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 …

Targeting MAPK signaling in cancer: mechanisms of drug resistance and sensitivity

S Lee, J Rauch, W Kolch - International journal of molecular sciences, 2020 - mdpi.com
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 …

[HTML][HTML] Predicting drug response and synergy using a deep learning model of human cancer cells

BM Kuenzi, J Park, SH Fong, KS Sanchez, J Lee… - Cancer cell, 2020 - cell.com
Most drugs entering clinical trials fail, often related to an incomplete understanding of the
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 …

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 …

Understanding and targeting resistance mechanisms in cancer

ZN Lei, Q Tian, QX Teng, JND Wurpel, L Zeng… - MedComm, 2023 - Wiley Online Library
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 …

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 …

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) …

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 …

Spermine synthase and MYC cooperate to maintain colorectal cancer cell survival by repressing Bim expression

Y Guo, Q Ye, P Deng, Y Cao, D He, Z Zhou… - Nature …, 2020 - nature.com
Dysregulation of polyamine metabolism has been linked to the development of colorectal
cancer (CRC), but the underlying mechanism is incompletely characterized. Here, we report …