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。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)
Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery
George M. Burslem et al.
CELL (2020)
Discovery of a first-in-class EZH2 selective degrader
Anqi Ma et al.
NATURE CHEMICAL BIOLOGY (2020)
Proteolysis targeting chimeras (PROTACs) for epigenetics research
Anja Vogelmann et al.
CURRENT OPINION IN CHEMICAL BIOLOGY (2020)
Epigenetic Therapies for Cancer
Susan E. Bates
NEW ENGLAND JOURNAL OF MEDICINE (2020)
Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs)
Daniela Tomaselli et al.
EUROPEAN 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)
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
William Farnaby et al.
NATURE CHEMICAL BIOLOGY (2019)
A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo
Longchuan Bai et al.
CANCER CELL (2019)
Targeted protein degradation: expanding the toolbox
Matthieu Schapira et al.
NATURE REVIEWS DRUG DISCOVERY (2019)
Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7
Vittoria Zoppi et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer
Xin Han et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression
Bing Zhou et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Novel combination of histone methylation modulators with therapeutic synergy against acute myeloid leukemia in vitro and in vivo
Shijun Wen et al.
CANCER LETTERS (2018)
PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies
Yonghui Sun et al.
CELL RESEARCH (2018)
Delineating the role of cooperativity in the design of potent PROTACs for BTK
Adelajda Zorba et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2018)
Targeting Epigenetic Crosstalk as a Therapeutic Strategy for EZH2-Aberrant Solid Tumors
Xun Huang et al.
CELL (2018)
Polycomb- and Methylation-Independent Roles of EZH2 as a Transcription Activator
Jung Kim et al.
CELL REPORTS (2018)
A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader
Hai-Tsang Huang et al.
CELL CHEMICAL BIOLOGY (2018)
Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead
Daniel P. Bondeson et al.
CELL CHEMICAL BIOLOGY (2018)
Enhancer of zeste homologue 2 plays an important role in neuroblastoma cell survival independent of its histone methyltransferase activity
Laurel T. Bate-Eya et al.
EUROPEAN JOURNAL OF CANCER (2017)
Chemotherapy induces tumor immune evasion by upregulation of programmed cell death ligand 1 expression in bone marrow stromal cells
Mengqi Yang et al.
MOLECULAR ONCOLOGY (2017)
Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation
Chiara Maniaci et al.
NATURE COMMUNICATIONS (2017)
Targeting EZH2 in cancer therapy
Makoto Yamagishi et al.
CURRENT OPINION IN ONCOLOGY (2017)
Oncogenic roles of SMARCB1/INI1 and its deficient tumors
Kenichi Kohashi et al.
CANCER SCIENCE (2017)
A covalently bound inhibitor triggers EZH2 degradation through CHIP-mediated ubiquitination
Xu Wang et al.
EMBO JOURNAL (2017)
Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands
David Remillard et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2017)
Development of secondary mutations in wild-type and mutant EZH2 alleles cooperates to confer resistance to EZH2 inhibitors
V. Gibaja et al.
ONCOGENE (2016)
The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat
Kevin W. Kuntz et al.
JOURNAL OF MEDICINAL CHEMISTRY (2016)
Targeting EZH2 in cancer
Kimberly H. Kim et al.
NATURE MEDICINE (2016)
Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition
Julianty Frost et al.
NATURE COMMUNICATIONS (2016)
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
Michael Zengerle et al.
ACS CHEMICAL BIOLOGY (2015)
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
Jing Lu et al.
CHEMISTRY & BIOLOGY (2015)
SWI/SNF-mutant cancers depend on catalytic and non-catalytic activity of EZH2
Kimberly H. Kim et al.
NATURE MEDICINE (2015)
Synthetic lethality by targeting EZH2 methyltransferase activity in ARID1A-mutated cancers
Benjamin G. Bitler et al.
NATURE MEDICINE (2015)
Phthalimide conjugation as a strategy for in vivo target protein degradation
Georg E. Winter et al.
SCIENCE (2015)
Structure-Guided Design and Optimization of Small Molecules Targeting the Protein Protein Interaction between the von Hippel- Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities
Carles Galdeano et al.
JOURNAL OF MEDICINAL CHEMISTRY (2014)
Transcriptional regulation by Polycomb group proteins
Luciano Di Croce et al.
NATURE STRUCTURAL & MOLECULAR BIOLOGY (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)
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)
Genetic inactivation of the polycomb repressive complex 2 in T cell acute lymphoblastic leukemia
Panagiotis Ntziachristos et al.
NATURE MEDICINE (2012)
EZH2 Oncogenic Activity in Castration-Resistant Prostate Cancer Cells Is Polycomb-Independent
Kexin Xu et al.
SCIENCE (2012)
The Polycomb complex PRC2 and its mark in life
Raphael Margueron et al.
NATURE (2011)
EZH2-mediated epigenetic silencing in germinal center B cells contributes to proliferation and lymphomagenesis
Irina Velichutina et al.
BLOOD (2010)
Molecular Signals of Epigenetic States
Roberto Bonasio et al.
SCIENCE (2010)
A role for transferrin receptor in triggering apoptosis when targeted with gambogic acid
S Kasibhatla et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2005)
分享论文
