相关参考文献
注意：仅列出部分参考文献，下载原文获取全部文献信息。Small-Molecule Inhibitors of SETD8 with Cellular Activity
Gil Blum et al.
ACS CHEMICAL BIOLOGY (2014)
Development and classes of epigenetic drugs for cancer
Dashyant Dhanak et al.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2014)
Design of small molecule epigenetic modulators
Boobalan Pachaiyappan et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2014)
Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor
Aravind Basavapathruni et al.
BIOPHARMACEUTICS & DRUG DISPOSITION (2014)
The promise and failures of epigenetic therapies for cancer treatment
Pasano Bojang et al.
CANCER TREATMENT REVIEWS (2014)
Mind the Methyl: Methyllysine Binding Proteins in Epigenetic Regulation
Tobias Wagner et al.
CHEMMEDCHEM (2014)
A Chemical Tool for In Vitro and In Vivo Precipitation of Lysine Methyltransferase G9a
Kyle D. Konze et al.
CHEMMEDCHEM (2014)
SET8 methyltransferase activity during the DNA double-strand break response is required for recruitment of 53BP1
Stanimir Dulev et al.
EMBO REPORTS (2014)
Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8
Anqi Ma et al.
JOURNAL OF MEDICINAL CHEMISTRY (2014)
Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant Non-Hodgkin Lymphoma
Sarah K. Knutson et al.
MOLECULAR CANCER THERAPEUTICS (2014)
Structure-activity relationship studies of SETD8 inhibitors
Anqi Ma et al.
MEDCHEMCOMM (2014)
Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors
Nitipol Srimongkolpithak et al.
MEDCHEMCOMM (2014)
Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a
Ramzi F. Sweis et al.
ACS MEDICINAL CHEMISTRY LETTERS (2014)
Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2
Christopher G. Nasveschuk et al.
ACS MEDICINAL CHEMISTRY LETTERS (2014)
An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1
Kyle D. Konze et al.
ACS CHEMICAL BIOLOGY (2013)
Bromo-deaza-SAH: A potent and selective DOT1L inhibitor
Wenyu Yu et al.
BIOORGANIC & MEDICINAL CHEMISTRY (2013)
Epidithiodiketopiperazine as a pharmacophore for protein lysine methyltransferase G9a inhibitors: Reducing cytotoxicity by structural simplification
Shinya Fujishiro et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2013)
Potent inhibition of DOT1L as treatment of MLL-fusion leukemia
Scott R. Daigle et al.
BLOOD (2013)
Identification of EZH2 and EZH1 Small Molecule Inhibitors with Selective Impact on Diffuse Large B Cell Lymphoma Cell Growth
Shivani Garapaty-Rao et al.
CHEMISTRY & BIOLOGY (2013)
Small-Molecule Modulators for Epigenetics Targets
Stefan Knapp et al.
CHEMMEDCHEM (2013)
Histone Lysine-Specific Methyltransferases and Demethylases in Carcinogenesis: New Targets for Cancer Therapy and Prevention
Xuejiao Tian et al.
CURRENT CANCER DRUG TARGETS (2013)
On the Histone Lysine Methyltransferase Activity of Fungal Metabolite Chaetocin
Fanny L. Cherblanc et al.
JOURNAL OF MEDICINAL CHEMISTRY (2013)
Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP
Feng Liu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2013)
Small-molecular modulators of cancer-associated epigenetic mechanisms
Yukihiro Itoh et al.
MOLECULAR BIOSYSTEMS (2013)
Chromatin proteins and modifications as drug targets
Kristian Helin et al.
NATURE (2013)
Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases
Fanny L. Cherblanc et al.
NATURE CHEMICAL BIOLOGY (2013)
Nahuoic Acid A Produced by a Streptomyces sp Isolated From a Marine Sediment Is a Selective SAM-Competitive Inhibitor of the Histone Methyltransferase SETD8
David E. Williams et al.
