3,5-Dimethylisoxazoles inhibit the bromodomain-histone protein-protein interaction

3,5-Dimethylisoxazoles inhibit the bromodomain-histone protein-protein interaction

Manylion Llyfryddiaeth
Prif Awduron:	Hewings, D, Wang, M, Philpott, M, Fedorov, O, Uttarkar, S, Filippakopoulos, P, Picaud, S, Vuppusetty, C, Marsden, B, Heightman, T, Knapp, S, Brennan, P, Conway, S
Fformat:	Conference item
Cyhoeddwyd:	2012

Eitemau Tebyg

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

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

Developing chemical probes for the BET bromodomains
gan: Hewings, D, et al.
Cyhoeddwyd: (2012)

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

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

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

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

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

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

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

Small-molecule bromodomain inhibitors for cancer therapy
gan: Qi, J, et al.
Cyhoeddwyd: (2010)

PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains.
gan: Picaud, S, et al.
Cyhoeddwyd: (2013)

Developing inhibitors of bromodomain-histone interactions
gan: Hewings, D
Cyhoeddwyd: (2014)

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

Isoxazole-derived amino acids are bromodomain-binding acetyl-lysine mimics: incorporation into histone H4 peptides and histone H3
gan: Conway, S, et al.
Cyhoeddwyd: (2016)

A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction
gan: Rooney, T, et al.
Cyhoeddwyd: (2014)

Selective inhibition of BET bromodomains.
gan: Filippakopoulos, P, et al.
Cyhoeddwyd: (2010)

Chemical probes for bromodomains outside the BET family
gan: Brennan, P, et al.
Cyhoeddwyd: (2013)

Histone recognition and large-scale structural analysis of the human bromodomain family.
gan: Filippakopoulos, P, et al.
Cyhoeddwyd: (2012)

Selective inhibition of BET bromodomains.
gan: Filippakopoulos, P, et al.
Cyhoeddwyd: (2010)

The bromodomain interaction module.
gan: Filippakopoulos, P, et al.
Cyhoeddwyd: (2012)

The bromodomain interaction module
gan: Filippakopoulos, P, et al.
Cyhoeddwyd: (2012)

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

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

Bromodomains as therapeutic targets.
gan: Muller, S, et al.
Cyhoeddwyd: (2011)

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

Functions of bromodomain-containing proteins and their roles in homeostasis and cancer
gan: Fujisawa, T, et al.
Cyhoeddwyd: (2017)

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

Targeting bromodomains: epigenetic readers of lysine acetylation.
gan: Filippakopoulos, P, et al.
Cyhoeddwyd: (2014)

Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.
gan: Ferguson, F, et al.
Cyhoeddwyd: (2013)

Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions.
gan: Hewings, D, et al.
Cyhoeddwyd: (2012)

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

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

Molecular basis of histone tail recognition by human TIP5 PHD finger and bromodomain of the chromatin remodeling complex NoRC.
gan: Tallant, C, et al.
Cyhoeddwyd: (2015)

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

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
gan: Ciceri, P, et al.
Cyhoeddwyd: (2014)

Bromodomains control amyloid-like aggregation of aberrantly acetylated proteins
gan: Olzscha, H, et al.
Cyhoeddwyd: (2018)

Developing small molecule inhibitors of bromodomain-histone interactions
gan: Wilson, B, et al.
Cyhoeddwyd: (2015)

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

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