From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
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RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonistThe bromodomain: from epigenome reader to druggable targetProtein lysine acetylation by p300/CBPDiscovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual ScreeningRVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomainDiscovery, Design, and Optimization of Isoxazole Azepine BET InhibitorsNaphthyridines as novel BET family bromodomain inhibitorsTargeting BET bromodomains for cancer treatmentBET bromodomain proteins and epigenetic regulation of inflammation: implications for type 2 diabetes and breast cancer.Drug Discovery Targeting Bromodomain-Containing Protein 4.Privileged diazepine compounds and their emergence as bromodomain inhibitors.BET bromodomain inhibitors: a patent review.[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomainsSelective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4.Inhibition of osteoclastogenesis and inflammatory bone resorption by targeting BET proteins and epigenetic regulationSmall-molecular modulators of cancer-associated epigenetic mechanisms.Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discoveryStructure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.Phenotypic screening and fragment-based approaches to the discovery of small-molecule bromodomain ligands.Bromodomains and their pharmacological inhibitors.Inhibition of bromodomain and extra-terminal proteins (BET) as a potential therapeutic approach in haematological malignancies: emerging preclinical and clinical evidence.Inhibitors of emerging epigenetic targets for cancer therapy: a patent review (2010-2014).Fragment-Based Drug Discovery in the Bromodomain and Extra-Terminal Domain Family.Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.Progress in the Development of non-BET Bromodomain Chemical Probes.The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.I-BET151 selectively regulates IL-6 production.Chemical probes and inhibitors of bromodomains outside the BET family.BET bromodomain proteins regulate enhancer function during adipogenesis.Discovery of BET bromodomain inhibitors and their role in target validation
P2860
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P2860
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
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2012 nî lūn-bûn
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2012年の論文
@ja
2012年学术文章
@wuu
2012年学术文章
@zh-cn
2012年学术文章
@zh-hans
2012年学术文章
@zh-my
2012年学术文章
@zh-sg
2012年學術文章
@yue
2012年學術文章
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2012年學術文章
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name
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
@en
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
@nl
type
label
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
@en
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
@nl
prefLabel
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
@en
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
@nl
P2093
P1476
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151
@en
P2093
Agnès Costaz
Alizon Riou
Anne Bouillot
Anne-Bénédicte Boullay
Delphine Delannée
Edwige Nicodeme
Eric Boursier
Florence Blandel
Françoise Gellibert
Frédéric Donche
P304
P356
10.1016/J.BMCL.2012.01.125
P407
P577
2012-02-08T00:00:00Z