Related references
Note: Only part of the references are listed.Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216
Mingxing Teng et al.
JOURNAL OF MEDICINAL CHEMISTRY (2022)
Targeting SWI/SNF ATPases in enhancer-addicted prostate cancer
Lanbo Xiao et al.
NATURE (2022)
Phenyl-Glutarimides: Alternative Cereblon Binders for the Design of PROTACs
Jaeki Min et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)
UM171 Preserves Epigenetic Marks that Are Reduced in Ex Vivo Culture of Human HSCs via Potentiation of the CLR3-KBTBD4 Complex
Jalila Chagraoui et al.
CELL STEM CELL (2021)
Design, Synthesis, and Biological Evaluation of Lysine Demethylase 5 C Degraders
Tetsuya Iida et al.
CHEMMEDCHEM (2021)
Targeting LSD1 for acute myeloid leukemia (AML) treatment
Shujing Zhang et al.
PHARMACOLOGICAL RESEARCH (2021)
Pharmacokinetics and Safety of PTC596, a Novel Tubulin-Binding Agent, in Subjects With Advanced Solid Tumors
Geoffrey I. Shapiro et al.
CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT (2021)
Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase
Sharan K. Bagal et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression
Rohan Kalyan Rej et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Discovery of a Highly Potent and Selective Degrader Targeting Hematopoietic Prostaglandin D Synthase via In Silico Design
Hidetomo Yokoo et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2
Zhihao Liu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Epigenetic regulator BMI1 promotes alveolar rhabdomyosarcoma proliferation and constitutes a novel therapeutic target
Cara E. Shields et al.
MOLECULAR ONCOLOGY (2021)
The roles of Polycomb repressive complexes in mammalian development and cancer
Andrea Piunti et al.
NATURE REVIEWS MOLECULAR CELL BIOLOGY (2021)
Polycomb Paralog Chromodomain Inhibitors Active against Both CBX6 and CBX8**
Natalia Milosevich et al.
CHEMMEDCHEM (2021)
Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma
Yalin Tu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction
Daohai Du et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Polycomb Repressive Complex 2 Modulation through the Development of EZH2-EED Interaction Inhibitors and EED Binders
Stefano Tomassi et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Preclinical and Early Clinical Development of PTC596, a Novel Small-Molecule Tubulin-Binding Agent
Finith Jernigan et al.
MOLECULAR CANCER THERAPEUTICS (2021)
Small-molecule inhibitors targeting Polycomb repressive complex 1 RING domain
Shirish Shukla et al.
NATURE CHEMICAL BIOLOGY (2021)
The molecular principles of gene regulation by Polycomb repressive complexes
Neil P. Blackledge et al.
NATURE REVIEWS MOLECULAR CELL BIOLOGY (2021)
Chemo-proteomics exploration of HDAC degradability by small molecule degraders
Yuan Xiong et al.
CELL CHEMICAL BIOLOGY (2021)
Recent developments in epigenetic cancer therapeutics: clinical advancement and emerging trends
Kunal Nepali et al.
JOURNAL OF BIOMEDICAL SCIENCE (2021)
LSD1-mediated repression of GFI1 super-enhancer plays an essential role in erythroleukemia
Goichi Tatsumi et al.
LEUKEMIA (2020)
Optimization of Ligands Using Focused DNA-Encoded Libraries To Develop a Selective, Cell-Permeable CBX8 Chromodomain Inhibitor
Sijie Wang et al.
ACS CHEMICAL BIOLOGY (2020)
Binding Modes of Small-Molecule Inhibitors to the EED Pocket of PRC2
Dading Huang et al.
CHEMPHYSCHEM (2020)
Histone deacetylase (HDAC) inhibitors in cancer: a patent review (2017-present)
Chunlong Zhao et al.
EXPERT OPINION ON THERAPEUTIC PATENTS (2020)
Mechanism of Crosstalk between the LSD1 Demethylase and HDAC1 Deacetylase in the CoREST Complex
Yun Song et al.
CELL REPORTS (2020)
The anti-mitotic agents PTC-028 and PTC596 display potent activity in pre-clinical models of multiple myeloma but challenge the role of BMI-1 as an essential tumour gene
Arnold Bolomsky et al.
BRITISH JOURNAL OF HAEMATOLOGY (2020)
Hydroxamic Acids Immobilized on Resins (HAIRs): Synthesis of Dual-Targeting HDAC Inhibitors and HDAC Degraders (PROTACs)
Laura Sinatra et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2020)
EEDi-5285: An Exceptionally Potent, Efficacious, and Orally Active Small-Molecule Inhibitor of Embryonic Ectoderm Development
Rohan Kalyan Rej et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer
M. Cynthia Martin et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex
Jessie Hao-Ru Hsu et al.
CELL CHEMICAL BIOLOGY (2020)
Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader
Frances Potjewyd et al.
CELL CHEMICAL BIOLOGY (2020)
EZH2 is overexpressed in transitional preplasmablasts and is involved in human plasma cell differentiation
Laurie Herviou et al.
