Targeting epigenetic modulators using PROTAC degraders: Current status and future perspective
出版年份 2022 全文链接
标题
Targeting epigenetic modulators using PROTAC degraders: Current status and future perspective
作者
关键词
Epigenetics, Chromatin, Multiprotein complexes, Targeted protein degradation, PROTACs, Degraders, Therapeutics
出版物
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 63, Issue -, Pages 128653
出版商
Elsevier BV
发表日期
2022-03-04
DOI
10.1016/j.bmcl.2022.128653
参考文献
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。- PROTAC targeted protein degraders: the past is prologue
- (2022) Miklós Békés et al. NATURE REVIEWS DRUG DISCOVERY
- 3D Functional Genomics Screens Identify CREBBP as a Targetable Driver in Aggressive Triple-Negative Breast Cancer
- (2021) Barrie Peck et al. CANCER RESEARCH
- Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2
- (2021) Zhihao Liu et al. JOURNAL OF MEDICINAL CHEMISTRY
- Transforming targeted cancer therapy with PROTACs: A forward-looking perspective
- (2021) William Farnaby et al. CURRENT OPINION IN PHARMACOLOGY
- Protein arginine methyltransferases: promising targets for cancer therapy
- (2021) Jee Won Hwang et al. EXPERIMENTAL AND MOLECULAR MEDICINE
- Genome-wide CRISPR screens reveal synthetic lethal interaction between CREBBP and EP300 in diffuse large B-cell lymphoma
- (2021) Man Nie et al. Cell Death & Disease
- Combined EZH2 Inhibition and IKAROS Degradation Leads to Enhanced Antitumor Activity in Diffuse Large B-cell Lymphoma
- (2021) Kit I. Tong et al. CLINICAL CANCER RESEARCH
- BAF complexes drive proliferation and block myogenic differentiation in fusion-positive rhabdomyosarcoma
- (2021) Dominik Laubscher et al. Nature Communications
- Genome-wide CRISPR-Cas9 screens identify mechanisms of BET bromodomain inhibitor sensitivity
- (2021) David Estoppey et al. iScience
- Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors
- (2020) Yaxi Yang et al. JOURNAL OF MEDICINAL CHEMISTRY
- Prey for the Proteasome: Targeted Protein Degradation – A Medicinal Chemist´s Perspective
- (2020) Laura M. Luh et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- EZH2 has a non-catalytic and PRC2-independent role in stabilizing DDB2 to promote nucleotide excision repair
- (2020) Allyson E. Koyen et al. ONCOGENE
- Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor
- (2020) Jonathan E. Wilson et al. ACS Medicinal Chemistry Letters
- Discovery of First-in-class Protein Arginine Methyltransferase 5 (PRMT5) Degraders
- (2020) Yudao Shen et al. JOURNAL OF MEDICINAL CHEMISTRY
- Nothing Is yet Set in (Hi)stone: Novel Post-Translational Modifications Regulating Chromatin Function
- (2020) Jennifer C. Chan et al. TRENDS IN BIOCHEMICAL SCIENCES
- Genome-wide CRISPR screens reveal host factors critical for SARS-CoV-2 infection
- (2020) Jin Wei et al. CELL
- Targeting PRC2 for the treatment of cancer: an updated patent review (2016 - 2020)
- (2020) Milly Dockerill et al. EXPERT OPINION ON THERAPEUTIC PATENTS
- Mammalian SWI/SNF Chromatin Remodeling Complexes: Emerging Mechanisms and Therapeutic Strategies
- (2020) Richard C. Centore et al. TRENDS IN GENETICS
- Building ubiquitination machineries: E3 ligase multi-subunit assembly and substrate targeting by PROTACs and molecular glues
- (2020) Sarath Ramachandran et al. CURRENT OPINION IN STRUCTURAL BIOLOGY
- Combination Targeting of the Bromodomain and Acetyltransferase Active Site of p300/CBP
- (2019) Beth E. Zucconi et al. BIOCHEMISTRY
- Molecular Mechanisms Directing PRC2 Recruitment and H3K27 Methylation
- (2019) Anne Laugesen et al. MOLECULAR CELL
- BRD9 defines a SWI/SNF sub-complex and constitutes a specific vulnerability in malignant rhabdoid tumors
- (2019) Xiaofeng Wang et al. Nature Communications
- BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
- (2019) William Farnaby et al. Nature Chemical Biology
- Bromodomains: a new target class for drug development
