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Nature (London), ISSN 1476-4687, 2010, Volume 468, Issue 7327, pp. 1119 - 1123
.... The scope of inflammatory responses reflects the activation state of signalling proteins upstream of inflammatory genes as well as signal-induced assembly of nuclear chromatin complexes that support mRNA expression 1 – 4... 
MACHINES | BINDING MODULES | CHROMATIN | MULTIDISCIPLINARY SCIENCES | COMPLEXES | GENE-EXPRESSION | BROMODOMAIN PROTEIN BRD4 | TRANSCRIPTIONAL ELONGATION | P-TEFB | Sepsis - prevention & control | Salmonella Infections - immunology | Shock, Septic - prevention & control | Salmonella Infections - physiopathology | Salmonella typhimurium | Heterocyclic Compounds, 4 or More Rings - pharmacology | Sepsis - drug therapy | Heterocyclic Compounds, 4 or More Rings - therapeutic use | Inflammation - drug therapy | Shock, Septic - drug therapy | Anti-Inflammatory Agents - therapeutic use | Hydroxamic Acids - pharmacology | Protein-Serine-Threonine Kinases - metabolism | Protein Structure, Tertiary | Salmonella Infections - drug therapy | Genome-Wide Association Study | Epigenomics | Anti-Inflammatory Agents - pharmacology | Mice, Inbred C57BL | Cells, Cultured | Heterocyclic Compounds, 4 or More Rings - chemistry | Kaplan-Meier Estimate | Models, Molecular | Salmonella Infections - prevention & control | Benzodiazepines | Gene Expression Regulation - drug effects | Acetylation - drug effects | Animals | Anti-Inflammatory Agents - chemistry | Lipopolysaccharides - pharmacology | Histone Deacetylase Inhibitors - pharmacology | Macrophages - drug effects | Inflammation - prevention & control | Mice | Proteins | Pathology | Eukaryotes | Chromatin | Immunology | Pharmacology | Gene expression
Journal Article
Nature (London), ISSN 1476-4687, 2012, Volume 486, Issue 7401, pp. 80 - 84
... Ret inhibitors imparted reduced efficacy and enhanced toxicity. Drosophila genetics and compound profiling defined three pathways accounting for the mechanistic basis of efficacy and dose-limiting toxicity... 
PATHWAYS | RET | CHROMOSOME | DROSOPHILA MODEL | TYROSINE KINASE | MULTIDISCIPLINARY SCIENCES | CELL-PROLIFERATION | PD-0325901 | INHIBITOR | SORAFENIB | CARCINOMA | Niacinamide - analogs & derivatives | Proto-Oncogene Proteins c-ret - metabolism | Humans | Extracellular Signal-Regulated MAP Kinases - antagonists & inhibitors | Male | Phenylurea Compounds | Extracellular Signal-Regulated MAP Kinases - metabolism | Protein Kinase Inhibitors - adverse effects | Drosophila Proteins - metabolism | Molecular Targeted Therapy | Drosophila melanogaster - genetics | Heterocyclic Compounds, 4 or More Rings - pharmacology | Multiple Endocrine Neoplasia Type 2b - genetics | Multiple Endocrine Neoplasia Type 2b - enzymology | Benzenesulfonates - pharmacology | Multiple Endocrine Neoplasia Type 2b - drug therapy | Protein Kinase Inhibitors - chemistry | Polypharmacy | Heterocyclic Compounds, 4 or More Rings - therapeutic use | Drug-Related Side Effects and Adverse Reactions | src-Family Kinases - metabolism | Receptor Protein-Tyrosine Kinases - antagonists & inhibitors | Drug Evaluation, Preclinical | Drosophila Proteins - antagonists & inhibitors | Disease Models, Animal | src-Family Kinases - antagonists & inhibitors | Heterocyclic Compounds, 4 or More Rings - chemistry | Heterocyclic Compounds, 4 or More Rings - adverse effects | Survival Rate | Drosophila melanogaster - drug effects | Xenograft Model Antitumor Assays | Animals | Signal Transduction - drug effects | Protein Kinase Inhibitors - therapeutic use | Sorafenib | Protein Kinase Inhibitors - pharmacology | Pyridines - pharmacology | Cell Transformation, Neoplastic - drug effects | Drosophila Proteins - genetics | Cell Transformation, Neoplastic - pathology | Proto-Oncogene Proteins c-ret - genetics | Chemotherapy | Physiological aspects | Genetic aspects | Cellular signal transduction | Research | Carcinogenesis | Risk factors | Cancer | Proteins | Nuclear magnetic resonance--NMR | Insects | Toxicity | Mutation | Kinases | Drug dosages | Cell adhesion & migration
Journal Article
Nature (London), ISSN 1476-4687, 2017, Volume 550, Issue 7674, pp. 128 - 132
..., and have also been implicated in human pathological conditions (including cancer(3)). Current inhibitors of the p300 and CBP histone acetyltransferase domains, including natural products(4... 