LEUKEMIA (2019)
CRISPR-suppressor scanning reveals a nonenzymatic role of LSD1 in AML
Michael E. Vinyard et al.
NATURE CHEMICAL BIOLOGY (2019)
The Polycomb Repressor Complex 1 Drives Double-Negative Prostate Cancer Metastasis by Coordinating Stemness and Immune Suppression
Wenjing Su et al.
CANCER CELL (2019)
Canonical PRC1 controls sequence-independent propagation of Polycomb-mediated gene silencing
Hagar F. Moussa et al.
NATURE COMMUNICATIONS (2019)
An Allosteric PRC2 Inhibitor Targeting EED Suppresses Tumor Progression by Modulating the Immune Response
Hongping Dong et al.
CANCER RESEARCH (2019)
Targeting epigenetic machinery: Emerging novel allosteric inhibitors
Fei Ye et al.
PHARMACOLOGY & THERAPEUTICS (2019)
Long Non-coding RNAs as Functional and Structural Chromatin Modulators in Acute Myeloid Leukemia
Alexander A. Wurm et al.
FRONTIERS IN ONCOLOGY (2019)
A novel BMI-1 inhibitor QW24 for the treatment of stem-like colorectal cancer
Jinhua Wang et al.
JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH (2019)
CoREST Complex-Selective Histone Deacetylase Inhibitors Show Prosynaptic' Effects and an Improved Safety Profile To Enable Treatment of Synaptopathies
Nathan O. Fuller et al.
ACS CHEMICAL NEUROSCIENCE (2019)
Targeting the GFI1/1B-CoREST Complex in Acute Myeloid Leukemia
Maaike G. J. M. van Bergen et al.
FRONTIERS IN ONCOLOGY (2019)
T-448, a specific inhibitor of LSD1 enzyme activity, improves learning function without causing thrombocytopenia in mice
Satoru Matsuda et al.
NEUROPSYCHOPHARMACOLOGY (2019)
The timeline of epigenetic drug discovery: from reality to dreams
A. Ganesan et al.
CLINICAL EPIGENETICS (2019)
Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7
Kelsey N. Lamb et al.
CELL CHEMICAL BIOLOGY (2019)
Evaluating the Mechanism and Therapeutic Potential of PTC-028, a Novel Inhibitor of BMI-1 Function in Ovarian Cancer
Anindya Dey et al.
MOLECULAR CANCER THERAPEUTICS (2018)
Mechanisms of resistance to EZH2 inhibitors in diffuse large B-cell lymphomas
Malik Bisserier et al.
BLOOD (2018)
ORY-1001, a Potent and Selective Covalent KDM1A Inhibitor, for the Treatment of Acute Leukemia
Tamara Maes et al.
CANCER CELL (2018)
Chemical Protein Degradation Approach and its Application to Epigenetic Targets
Yukihiro Itoh
CHEMICAL RECORD (2018)
Unique Structural Platforms of Suz12 Dictate Distinct Classes of PRC2 for Chromatin Binding
Siming Chen et al.
MOLECULAR CELL (2018)
Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors
Jay H. Kalin et al.
NATURE COMMUNICATIONS (2018)
Enhancer Activation by Pharmacologic Displacement of LSD1 from GFI1 Induces Differentiation in Acute Myeloid Leukemia
Alba Maiques-Diaz et al.
CELL REPORTS (2018)
Synthesis of Cyanoenone-Modified Diterpenoid Analogs as Novel Bmi-1-Mediated Antitumor Agents
Lian-Fang Yang et al.
ACS MEDICINAL CHEMISTRY LETTERS (2018)
Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers
Julien P. N. Papillon et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
A Novel LSD1 Inhibitor T-3775440 Disrupts GFI1B-Containing Complex Leading to Transdifferentiation and Impaired Growth of AML Cells
Yoshinori Ishikawa et al.
MOLECULAR CANCER THERAPEUTICS (2017)
Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy
Ying Huang et al.
JOURNAL OF MEDICINAL CHEMISTRY (2017)
Allosteric Inactivation of Polycomb Repressive Complex 2 (PRC2) by Inhibiting Its Adapter Protein: Embryonic Ectodomain Development (EED)
Chao-Yie Yang et al.
JOURNAL OF MEDICINAL CHEMISTRY (2017)
A novel LSD1 inhibitor NCD38 ameliorates MDS-related leukemia with complex karyotype by attenuating leukemia programs via activating super-enhancers
N. Sugino et al.
LEUKEMIA (2017)
An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED
Wei Qi et al.
NATURE CHEMICAL BIOLOGY (2017)
The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex
Yupeng He et al.
NATURE CHEMICAL BIOLOGY (2017)
Mechanisms Regulating PRC2 Recruitment and Enzymatic Activity
Daniel Holoch et al.
TRENDS IN BIOCHEMICAL SCIENCES (2017)
Targeting Class I Histone Deacetylases in a Complex Environment
Christopher J. Millard et al.
