H3K36 methyltransferases as cancer drug targets: rationale and perspectives for inhibitor development

SMYD2 overexpression is associated with tumor cell proliferation and a worse outcome in human papillomavirus–unrelated nonmultiple head and neck carcinomas

(2016) Rie Ohtomo-Oda et al.   HUMAN PATHOLOGY

A PWWP Domain of Histone-LysineN-Methyltransferase NSD2 Binds to Dimethylated Lys-36 of Histone H3 and Regulates NSD2 Function at Chromatin

(2016) Saumya M. Sankaran et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat

(2016) Kevin W. Kuntz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Transition state for the NSD2-catalyzed methylation of histone H3 lysine 36

(2016) Myles B. Poulin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Dynamic behavior of the post-SET loop region of NSD1: Implications for histone binding and drug development

(2016) Sarah E. Graham et al.   PROTEIN SCIENCE

ASH1L Links Histone H3 Lysine 36 Dimethylation to MLL Leukemia

(2016) L. Zhu et al.   Cancer Discovery

SAM/SAH Analogs as Versatile Tools for SAM-Dependent Methyltransferases

(2015) Jing Zhang et al.   ACS Chemical Biology

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

(2015) David S. Rogawski et al.   BIOCHEMISTRY

Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human

(2015) Nigel J. Waters et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

A fluorescent bimolecular complementation screen reveals MAF1, RNF7 and SETD3 as PCNA-associated proteins in human cells

(2015) Simon E Cooper et al.   CELL CYCLE

Expression of histone methyltransferases as novel biomarkers for renal cell tumor diagnosis and prognostication

(2015) Ana Sílvia Pires-Luís et al.   Epigenetics

H3K36 methylation promotes longevity by enhancing transcriptional fidelity

(2015) Payel Sen et al.   GENES & DEVELOPMENT

A Proteomic Strategy Identifies Lysine Methylation of Splicing Factor snRNP70 by the SETMAR Enzyme

(2015) Scott M. Carlson et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Histone Methyltransferase Smyd2 Is a Negative Regulator of Macrophage Activation by Suppressing Interleukin 6 (IL-6) and Tumor Necrosis Factor α (TNF-α) Production

(2015) Guiliang Xu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2

(2015) Hannah Nguyen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

miR-142–3p Down-Regulation Contributes to Thyroid Follicular Tumorigenesis by Targeting ASH1L and MLL1

(2015) Marianna Colamaio et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Ash1l controls quiescence and self-renewal potential in hematopoietic stem cells

(2015) Morgan Jones et al.   JOURNAL OF CLINICAL INVESTIGATION

NSD3-Short Is an Adaptor Protein that Couples BRD4 to the CHD8 Chromatin Remodeler

(2015) Chen Shen et al.   MOLECULAR CELL

Comprehensive genomic characterization of head and neck squamous cell carcinomas

(2015)   NATURE

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

SETD2 loss-of-function promotes renal cancer branched evolution through replication stress and impaired DNA repair

(2015) N Kanu et al.   ONCOGENE

The SET Domain Is Essential for Metnase Functions in Replication Restart and the 5’ End of SS-Overhang Cleavage

(2015) Hyun-Suk Kim et al.   PLoS One

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

NF-κB-dependent and -independent epigenetic modulation using the novel anti-cancer agent DMAPT

(2015) H Nakshatri et al.   Cell Death & Disease

Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2

(2015) Ramzi F. Sweis et al.   ACS Medicinal Chemistry Letters

Recurrent chromosomal gains and heterogeneous driver mutations characterise papillary renal cancer evolution

(2015) Michal Kovac et al.   Nature Communications

miR-106b-5p targets tumor suppressor gene SETD2 to inactive its function in clear cell renal cell carcinoma

(2015) Wei Xiang et al.   Oncotarget

Pervasive transcription read-through promotes aberrant expression of oncogenes and RNA chimeras in renal carcinoma

(2015) Ana R Grosso et al.   eLife

Reprogramming of Polycomb-Mediated Gene Silencing in Embryonic Stem Cells by the miR-290 Family and the Methyltransferase Ash1l

