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8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase InhibitorsRVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomainPlant Growth Regulator Daminozide Is a Selective Inhibitor of Human KDM2/7 Histone DemethylasesK2P channel gating mechanisms revealed by structures of TREK-2 and a complex with ProzacStructure of the Human Protein Kinase ZAK in Complex with VemurafenibStructural analysis of human KDM5B guides histone demethylase inhibitor developmentDevelopment of Selective CBP/P300 Benzoxazepine Bromodomain InhibitorsLP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain InhibitorGeneration of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia TherapyAssessing histone demethylase inhibitors in cells: lessons learned.Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells.Synthesis of carbohydrate derivatives using solid-phase work-up and scavenging techniques.Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.PFI-1, a highly selective protein interaction inhibitor, targeting BET BromodomainsThe promise and peril of chemical probes.Fragment-based hit identification: thinking in 3D.Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks.Recent Progress in Histone Demethylase Inhibitors.Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain.CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responsesBET inhibition as a new strategy for the treatment of gastric cancer.Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors.Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions.Highly selective inhibition of histone demethylases by de novo macrocyclic peptides.Discovery of a PCAF Bromodomain Chemical Probe.Selective targeting of Bromodomains of the Bromodomain-PHD Fingers family impairs osteoclast differentiation.Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF.Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins.Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.Development of chemical probes for the bromodomains of BRD7 and BRD9.Advances and challenges in understanding histone demethylase biology.Deciphering the true antiproliferative target of an MK2 activation inhibitor in glioblastoma.Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment HitSelective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.BRD3 and BRD4 BET Bromodomain Proteins Differentially Regulate Skeletal Myogenesis.Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex.A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction.The SGC beyond structural genomics: redefining the role of 3D structures by coupling genomic stratification with fragment-based discovery.
P50
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P50
description
hulumtues
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researcher
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հետազոտող
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name
Paul E Brennan
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Paul E Brennan
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Paul E Brennan
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Paul E Brennan
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Paul E Brennan
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Paul E Brennan
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Paul E Brennan
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Paul E Brennan
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Paul E Brennan
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Paul E Brennan
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Paul E Brennan
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Paul E Brennan
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Paul E Brennan
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Paul E Brennan
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P106
P21
P31
P3835
paul-brennan10
P496
0000-0002-8950-7646