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Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines.
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What this work says
Outgoing claims: the papers this work cites, builds on, or argues with.
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The Emerging Therapeutic Potential of Histone Methyltransferase and Demethylase Inhibitors
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Kinetics of the reversible inhibition of enzyme-catalysed reactions by tight-binding inhibitors
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[17] The kinetics of reversible tight-binding inhibition
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A coupled fluorescent assay for histone methyltransferases
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Cancer treatment of the future: Inhibitors of histone methyltransferases
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Chromatin Modifications and Their Function
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Accessing Protein Methyltransferase and Demethylase Enzymology Using Microfluidic Capillary Electrophoresis
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Reversal of H3K9me2 by a Small-Molecule Inhibitor for the G9a Histone Methyltransferase
inferredcites →https://doi.org/10.1016/j.neuron.2009.11.019openalex-snapshot
Control of Cognition and Adaptive Behavior by the GLP/G9a Epigenetic Suppressor Complex
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A Combined Chemical and Genetic Approach for the Generation of Induced Pluripotent Stem Cells
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inferredcites →https://doi.org/10.1016/s0065-7743(10)45020-4openalex-snapshot
Targeting Methyl Lysine
inferredcites →https://doi.org/10.1021/jm901543mopenalex-snapshot
Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a
inferredcites →https://doi.org/10.1038/35020506openalex-snapshot
Regulation of chromatin structure by site-specific histone H3 methyltransferases
inferredcites →https://doi.org/10.1038/47412openalex-snapshot
The language of covalent histone modifications
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Chemical probes for histone-modifying enzymes
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Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9
inferredcites →https://doi.org/10.1038/nprot.2007.321openalex-snapshot
The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability
inferredcites →https://doi.org/10.1038/nrd2974openalex-snapshot
Protein methyltransferases as a target class for drug discovery
inferredcites →https://doi.org/10.1038/nrm1761openalex-snapshot
The diverse functions of histone lysine methylation
inferredcites →https://doi.org/10.1038/nsmb.1560openalex-snapshot
Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294
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L3MBTL1 recognition of mono- and dimethylated histones
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A miniaturized screen for inhibitors of Jumonji histonedemethylases
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A chemiluminescence-based method for identification of histone lysine methyltransferase inhibitors
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A survey of proteins encoded by non-synonymous single nucleotide polymorphisms reveals a significant fraction with altered stability and activity
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Chemical screening methods to identify ligands that promote protein stability, protein crystallization, and structure determination
inferredcites →https://doi.org/10.1074/jbc.m109.062588openalex-snapshot
G9a and Glp Methylate Lysine 373 in the Tumor Suppressor p53
inferredcites →https://doi.org/10.1074/jbc.m110.103531openalex-snapshot
Involvement of Histone H3 Lysine 9 (H3K9) Methyltransferase G9a in the Maintenance of HIV-1 Latency and Its Reactivation by BIX01294
inferredcites →https://doi.org/10.1074/jbc.m802800200openalex-snapshot
