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Journal of Medicinal Chemistry, ISSN 0022-2623, 07/2018, Volume 61, Issue 14, pp. 6110 - 6120
We report the structure-based discovery of CF53 (28) as a highly potent and orally active inhibitor of bromodomain and extra-terminal (BET) proteins. By the... 
CHEMISTRY, MEDICINAL | PROTEIN | CHROMATIN | TRANSCRIPTIONAL REGULATORS | ACETYLATION | TESTIS | CANDIDATE | IDENTIFICATION | RVX-208 | FAMILY | BRD4
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 12/2017, Volume 60, Issue 24, pp. 9990 - 10012
Upon the basis of The Cancer Genome Atlas (TCGA) data set, we identified that several autophagy-related proteins such as AMP-activated protein kinase (AMPK)... 
APOPTOSIS | CHEMISTRY, MEDICINAL | THERAPY | MODELS | HIGH-THROUGHPUT | DOCKING | LARGE GENE LISTS | RVX-208 | BINDING | BET BROMODOMAINS | Index Medicus
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 08/2019, Volume 29, Issue 16, pp. 2168 - 2172
Bromodomain-containing protein 4 (BRD4) is a new therapeutic target for the treatment of diseases including cardiovascular diseases, cancer, inflammation and... 
Phenoxyacetic derivatives | Dual-active | RVX-208 | BRD4 inhibitor | Hyperlipoidemia | VITRO | CHEMISTRY, MEDICINAL | CHOLESTEROL | ATHEROSCLEROSIS | PREVENTION | CHEMISTRY, ORGANIC | RISK | HDL | REDUCTION | DISEASE | APOLIPOPROTEIN-A-I | Medical research | Biological products | Analysis | Therapeutics | Medicine, Experimental | Biomedical engineering | Homeopathy | Materia medica and therapeutics | Index Medicus
Journal Article
Atherosclerosis, ISSN 0021-9150, 2016, Volume 247, pp. 48 - 57
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 | Index Medicus
Journal Article
Journal Article
Journal of Neuroinflammation, ISSN 1742-2094, 01/2017, Volume 14, Issue 1, pp. 14 - 14
Background: The bromodomain and extraterminal domain (BET) family proteins (BET2, BET3, and BET4) "read" (bind) histone acetylation marks via two distinct... 
Retinal degeneration | Bromodomain and extraterminal domain (BET) proteins | JQ1 | Rd10 mice | Epigenetic readers | Microglial activation | ACTIVATION | TRANSCRIPTION | MECHANISMS | IMMUNOLOGY | SUPPRESSION | ENHANCERS | RVX-208 | NEUROSCIENCES | rd10 mice | INFLAMMATION | NEURONS | INHIBITOR | SELECTIVITY | Epigenetic inheritance | Genetic aspects | Research | Index Medicus
Journal Article
Journal of Cellular Biochemistry, ISSN 0730-2312, 08/2017, Volume 118, Issue 8, pp. 2161 - 2167
In HepG2 cells, the ER‐stress mediated reduction in apoA‐I transcription is partly mediated via the inhibition of PPARα mRNA expression and activity. In... 
PEROXISOME PROLIFERATOR‐ACTIVATED RECEPTOR (PPAR) ALPHA | BROMODOMAIN AND EXTRA‐TERMINAL (BET) PROTEIN INHIBITION | ENDOPLASMIC RETICULUM STRESS (ER‐STRESS) | APOLIPOPROTEIN A‐I (apoA‐I) | TRANSCRIPTION | APOLIPOPROTEIN A-I (apoA-I) | BROMODOMAIN AND EXTRA-TERMINAL (BET) PROTEIN INHIBITION | ENDOPLASMIC RETICULUM STRESS (ER-STRESS) | PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR (PPAR) ALPHA | SMALL-MOLECULE | BIOCHEMISTRY & MOLECULAR BIOLOGY | ENDOPLASMIC-RETICULUM STRESS | RVX-208 | SIRT1 | DISCOVERY | CELL BIOLOGY | REDUCTION | INSULIN-RESISTANCE | DISEASE | BROMODOMAIN INHIBITION | HEPATIC STEATOSIS | Humans | PPAR alpha - genetics | Kelch-Like ECH-Associated Protein 1 - metabolism | Apolipoprotein A-I - metabolism | Endoplasmic Reticulum Stress - genetics | RNA, Messenger - metabolism | Blotting, Western | Hep G2 Cells | Kelch-Like ECH-Associated Protein 1 - genetics | Proteins - genetics | Apolipoprotein A-I - genetics | Proteins - metabolism | PPAR alpha - metabolism | Endoplasmic Reticulum Stress - physiology | RNA | Apolipoproteins | Genetic transcription | Stresses | Markers | Biochemistry | Gene expression | Stress | Western blotting | Thapsigargin | Apolipoprotein A | Inhibitors | Apolipoprotein A-I | Links | Peroxisome proliferator-activated receptors | Inhibition | Endoplasmic reticulum | Activation analysis | Index Medicus
Journal Article
Kidney and Blood Pressure Research, ISSN 1420-4096, 06/2018, Volume 43, Issue 2, pp. 449 - 457
Journal Article
Data in Brief, ISSN 2352-3409, 09/2016, Volume 8, pp. 1280 - 1288
Apabetalone (RVX-208) inhibits the interaction between epigenetic regulators known as bromodomain and extraterminal (BET) proteins and acetyl-lysine marks on... 
BET proteins | ApoA-I | African green monkey | Microarrays | Apolipoprotein A-I | Bromodomain | BET inhibitor | JQ1 | Vascular inflammation | RVX-208 | Primary human hepatocytes | Gene expression
Journal Article