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Journal of Medicinal Chemistry, ISSN 0022-2623, 10/2018, Volume 61, Issue 20, pp. 9316 - 9334
As regulators of transcription, epigenetic proteins that interpret post-translational modifications to N-terminal histone tails are essential for maintaining... 
CELLS | THERMAL SHIFT ASSAY | DESIGN | CHEMISTRY, MEDICINAL | OBSERVED FLUORINE NMR | PROTEIN | DISRUPTION | INFLAMMATION | KAPPA-B | HOLE APPROACH | BET BROMODOMAINS
Journal Article
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 2014, Volume 20, Issue 4, pp. 912 - 925
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 05/2017, Volume 27, Issue 10, pp. 2225 - 2233
Journal Article
Journal of the American Chemical Society, ISSN 0002-7863, 07/2014, Volume 136, Issue 26, pp. 9308 - 9319
Journal Article
Journal Article
Cancer Discovery, ISSN 2159-8274, 03/2013, Volume 3, Issue 3, pp. 309 - 323
Bromodomain inhibition comprises a promising therapeutic strategy in cancer, particularly for hematologic malignancies. To date, however, genomic biomarkers to... 
ANAPLASTIC LYMPHOMA KINASE | CELL LUNG-CANCER | DRUG-SENSITIVITY | ONCOLOGY | ACUTE LYMPHOBLASTIC-LEUKEMIA | THERAPEUTIC TARGET | N-MYC | C-MYC | ALK KINASE | ACUTE MYELOID-LEUKEMIA | ACTIVATING MUTATIONS | Oncogene Proteins - genetics | RNA, Small Interfering - genetics | Apoptosis - drug effects | Humans | Transcription Factors - deficiency | Apoptosis - genetics | Molecular Targeted Therapy | Transfection | Nuclear Proteins - deficiency | Cell Cycle Checkpoints - genetics | Female | N-Myc Proto-Oncogene Protein | Cell Growth Processes - genetics | Nuclear Proteins - genetics | Child | Neuroblastoma - pathology | Protein Structure, Tertiary | Promoter Regions, Genetic | Neuroblastoma - genetics | Oncogene Proteins - metabolism | Nuclear Proteins - metabolism | Transcription Factors - antagonists & inhibitors | Transcription Factors - genetics | Down-Regulation - drug effects | Azepines - pharmacology | Transcription Factors - metabolism | Triazoles - pharmacology | Xenograft Model Antitumor Assays | Animals | Gene Amplification | Cell Cycle Checkpoints - drug effects | Neuroblastoma - drug therapy | Nuclear Proteins - antagonists & inhibitors | Cell Line, Tumor | Mice | Neuroblastoma - metabolism | Proto-Oncogene Proteins c-myc - genetics | RNA, Small Interfering - administration & dosage | Index Medicus | neuroblastoma | BET bromodomain inhibitor | MYCN | JQ1 | BRD4
Journal Article
Molecular Cell, ISSN 1097-2765, 02/2019, Volume 73, Issue 3, pp. 621 - 638.e17
Targeting bromodomains (BRDs) of the bromo-and-extra-terminal (BET) family offers opportunities for therapeutic intervention in cancer and other diseases.... 
BET | bromodomain | protein crystallography | rRNA | nucleolus | proteomic network | JQ1 | rewiring | AP-MS | KacY | SELECTIVE-INHIBITION | PROTEIN | CHROMATIN | RECOGNITION | MECHANISM | EXTRATERMINAL DOMAIN | BIOCHEMISTRY & MOLECULAR BIOLOGY | TRANSCRIPTION | AFFINITY PURIFICATION | P-TEFB | BRD4 | CELL BIOLOGY | Neoplasms - metabolism | RNA-Binding Proteins - genetics | Protein Interaction Maps - drug effects | Triazoles - chemistry | Humans | Gene Expression Regulation, Neoplastic | Structure-Activity Relationship | Azepines - chemistry | Neoplasms - genetics | HEK293 Cells | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Antineoplastic Agents - pharmacology | Protein Interaction Domains and Motifs | Proteomics - methods | Nuclear Proteins - genetics | Molecular Targeted Therapy - methods | Protein-Serine-Threonine Kinases - metabolism | RNA-Binding Proteins - antagonists & inhibitors | Protein-Serine-Threonine Kinases - genetics | Models, Molecular | Nuclear Proteins - metabolism | Transcription Factors - antagonists & inhibitors | Transcription Factors - genetics | Antineoplastic Agents - chemistry | Neoplasms - drug therapy | Azepines - pharmacology | Transcription Factors - metabolism | Triazoles - pharmacology | Signal Transduction - drug effects | Nuclear Proteins - antagonists & inhibitors | K562 Cells | Protein Binding | Protein Conformation | Cell Proliferation - drug effects | HeLa Cells | Neoplasms - pathology | RNA-Binding Proteins - metabolism | Proteins | Yuan (China) | RNA | Gene expression | Index Medicus
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 | Index Medicus | Secondary AML | PROTAC | protein degradation
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 01/2015, Volume 21, Issue 1, pp. 4 - 6
Journal Article
Journal Article