ORGANIC LETTERS (2013)
Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2
Sarah K. Knutson et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2013)
Smallmolecule epigenetic inhibitors targeted tohistone lysinemethyltransferases and demethylases
Zhanxin Wang et al.
QUARTERLY REVIEWS OF BIOPHYSICS (2013)
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors (vol 3, 1288, 2012)
Wenyu Yu et al.
NATURE COMMUNICATIONS (2013)
A Small-Molecule Probe of the Histone Methyltransferase G9a Induces Cellular Senescence in Pancreatic Adenocarcinoma
Yuan Yuan et al.
ACS CHEMICAL BIOLOGY (2012)
Targeting protein lysine methylation and demethylation in cancers
Yunlong He et al.
ACTA BIOCHIMICA ET BIOPHYSICA SINICA (2012)
Histone Lysine Methyltransferase SETD8 Promotes Carcinogenesis by Deregulating PCNA Expression
Masashi Takawa et al.
CANCER RESEARCH (2012)
Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L
Aravind Basavapathruni et al.
CHEMICAL BIOLOGY & DRUG DESIGN (2012)
SET8 promotes epithelial-mesenchymal transition and confers TWIST dual transcriptional activities
Fen Yang et al.
EMBO JOURNAL (2012)
PR-Set7 and H4K20me1: at the crossroads of genome integrity, cell cycle, chromosome condensation, and transcription
David B. Beck et al.
GENES & DEVELOPMENT (2012)
Selective Inhibitors of Histone Methyltransferase DOT1L: Design, Synthesis, and Crystallographic Studies
Yuan Yao et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2012)
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations
Michael T. McCabe et al.
NATURE (2012)
A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells
Sarah K. Knutson et al.
NATURE CHEMICAL BIOLOGY (2012)
Epigenetic protein families: a new frontier for drug discovery
Cheryl H. Arrowsmith et al.
NATURE REVIEWS DRUG DISCOVERY (2012)
Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation
Wei Qi et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2012)
Synthesis and biological activities of chaetocin and its derivatives
Mikiko Sodeoka et al.
PURE AND APPLIED CHEMISTRY (2012)
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2
Sharad K. Verma et al.
ACS MEDICINAL CHEMISTRY LETTERS (2012)
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors
Wenyu Yu et al.
NATURE COMMUNICATIONS (2012)
Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor
Scott R. Daigle et al.
CANCER CELL (2011)
H3K9 methyltransferase G9a and the related molecule GLP
Yoichi Shinkai et al.
GENES & DEVELOPMENT (2011)
The diverse functions of Dot1 and H3K79 methylation
Anh Tram Nguyen et al.
GENES & DEVELOPMENT (2011)
Epipolythiodiketopiperazine Alkaloids: Total Syntheses and Biological Activities
Eriko Iwasa et al.
ISRAEL JOURNAL OF CHEMISTRY (2011)
Optimization of Cellular Activity of G9a Inhibitors 7-Aminoalkoxy-quinazolines
Feng Liu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2011)
Selective Inhibitors of Histone Methyltransferase DOT1L: Design, Synthesis, and Crystallographic Studies
Yuan Yao et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2011)
The Polycomb complex PRC2 and its mark in life
Raphael Margueron et al.
NATURE (2011)
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells
Masoud Vedadi et al.
NATURE CHEMICAL BIOLOGY (2011)
Histone H4 Lys 20 monomethylation by histone methylase SET8 mediates Wnt target gene activation
Zhenfei Li et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2011)
Total syntheses of chaetocin and ent-chaetocin
Eriko Iwasa et al.
TETRAHEDRON (2011)
H3K9 Histone Methyltransferase G9a Promotes Lung Cancer Invasion and Metastasis by Silencing the Cell Adhesion Molecule Ep-CAM
Min-Wei Chen et al.
CANCER RESEARCH (2010)
Dynamic regulation of the PR-Set7 histone methyltransferase is required for normal cell cycle progression
Shumin Wu et al.