Role of the Histone H3 Lysine 4 Methyltransferase, SET7/9, in the Regulation of NF-κB-dependent Inflammatory Genes
inferredcites →https://doi.org/10.1093/jnci/dji311openalex-snapshot
DNA Methyltransferase Inhibitors and the Development of Epigenetic Cancer Therapies
inferredcites →https://doi.org/10.1101/gad.989402openalex-snapshot
G9a histone methyltransferase plays a dominant role in euchromatic histone H3 lysine 9 methylation and is essential for early embryogenesis
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Chromatin‐modifying proteins in cancer
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Essential Role of the Histone Methyltransferase G9a in Cocaine-Induced Plasticity
inferredcites →https://doi.org/10.1158/0008-5472.can-05-2481openalex-snapshot
Silenced Tumor Suppressor Genes Reactivated by DNA Demethylation Do Not Return to a Fully Euchromatic Chromatin State
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Lanthanum Chloride Inhibits LPS Mediated Expressions of Pro-Inflammatory Cytokines and Adhesion Molecules in HUVECs: Involvement of NF-κB-Jmjd3 Signaling
inferredcites →https://doi.org/10.1371/journal.pone.0002037openalex-snapshot
Downregulation of Histone H3 Lysine 9 Methyltransferase G9a Induces Centrosome Disruption and Chromosome Instability in Cancer Cells
inferredcites →https://doi.org/10.1515/bc.2008.048openalex-snapshot
Role of histone modifications in defining chromatin structure and function
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Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP
inferred← citeshttps://doi.org/10.1021/jm500871sopenalex-snapshot
Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8
inferred← citeshttps://doi.org/10.1021/jm501234aopenalex-snapshot
Selective Inhibitors of Protein Methyltransferases
inferred← citeshttps://doi.org/10.1021/ml3003346openalex-snapshot
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2
inferred← citeshttps://doi.org/10.1021/ml4002503openalex-snapshot
Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2
inferred← citeshttps://doi.org/10.1021/ml400496hopenalex-snapshot
Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a
inferred← citeshttps://doi.org/10.1038/ja.2012.6openalex-snapshot
Inhibition of histone H3K9 methyltransferases by gliotoxin and related epipolythiodioxopiperazines
inferred← citeshttps://doi.org/10.1038/nature12751openalex-snapshot
Chromatin proteins and modifications as drug targets
inferred← citeshttps://doi.org/10.1038/nchembio.599openalex-snapshot
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells
inferred← citeshttps://doi.org/10.1038/ncomms10810openalex-snapshot
G9a-mediated methylation of ERα links the PHF20/MOF histone acetyltransferase complex to hormonal gene expression
inferred← citeshttps://doi.org/10.1038/ncomms15424openalex-snapshot
Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies
inferred← citeshttps://doi.org/10.1038/nm.3461openalex-snapshot
Persistence and activation of malaria hypnozoites in long-term primary hepatocyte cultures
inferred← citeshttps://doi.org/10.1038/nrc.2016.148openalex-snapshot
A chemical probe toolbox for dissecting the cancer epigenome
inferred← citeshttps://doi.org/10.1038/nrd3674openalex-snapshot
Epigenetic protein families: a new frontier for drug discovery
inferred← citeshttps://doi.org/10.1038/s41380-019-0351-2openalex-snapshot
Amelioration of autism-like social deficits by targeting histone methyltransferases EHMT1/2 in Shank3-deficient mice
inferred← citeshttps://doi.org/10.1038/s41420-022-01081-7openalex-snapshot
M2-like tumor-associated macrophages transmit exosomal miR-27b-3p and maintain glioblastoma stem-like cell properties
inferred← citeshttps://doi.org/10.1038/s41598-020-70523-yopenalex-snapshot
Epigenetics meets GPCR: inhibition of histone H3 methyltransferase (G9a) and histamine H3 receptor for Prader–Willi Syndrome
inferred← citeshttps://doi.org/10.1038/tpj.2011.64openalex-snapshot