(2015) Chryssa Kanellopoulou et al.   Stem Cell Reports

Distribution and Maintenance of Histone H3 Lysine 36 Trimethylation in Transcribed Locus

(2015) Henel Sein et al.   PLoS One

Genetic alterations of histone lysine methyltransferases and their significance in breast cancer

(2015) Lanxin Liu et al.   Oncotarget

RB1 Methylation by SMYD2 Enhances Cell Cycle Progression through an Increase of RB1 Phosphorylation

(2015) Hyun-Soo Cho et al.   NEOPLASIA

NUP98/NSD1 and FLT3/ITD coexpression is more prevalent in younger AML patients and leads to induction failure: a COG and SWOG report

(2014) F. Ostronoff et al.   BLOOD

Overexpression of SMYD2 contributes to malignant outcome in gastric cancer

(2014) S Komatsu et al.   BRITISH JOURNAL OF CANCER

AF10 Regulates Progressive H3K79 Methylation and HOX Gene Expression in Diverse AML Subtypes

(2014) Aniruddha J. Deshpande et al.   CANCER CELL

Mutations inSETD2cause a novel overgrowth condition

(2014) Armelle Luscan et al.   JOURNAL OF MEDICAL GENETICS

Structural Insights into Estrogen Receptor α Methylation by Histone Methyltransferase SMYD2, a Cellular Event Implicated in Estrogen Signaling Regulation

(2014) Yuanyuan Jiang et al.   JOURNAL OF MOLECULAR BIOLOGY

SMYD2 is highly expressed in pediatric acute lymphoblastic leukemia and constitutes a bad prognostic factor

(2014) Luis Henrique Toshihiro Sakamoto et al.   LEUKEMIA RESEARCH

Neural crest specification and migration independently require NSD3-related lysine methyltransferase activity

(2014) Bridget T. Jacques-Fricke et al.   MOLECULAR BIOLOGY OF THE CELL

BS69/ZMYND11 Reads and Connects Histone H3.3 Lysine 36 Trimethylation-Decorated Chromatin to Regulated Pre-mRNA Processing

(2014) Rui Guo et al.   MOLECULAR CELL

ZMYND11 links histone H3.3K36me3 to transcription elongation and tumour suppression

(2014) Hong Wen et al.   NATURE

Identification of functional cooperative mutations of SETD2 in human acute leukemia

(2014) Xiaofan Zhu et al.   NATURE GENETICS

Identification of Druggable Cancer Driver Genes Amplified across TCGA Datasets

(2014) Ying Chen et al.   PLoS One

Potential Role for the Metnase Transposase Fusion Gene in Colon Cancer through the Regulation of Key Genes

(2014) Panagiotis Apostolou et al.   PLoS One

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

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

EZH2 as a potential target in cancer therapy

(2014) Michael T McCabe et al.   Epigenomics

Mutations in epigenetic regulators including SETD2 are gained during relapse in paediatric acute lymphoblastic leukaemia

(2014) Brenton G. Mar et al.   Nature Communications

A histone H3K36 chromatin switch coordinates DNA double-strand break repair pathway choice

(2014) Chen-Chun Pai et al.   Nature Communications

An RNA polymerase II-coupled function for histone H3K36 methylation in checkpoint activation and DSB repair

(2014) Deepak Kumar Jha et al.   Nature Communications

NSD3-NUT Fusion Oncoprotein in NUT Midline Carcinoma: Implications for a Novel Oncogenic Mechanism

(2014) C. A. French et al.   Cancer Discovery

SETD2-Dependent Histone H3K36 Trimethylation Is Required for Homologous Recombination Repair and Genome Stability

(2014) Sophia X. Pfister et al.   Cell Reports

Histone Methyltransferase MMSET/NSD2 Alters EZH2 Binding and Reprograms the Myeloma Epigenome through Global and Focal Changes in H3K36 and H3K27 Methylation