ANDROGEN RECEPTOR | ACETYLTRANSFERASES P300 | MULTIDISCIPLINARY SCIENCES | SMALL-MOLECULE INHIBITOR | HISTONE | Catalytic Domain - drug effects | p300-CBP Transcription Factors - antagonists & inhibitors | Prostatic Neoplasms, Castration-Resistant - enzymology | Histone Acetyltransferases - chemistry | Humans | Receptors, Androgen - metabolism | Crystallography, X-Ray | Male | Antineoplastic Agents - therapeutic use | Hematologic Neoplasms - enzymology | Hematologic Neoplasms - pathology | Cell Lineage - drug effects | Heterocyclic Compounds, 4 or More Rings - pharmacology | Prostatic Neoplasms, Castration-Resistant - pathology | Heterocyclic Compounds, 4 or More Rings - therapeutic use | Biocatalysis - drug effects | Histone Acetyltransferases - metabolism | Antineoplastic Agents - pharmacology | Gene Expression Regulation, Neoplastic - drug effects | p300-CBP Transcription Factors - chemistry | Binding, Competitive | Enzyme Inhibitors - pharmacology | Heterocyclic Compounds, 4 or More Rings - chemistry | Models, Molecular | Neoplasms - enzymology | Prostatic Neoplasms, Castration-Resistant - drug therapy | Antineoplastic Agents - chemistry | Mice, SCID | Enzyme Inhibitors - therapeutic use | Acetyl Coenzyme A - metabolism | Neoplasms - drug therapy | Xenograft Model Antitumor Assays | p300-CBP Transcription Factors - metabolism | Animals | Histone Acetyltransferases - antagonists & inhibitors | Cell Line, Tumor | Hematologic Neoplasms - drug therapy | Protein Conformation | Cell Proliferation - drug effects | Mice | Neoplasms - pathology | Care and treatment | Chemical inhibitors | Usage | Transferases | Binding proteins | Health aspects | Tumors | Histone deacetylase | Transcription factors | Molecular structure | Transcription | Peptides | Androgen receptors | Amino acids | Event-related potentials | Selectivity | Catalytic activity | Kinases | Experiments | Crystallography | Proteins | CREB-binding protein | Castration | Xenografts | Coenzyme A | Acetylation | Catalysis | Inhibition | Crystal structure | Hematology | Feasibility studies | Cyclic AMP response element-binding protein | Histone acetyltransferase | Inhibitors | Microscopy | Natural products | Regulatory mechanisms (biology) | Epigenetics | Ligands | Prostate cancer | Prostate | Cancer | INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY
Journal Article
Chembiochem : a European journal of chemical biology, ISSN 1439-4227, 2017, Volume 18, Issue 16, pp. 1583 - 1588
Journal Article
Immunity (Cambridge, Mass.), ISSN 1074-7613, 2014, Volume 40, Issue 4, pp. 477 - 489
We identified three retinoid-related orphan receptor gamma t (RORγt)-specific inhibitors that suppress T helper 17 (Th17) cell responses, including... 
PATHWAYS | TARGET GENES | FOXP3 OCCUPANCY | T(H)17 | REGULATORY NETWORK | RECEPTOR | DIFFERENTIATION | IMMUNOLOGY | PSORIASIS | ANTI-INTERLEUKIN-17 MONOCLONAL-ANTIBODY | TH17 CELLS | Myelin-Oligodendrocyte Glycoprotein - immunology | T-Lymphocyte Subsets - immunology | Transcription, Genetic - drug effects | Nuclear Receptor Subfamily 1, Group F, Member 3 - antagonists & inhibitors | Humans | Transcriptional Activation - drug effects | Encephalomyelitis, Autoimmune, Experimental - immunology | Structure-Activity Relationship | Gene Regulatory Networks - drug effects | Cell Lineage - drug effects | Systems Biology | Benzhydryl Compounds - chemistry | Heterocyclic Compounds, 4 or More Rings - pharmacology | Th17 Cells - drug effects | T-Lymphocyte Subsets - drug effects | Peptide Fragments - immunology | Protein Binding - drug effects | Benzeneacetamides - chemistry | Benzeneacetamides - pharmacology | Nuclear Receptor Subfamily 1, Group F, Member 3 - genetics | Cytokines - metabolism | Encephalomyelitis, Autoimmune, Experimental - drug therapy | Mice, Inbred C57BL | Heterocyclic Compounds, 4 or More Rings - chemistry | Digoxin - chemistry | Digoxin - pharmacology | Mice, Knockout | Animals | Androstenols - chemistry | Cell Differentiation - drug effects | Cell Line, Tumor | Multiple Sclerosis - immunology | Th17 Cells - immunology | Benzhydryl Compounds - pharmacology | Mice | Multiple Sclerosis - drug therapy
Journal Article
Chembiochem : a European journal of chemical biology, ISSN 1439-7633, 2019, Volume 20, Issue 13, pp. 1712 - 1716
Journal Article
Cell cycle (Georgetown, Tex.), ISSN 1551-4005, 2014, Volume 12, Issue 3, pp. 452 - 462
...) proteins has recently emerged in hematological malignancies and chronic inflammation. We find that BET inhibitor compounds... 