Heterochromatin as an incubator for pathology and treatment non-response: implication for neuropsychiatric illness
inferred← citeshttps://doi.org/10.1039/9781782628484-00127openalex-snapshot
Targeting Histone Lysine Methyltransferases in Cancer
inferred← citeshttps://doi.org/10.1039/c1md00199jopenalex-snapshot
Development of second generation epigenetic agents
inferred← citeshttps://doi.org/10.1039/c3mb25410kopenalex-snapshot
Small-molecular modulators of cancer-associated epigenetic mechanisms
inferred← citeshttps://doi.org/10.1039/c4md00274aopenalex-snapshot
Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors
inferred← citeshttps://doi.org/10.1039/c4md00317aopenalex-snapshot
Structure–activity relationship studies of SETD8 inhibitors
inferred← citeshttps://doi.org/10.1039/c5ob00120jopenalex-snapshot
Design, synthesis, and kinetic analysis of potent protein N-terminal methyltransferase 1 inhibitors
inferred← citeshttps://doi.org/10.1039/c6md00130kopenalex-snapshot
Non-substrate based, small molecule inhibitors of the human isoprenylcysteine carboxyl methyltransferase
inferred← citeshttps://doi.org/10.1039/c7md00052aopenalex-snapshot
Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-Plasmodium activity
inferred← citeshttps://doi.org/10.1039/c7md00097aopenalex-snapshot
An insight into the therapeutic potential of quinazoline derivatives as anticancer agents
inferred← citeshttps://doi.org/10.1039/d1cb00016kopenalex-snapshot
Chemogenomics for drug discovery: clinical molecules from open access chemical probes
inferred← citeshttps://doi.org/10.1039/d1cb00196eopenalex-snapshot
Lysine methyltransferase inhibitors: where we are now
inferred← citeshttps://doi.org/10.1039/d3md00366copenalex-snapshot
SETDB1 as a cancer target: challenges and perspectives in drug design
inferred← citeshttps://doi.org/10.1039/d4ob00885eopenalex-snapshot
Synthesis of diversely substituted quinazoline-2,4(1 H ,3 H )-diones by cyclization of tert -butyl (2-cyanoaryl)carbamates
inferred← citeshttps://doi.org/10.1073/pnas.1205414109openalex-snapshot
Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum
inferred← citeshttps://doi.org/10.1073/pnas.1211803109openalex-snapshot
G9a functions as a molecular scaffold for assembly of transcriptional coactivators on a subset of Glucocorticoid Receptor target genes
inferred← citeshttps://doi.org/10.1080/07391102.2023.2213346openalex-snapshot
Integration of ligand and structure-based pharmacophore screening for the identification of novel natural leads against Euchromatic histone lysine methyltransferase 2 (EHMT2/G9a)
inferred← citeshttps://doi.org/10.1089/adt.2011.0390openalex-snapshot
Thermal Denaturation Assays in Chemical Biology
inferred← citeshttps://doi.org/10.1089/adt.2012.480openalex-snapshot
Assay Development for Histone Methyltransferases
inferred← citeshttps://doi.org/10.1089/omi.2019.0093openalex-snapshot
Cancer Drug Repositioning by Comparison of Gene Expression in Humans and Axolotl ( Ambystoma mexicanum ) During Wound Healing
inferred← citeshttps://doi.org/10.1093/abbs/gmr109openalex-snapshot
Targeting protein lysine methylation and demethylation in cancers
inferred← citeshttps://doi.org/10.1093/cercor/bhw170openalex-snapshot
Inhibition of G9a/GLP Complex Promotes Long-Term Potentiation and Synaptic Tagging/Capture in Hippocampal CA1 Pyramidal Neurons
inferred← citeshttps://doi.org/10.1093/cercor/bhy161openalex-snapshot
G9a/GLP Complex Acts as a Bidirectional Switch to Regulate Metabotropic Glutamate Receptor-Dependent Plasticity in Hippocampal CA1 Pyramidal Neurons
inferred← citeshttps://doi.org/10.1093/ijnp/pyac008openalex-snapshot
Inhibitory Metaplasticity in Juvenile Stressed Rats Restores Associative Memory in Adulthood by Regulating Epigenetic Complex G9a/GLP
inferred← citeshttps://doi.org/10.1098/rstb.2017.0080openalex-snapshot
Protein methyltransferase inhibitors as precision cancer therapeutics: a decade of discovery
inferred← citeshttps://doi.org/10.1101/gad.2027411openalex-snapshot
H3K9 methyltransferase G9a and the related molecule GLP
