PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains.

PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains.

Bromo and extra terminal (BET) proteins (BRD2, BRD3, BRD4, and BRDT) are transcriptional regulators required for efficient expression of several growth promoting and antiapoptotic genes as well as for cell-cycle progression. BET proteins are recruited on transcriptionally active chromatin via their...

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Bibliografiske detaljer
Main Authors:	Picaud, S, Da Costa, D, Thanasopoulou, A, Filippakopoulos, P, Fish, P, Philpott, M, Fedorov, O, Brennan, P, Bunnage, M, Owen, DR, Bradner, J, Taniere, P, O'Sullivan, B, Müller, S, Schwaller, J, Stankovic, T, Knapp, S
Format:	Journal article
Sprog:	English
Udgivet:	2013

Lignende værker

Developing chemical probes for the BET bromodomains
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Udgivet: (2012)

The design and synthesis of 5-and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains
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Chemical probes for bromodomains outside the BET family
af: Brennan, P, et al.
Udgivet: (2013)

Selective inhibition of BET bromodomains.
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Udgivet: (2010)

Selective inhibition of BET bromodomains.
af: Filippakopoulos, P, et al.
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Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
af: Filippakopoulos, P, et al.
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Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family
af: Filippakopoulos, P, et al.
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RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
af: Picaud, S, et al.
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RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain
af: Picaud, S, et al.
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Small-molecule bromodomain inhibitors for cancer therapy
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Promiscuous targeting of bromodomains by Bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia
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Evaluation of linker length effects on a BET bromodomain probe
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Udgivet: (2019)

3,5-Dimethylisoxazoles inhibit the bromodomain-histone protein-protein interaction
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Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.
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Udgivet: (2011)

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.
af: Philpott, M, et al.
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Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains
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3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
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Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.
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Interactome rewiring following pharmacological targeting of BET bromodomains
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BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability
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The bromodomain interaction module.
af: Filippakopoulos, P, et al.
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The bromodomain interaction module
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Udgivet: (2012)

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands
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Stimulation of Hepatic Apolipoprotein A-I Production by Novel Thieno-Triazolodiazepines: Roles of the Classical Benzodiazepine Receptor, PAF Receptor, and Bromodomain Binding.
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Bromodomains as therapeutic targets.
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Chemical probes and inhibitors of bromodomains outside the BET family
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Udgivet: (2016)

Targeting bromodomains: epigenetic readers of lysine acetylation.
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BET bromodomain inhibitors PFI-1 and CPI-203 suppress the development of follicular lymphoma via regulating Wnt/β-catenin signaling
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Discovery of BET bromodomain inhibitors and their role in target validation
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Dissecting the Role of BET Bromodomain Proteins BRD2 and BRD4 in Human NK Cell Function
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Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
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Udgivet: (2014)

Corrigendum: Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
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Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
af: Hewings, D, et al.
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Dissecting the Role of BET Bromodomain Proteins BRD2 and BRD4 in Human NK Cell Function
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Inhibition of BET Bromodomain Targets Genetically Diverse Glioblastoma
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