Results 11 to 20 of about 24,956 (275)

Stereoselective synthesis of allele-specific BET inhibitors [PDF]

Organic & Biomolecular Chemistry, 2020
Developing stereoselective synthetic routes that are efficient and cost-effective allows easy access to allele-selective bumped BET inhibitors.
Adam G. Bond, Andrea Testa, Alessio Ciulli   +2 more
openaire   +5 more sources

Impact of structurally diverse BET inhibitors on SIRT1

Gene, 2020
The epigenetic regulation of gene expression is controlled by various processes, of which one is histone acetylation. Many proteins control gene expression via histone acetylation. Those proteins include sirtuins (SIRTs) and bromodomain and extraterminal proteins (BETs), which are known to regulate same cellular processes and pathways.
Jonna Tenhunen, Tarja Kokkola, Marjo Huovinen, Minna Rahnasto-Rilla, Maija Lahtela-Kakkonen   +4 more
openaire   +5 more sources

BET bromodomain inhibitors synergize with ATR inhibitors in melanoma [PDF]

Cell Death & Disease, 2017
AbstractMetastatic malignant melanoma continues to be a challenging disease despite clinical translation of the comprehensive understanding of driver mutations and how melanoma cells evade immune attack. In Myc-driven lymphoma, efficacy of epigenetic inhibitors of the bromodomain and extra-terminal domain (BET) family of bromodomain proteins can be ...
Somsundar Veppil Muralidharan, Berglind Osk Einarsdottir, Joydeep Bhadury, Mattias F Lindberg, Jin Wu, Eric Campeau, Roger Olofsson Bagge, Ulrika Stierner, Lars Ny, Lisa M Nilsson, Jonas A Nilsson   +10 more
openaire   +4 more sources

Targeting Cancer Cells with BET Bromodomain Inhibitors [PDF]

Cold Spring Harbor Perspectives in Medicine, 2017
Cancer cells are often hypersensitive to the targeting of transcriptional regulators, which may reflect the deregulated gene expression programs that underlie malignant transformation. One of the most prominent transcriptional vulnerabilities in human cancer to emerge in recent years is the bromodomain and extraterminal (BET) family of proteins, which ...
Yali, Xu, Christopher R, Vakoc
openaire   +3 more sources

BET Bromodomain Inhibitors Suppress Inflammatory Activation of Gingival Fibroblasts and Epithelial Cells From Periodontitis Patients [PDF]

Frontiers in Immunology, 2019
BET bromodomain proteins are important epigenetic regulators of gene expression that bind acetylated histone tails and regulate the formation of acetylation-dependent chromatin complexes.
Anna Maksylewicz, Agnieszka Bysiek, Katarzyna B. Lagosz, Justyna M. Macina, Malgorzata Kantorowicz, Grzegorz Bereta, Maja Sochalska, Katarzyna Gawron, Maria Chomyszyn-Gajewska, Jan Potempa, Jan Potempa, Aleksander M. Grabiec   +11 more
doaj   +2 more sources

Bromodomain and Extra-Terminal (BET) Domain Protein Inhibitors for Solid Tumor Cancers [PDF]

Journal of Immunotherapy and Precision Oncology, 2020
The bromodomain and extraterminal (BET) domain protein family is involved in the process of transcription of genetic information. The BET protein family includes BRD2, BRD3, BRD4, and bromodomain testis-specific protein.
Martin V. Nguyen, Lydia Loof, Gerald S. Falchook   +2 more
doaj   +2 more sources

Potent and selective bivalent inhibitors of BET bromodomains [PDF]

Nature Chemical Biology, 2016
Proteins of the bromodomain and extraterminal (BET) family, in particular bromodomain-containing protein 4 (BRD4), are of great interest as biological targets. BET proteins contain two separate bromodomains, and existing inhibitors bind to them monovalently.
Michael J Waring, Huawei Chen, Alfred A Rabow, Graeme Walker, Romel Bobby, Scott Boiko, Rob H Bradbury, Rowena Callis, Edwin Clark, Ian Dale, Danette L Daniels, Austin Dulak, Liz Flavell, Geoff Holdgate, Thomas A Jowitt, Alexey Kikhney, Mark McAlister, Jacqui Méndez, Derek Ogg, Joe Patel, Philip Petteruti, Graeme R Robb, Matthew B Robers, Sakina Saif, Natalie Stratton, Dmitri I Svergun, Wenxian Wang, David Whittaker, David M Wilson, Yi Yao   +29 more
openaire   +4 more sources

BET Isoform Selectivity through Diverse Linkers for Bivalent Inhibitors: GSK785, a BRD2/4-Selective Bivalent BET Inhibitor [PDF]

Journal of Medicinal Chemistry
The inhibition of the Bromodomain and Extra Terminal (BET) family of proteins has been widely studied for over a decade for its potential therapeutic benefit in cancer and immuno-inflammatory diseases. Selective inhibition within the four BET isoforms has been sought to facilitate the understanding of the individual role played by each family member ...
Francesco Rianjongdee, Stephen J. Atkinson, Paul Bamborough, Heather A Barnett, Kallie Friston, Paola Grandi, Christopher E Neipp, Massimo Petretich, Alex Phillipou, Alex G. S. Preston, Rab K. Prinjha, Nicholas C. O. Tomkinson, Emmanuel H. Demont   +12 more
openaire   +4 more sources

Cytoprotective, Cytotoxic and Cytostatic Roles of Autophagy in Response to BET Inhibitors. [PDF]

Int J Mol Sci, 2023
The bromodomain and extra-terminal domain (BET) family inhibitors are small molecules that target the dysregulated epigenetic readers, BRD2, BRD3, BRD4 and BRDT, at various transcription-related sites, including super-enhancers.
Elshazly AM, Gewirtz DA.
europepmc   +2 more sources

Role of BET Inhibitors in Triple Negative Breast Cancers. [PDF]

Cancers (Basel), 2020
Bromodomain and extraterminal domain (BET) proteins have evolved as key multifunctional super-regulators that control gene expression. These proteins have been shown to upregulate transcriptional machinery leading to over expression of genes involved in ...
Khandekar D, Tiriveedhi V.
europepmc   +3 more sources