- (2019) Andrea G. Cochran et al. NATURE REVIEWS DRUG DISCOVERY
- An Evolutionarily Conserved Function of Polycomb Silences the MHC Class I Antigen Presentation Pathway and Enables Immune Evasion in Cancer
- (2019) Marian L. Burr et al. CANCER CELL
- Histone lysine methyltransferases in biology and disease
- (2019) Dylan Husmann et al. NATURE STRUCTURAL & MOLECULAR BIOLOGY
- Discovery of a first-in-class EZH2 selective degrader
- (2019) Anqi Ma et al. Nature Chemical Biology
- Chemical Protein Degradation Approach and its Application to Epigenetic Targets
- (2018) Yukihiro Itoh CHEMICAL RECORD
- N 6 -Methyladenine DNA Modification in the Human Genome
- (2018) Chuan-Le Xiao et al. MOLECULAR CELL
- Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition
- (2018) A. C. Runcie et al. Chemical Science
- Discovery of Spiro Oxazolidinediones as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases
- (2018) Michael R. Michaelides et al. ACS Medicinal Chemistry Letters
- Structural determinants of 5-HT2B receptor activation and biased agonism
- (2018) John D. McCorvy et al. NATURE STRUCTURAL & MOLECULAR BIOLOGY
- Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers
- (2018) Julien P. N. Papillon et al. JOURNAL OF MEDICINAL CHEMISTRY
- 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
- (2018) Vittoria Zoppi et al. JOURNAL OF MEDICINAL CHEMISTRY
- CRISPR-Cas9 screen reveals a MYCN-amplified neuroblastoma dependency on EZH2
- (2017) Liying Chen et al. JOURNAL OF CLINICAL INVESTIGATION
- GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP)
- (2017) F. Anthony Romero et al. JOURNAL OF MEDICINAL CHEMISTRY
- Selective Killing of SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models
- (2017) Elayne Chan-Penebre et al. MOLECULAR CANCER THERAPEUTICS
- Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours
- (2017) Loren M. Lasko et al. NATURE
- An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED
- (2017) Wei Qi et al. Nature Chemical Biology
- The EED protein–protein interaction inhibitor A-395 inactivates the PRC2 complex
- (2017) Yupeng He et al. Nature Chemical Biology
- Computational correction of copy number effect improves specificity of CRISPR–Cas9 essentiality screens in cancer cells
- (2017) Robin M Meyers et al. NATURE GENETICS
- Functions of bromodomain-containing proteins and their roles in homeostasis and cancer
- (2017) Takao Fujisawa et al. NATURE REVIEWS MOLECULAR CELL BIOLOGY
- Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation
- (2017) Chiara Maniaci et al. Nature Communications
- Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors
- (2017) Jayme L. Dahlin et al. Nature Communications
- Chromatin-Remodeling Complex SWI/SNF Controls Multidrug Resistance by Transcriptionally Regulating the Drug Efflux Pump ABCB1
- (2016) Ramin Dubey et al. CANCER RESEARCH
- Functional Genomic Landscape of Human Breast Cancer Drivers, Vulnerabilities, and Resistance
- (2016) Richard Marcotte et al. CELL
- Romidepsin for the treatment of relapsed/refractory cutaneous T-cell lymphoma (mycosis fungoides/Sézary syndrome): Use in a community setting
- (2016) Sunil A. Reddy CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY
- Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas
- (2016) Rishi G. Vaswani et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex
- (2016) Charlotte L. Sutherell et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor
- (2016) Laetitia J. Martin et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit
- (2016) Brian S. Gerstenberger et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis
- (2016) Vassilios Myrianthopoulos et al. JOURNAL OF MEDICINAL CHEMISTRY
- Engineering Biological C–H Functionalization Leads to Allele-Specific Regulation of Histone Demethylases
- (2016) Megan Breski et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Targeting EZH2 in cancer
- (2016) Kimberly H Kim et al. NATURE MEDICINE
