BET proteins as targets for anticancer treatment
A Stathis, F Bertoni - Cancer discovery, 2018 - AACR
Bromodomain and extraterminal domain (BET) proteins are epigenetic readers that regulate
gene expression and are involved in cancer pathogenesis. Over the last years, several BET …
gene expression and are involved in cancer pathogenesis. Over the last years, several BET …
Transcriptional addiction in cancer cells is mediated by YAP/TAZ through BRD4
F Zanconato, G Battilana, M Forcato, L Filippi… - Nature medicine, 2018 - nature.com
Cancer cells rely on dysregulated gene expression. This establishes specific transcriptional
addictions that may be therapeutically exploited. Yet, the mechanisms that are ultimately …
addictions that may be therapeutically exploited. Yet, the mechanisms that are ultimately …
Epigenetic drug discovery for Alzheimer's disease
R Cacabelos, O Teijido - Epigenetics of aging and longevity, 2018 - Elsevier
Alzheimer's disease (AD) is the most important neurodegenerative disorder in Western
countries. Pathological phenotypes of neurodegeneration result from a combination of …
countries. Pathological phenotypes of neurodegeneration result from a combination of …
Discovery of QCA570 as an exceptionally potent and efficacious proteolysis targeting chimera (PROTAC) degrader of the bromodomain and extra-terminal (BET) …
C Qin, Y Hu, B Zhou, E Fernandez-Salas… - Journal of medicinal …, 2018 - ACS Publications
Proteins of the bromodomain and extra-terminal (BET) family are epigenetics “readers” and
promising therapeutic targets for cancer and other human diseases. We describe herein a …
promising therapeutic targets for cancer and other human diseases. We describe herein a …
Discovery of tetrahydroquinoxalines as bromodomain and extra-terminal domain (BET) inhibitors with selectivity for the second bromodomain
RP Law, SJ Atkinson, P Bamborough… - Journal of Medicinal …, 2018 - ACS Publications
The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine
residues on histone proteins. The four BET bromodomains—BRD2, BRD3, BRD4, and …
residues on histone proteins. The four BET bromodomains—BRD2, BRD3, BRD4, and …
Modeling combination therapy for breast cancer with BET and immune checkpoint inhibitors
X Lai, A Stiff, M Duggan… - Proceedings of the …, 2018 - National Acad Sciences
CTLA-4 is an immune checkpoint expressed on active anticancer T cells. When it combines
with its ligand B7 on dendritic cells, it inhibits the activity of the T cells. The Bromo-and Extra …
with its ligand B7 on dendritic cells, it inhibits the activity of the T cells. The Bromo-and Extra …
Molecular basis for the N-terminal bromodomain-and-extra-terminal-family selectivity of a dual kinase–bromodomain inhibitor
As regulators of transcription, epigenetic proteins that interpret post-translational
modifications to N-terminal histone tails are essential for maintaining cellular homeostasis …
modifications to N-terminal histone tails are essential for maintaining cellular homeostasis …
BET bromodomain proteins regulate enhancer function during adipogenesis
JD Brown, ZB Feldman, SP Doherty… - Proceedings of the …, 2018 - National Acad Sciences
Developmental transitions are guided by master regulatory transcription factors. During
adipogenesis, a transcriptional cascade culminates in the expression of PPARγ and …
adipogenesis, a transcriptional cascade culminates in the expression of PPARγ and …
Alkaline phosphatases in the complex chronic kidney disease-mineral and bone disorders
J Bover, P Ureña, A Aguilar, S Mazzaferro… - Calcified tissue …, 2018 - Springer
Alkaline phosphatases (APs) remove the phosphate (dephosphorylation) needed in multiple
metabolic processes (from many molecules such as proteins, nucleotides, or …
metabolic processes (from many molecules such as proteins, nucleotides, or …
Pharmacoepigenomic interventions as novel potential treatments for Alzheimer's and Parkinson's diseases
O Teijido, R Cacabelos - International Journal of Molecular Sciences, 2018 - mdpi.com
Cerebrovascular and neurodegenerative disorders affect one billion people around the
world and result from a combination of genomic, epigenomic, metabolic, and environmental …
world and result from a combination of genomic, epigenomic, metabolic, and environmental …