I-BET151 | BRD2 | HIV | Tat | latency | MS417 | I-BET | JQ1 | P-TEFb | BRD4 | Latency | RNA-POLYMERASE-II | TRANSCRIPTION ELONGATION-FACTOR | DEPENDENT TRANSCRIPTION | HISTONE ACETYLATION | CELL BIOLOGY | IN-VITRO | T-CELL-ACTIVATION | POSTINTEGRATION LATENCY | NF-KAPPA-B | PCAF BROMODOMAIN | Transcription, Genetic - drug effects | Virus Latency | Humans | Positive Transcriptional Elongation Factor B - metabolism | Positive Transcriptional Elongation Factor B - genetics | Promoter Regions, Genetic - drug effects | Heterocyclic Compounds, 4 or More Rings - pharmacology | HIV-1 - physiology | RNA Interference | HEK293 Cells | Protein-Serine-Threonine Kinases - antagonists & inhibitors | CD4-Positive T-Lymphocytes - virology | Nuclear Proteins - genetics | Protein-Serine-Threonine Kinases - metabolism | Benzodiazepines - pharmacology | HIV-1 - drug effects | Jurkat Cells | tat Gene Products, Human Immunodeficiency Virus - genetics | HIV Infections - virology | Cells, Cultured | Protein-Serine-Threonine Kinases - genetics | Nuclear Proteins - metabolism | Transcription Factors - antagonists & inhibitors | Transcription Factors - genetics | HIV-1 - genetics | Azepines - pharmacology | Transcription Factors - metabolism | Triazoles - pharmacology | Nuclear Proteins - antagonists & inhibitors | RNA, Small Interfering | tat Gene Products, Human Immunodeficiency Virus - metabolism | Report
Journal Article
Journal Article
Science (American Association for the Advancement of Science), ISSN 1095-9203, 2003, Volume 299, Issue 5613, pp. 1743 - 1747
Journal Article
Cancer Chemotherapy and Pharmacology, ISSN 0344-5704, 12/2014, Volume 74, Issue 6, pp. 1125 - 1137
The aim of the study was to demonstrate the activity of etirinotecan pegol, a polymer conjugate of irinotecan, in multiple human tumor models and to establish... 
Medicine & Public Health | SN38 | Anticancer activity | Etirinotecan pegol | Oncology | Cancer Research | Pharmacology/Toxicology | Pharmacokinetics | Topoisomerase 1 inhibition | XENOGRAFT MODELS | IRINOTECAN CPT-11 | SOLID TUMORS | MULTICENTER PHASE-II | ANTICANCER AGENTS | OVARIAN-CANCER | METASTATIC COLORECTAL-CANCER | CELL LUNG-CANCER | BREAST-CANCER | 2 SCHEDULES | ONCOLOGY | PHARMACOLOGY & PHARMACY | Species Specificity | Humans | Male | Antineoplastic Agents - administration & dosage | Heterocyclic Compounds, 4 or More Rings - pharmacology | Neoplasms, Experimental - pathology | Topoisomerase I Inhibitors - pharmacology | Female | Antineoplastic Agents - pharmacokinetics | Antineoplastic Agents - pharmacology | Camptothecin - analogs & derivatives | Polyethylene Glycols - pharmacology | Heterocyclic Compounds, 4 or More Rings - administration & dosage | Topoisomerase I Inhibitors - pharmacokinetics | Topoisomerase I Inhibitors - administration & dosage | Polyethylene Glycols - pharmacokinetics | Rats | Treatment Outcome | Mice, SCID | Rats, Sprague-Dawley | Polyethylene Glycols - administration & dosage | Xenograft Model Antitumor Assays | Animals | Heterocyclic Compounds, 4 or More Rings - pharmacokinetics | Mice, Nude | Dogs | Mice | Camptothecin - pharmacology | Neoplasms, Experimental - drug therapy | Plasma physics | Polymers | Analysis | Lung cancer | Cancer | Original
Journal Article