- Exploitation of EP300 and CREBBP Lysine Acetyltransferases by Cancer
- (2016) Narsis Attar et al. Cold Spring Harbor Perspectives in Medicine
- Targeting Cullin–RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation
- (2015) Emil Bulatov et al. BIOCHEMICAL JOURNAL
- Genome-Wide Identification and Characterization of Novel Factors Conferring Resistance to Topoisomerase II Poisons in Cancer
- (2015) R. H. Wijdeven et al. CANCER RESEARCH
- The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies
- (2015) Bhavatarini Vangamudi et al. CANCER RESEARCH
- New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition
- (2015) Matthias G. J. Baud et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition
- (2015) Natalie H. Theodoulou et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of cancer drug targets by CRISPR-Cas9 screening of protein domains
- (2015) Junwei Shi et al. NATURE BIOTECHNOLOGY
- A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models
- (2015) Elayne Chan-Penebre et al. Nature Chemical Biology
- Targeting p300 Addiction in CBP-Deficient Cancers Causes Synthetic Lethality by Apoptotic Cell Death due to Abrogation of MYC Expression
- (2015) H. Ogiwara et al. Cancer Discovery
- Dysregulated Class I histone deacetylases are indicators of poor prognosis in multiple myeloma
- (2014) Sridurga Mithraprabhu et al. Epigenetics
- Residual Complexes Containing SMARCA2 (BRM) Underlie the Oncogenic Drive of SMARCA4 (BRG1) Mutation
- (2014) B. G. Wilson et al. MOLECULAR AND CELLULAR BIOLOGY
- Targeting bromodomains: epigenetic readers of lysine acetylation
- (2014) Panagis Filippakopoulos et al. NATURE REVIEWS DRUG DISCOVERY
- Functional epigenetics approach identifies BRM/SMARCA2 as a critical synthetic lethal target in BRG1-deficient cancers
- (2014) G. R. Hoffman et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes
- (2014) M. G. J. Baud et al. SCIENCE
- Exploiting epigenetic vulnerabilities for cancer therapeutics
- (2014) Barbara Mair et al. TRENDS IN PHARMACOLOGICAL SCIENCES
- Mechanisms by which SMARCB1 loss drives rhabdoid tumor growth
- (2014) Kimberly H. Kim et al. Cancer Genetics
- A Synthetic Lethality-Based Strategy to Treat Cancers Harboring a Genetic Deficiency in the Chromatin Remodeling Factor BRG1
- (2013) T. Oike et al. CANCER RESEARCH
- Role of SWI/SNF in acute leukemia maintenance and enhancer-mediated Myc regulation
- (2013) J. Shi et al. GENES & DEVELOPMENT
- Current Chemical Biology Approaches to Interrogate Protein Methyltransferases
- (2012) Minkui Luo ACS Chemical Biology
- Histone Lysine Methylation Dynamics: Establishment, Regulation, and Biological Impact
- (2012) Joshua C. Black et al. MOLECULAR CELL
- Greasy tags for protein removal
- (2012) Taavi K. Neklesa et al. NATURE
- A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells
- (2012) Sarah K Knutson et al. Nature Chemical Biology
- Epigenetic protein families: a new frontier for drug discovery
- (2012) Cheryl H. Arrowsmith et al. NATURE REVIEWS DRUG DISCOVERY
- Structure-Guided Design of a Methyl Donor Cofactor That Controls a Viral Histone H3 Lysine 27 Methyltransferase Activity
- (2011) Jiaojie Li et al. JOURNAL OF MEDICINAL CHEMISTRY
- RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia
- (2011) Johannes Zuber et al. NATURE
- The Polycomb complex PRC2 and its mark in life
- (2011) Raphaël Margueron et al. NATURE
- Virtual Ligand Screening of the p300/CBP Histone Acetyltransferase: Identification of a Selective Small Molecule Inhibitor
- (2010) Erin M. Bowers et al. CHEMISTRY & BIOLOGY
- Target gene context influences the transcriptional requirement for the KAT3 family of CBP and p300 histone acetyltransferases
- (2010) David C. Bedford et al. Epigenetics
- Epigenetic modifications and human disease
- (2010) Anna Portela et al. NATURE BIOTECHNOLOGY
- Chromatin mechanisms in genomic imprinting
- (2009) Slim Kacem et al. MAMMALIAN GENOME
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