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Nature Medicine, ISSN 1078-8956, 09/2017, Volume 23, Issue 9, pp. 1055 - 1062
Bromodomain and extraterminal domain (BET) protein inhibitors are emerging as promising anticancer therapies. The gene encoding the E3 ubiquitin ligase... 
SELECTIVE-INHIBITION | TARGET | MEDICINE, RESEARCH & EXPERIMENTAL | ANDROGEN RECEPTOR | STEM-CELLS | BIOCHEMISTRY & MOLECULAR BIOLOGY | ACUTE MYELOID-LEUKEMIA | ENHANCERS | CELL BIOLOGY | RNA-SEQ | BROMODOMAIN INHIBITION | MUTATIONS | BRD4 | Prostatic Neoplasms - metabolism | Immunoprecipitation | TOR Serine-Threonine Kinases - metabolism | Humans | Drug Resistance, Neoplasm | Male | Gene Expression Profiling | Molecular Targeted Therapy | Mechanistic Target of Rapamycin Complex 1 | Transcription Factors - drug effects | Multiprotein Complexes - metabolism | Prostatic Neoplasms - genetics | Proteasome Endopeptidase Complex - drug effects | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Nuclear Proteins - drug effects | Nuclear Proteins - genetics | Proto-Oncogene Proteins c-akt - metabolism | TOR Serine-Threonine Kinases - drug effects | Multiprotein Complexes - drug effects | Prostatic Neoplasms - drug therapy | Protein-Serine-Threonine Kinases - metabolism | Repressor Proteins - metabolism | RNA-Binding Proteins - antagonists & inhibitors | Triazoles - therapeutic use | Cell Survival | Repressor Proteins - genetics | Nuclear Proteins - metabolism | Transcription Factors - antagonists & inhibitors | Reverse Transcriptase Polymerase Chain Reaction | Blotting, Western | Azepines - therapeutic use | RNA-Binding Proteins - drug effects | Azepines - pharmacology | Transcription Factors - metabolism | Triazoles - pharmacology | Nuclear Proteins - antagonists & inhibitors | Protein-Serine-Threonine Kinases - drug effects | Cell Line, Tumor | Cell Proliferation - drug effects | Mutation | RNA-Binding Proteins - metabolism | rac1 GTP-Binding Protein - metabolism | Proto-Oncogene Proteins c-akt - drug effects | rac1 GTP-Binding Protein - genetics | Gene mutations | Physiological aspects | Genetic aspects | Research | Drug resistance | Drug therapy | Prostate cancer | Ubiquitin | Inhibitor drugs | Stabilization | AKT protein | Activation | Biosynthesis | Degradation | Proteins | Ubiquitination | Transcription activation | Bioindicators | Ubiquitin-protein ligase | Binding | Rac1 protein | Tumor cell lines | Gene expression | Cholesterol | Mutants | Inhibitors | Proteasomes | Biomarkers | Bet protein | Prostate | Cancer | Guanosinetriphosphatase
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
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
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
Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 01/2019, Volume 116, Issue 2, pp. 619 - 624
Ovarian cancer remains the most lethal gynecologic malignancy. We analyzed the mutational landscape of 64 primary, 41 metastatic, and 17 recurrent fresh-frozen... 
Ovarian carcinoma | Whole-exome sequencing | BET inhibitors | Bilateral ovarian tumors | PIK3CA | COPY-NUMBER | MULTIDISCIPLINARY SCIENCES | ovarian carcinoma | whole-exome sequencing | bilateral ovarian tumors | Class I Phosphatidylinositol 3-Kinases - genetics | Class I Phosphatidylinositol 3-Kinases - metabolism | Humans | Neoplasm Recurrence, Local - drug therapy | Tumor Suppressor Protein p53 - genetics | Neoplasm Metastasis | BRCA1 Protein - metabolism | Female | Antineoplastic Agents - pharmacology | Ovarian Neoplasms | Neoplasm Recurrence, Local - metabolism | Tumor Suppressor Protein p53 - metabolism | Proto-Oncogene Proteins c-myc - metabolism | Azepines - pharmacology | Proteins - genetics | Triazoles - pharmacology | Xenograft Model Antitumor Assays | BRCA1 Protein - genetics | Animals | BRCA2 Protein - metabolism | Proteins - metabolism | Cell Line, Tumor | Neoplasm Recurrence, Local - genetics | Mice | Proto-Oncogene Proteins c-myc - genetics | Mutation | Proteins - antagonists & inhibitors | BRCA2 Protein - genetics | Relapse | Genetic aspects | Metastasis | Health aspects | Mutation (Biology) | Ovarian cancer | Cancer | p53 Protein | Genes | Xenotransplantation | c-Myc protein | Malignancy | Myc protein | Metastases | Gene sequencing | Xenografts | Evolution | Deoxyribonucleic acid--DNA | Nucleotide sequence | BRCA1 protein | Therapeutic applications | Gynecology | Breast cancer | Patients | Amplification | Chemotherapy | Inhibitors | Cell lines | Gain | DNA sequencing | Tumors | Biological Sciences
Journal Article
Journal of Biological Chemistry, ISSN 0021-9258, 2017, Volume 292, Issue 32, pp. 13284 - 13295
Lytic infection by the Epstein-Barr virus (EBV) poses numerous health risks, such as infectious mononucleosis and lymphoproliferative disorder. Proteins in the... 