(2014) Relja Popovic et al.   PLoS Genetics

The Histone Methyltransferase SMYD2 Methylates PARP1 and Promotes Poly(ADP-ribosyl)ation Activity in Cancer Cells

(2014) Lianhua Piao et al.   NEOPLASIA

NSD2 Is Recruited through Its PHD Domain to Oncogenic Gene Loci to Drive Multiple Myeloma

(2013) Z. Huang et al.   CANCER RESEARCH

The Histone Mark H3K36me3 Regulates Human DNA Mismatch Repair through Its Interaction with MutSα

(2013) Feng Li et al.   CELL

Adverse Outcomes in Clear Cell Renal Cell Carcinoma with Mutations of 3p21 Epigenetic Regulators BAP1 and SETD2: A Report by MSKCC and the KIRC TCGA Research Network

(2013) A. A. Hakimi et al.   CLINICAL CANCER RESEARCH

The trithorax group proteins Kismet and ASH1 promote H3K36 dimethylation to counteract Polycomb group repression in Drosophila

(2013) K. M. Dorighi et al.   DEVELOPMENT

Variation in chromatin accessibility in human kidney cancer links H3K36 methyltransferase loss with widespread RNA processing defects

(2013) J. M. Simon et al.   GENOME RESEARCH

Histone H2A Ubiquitination Inhibits the Enzymatic Activity of H3 Lysine 36 Methyltransferases

(2013) Gang Yuan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Point mutation E1099K in MMSET/NSD2 enhances its methyltranferase activity and leads to altered global chromatin methylation in lymphoid malignancies

(2013) J A Oyer et al.   LEUKEMIA

Mutational landscape and significance across 12 major cancer types

(2013) Cyriac Kandoth et al.   NATURE

Global chromatin profiling reveals NSD2 mutations in pediatric acute lymphoblastic leukemia

(2013) Jacob D Jaffe et al.   NATURE GENETICS

Structural basis for high-affinity binding of LEDGF PWWP to mononucleosomes

(2013) Jocelyn O. Eidahl et al.   NUCLEIC ACIDS RESEARCH

Histone methyltransferase SETD2 coordinates FACT recruitment with nucleosome dynamics during transcription

(2013) Sílvia Carvalho et al.   NUCLEIC ACIDS RESEARCH

Hallmarks of alternative splicing in cancer

(2013) S Oltean et al.   ONCOGENE

Regulation of estrogen receptor   by histone methyltransferase SMYD2-mediated protein methylation

(2013) X. Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Histone H4 deacetylation facilitates 53BP1 DNA damage signaling and double-strand break repair

(2013) K.-Y. Hsiao et al.   Journal of Molecular Cell Biology

MMSET is the key molecular target in t(4;14) myeloma

(2013) F Mirabella et al.   Blood Cancer Journal

Ash1l Methylates Lys36 of Histone H3 Independently of Transcriptional Elongation to Counteract Polycomb Silencing

(2013) Hitomi Miyazaki et al.   PLoS Genetics

Transition States, Analogues, and Drug Development

(2012) Vern L. Schramm   ACS Chemical Biology

Cancer Epigenetics: From Mechanism to Therapy

(2012) Mark A. Dawson et al.   CELL

A Long ncRNA Links Copy Number Variation to a Polycomb/Trithorax Epigenetic Switch in FSHD Muscular Dystrophy

(2012) Daphne S. Cabianca et al.   CELL

The histone methyltransferase Wolf-Hirschhorn syndrome candidate 1-like 1 (WHSC1L1) is involved in human carcinogenesis

(2012) Daechun Kang et al.   GENES CHROMOSOMES & CANCER

Histone methyltransferase ASH1 orchestrates fibrogenic gene transcription during myofibroblast transdifferentiation

(2012) Maria Jesus Perugorria et al.   HEPATOLOGY

Sinefungin Derivatives as Inhibitors and Structure Probes of Protein Lysine Methyltransferase SETD2

(2012) Weihong Zheng et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

MMSET stimulates myeloma cell growth through microRNA-mediated modulation of c-MYC