TRENDS IN PHARMACOLOGICAL SCIENCES (2017)
The novel BMI-1 inhibitor PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells
Y. Nishida et al.
BLOOD CANCER JOURNAL (2017)
Structure based design, synthesis and activity studies of small hybrid molecules as HDAC and G9a dual inhibitors
Lanlan Zang et al.
ONCOTARGET (2017)
Targeting Cancer with PCPA-Drug Conjugates: LSD1 Inhibition-Triggered Release of 4-Hydroxytamoxifen
Yosuke Ota et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2016)
BMI-1 Targeting Interferes with Patient-Derived Tumor-Initiating Cell Survival and Tumor Growth in Prostate Cancer
Nitu Bansal et al.
CLINICAL CANCER RESEARCH (2016)
Structure-Activity Relationships and Kinetic Studies of Peptidic Antagonists of CBX Chromodomains
Jacob I. Stuckey et al.
JOURNAL OF MEDICINAL CHEMISTRY (2016)
A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1
Jacob I. Stuckey et al.
NATURE CHEMICAL BIOLOGY (2016)
LSD1 engages a corepressor complex for the activation of the estrogen receptor α by estrogen and cAMP
Marcela A. Bennesch et al.
NUCLEIC ACIDS RESEARCH (2016)
Targeting the Notch-regulated non-coding RNA TUG1 for glioma treatment
Keisuke Katsushima et al.
NATURE COMMUNICATIONS (2016)
Preclinical activity of the novel B-cell-specific Moloney murine leukemia virus integration site 1 inhibitor PTC-209 in acute myeloid leukemia: Implications for leukemia therapy
Yuki Nishida et al.
CANCER SCIENCE (2015)
Wedelolactone disrupts the interaction of EZH2-EED complex and inhibits PRC2-dependent cancer
Huiming Chen et al.
ONCOTARGET (2015)
Variant PRC1 Complex-Dependent H2A Ubiquitylation Drives PRC2 Recruitment and Polycomb Domain Formation
Neil P. Blackledge et al.
CELL (2014)
Astemizole Arrests the Proliferation of Cancer Cells by Disrupting the EZH2-EED Interaction of Polycomb Repressive Complex 2
Xiangqian Kong et al.
JOURNAL OF MEDICINAL CHEMISTRY (2014)
Chromodomain Antagonists That Target the Polycomb-Group Methyllysine Reader Protein Chromobox Homo log 7 (CBX7)
Chakravarthi Simhadri et al.
JOURNAL OF MEDICINAL CHEMISTRY (2014)
Self-renewal as a therapeutic target in human colorectal cancer
Antonija Kreso et al.
NATURE MEDICINE (2014)
Lysine-Specific Demethylase 1 Has Dual Functions as a Major Regulator of Androgen Receptor Transcriptional Activity
Changmeng Cai et al.
CELL REPORTS (2014)
Lysine-Specific Demethylase 1-Selective Inactivators: Protein-Targeted Drug Delivery Mechanism
Daisuke Ogasawara et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2013)
The physiological roles of histone deacetylase (HDAC) 1 and 2: complex co-stars with multiple leading parts
Richard D. W. Kelly et al.
BIOCHEMICAL SOCIETY TRANSACTIONS (2013)
A Small Molecule Inhibitor of Polycomb Repressive Complex 1 Inhibits Ubiquitin Signaling at DNA Double-strand Breaks
Ismail Hassan Ismail et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2013)
Targeted disruption of the EZH2-EED complex inhibits EZH2-dependent cancer
Woojin Kim et al.
NATURE CHEMICAL BIOLOGY (2013)
Transcriptional regulation by Polycomb group proteins
Luciano Di Croce et al.
NATURE STRUCTURAL & MOLECULAR BIOLOGY (2013)
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations
Michael T. McCabe et al.
NATURE (2012)
Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)
Michael T. McCabe et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2012)
Histone Methylation by PRC2 Is Inhibited by Active Chromatin Marks
Frank W. Schmitges et al.
MOLECULAR CELL (2011)
Long non-coding RNA HOTAIR reprograms chromatin state to promote cancer metastasis
Rajnish A. Gupta et al.
NATURE (2010)
Long Noncoding RNA as Modular Scaffold of Histone Modification Complexes
Miao-Chih Tsai et al.
SCIENCE (2010)
The E3 Ubiquitin-Ligase Bmi1/Ring1A Controls the Proteasomal Degradation of Top2α Cleavage Complex - A Potentially New Drug Target
Iris Alchanati et al.
PLOS ONE (2009)
Structural basis of histone H4 recognition by p55
Ji-Joon Song et al.
GENES & DEVELOPMENT (2008)
Structural basis of LSD1-CoREST selectivity in histone H3 recognition
Federico Forneris et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2007)
Genome regulation by polycomb and trithorax proteins
Bernd Schuettengruber et al.
CELL (2007)
Share Paper
