DPY30 subunit in SET1/MLL complexes regulates the proliferation and differentiation of hematopoietic progenitor cells

(2014) Z. Yang et al.   BLOOD

A systematic description of MLL fusion gene formation

(2014) Rebecca L. Wright et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Identification of anMLL4-GPS2fusion as an oncogenic driver of undifferentiated spindle cell sarcoma in a child

(2014) Elaine O'Meara et al.   GENES CHROMOSOMES & CANCER

Trimethylation of Histone H3 Lysine 36 by Human Methyltransferase PRDM9 Protein

(2014) Mohammad S. Eram et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

High-Affinity Small-Molecule Inhibitors of the Menin-Mixed Lineage Leukemia (MLL) Interaction Closely Mimic a Natural Protein–Protein Interaction

(2014) Shihan He et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting MLL1 H3K4 Methyltransferase Activity in Mixed-Lineage Leukemia

(2014) Fang Cao et al.   MOLECULAR CELL

DOT1L Inhibition Sensitizes MLL-Rearranged AML to Chemotherapy

(2014) Wei Liu et al.   PLoS One

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells

(2014) D. Barsyte-Lovejoy et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Histone Methyltransferase Activity of MLL1 Is Dispensable for Hematopoiesis and Leukemogenesis

(2014) Bibhu P. Mishra et al.   Cell Reports

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

Exploiting an Allosteric Binding Site of PRMT3 Yields Potent and Selective Inhibitors

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

The role of different genetic subtypes of CEBPA mutated AML

(2013) A Fasan et al.   LEUKEMIA

The MLL recombinome of acute leukemias in 2013

(2013) C Meyer et al.   LEUKEMIA

Mutational landscape and significance across 12 major cancer types

(2013) Cyriac Kandoth et al.   NATURE

Mutations in Mll2, an H3K4 Methyltransferase, Result in Insulin Resistance and Impaired Glucose Tolerance in Mice

(2013) Michelle Goldsworthy et al.   PLoS One

Synthesis, Optimization, and Evaluation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction

(2013) Yuri Bolshan et al.   ACS Medicinal Chemistry Letters

The COMPASS Family of Histone H3K4 Methylases: Mechanisms of Regulation in Development and Disease Pathogenesis

(2012) Ali Shilatifard   Annual Review of Biochemistry

Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5

(2012) Guillermo Senisterra et al.   BIOCHEMICAL JOURNAL

The many facets of MLL1 regulation

(2012) Pamela Zhang et al.   BIOPOLYMERS

Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia

(2012) A. Shi et al.   BLOOD

Skirting the pitfalls: a clear-cut nomenclature for H3K4 methyltransferases

(2012) N Bögershausen et al.   CLINICAL GENETICS

Structural Basis for WDR5 Interaction (Win) Motif Recognition in Human SET1 Family Histone Methyltransferases

(2012) Venkatasubramanian Dharmarajan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure-Based Design of High-Affinity Macrocyclic Peptidomimetics to Block the Menin-Mixed Lineage Leukemia 1 (MLL1) Protein–Protein Interaction

(2012) Haibin Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

High-Affinity, Small-Molecule Peptidomimetic Inhibitors of MLL1/WDR5 Protein–Protein Interaction

(2012) Hacer Karatas et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The role of HOX genes in normal hematopoiesis and acute leukemia

(2012) R A Alharbi et al.   LEUKEMIA

Medulloblastoma exome sequencing uncovers subtype-specific somatic mutations

(2012) Trevor J. Pugh et al.   NATURE

Dissecting the genomic complexity underlying medulloblastoma

(2012) David T. W. Jones et al.   NATURE

Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia

(2012) Jolanta Grembecka et al.   Nature Chemical Biology

The plasticity of WDR5 peptide-binding cleft enables the binding of the SET1 family of histone methyltransferases

(2012) Pamela Zhang et al.   NUCLEIC ACIDS RESEARCH

Histone methylase MLL1 has critical roles in tumor growth and angiogenesis and its knockdown suppresses tumor growth in vivo

(2012) K I Ansari et al.   ONCOGENE

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

(2012) Wenyu Yu et al.   Nature Communications

MLL fusion proteins preferentially regulate a subset of wild-type MLL target genes in the leukemic genome

