Bromodomain inhibitors
Clinical progress and pharmacology of small molecule bromodomain inhibitors
... BET bromodomain inhibition has led to the instigation of multiple human clinical trials with small molecule BET bromodomain ...BET bromodomain inhibitors for treating human disease will be ...
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BET bromodomain inhibitors suppress EWS-FLI1-dependent transcription and the IGF1 autocrine mechanism in Ewing sarcoma
... the bromodomain and extra-terminal domain (BET) family ...BET bromodomain inhibitors have exhibited promising antineoplastic activities via suppression of oncogenic transcription factors in various ...
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Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching
... specific bromodomain-containing protein remains unknown. In addition, bromodomain-containing proteins have been implicated in a wide range of ...respectively. Bromodomain-containing proteins have ...
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SMAC mimetic Debio 1143 synergizes with taxanes, topoisomerase inhibitors and bromodomain inhibitors to impede growth of lung adenocarcinoma cells
... topoisomerase inhibitors, and bromodomain inhibitors, super-additively inhibited growth and clonogenicity of lung adenocarcinoma ...the bromodomain inhibitor JQ1 suppresses the expression of ...
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BET bromodomain inhibitors and agonists of the beta-2 adrenergic receptor identified in screens for compounds that inhibit DUX4 expression in FSHD muscle cells
... In addition, the conclusion that these compounds are acting as beta-2 agonists to inhibit DUX4 levels was further supported by several other observations: (1) a beta-3 selective adrenerg[r] ...
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Drug Repurposing of Bromodomain Inhibitors as Potential Novel Therapeutic Leads for Lymphatic Filariasis Guided by Multispecies Transcriptomics
... samples. Bromodomain-containing proteins interact with chromatin remodeling com- plexes to regulate transcription or to facilitate DNA repair protein accessibility (40), leading to their study in cancer biology as ...
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Targeting MYC activity in double-hit lymphoma with MYC and BCL2 and/or BCL6 rearrangements with epigenetic bromodomain inhibitors
... Effect of BET inhibitors on survival of DHL and THL cells We extended the study of BET inhibition to examine the effect on survival of DHL/THL DLBCL cell lines. DLBCL cell lines expressing WT-MYC (U2932), SH ...
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BET Bromodomain Inhibition as a Therapeutic Strategy in Ovarian Cancer by Downregulating FoxM1
... the bromodomain and extraterminal domain (BET) protein BRD4 as a potential therapeutic target in ovarian ...BET inhibitors JQ1 and I-BET151, or dual kinase-bromodomain inhibitor vo- lasertib, led to ...
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Enhanced efficacy of histone deacetylase inhibitor combined with bromodomain inhibitor in glioblastoma
... Bromodomain inhibitors exert biological effects by dis- lodging the acetylated histone readers BRD3 and BRD4 from chromatin, leading to the transcriptional repression of oncogenes ...HDAC inhibitors ...
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Antiinflammatory effects of bromodomain and extraterminal domain inhibition in cystic fibrosis lung inflammation
... BET bromodomain inhibitor derived from JQ1, anoth- er well-characterized BET bromodomain ...selective inhibitors with no known off target effects at biologically relevant concentrations and even at ...
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CBP bromodomain TR-FRET Assay Kit
... molecule bromodomain inhibitors have focused on the BET family of proteins, a class of proteins that contain tandem bromodomains and an Extra Terminal ...
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The bromodomain inhibitor N-methyl pyrrolidone reduced fat accumulation in an ovariectomized rat model
... affinity bromodomain inhibitor for BRD2, BRD3, BRD4, and BRDT and has potential for osteoporosis treatment ...by bromodomain inhibitors JQ1 and NMP, as shown here, prevents transcriptional activation ...
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Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain
... The fragment-based approach coupled with structural informa- tion presented here o ff ers a platform expanding the knowledge on PCAF Kac-mimetic sca ff olds and binding modes to aid development of potent and selective PCAF ...
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Selective inhibition of BET bromodomain epigenetic signalling interferes with the bone-associated tumour vicious cycle
... BET bromodomain signalling plays a role in osteosarcoma and that inhibition of this epigenetic recognition pathway suppresses osteosarcoma tumour growth both in vitro and in ...BET bromodomain signalling ...
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Inhibitors of Tyrosinase
... This suggests that the 'skins' are richer in both enzyme and aromatic substrate, and that the extended oxygen consumption sometimes shown by the 'blood and guts' is due to the presence o[r] ...
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Function of Bromodomain and Extra-Terminal Motif Proteins (bets) in Gata1-Mediated Transcription
... previous cell cycle (John & Workman, 1998; Michelotti, Sanford, & Levens, 1997). DNA methylation and some histone modifications remain largely unchanged during mitosis and may also function in mitotic memory of ...
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Original Article Bromodomain 4 protein is a predictor of survival for urothelial carcinoma of bladder
... In the present study, we found the expression level of BRD4 in nucleus was significantly asso- ciated with histological grade (P < 0.001), lymph node metastasis (P < 0.001) and distant metastasis (P < 0.001). It ...
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Bromodomain-containing protein 7 (BRD7) as a potential tumor suppressor in hepatocellular carcinoma
... Bromodomain-containing protein 7 (BRD7) is a subunit of the PBAF complex, which functions as a transcriptional cofactor for the tumor suppressor protein p53. Down-regulation of BRD7 has been demonstrated in ...
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Screening of protein kinase inhibitors identifies PKC inhibitors as inhibitors of osteoclastic acid secretion and bone resorption
... Furthermore, the discrepancies between acid influx and acidification in intact osteoclasts are not fully clear yet. Some of the inhibitors are effective inhibitors of bone resorption and acid influx, but ...
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Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites
... potent inhibitors, sparking an interest in protein − protein interaction inhibitors that directly target gene ...the bromodomain family using SiteMap and show that there are signi fi cant di ff erences ...
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