Cargando…

An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains

Bromodomain‐containing proteins are epigenetic modulators involved in a wide range of cellular processes, from recruitment of transcription factors to pathological disruption of gene regulation and cancer development. Since the druggability of these acetyl‐lysine reader domains was established, effo...

Descripción completa

Detalles Bibliográficos
Autores principales:	D'Ascenzio, Melissa, Pugh, Kathryn M., Konietzny, Rebecca, Berridge, Georgina, Tallant, Cynthia, Hashem, Shaima, Monteiro, Octovia, Thomas, Jason R., Schirle, Markus, Knapp, Stefan, Marsden, Brian, Fedorov, Oleg, Bountra, Chas, Kessler, Benedikt M., Brennan, Paul E.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	John Wiley and Sons Inc. 2018
Materias:	Communications
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6492141/ https://www.ncbi.nlm.nih.gov/pubmed/30589164 http://dx.doi.org/10.1002/anie.201807825

Ejemplares similares

Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF
por: Bennett, James, et al.
Publicado: (2015)

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

Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex
por: Sutherell, Charlotte L., et al.
Publicado: (2016)

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor**
por: Clark, Peter G K, et al.
Publicado: (2015)

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor
por: Clark, Peter G. K., et al.
Publicado: (2015)

[1,2,4]Triazolo[4,3-a]phthalazines: Inhibitors of Diverse Bromodomains
por: Fedorov, Oleg, et al.
Publicado: (2013)

Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains
por: Hay, Duncan A., et al.
Publicado: (2014)

Structure Enabled Design of BAZ2-ICR, A Chemical Probe Targeting the Bromodomains of BAZ2A and BAZ2B
por: Drouin, Ludovic, et al.
Publicado: (2015)

A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain
por: Cox, Oakley B., et al.
Publicado: (2016)

CBP/p300 Bromodomains Regulate Amyloid-like Protein Aggregation upon Aberrant Lysine Acetylation
por: Olzscha, Heidi, et al.
Publicado: (2017)

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B
por: Chen, Peiling, et al.
Publicado: (2015)

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia
por: Picaud, Sarah, et al.
Publicado: (2016)

Molecular Basis of Histone Tail Recognition by Human TIP5 PHD Finger and Bromodomain of the Chromatin Remodeling Complex NoRC
por: Tallant, Cynthia, et al.
Publicado: (2015)

Discovery of a PCAF Bromodomain Chemical Probe
por: Moustakim, Moses, et al.
Publicado: (2016)

Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation
por: Meier, Julia C., et al.
Publicado: (2017)

Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains
por: Bouché, Léa, et al.
Publicado: (2017)

3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands
por: Hewings, David S., et al.
Publicado: (2011)

The bromodomain inhibitor JQ1+ reduces calcium-sensing receptor activity in pituitary cell lines
por: Lines, Kate E, et al.
Publicado: (2021)

Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability
por: Lori, Laura, et al.
Publicado: (2016)

Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain
por: Ferguson, Fleur M., et al.
Publicado: (2013)

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family
por: Filippakopoulos, Panagis, et al.
Publicado: (2012)

Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain
por: Chaikuad, Apirat, et al.
Publicado: (2016)

A chemical toolbox for the study of bromodomains and epigenetic signaling
por: Wu, Qin, et al.
Publicado: (2019)

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands
por: Hewings, David S., et al.
Publicado: (2013)

Bromodomains as therapeutic targets
por: Muller, Susanne, et al.
Publicado: (2011)

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology
por: Ciceri, Pietro, et al.
Publicado: (2014)

Selective inhibition of BET bromodomains
por: Filippakopoulos, Panagis, et al.
Publicado: (2010)

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

BET inhibition as a new strategy for the treatment of gastric cancer
por: Montenegro, Raquel C., et al.
Publicado: (2016)

Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis
por: Myrianthopoulos, Vassilios, et al.
Publicado: (2016)

Open saccharin-based secondary sulfonamides as potent and selective inhibitors of cancer-related carbonic anhydrase IX and XII isoforms
por: D’Ascenzio, Melissa, et al.
Publicado: (2016)

CDA directs metabolism of epigenetic nucleosides revealing a therapeutic window in cancer
por: Zauri, Melania, et al.
Publicado: (2015)

4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis
por: Secci, Daniela, et al.
Publicado: (2019)

Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2
por: Moustakim, Moses, et al.
Publicado: (2018)

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit
por: Fish, Paul V., et al.
Publicado: (2012)

A Series of Potent CREBBP Bromodomain Ligands Reveals an Induced-Fit Pocket Stabilized by a Cation–π Interaction**
por: Rooney, Timothy P C, et al.
Publicado: (2014)

New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition
por: Baud, Matthias G. J., et al.
Publicado: (2015)

Accelerating target discovery using pre-competitive open science—patients need faster innovation more than anyone else
por: Low, Eric, et al.
Publicado: (2016)

Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites
por: Vidler, Lewis R., et al.
Publicado: (2012)

Open innovation in neuroscience research and drug discovery
por: Hunter, Ann J., et al.
Publicado: (2018)

Cannot write session to /tmp/vufind_sessions/sess_8ngqitvl1fj3jg6m1kqu24pja0