Achieving clinical success with BET inhibitors as anti-cancer agents
T Shorstova, WD Foulkes, M Witcher - British journal of cancer, 2021 - nature.com
The transcriptional upregulation of oncogenes is a driving force behind the progression of
many tumours. However, until a decade ago, the concept of 'switching off'these oncogenic …
many tumours. However, until a decade ago, the concept of 'switching off'these oncogenic …
Targeting MAPK signaling in cancer: mechanisms of drug resistance and sensitivity
Mitogen-activated protein kinase (MAPK) pathways represent ubiquitous signal transduction
pathways that regulate all aspects of life and are frequently altered in disease. Here, we …
pathways that regulate all aspects of life and are frequently altered in disease. Here, we …
[HTML][HTML] Predicting drug response and synergy using a deep learning model of human cancer cells
Most drugs entering clinical trials fail, often related to an incomplete understanding of the
mechanisms governing drug response. Machine learning techniques hold immense promise …
mechanisms governing drug response. Machine learning techniques hold immense promise …
Bromodomains: a new target class for drug development
AG Cochran, AR Conery, RJ Sims III - Nature Reviews Drug Discovery, 2019 - nature.com
Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …
found in proteins with varied functions, were highly tractable small-molecule targets. This is …
A Phase 1 study of RO6870810, a novel bromodomain and extra-terminal protein inhibitor, in patients with NUT carcinoma, other solid tumours, or diffuse large B-cell …
GI Shapiro, P LoRusso, A Dowlati, K T. Do… - British journal of …, 2021 - nature.com
Background Bromodomain and extra-terminal (BET) proteins are epigenetic readers that
can drive carcinogenesis and therapy resistance. RO6870810 is a novel, small-molecule …
can drive carcinogenesis and therapy resistance. RO6870810 is a novel, small-molecule …
Understanding and targeting resistance mechanisms in cancer
Resistance to cancer therapies has been a commonly observed phenomenon in clinical
practice, which is one of the major causes of treatment failure and poor patient survival. The …
practice, which is one of the major causes of treatment failure and poor patient survival. The …
BET proteins: Biological functions and therapeutic interventions
J Guo, Q Zheng, Y Peng - Pharmacology & Therapeutics, 2023 - Elsevier
Bromodomain and extra-terminal (BET) family member proteins (BRD2, BRD3, BRD4 and
BRDT) play a pivotal role in interpreting the epigenetic information of histone Kac …
BRDT) play a pivotal role in interpreting the epigenetic information of histone Kac …
Make your best BET: The emerging role of BET inhibitor treatment in malignant tumors
O Bechter, P Schöffski - Pharmacology & therapeutics, 2020 - Elsevier
Bromodomains are protein-protein interaction modules with a great diversity in terms of
number of proteins and their function. The bromodomain and extraterminal protein (BET) …
number of proteins and their function. The bromodomain and extraterminal protein (BET) …
BET proteins as attractive targets for cancer therapeutics
J Sarnik, T Popławski, P Tokarz - International journal of molecular …, 2021 - mdpi.com
Transcriptional dysregulation is a hallmark of cancer and can be an essential driver of
cancer initiation and progression. Loss of transcriptional control can cause cancer cells to …
cancer initiation and progression. Loss of transcriptional control can cause cancer cells to …
Spermine synthase and MYC cooperate to maintain colorectal cancer cell survival by repressing Bim expression
Dysregulation of polyamine metabolism has been linked to the development of colorectal
cancer (CRC), but the underlying mechanism is incompletely characterized. Here, we report …
cancer (CRC), but the underlying mechanism is incompletely characterized. Here, we report …