GENES & DEVELOPMENT (2010)
PR-Set7-Mediated Monomethylation of Histone H4 Lysine 20 at Specific Genomic Regions Induces Transcriptional Repression
Lauren M. Congdon et al.
JOURNAL OF CELLULAR BIOCHEMISTRY (2010)
Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines.
Feng Liu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2010)
Adding a Lysine Mimic in the Design of Potent Inhibitors of Histone Lysine Methyltransferases
Yanqi Chang et al.
JOURNAL OF MOLECULAR BIOLOGY (2010)
General Approach to Epipolythiodiketopiperazine Alkaloids: Total Synthesis of (+)-Chaetocins A and C and (+)-12,12′-Dideoxychetracin A
Justin Kim et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2010)
Total Synthesis of (+)-Chaetocin and its Analogues: Their Histone Methyltransferase G9a Inhibitory Activity
Eriko Iwasa et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2010)
CRL4Cdt2-Mediated Destruction of the Histone Methyltransferase Set8 Prevents Premature Chromatin Compaction in S Phase
Richard C. Centore et al.
MOLECULAR CELL (2010)
CRL4Cdt2 Regulates Cell Proliferation and Histone Gene Expression by Targeting PR-Set7/Set8 for Degradation
Tarek Abbas et al.
MOLECULAR CELL (2010)
Covalent histone modifications - miswritten, misinterpreted and mis-erased in human cancers
Ping Chi et al.
NATURE REVIEWS CANCER (2010)
The Emerging Therapeutic Potential of Histone Methyltransferase and Demethylase Inhibitors
Astrid Spannhoff et al.
CHEMMEDCHEM (2009)
New Insights into the Design of Inhibitors of Human S-Adenosylmethionine Decarboxylase: Studies of Adenine C8 Substitution in Structural Analogues of S-Adenosylmethionine
Diane E. McCloskey et al.
JOURNAL OF MEDICINAL CHEMISTRY (2009)
Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a
Feng Liu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2009)
Monomethylation of Histone H4-Lysine 20 Is Involved in Chromosome Structure and Stability and Is Essential for Mouse Development
Hisanobu Oda et al.
MOLECULAR AND CELLULAR BIOLOGY (2009)
Protein methyltransferases as a target class for drug discovery
Robert A. Copeland et al.
NATURE REVIEWS DRUG DISCOVERY (2009)
Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294
Yanqi Chang et al.
NATURE STRUCTURAL & MOLECULAR BIOLOGY (2009)
Total Synthesis of (+)-11,11′-Dideoxyverticillin A
Justin Kim et al.
SCIENCE (2009)
Concise Total Synthesis of (+)-WIN 64821 and (-)-ditryptophenaline
Mohammad Movassaghi et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2008)
Catalytic function of the PR-Set7 histone H4 lysine 20 monomethyltransferase is essential for mitotic entry and genomic stability
Sabrina I. Houston et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2008)
Discovery of Quinazolines as Histamine H4 Receptor Inverse Agonists Using a Scaffold Hopping Approach
Rogier A. Smits et al.
JOURNAL OF MEDICINAL CHEMISTRY (2008)
Nonprocessive methylation by Dot1 leads to functional redundancy of histone H3K79 methylation states
Floor Frederiks et al.
NATURE STRUCTURAL & MOLECULAR BIOLOGY (2008)
The histone methyltransferase SET8 is required for S-phase progression
Stine Jorgensen et al.
JOURNAL OF CELL BIOLOGY (2007)
7-Functionalized 7-deazapurine β-D and β-L-ribonucleosides related to tubercidin and 7-deazainosine:: glycosylation of pyrrolo[2,3-d] pyrimidines with 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D or β-L-ribofuranose
Frank Seela et al.
TETRAHEDRON (2007)
Modulation of p53 function by SET8-mediated methylation at lysine 382
Xiaobing Shi et al.
MOLECULAR CELL (2007)
Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase
Stefan Kubicek et al.