inferred← citeshttps://doi.org/10.1111/acel.12634openalex-snapshot
Epigenetic regulation by G9a/ GLP complex ameliorates amyloid‐beta 1‐42 induced deficits in long‐term plasticity and synaptic tagging/capture in hippocampal pyramidal neurons
inferred← citeshttps://doi.org/10.1111/bph.12844openalex-snapshot
Targeting the histone orthography of cancer: drugs for writers, erasers and readers
inferred← citeshttps://doi.org/10.1124/mol.112.080697openalex-snapshot
Writing and Rewriting the Epigenetic Code of Cancer Cells: From Engineered Proteins to Small Molecules
inferred← citeshttps://doi.org/10.1128/aac.04419-14openalex-snapshot
Histone Methyltransferase Inhibitors Are Orally Bioavailable, Fast-Acting Molecules with Activity against Different Species Causing Malaria in Humans
inferred← citeshttps://doi.org/10.1139/cjc-2018-0193openalex-snapshot
Preliminary investigations into the synthesis and antimicrobial activities of boron-containing capsaicinoids
inferred← citeshttps://doi.org/10.1146/annurev-biochem-060614-033923openalex-snapshot
Along the Central Dogma—Controlling Gene Expression with Small Molecules
inferred← citeshttps://doi.org/10.1155/2018/5492941openalex-snapshot
Development of a Cell-Based High-Throughput Screening Assay to Identify Porcine Host Defense Peptide-Inducing Compounds
inferred← citeshttps://doi.org/10.1177/1087057111422256openalex-snapshot
Fluorescence-Based Methods for Screening Writers and Readers of Histone Methyl Marks
inferred← citeshttps://doi.org/10.1177/1087057111422823openalex-snapshot
Efficient Hit-Finding Approaches for Histone Methyltransferases: The Key Parameters
inferred← citeshttps://doi.org/10.1177/1087057111422943openalex-snapshot
TR-FRET Cellular Assays for Interrogating Posttranslational Modifications of Histone H3
inferred← citeshttps://doi.org/10.1177/1087057112437763openalex-snapshot
Perspectives on the Discovery of Small-Molecule Modulators for Epigenetic Processes
inferred← citeshttps://doi.org/10.1177/1087057112452137openalex-snapshot
Small-Molecule Inhibitors of the Protein Methyltransferase SET7/9 Identified in a High-Throughput Screen
inferred← citeshttps://doi.org/10.1177/2472555220949166openalex-snapshot
Development of a Microscale Thermophoresis-Based Method for Screening and Characterizing Inhibitors of the Methyl-Lysine Reader Protein MRG15
inferred← citeshttps://doi.org/10.1186/1756-8935-6-s1-p112openalex-snapshot
Analogues of the natural product Sinefungin as potent inhibitors of EHMT1 and EHMT2
inferred← citeshttps://doi.org/10.1186/s12935-024-03441-yopenalex-snapshot
GLP and G9a histone methyltransferases as potential therapeutic targets for lymphoid neoplasms
inferred← citeshttps://doi.org/10.1186/s13148-015-0118-9openalex-snapshot
Dual EZH2 and EHMT2 histone methyltransferase inhibition increases biological efficacy in breast cancer cells
inferred← citeshttps://doi.org/10.1186/s13148-016-0268-4openalex-snapshot
The emerging role of lysine methyltransferase SETD8 in human diseases
inferred← citeshttps://doi.org/10.1186/s13148-018-0583-zopenalex-snapshot
Tackling malignant melanoma epigenetically: histone lysine methylation
inferred← citeshttps://doi.org/10.1210/endocr/bqab088openalex-snapshot
Control of Breast Cancer Pathogenesis by Histone Methylation and the Hairless Histone Demethylase
inferred← citeshttps://doi.org/10.1248/cpb.c12-00980openalex-snapshot
Development of Functional Molecules for Elucidation of the Physiological Roles of Several Nuclear Receptors and Their Endogenous Ligands
inferred← citeshttps://doi.org/10.1371/journal.pone.0029181openalex-snapshot
DNA Methylation-Independent Reversion of Gemcitabine Resistance by Hydralazine in Cervical Cancer Cells
inferred← citeshttps://doi.org/10.1371/journal.pone.0106962openalex-snapshot
Inhibition of H3K9 Methyltransferase G9a Repressed Cell Proliferation and Induced Autophagy in Neuroblastoma Cells
inferred← citeshttps://doi.org/10.1371/journal.pone.0122983openalex-snapshot
