Bromodomain inhibitor
Enhanced efficacy of histone deacetylase inhibitor combined with bromodomain inhibitor in glioblastoma
... In one of our previous studies, we have shown that panobinsotat levels could achieved 200 nM in the brain following a single 20 mg/kg intraperitoneal (i.p.) dose [36]. Panobinostat also has been tested in clinical II ...
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The BET bromodomain inhibitor exerts the most potent synergistic anticancer effects with quinone-containing compounds and anti- microtubule drugs
... BET bromodomain inhibitors are very promising novel anticancer agents, however, single therapy does not cause tumor regression in mice, suggesting the need for combination ...BET bromodomain ...
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Small molecule inhibitor screen identifies synergistic activity of the bromodomain inhibitor CPI203 and bortezomib in drug resistant myeloma
... A bromodomain inhibitor was among the compounds that showed particular promise in the drug resistant cell lines and therefore was the focus of our follow-up ...code”. Bromodomain (BRD)-containing ...
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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 ...modomain inhibitor targeting BRD2, BRD3, BRDT, and preferentially BRD4 ...by ...
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Therapeutic efficacy of the bromodomain inhibitor OTX015/ MK-8628 in ALK-positive anaplastic large cell lymphoma: an alternative modality to overcome resistant phenotypes
... To broaden our knowledge of the mechanism of action of OTX015, we performed a gene expression profiling (GEP) study on three ALCL cell lines (L82, SUDHL1, Karpas299) exposed to DMSO or OTX015 (500 nM) for 2, 4, 8 or 12 ...
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MYCL is a target of a BET bromodomain inhibitor, JQ1, on growth suppression efficacy in small cell lung cancer cells
... BET bromodomain inhibitors other than JQ1 has been used in clinical trials in solid tumors ...BET bromodomain inhibitors as well as CDK6 inhibitors for SCLC ...
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BET bromodomain inhibitor birabresib in mantle cell lymphoma: in vivo activity and identification of novel combinations to overcome adaptive resistance
... BET inhibitor as a single ...BET inhibitor birabresib in combination with the MEK inhibitor pimasertib, the SRC kinase inhibitor dasatinib, the FGRF inhibitor PD173074, the ATR ...
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The BET bromodomain inhibitor, JQ1, facilitates c-FLIP degradation and enhances TRAIL-induced apoptosis independent of BRD4 and c-Myc inhibition
... We found that c-Myc siRNA effectively decreased c-Myc expression, but failed to prevent c-FLIP reduction induced by JQ1 although the basal levels of c-FLIP were elevated by c-Myc knockdo[r] ...
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Progress in the development of non-BET bromodomain chemical probes
... full-length bromodomain proteins that bound to the immobilsed compound, only BAZ2A and BAZ2B displayed a dose-dependent reduction in the presence of GSK2801 ...BAZ2A/B bromodomain inhibitor in ...
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CREBBP/EP300 bromodomains are critical to sustain the GATA1/MYC regulatory axis in proliferation
... Bromodomains are attractive targets due to their drug- gability [21]. However, it is also known that a potential complication of bromodomain inhibitor development is promiscuity among different ...
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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 ...kinase-bromodomain inhibitor vo- lasertib, led to robust and broad antitumor effects across ...
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Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia (AML)
... ‘reader’ Bromodomain-containing 4 Protein (BRD4) as a new potential target in AML ...BET bromodomain inhibitor that blocks BRD4-binding to acetylated histones, showed profound antileukemic effects in ...
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The first bromodomain of Brdt, a testis specific member of the BET sub family of double bromodomain containing proteins, is essential for male germ cell differentiation
... Finally, it is of great interest to note that there are concurrent studies that suggest a role for BRDT during human spermatogenesis as well. It should be recalled that this member of the BET sub-family was actually ...
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Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer.
... BET inhibitor silences c-Myc expression and downstream pathways in prostate cancer cell lines is consistent with a previous report ...BET inhibitor treatment decreases MYC expression only in a subset of ...
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Bromo- and Extraterminal Domain Chromatin Regulators Serve as Cofactors for Murine Leukemia Virus Integration
... proteins (37). Five mammalian BET family members are known: BRD2/RING3, BRD3/ORFX, BRD4 (includes two splice variants, a short variant termed BRD4/HUNK-1 and a long variant, BRD4/ MCAP), and BRD6/BRDT (specifically ...
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Bromodomain and extra-terminal domain (BET) proteins regulate melanocyte differentiation
... acetylated, there are several lysine residues upstream of the basic helix loop helix domain that are predicted to be acetylation sites [65]. These are in regions of MITF that modulate its localization to the nucleus [65, ...
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Immunogenicity of prostate cancer is augmented by BET bromodomain inhibition
... Taken together, these data demonstrate the activity of anti-CTLA-4 and BET bromodomain inhibition in a mur- ine prostate cancer model. Previous work in a murine lymphoma model showed a similar decrease in PD-L1 ...
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Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery
... Hitherto, the limitation of BET proteins inhibitors also emerged, the negative finding of RVX-208 is disappointing for the potency and selectivity of this agent have not been disclosed in previous literatures. The ...
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Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases
... by bromodomain (BRD) proteins is a key event in transcriptional ...targeting bromodomain and extra-terminal (BeT) proteins compete for binding to acetylated ...
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BET inhibitors block pancreatic stellate cell collagen I production and attenuate fibrosis in vivo
... the bromodomain and extraterminal (BET) family of proteins are expressed in primary PSCs isolated from human PDAC tumors, with BRD4 positively regulating, and BRD2 and BRD3 negatively regulating, collagen I ...
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