(2011) Q.-f. Wang 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

MLL-Rearranged Leukemia Is Dependent on Aberrant H3K79 Methylation by DOT1L

(2011) Kathrin M. Bernt et al.   CANCER CELL

Frequent mutation of histone-modifying genes in non-Hodgkin lymphoma

(2011) Ryan D. Morin et al.   NATURE

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

(2011) Masoud Vedadi et al.   Nature Chemical Biology

Structural and Biochemical Insights into MLL1 Core Complex Assembly

(2011) Vanja Avdic et al.   STRUCTURE

Early mammalian erythropoiesis requires the Dot1L methyltransferase

(2010) Y. Feng et al.   BLOOD

Mechanisms of leukemogenesis by MLL fusion proteins

(2010) Rolf Marschalek   BRITISH JOURNAL OF HAEMATOLOGY

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

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

Nebulette is the second member of the nebulin family fused to the MLL gene in infant leukemia

(2010) Virginia M. Cóser et al.   CANCER GENETICS AND CYTOGENETICS

Accessing Protein Methyltransferase and Demethylase Enzymology Using Microfluidic Capillary Electrophoresis

(2010) Tim J. Wigle et al.   CHEMISTRY & BIOLOGY

Molecular Basis of the Mixed Lineage Leukemia-Menin Interaction

(2010) Jolanta Grembecka et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Characterization of a Novel WDR5-binding Site That Recruits RbBP5 through a Conserved Motif to Enhance Methylation of Histone H3 Lysine 4 by Mixed Lineage Leukemia Protein-1

(2010) Zain Odho et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Novel Non-SET Domain Multi-subunit Methyltransferase Required for Sequential Nucleosomal Histone H3 Methylation by the Mixed Lineage Leukemia Protein-1 (MLL1) Core Complex

(2010) Anamika Patel et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Analysis of the Binding of Mixed Lineage Leukemia 1 (MLL1) and Histone 3 Peptides to WD Repeat Domain 5 (WDR5) for the Design of Inhibitors of the MLL1−WDR5 Interaction

(2010) Hacer Karatas et al.   JOURNAL OF MEDICINAL CHEMISTRY

A chemiluminescence-based method for identification of histone lysine methyltransferase inhibitors

(2010) Amy M. Quinn et al.   Molecular BioSystems

Multiple Interactions Recruit MLL1 and MLL1 Fusion Proteins to the HOXA9 Locus in Leukemogenesis

(2010) Thomas A. Milne et al.   MOLECULAR CELL

An Ash2L/RbBP5 Heterodimer Stimulates the MLL1 Methyltransferase Activity through Coordinated Substrate Interactions with the MLL1 SET Domain

(2010) Fang Cao et al.   PLoS One

The Genetic Landscape of the Childhood Cancer Medulloblastoma

(2010) D. W. Parsons et al.   SCIENCE

The MLL recombinome of adult CD10-negative B-cell precursor acute lymphoblastic leukemia: results from the GMALL study group

(2009) T. Burmeister et al.   BLOOD

On the Mechanism of Multiple Lysine Methylation by the Human Mixed Lineage Leukemia Protein-1 (MLL1) Core Complex

(2009) Anamika Patel 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

New insights to the MLL recombinome of acute leukemias

(2009) C Meyer et al.   LEUKEMIA

Global Analysis of H3K4 Methylation Defines MLL Family Member Targets and Points to a Role for MLL1-Mediated H3K4 Methylation in the Regulation of Transcriptional Initiation by RNA Polymerase II

(2009) P. Wang et al.   MOLECULAR AND CELLULAR BIOLOGY

Chromatin remodelling factor Mll1 is essential for neurogenesis from postnatal neural stem cells

(2009) Daniel A. Lim et al.   NATURE

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

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

Integration of hepatitis B virus DNA into the myeloid/lymphoid or mixed-lineage leukemia (MLL4) gene and rearrangements of MLL4 in human hepatocellular carcinoma

(2008) Kenichi Saigo et al.   HUMAN MUTATION

Structure of WDR5 Bound to Mixed Lineage Leukemia Protein-1 Peptide

(2008) Anamika Patel et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Conserved Arginine-containing Motif Crucial for the Assembly and Enzymatic Activity of the Mixed Lineage Leukemia Protein-1 Core Complex

(2008) Anamika Patel et al.   JOURNAL OF BIOLOGICAL CHEMISTRY