(2012) D-J Min et al.   LEUKEMIA

Histone Methyltransferase NSD2/MMSET Mediates Constitutive NF- B Signaling for Cancer Cell Proliferation, Survival, and Tumor Growth via a Feed-Forward Loop

(2012) P. Yang et al.   MOLECULAR AND CELLULAR BIOLOGY

Characterization of the EZH2-MMSET Histone Methyltransferase Regulatory Axis in Cancer

(2012) Irfan A. Asangani et al.   MOLECULAR CELL

An H3K36 Methylation-Engaging Tudor Motif of Polycomb-like Proteins Mediates PRC2 Complex Targeting

(2012) Ling Cai et al.   MOLECULAR CELL

Set2 methylation of histone H3 lysine 36 suppresses histone exchange on transcribed genes

(2012) Swaminathan Venkatesh et al.   NATURE

Chromatin remodelers Isw1 and Chd1 maintain chromatin structure during transcription by preventing histone exchange

(2012) Michaela Smolle et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Intratumor Heterogeneity and Branched Evolution Revealed by Multiregion Sequencing

(2012) Marco Gerlinger et al.   NEW ENGLAND JOURNAL OF MEDICINE

The histone methyltransferase MMSET/WHSC1 activates TWIST1 to promote an epithelial–mesenchymal transition and invasive properties of prostate cancer

(2012) T Ezponda et al.   ONCOGENE

Impact of Histone H4 Lysine 20 Methylation on 53BP1 Responses to Chromosomal Double Strand Breaks

(2012) Andrea J. Hartlerode et al.   PLoS One

Psip1/Ledgf p52 Binds Methylated Histone H3K36 and Splicing Factors and Contributes to the Regulation of Alternative Splicing

(2012) Madapura M. Pradeepa et al.   PLoS Genetics

NUP98/NSD1 characterizes a novel poor prognostic group in acute myeloid leukemia with a distinct HOX gene expression pattern

(2011) I. H. I. M. Hollink 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

MMSET Is Highly Expressed and Associated with Aggressiveness in Neuroblastoma

(2011) H. R. Hudlebusch et al.   CANCER RESEARCH

The Histone Methyltransferase and Putative Oncoprotein MMSET Is Overexpressed in a Large Variety of Human Tumors

(2011) H. R. Hudlebusch et al.   CLINICAL CANCER RESEARCH

KDM5B regulates embryonic stem cell self-renewal and represses cryptic intragenic transcription

(2011) Liangqi Xie et al.   EMBO JOURNAL

The Structure of NSD1 Reveals an Autoregulatory Mechanism Underlying Histone H3K36 Methylation

(2011) Qi Qiao et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Direct Evidence for Methyl Group Coordination by Carbon-Oxygen Hydrogen Bonds in the Lysine Methyltransferase SET7/9

(2011) Scott Horowitz et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Crystal Structure of the Human Histone Methyltransferase ASH1L Catalytic Domain and Its Implications for the Regulatory Mechanism

(2011) Sojin An et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Histone Methyltransferase SETD3 Regulates Muscle Differentiation

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

H3K36 Methylation Antagonizes PRC2-mediated H3K27 Methylation

(2011) Wen Yuan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure of Human SMYD2 Protein Reveals the Basis of p53 Tumor Suppressor Methylation

(2011) Li Wang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural Chemistry of the Histone Methyltransferases Cofactor Binding Site

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

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

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

NSD2 Links Dimethylation of Histone H3 at Lysine 36 to Oncogenic Programming

(2011) Alex J. Kuo et al.   MOLECULAR CELL

MMSET regulates histone H4K20 methylation and 53BP1 accumulation at DNA damage sites

(2011) Huadong Pei et al.   NATURE

Exome sequencing identifies somatic mutations of DNA methyltransferase gene DNMT3A in acute monocytic leukemia

(2011) Xiao-Jing Yan et al.   NATURE GENETICS

Splicing enhances recruitment of methyltransferase HYPB/Setd2 and methylation of histone H3 Lys36

