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Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 8/2015, Volume 112, Issue 34, pp. 10768 - 10773
Th17 responses are critical to a variety of human autoimmune diseases, and therapeutic targeting with monoclonal antibodies against IL-17 and IL-23 has shown... 
Epigenetic inhibitors | Bromodomain | Th17 | CBP/p300 | Ankylosing spondylitis | RHEUMATOID-ARTHRITIS | CELLS | epigenetic inhibitors | EFFICACY | P300 | MULTIDISCIPLINARY SCIENCES | ankylosing spondylitis | CRYSTALLOGRAPHY | ANKYLOSING-SPONDYLITIS | BINDING PROTEIN | bromodomain | LIGANDS | DOUBLE-BLIND | BET BROMODOMAINS | p300-CBP Transcription Factors - antagonists & inhibitors | Humans | Middle Aged | Crystallography, X-Ray | Male | Structure-Activity Relationship | Benzimidazoles - chemistry | Th17 Cells - drug effects | Arthritis, Psoriatic - pathology | Adult | Female | Molecular Structure | Drug Evaluation, Preclinical | Immunosuppressive Agents - pharmacology | Arthritis, Psoriatic - metabolism | Recombinant Proteins - metabolism | Interleukin-17 - secretion | CD4-Positive T-Lymphocytes - metabolism | Cells, Cultured | Interleukin-17 - genetics | Models, Molecular | Interleukin-17 - biosynthesis | Isoxazoles - chemistry | Spondylitis, Ankylosing - metabolism | Azepines - pharmacology | Gene Expression Regulation - drug effects | Isoxazoles - pharmacology | Triazoles - pharmacology | Th17 Cells - immunology | Benzimidazoles - pharmacology | Calorimetry | Protein Conformation | Aged | Kinetics | Spondylitis, Ankylosing - pathology | CD4-Positive T-Lymphocytes - drug effects | Immunosuppressive Agents - chemistry | Protein Structure, Tertiary - drug effects | Immune response | Development and progression | Genetic aspects | Genetic transcription | Binding proteins | Properties | Autoimmune diseases | Health aspects | CBP | p300 | Biological Sciences
Journal Article
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 02/2016, Volume 59, Issue 4, pp. 1271 - 1298
Bromodomains, small protein modules that recognize acetylated lysine on histones, play a significant role in the epigenome, where they function as "readers"... 
CHEMISTRY, MEDICINAL | SWI/SNF COMPLEXES | SMALL-MOLECULE INHIBITORS | PROSTATE-CANCER | SELECTIVE INHIBITORS | GENE-EXPRESSION | CHEMICAL PROBE | TUMOR-SUPPRESSOR | BET INHIBITORS | HISTONE ACETYLTRANSFERASE | PHD FINGER | Small Molecule Libraries - pharmacology | Antigens, Nuclear - metabolism | Humans | Drug Discovery - methods | CREB-Binding Protein - antagonists & inhibitors | Chromosomal Proteins, Non-Histone - antagonists & inhibitors | DNA-Binding Proteins - metabolism | CREB-Binding Protein - metabolism | Protein Processing, Post-Translational - drug effects | Adaptor Proteins, Signal Transducing - antagonists & inhibitors | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Lysine - metabolism | Protein-Serine-Threonine Kinases - metabolism | RNA-Binding Proteins - antagonists & inhibitors | Nerve Tissue Proteins - antagonists & inhibitors | ATPases Associated with Diverse Cellular Activities | DNA-Binding Proteins - antagonists & inhibitors | Chromosomal Proteins, Non-Histone - metabolism | Carrier Proteins - antagonists & inhibitors | Adenosine Triphosphatases - metabolism | Models, Molecular | Nuclear Proteins - metabolism | Transcription Factors - antagonists & inhibitors | Nerve Tissue Proteins - metabolism | Transcription Factors - metabolism | Adenosine Triphosphatases - antagonists & inhibitors | DNA Helicases - metabolism | Small Molecule Libraries - chemistry | Acetylation - drug effects | Animals | Carrier Proteins - metabolism | Nuclear Proteins - antagonists & inhibitors | DNA Helicases - antagonists & inhibitors | Histones - metabolism | Adaptor Proteins, Signal Transducing - metabolism | RNA-Binding Proteins - metabolism
Journal Article
Current Opinion in Chemical Biology, ISSN 1367-5931, 08/2016, Volume 33, pp. 58 - 66
Journal Article
Journal Article
Journal Article
Leukemia, ISSN 0887-6924, 09/2017, Volume 31, Issue 9, pp. 1951 - 1961
The PROTAC (proteolysis-targeting chimera) ARV-825 recruits bromodomain and extraterminal (BET) proteins to the E3 ubiquitin ligase cereblon, leading to... 
