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...

Volledige beschrijving

Bibliografische gegevens
Hoofdauteurs:	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
Formaat:	Journal article
Taal:	English
Gepubliceerd in:	2013

Gelijkaardige items

Developing chemical probes for the BET bromodomains
door: Hewings, D, et al.
Gepubliceerd in: (2012)

The design and synthesis of 5-and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains
door: Hay, D, et al.
Gepubliceerd in: (2013)

Chemical probes for bromodomains outside the BET family
door: Brennan, P, et al.
Gepubliceerd in: (2013)

Selective inhibition of BET bromodomains.
door: Filippakopoulos, P, et al.
Gepubliceerd in: (2010)

Selective inhibition of BET bromodomains.
door: Filippakopoulos, P, et al.
Gepubliceerd in: (2010)

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
door: Filippakopoulos, P, et al.
Gepubliceerd in: (2012)

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family
door: Filippakopoulos, P, et al.
Gepubliceerd in: (2012)

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
door: Picaud, S, et al.
Gepubliceerd in: (2013)

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain
door: Picaud, S, et al.
Gepubliceerd in: (2013)

Small-molecule bromodomain inhibitors for cancer therapy
door: Qi, J, et al.
Gepubliceerd in: (2010)

Promiscuous targeting of bromodomains by Bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia
door: Picaud, S, et al.
Gepubliceerd in: (2016)

Evaluation of linker length effects on a BET bromodomain probe
door: Traquete, R, et al.
Gepubliceerd in: (2019)

3,5-Dimethylisoxazoles inhibit the bromodomain-histone protein-protein interaction
door: Hewings, D, et al.
Gepubliceerd in: (2012)

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.
door: Philpott, M, et al.
Gepubliceerd in: (2011)

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.
door: Philpott, M, et al.
Gepubliceerd in: (2011)

Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains
door: Hay, D, et al.
Gepubliceerd in: (2014)

Synthesis and biological investigation of (+)-JD1, an organometallic BET bromodomain inhibitor
door: Hassell-Hart, S, et al.
Gepubliceerd in: (2019)

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
door: Hewings, D, et al.
Gepubliceerd in: (2011)

Developing small molecule inhibitors of the CREBBP bromodomain-histone interaction
door: Rooney, T, et al.
Gepubliceerd in: (2012)

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.
door: Fedorov, O, et al.
Gepubliceerd in: (2015)

Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.
door: Fish, P, et al.
Gepubliceerd in: (2012)

[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains.
door: Fedorov, O, et al.
Gepubliceerd in: (2014)

Interactome rewiring following pharmacological targeting of BET bromodomains
door: Lambert, J-P, et al.
Gepubliceerd in: (2018)

BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability
door: Jennings, L, et al.
Gepubliceerd in: (2018)

The bromodomain interaction module.
door: Filippakopoulos, P, et al.
Gepubliceerd in: (2012)

The bromodomain interaction module
door: Filippakopoulos, P, et al.
Gepubliceerd in: (2012)

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands
door: Hewings, D, et al.
Gepubliceerd in: (2011)

Stimulation of Hepatic Apolipoprotein A-I Production by Novel Thieno-Triazolodiazepines: Roles of the Classical Benzodiazepine Receptor, PAF Receptor, and Bromodomain Binding.
door: Kempen, H, et al.
Gepubliceerd in: (2013)

Bromodomains as therapeutic targets.
door: Muller, S, et al.
Gepubliceerd in: (2011)

Chemical probes and inhibitors of bromodomains outside the BET family
door: Moustakim, M, et al.
Gepubliceerd in: (2016)

Targeting bromodomains: epigenetic readers of lysine acetylation.
door: Filippakopoulos, P, et al.
Gepubliceerd in: (2014)

BET bromodomain inhibitors PFI-1 and CPI-203 suppress the development of follicular lymphoma via regulating Wnt/β-catenin signaling
door: Min Bai, et al.
Gepubliceerd in: (2024-03-01)

Discovery of BET bromodomain inhibitors and their role in target validation
door: Mueller, S, et al.
Gepubliceerd in: (2014)

Dissecting the Role of BET Bromodomain Proteins BRD2 and BRD4 in Human NK Cell Function
door: Cribbs, AP, et al.
Gepubliceerd in: (2021)

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
door: Ciceri, P, et al.
Gepubliceerd in: (2014)

Corrigendum: Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
door: Ciceri, P, et al.
Gepubliceerd in: (2014)

Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
door: Hewings, D, et al.
Gepubliceerd in: (2013)

Dissecting the Role of BET Bromodomain Proteins BRD2 and BRD4 in Human NK Cell Function
door: Adam P. Cribbs, et al.
Gepubliceerd in: (2021-02-01)

BET bromodomain proteins regulate enhancer function during adipogenesis
door: Brown, Jonathan D., et al.
Gepubliceerd in: (2018)

Inhibition of BET Bromodomain Targets Genetically Diverse Glioblastoma
door: Cheng, Z, et al.
Gepubliceerd in: (2013)