(2011) Sérgio Fernandes de Almeida et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Crystal Structures of Histone and p53 Methyltransferase SmyD2 Reveal a Conformational Flexibility of the Autoinhibitory C-Terminal Domain

(2011) Yuanyuan Jiang et al.   PLoS One

Dual Function of Histone H3 Lysine 36 Methyltransferase ASH1 in Regulation of Hox Gene Expression

(2011) Yujiro Tanaka et al.   PLoS One

Wolf–Hirschhorn syndrome candidate 1 is involved in the cellular response to DNA damage

(2011) Ildiko Hajdu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Pre-mRNA splicing is a determinant of histone H3K36 methylation

(2011) S. Kim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Basis of Substrate Methylation and Inhibition of SMYD2

(2011) Andrew D. Ferguson et al.   STRUCTURE

Proteomic analyses of the SMYD family interactomes identify HSP90 as a novel target for SMYD2

(2011) Mohamed Abu-Farha et al.   Journal of Molecular Cell Biology

Structure of human lysine methyltransferase Smyd2 reveals insights into the substrate divergence in Smyd proteins

(2011) Shutong Xu et al.   Journal of Molecular Cell Biology

Transforming Properties of 8p11-12 Amplified Genes in Human Breast Cancer

(2010) Z.-Q. Yang et al.   CANCER RESEARCH

Pro Isomerization in MLL1 PHD3-Bromo Cassette Connects H3K4me Readout to CyP33 and HDAC-Mediated Repression

(2010) Zhanxin Wang et al.   CELL

Methylation of the Retinoblastoma Tumor Suppressor by SMYD2

(2010) Louis A. Saddic et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Human LSD2/KDM1b/AOF1 Regulates Gene Transcription by Modulating Intragenic H3K4me2 Methylation

(2010) Rui Fang et al.   MOLECULAR CELL

Systematic sequencing of renal carcinoma reveals inactivation of histone modifying genes

(2010) Gillian L. Dalgliesh et al.   NATURE

Discovery and characterization of chromatin states for systematic annotation of the human genome

(2010) Jason Ernst et al.   NATURE BIOTECHNOLOGY

Methylation of histone H3 lysine 36 enhances DNA repair by nonhomologous end-joining

(2010) S. Fnu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Regulation of Alternative Splicing by Histone Modifications

(2010) R. F. Luco et al.   SCIENCE

The mRNA expression of SETD2 in human breast cancer: correlation with clinico-pathological parameters

(2009) W Al Sarakbi et al.   BMC CANCER

NUP98–NSD3 fusion gene in radiation-associated myelodysplastic syndrome with t(8;11)(p11;p15) and expression pattern of NSD family genes

(2009) Takeshi Taketani et al.   CANCER GENETICS AND CYTOGENETICS

Overexpression of SMYD2 relates to tumor cell proliferation and malignant outcome of esophageal squamous cell carcinoma

(2009) Shuhei Komatsu et al.   CARCINOGENESIS

The histone methyltransferase, NSD2, enhances androgen receptor-mediated transcription

(2009) Hee-Bum Kang et al.   FEBS LETTERS

The Target of the NSD Family of Histone Lysine Methyltransferases Depends on the Nature of the Substrate

(2009) Yan Li et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

NF-κB and cancer: how intimate is this relationship

(2009) Sahdeo Prasad et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

Chromatin organization marks exon-intron structure

(2009) Schraga Schwartz et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Epigenetic inactivation of the Sotos overgrowth syndrome gene histone methyltransferase NSD1 in human neuroblastoma and glioma

(2009) M. Berdasco et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Regulation of NF- B by NSD1/FBXL11-dependent reversible lysine methylation of p65

(2009) T. Lu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

HOXA9 is required for survival in human MLL-rearranged acute leukemias

(2008) J. Faber et al.   BLOOD

HOX expression patterns identify a common signature for favorable AML

(2008) M Andreeff et al.   LEUKEMIA

The SET and transposase domain protein Metnase enhances chromosome decatenation: regulation by automethylation

(2008) E. A. Williamson et al.   NUCLEIC ACIDS RESEARCH