Functional Characterization of D9, a Novel Deazaneplanocin A (DZNep) Analog, in Targeting Acute Myeloid Leukemia (AML)
inferred← citeshttps://doi.org/10.1371/journal.pone.0197082openalex-snapshot
Identification of a peptide inhibitor for the histone methyltransferase WHSC1
inferred← citeshttps://doi.org/10.1523/jneurosci.0147-12.2012openalex-snapshot
G9a/GLP Histone Lysine Dimethyltransferase Complex Activity in the Hippocampus and the Entorhinal Cortex Is Required for Gene Activation and Silencing during Memory Consolidation
inferred← citeshttps://doi.org/10.17554/j.issn.2313-5611.2015.01.17openalex-snapshot
Protein Methylation and Demethylation in Cancer
inferred← citeshttps://doi.org/10.17615/sbg1-mk36openalex-snapshot
Chemical Probes for the Lysine Methyltransferases EZH2 and G9a: Design, Development, and Application
inferred← citeshttps://doi.org/10.2174/0113852728349742241115060532openalex-snapshot
Synthesis of Quinazoline Derivatives
inferred← citeshttps://doi.org/10.2174/1570159x14666161213143907openalex-snapshot
Implications of Epigenetic Mechanisms and their Targets in Cerebral Ischemia Models
inferred← citeshttps://doi.org/10.2174/1875397301005010048openalex-snapshot
Promoting Illiteracy in Epigenetics: An Emerging Therapeutic Strategy
inferred← citeshttps://doi.org/10.2174/1875397301005010072openalex-snapshot
Targets in Epigenetics: Inhibiting the Methyl Writers of the Histone Code
inferred← citeshttps://doi.org/10.2174/1875397301005010095openalex-snapshot
Methods for Activity Analysis of the Proteins that Regulate Histone Methylation
inferred← citeshttps://doi.org/10.2217/epi.11.73openalex-snapshot
Epigenomics of leukemia: from mechanisms to therapeutic applications
inferred← citeshttps://doi.org/10.2217/epi.15.87openalex-snapshot
Inhibitors of Protein Methyltransferases as Chemical Tools
inferred← citeshttps://doi.org/10.3389/fchem.2015.00044openalex-snapshot
Synthesis of lysine methyltransferase inhibitors
inferred← citeshttps://doi.org/10.3390/biomedicines10030638openalex-snapshot
High-Throughput Drug Library Screening in Primary KMT2A-Rearranged Infant ALL Cells Favors the Identification of Drug Candidates That Activate P53 Signaling
inferred← citeshttps://doi.org/10.3390/cancers14122855openalex-snapshot
Potential Therapeutics Targeting Upstream Regulators and Interactors of EHMT1/2
inferred← citeshttps://doi.org/10.3390/cancers16122175openalex-snapshot
G9a in Cancer: Mechanisms, Therapeutic Advancements, and Clinical Implications
inferred← citeshttps://doi.org/10.3390/ijms222011292openalex-snapshot
EHMT2/G9a as an Epigenetic Target in Pediatric and Adult Brain Tumors
inferred← citeshttps://doi.org/10.3390/molecules23123282openalex-snapshot
Activity Landscape and Molecular Modeling to Explore the SAR of Dual Epigenetic Inhibitors: A Focus on G9a and DNMT1
inferred← citeshttps://doi.org/10.3390/molecules28010003openalex-snapshot
Medicinal Chemistry of Anti-HIV-1 Latency Chemotherapeutics: Biotargets, Binding Modes and Structure-Activity Relationship Investigation
inferred← citeshttps://doi.org/10.3987/com-12-12466openalex-snapshot
Facile and Efficient Cyclization of Anthranilonitrile to 2,4-Dichloroquinazoline by Bis(trichloromethyl) Carbonate and Catalytic Amount Triphenylphosphine Oxide
inferred← citeshttps://doi.org/10.4137/geg.s12270openalex-snapshot
Use of Epigenetic Drugs in Disease: An Overview
inferred← citeshttps://doi.org/10.4155/fmc-2016-0096openalex-snapshot
Recently Discovered Ezh2 and Ehmt2 (G9A) Inhibitors
inferred← citeshttps://doi.org/10.4155/fmc-2018-0396openalex-snapshot
Insights for the Design of Protein Lysine Methyltransferase G9a Inhibitors
inferred← citeshttps://doi.org/10.4155/fmc.12.7openalex-snapshot
Current Limitations And Future Opportunities For Epigenetic Therapies
inferred← citeshttps://doi.org/10.4155/fmc.13.136openalex-snapshot
Recent Progress in the Discovery of Small-Molecule Inhibitors of the Hmt Ezh2 for the Treatment of Cancer
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