TRANSFORMATION | PATHOGENESIS | JAK2 INHIBITOR | ONCOLOGY | ACUTE MYELOGENOUS LEUKEMIA | KINASE | DEGRADATION | ACUTE MYELOID-LEUKEMIA | OVERCOMES RESISTANCE | HEMATOLOGY | CANCER | BRD4 | Antigens, CD34 | Apoptosis - drug effects | Leukemia, Myeloid, Acute - pathology | Humans | Leukemia | Ubiquitin-Protein Ligases - metabolism | Nuclear Proteins - metabolism | Myeloproliferative Disorders - pathology | Thalidomide - pharmacology | Azepines - therapeutic use | Azepines - pharmacology | Transcription Factors - metabolism | Thalidomide - analogs & derivatives | Animals | Tumor Burden - drug effects | Proteolysis | Cell Line, Tumor | Leukemia, Myeloid, Acute - drug therapy | Mice | Thalidomide - therapeutic use | Chimera | Pyrazoles - pharmacology | Care and treatment | Usage | Messenger RNA | Chimeras (Organisms) | Research | Mass spectrometry | Myeloproliferative disorders | Ubiquitin | Surgical implants | c-Myc protein | In vitro testing | mRNA | Myc protein | Cyclin-dependent kinase 4 | Degradation | Proteins | Biomedical materials | Bcl-x protein | Janus kinase 2 | Biocompatibility | Ubiquitin-protein ligase | CD34 antigen | Cell survival | Stat3 protein | Hemopoiesis | Cytometry | Protein arrays | Depletion | Inhibitors | Ribonucleic acids | Cells (biology) | Bcl protein | Bet protein | In vivo methods and tests | Acute myeloid leukemia | Apoptosis | Secondary AML | PROTAC | protein degradation
Journal Article
Journal Article
Atherosclerosis, ISSN 0021-9150, 2014, Volume 236, Issue 1, pp. 91 - 100
Abstract Despite the benefit of statins in reducing cardiovascular risk, a sizable proportion of patients still remain at risk. Since HDL reduces CVD risk... 
Cardiovascular | apoE deficient | Preβ-HDL | Atherosclerosis | Inflammation | BET inhibitor | apoA-I-inducer | RVX-208 | ApoE deficient | ApoA-I-inducer | C-REACTIVE PROTEIN | CARDIAC & CARDIOVASCULAR SYSTEMS | RISK-FACTORS | PRIMARY-PREVENTION TRIAL | HIGH-DENSITY-LIPOPROTEIN | HEART-DISEASE | SCAVENGER RECEPTOR | REVERSE CHOLESTEROL TRANSPORT | CARDIOVASCULAR-DISEASE | Pre beta-HDL | PERIPHERAL VASCULAR DISEASE | CORONARY-ARTERY-DISEASE | APOLIPOPROTEIN-A-I | Hyperlipidemias - genetics | Endothelial Cells | Hyperlipidemias - blood | Apolipoproteins E - deficiency | Humans | Aortic Diseases - blood | RNA, Messenger - analysis | Male | Gene Expression Profiling | Aorta - metabolism | Inflammation - blood | Atherosclerosis - etiology | Liver - drug effects | U937 Cells | Aortic Diseases - prevention & control | Betaine-Homocysteine S-Methyltransferase - antagonists & inhibitors | Cholesterol, LDL - blood | Hyperlipidemias - diet therapy | Drug Evaluation, Preclinical | Hyperlipidemias - complications | Aortic Diseases - pathology | Cytokines - blood | Cell Line | Atherosclerosis - pathology | Aorta - drug effects | Hyperlipidemias - drug therapy | Liver - metabolism | Mice, Inbred C57BL | Diet, Western - adverse effects | Mice, Knockout | Aorta - pathology | Atherosclerosis - blood | Animals | Quinazolines - therapeutic use | Diet, Fat-Restricted | Cholesterol, HDL - blood | Inflammation - prevention & control | Mice | Quinazolines - pharmacology | Aortic Diseases - etiology | Atherosclerosis - prevention & control | Apolipoprotein A-I - blood | Haptoglobin | Apolipoproteins | Low density lipoproteins | Statins | Protein binding | Triglycerides | Interferon | Cardiovascular agents
Journal Article
Journal Article