MOLECULAR CELL (2007)
Concise total synthesis of (-)-calycanthine, (+)-chimonanthine, and (+)-folicanthine
Mohammad Movassaghi et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2007)
Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9
D Greiner et al.
NATURE CHEMICAL BIOLOGY (2005)
hDOT1L links histone methylation to leukemogenesis
Y Okada et al.
CELL (2005)
Histone methyltransferases G9a and GLP form heteromeric complexes and are both crucial for methylation of euchromatin at H3-K9
M Tachibana et al.
GENES & DEVELOPMENT (2005)
EZH2 is a marker of aggressive breast cancer and promotes neoplastic transformation of breast epithelial cells
CG Kleer et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2003)
An efficient synthesis of N-methyl amino acids by way of intermediate 5-oxazolidinones
L Aurelio et al.
JOURNAL OF ORGANIC CHEMISTRY (2003)
Structure of the catalytic domain of human DOT1L, a Non-SET domain nucleosomal histone methyltransferase
JR Min et al.
CELL (2003)
Histone methyltransferase activity associated with a human multiprotein complex containing the Enhancer of Zeste protein
A Kuzmichev et al.
GENES & DEVELOPMENT (2002)
A modified synthesis of iodoazidoaryl prazosin
MB Andrus et al.
JOURNAL OF ORGANIC CHEMISTRY (2002)
Role of histone H3 lysine 27 methylation in polycomb-group silencing
R Cao et al.
SCIENCE (2002)
MLL targets SET domain methyltransferase activity to Hox gene promoters
TA Milne et al.
MOLECULAR CELL (2002)
Drosophila enhancer of Zeste/ESC complexes have a histone H3 methyltransferase activity that marks chromosomal polycomb sites
B Czermin et al.
CELL (2002)
Histone methyltransferase activity of a Drosophila polycomb group repressor complex
J Müller et al.
CELL (2002)
The polycomb group protein EZH2 is involved in progression of prostate cancer
S Varambally et al.
NATURE (2002)
Disruptor of telomeric silencing-1 is a chromatin-specific histone H3 methyltransferase
N Lacoste et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2002)
G9a histone methyltransferase plays a dominant role in euchromatic histone H3 lysine 9 methylation and is essential for early embryogenesis
M Tachibana et al.
GENES & DEVELOPMENT (2002)
Purification and functional characterization of SET8, a nucleosomal histone H4-lysine 20-specific methyltransferase
J Fang et al.
CURRENT BIOLOGY (2002)
Methylation of H3-lysine 79 is mediated by a new family of HMTases without a SET domain
Q Feng et al.
CURRENT BIOLOGY (2002)
Lysine methylation within the globular domain of histone H3 by Dot1 is important for telomeric silencing and Sir protein association
HH Ng et al.
GENES & DEVELOPMENT (2002)
Dot1p modulates silencing in yeast by methylation of the nucleosome core
F van Leeuwen et al.
CELL (2002)
PR-Set7 is a nucleosome-specific methyltransferase that modifies lysine 20 of histone H4 and is associated with silent chromatin
K Nishioka et al.
MOLECULAR CELL (2002)
Set2 is a nucleosomal histone H3-selective methyltransferase that mediates transcriptional repression
BD Strahl et al.
MOLECULAR AND CELLULAR BIOLOGY (2002)
Purification and functional characterization of a histone H3-lysine 4-specific methyltransferase
HB Wang et al.
MOLECULAR CELL (2001)
Molecular mechanisms of leukemogenesis mediated by MLL fusion proteins
PM Ayton et al.
ONCOGENE (2001)
An efficient synthesis of pyrrolo[2,1-c][1,4]benzodiazepine.: Synthesis of the antibiotic DC-81
WP Hu et al.
JOURNAL OF ORGANIC CHEMISTRY (2001)
Regulation of chromatin structure by site-specific histone H3 methyltransferases
S Rea et al.
NATURE (2000)
分享论文