HOST MITOTIC CHROMOSOMES | HERPESVIRUS | ACTIVATION | HIV | VIRAL-DNA | REACTIVATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | PAPILLOMAVIRUS E2 PROTEIN | LATENCY | EXPRESSION | BRD4 | Gene Expression Regulation, Viral - drug effects | Basic-Leucine Zipper Transcription Factors - metabolism | Transcription Factors - chemistry | Humans | Herpesvirus 4, Human - drug effects | Host-Pathogen Interactions - drug effects | Protein Transport - drug effects | Trans-Activators - chemistry | Fanconi Anemia Complementation Group Proteins - chemistry | Viral Proteins - metabolism | Fanconi Anemia Complementation Group Proteins - metabolism | RNA Interference | Trans-Activators - genetics | Lysine - metabolism | Protein Interaction Domains and Motifs | Acetylation | Basic-Leucine Zipper Transcription Factors - antagonists & inhibitors | Nuclear Proteins - genetics | Cell Line | Antiviral Agents - pharmacology | Fanconi Anemia Complementation Group Proteins - antagonists & inhibitors | Viral Proteins - chemistry | Herpesvirus 4, Human - physiology | Fanconi Anemia Complementation Group Proteins - genetics | Viral Proteins - genetics | Nuclear Proteins - metabolism | Transcription Factors - antagonists & inhibitors | Viral Proteins - antagonists & inhibitors | Basic-Leucine Zipper Transcription Factors - genetics | Transcription Factors - genetics | Nuclear Proteins - chemistry | Azepines - pharmacology | Replication Origin - drug effects | Transcription Factors - metabolism | Triazoles - pharmacology | Virus Activation - drug effects | Basic-Leucine Zipper Transcription Factors - chemistry | Nuclear Proteins - antagonists & inhibitors | Trans-Activators - metabolism | Protein Processing, Post-Translational | Virus Physiological Phenomena - drug effects | Trans-Activators - antagonists & inhibitors | bromodomain-containing protein 4 (BRD4) | DNA replication | Microbiology | transcription | herpesvirus | Epstein-Barr virus | JQ1 | chromatin | BET inhibitors
Journal Article
Journal Article
Proteins: Structure, Function, and Bioinformatics, ISSN 0887-3585, 02/2013, Volume 81, Issue 2, pp. 300 - 315
Polcalcins are small EF‐hand proteins believed to assist in regulating pollen‐tube growth. Phl p 7, from timothy grass (Phleum pratense), crystallizes as a... 
protein structure | EF‐hand protein | NMR | polcalcin | protein‐ligand interaction | Ca2+‐binding protein | Polcalcin | Protein structure | Protein-ligand interaction | EF-hand protein | binding protein | MAGNETIC-RESONANCE RELAXATION | RAT ALPHA-PARVALBUMIN | BIOCHEMISTRY & MOLECULAR BIOLOGY | Ca2+-binding protein | LARGER PROTEINS | ROTATIONAL DIFFUSION | MODEL-FREE APPROACH | BIRCH POLLEN ALLERGEN | BET V 4 | BIOPHYSICS | protein-ligand interaction | SIDE-CHAIN RESONANCES | SEQUENTIAL ASSIGNMENT | CALCIUM-BINDING PROTEIN | Apoproteins - chemistry | Calcium-Binding Proteins - chemistry | Calcium-Binding Proteins - metabolism | Cations, Divalent - chemistry | Recombinant Proteins - metabolism | Amino Acid Sequence | EF Hand Motifs | Calcium - metabolism | Models, Molecular | Molecular Sequence Data | Recombinant Proteins - chemistry | Magnesium - metabolism | Antigens, Plant - chemistry | Calcium - chemistry | Solutions - chemistry | Magnesium - chemistry | Sequence Alignment | Plant Proteins - chemistry | Cations, Divalent - metabolism | Antigens, Plant - metabolism | Nuclear Magnetic Resonance, Biomolecular | Protein Binding | Plant Proteins - metabolism | Apoproteins - metabolism | Aspartate | Surface active agents | Structure | Recombinant proteins | Crystals | Protein binding | Proteins | Ligands | Crystal structure
Journal Article