[HTML][HTML] 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 …

[HTML][HTML] The BET family in immunity and disease

N Wang, R Wu, D Tang, R Kang - Signal transduction and targeted …, 2021 - nature.com
Innate immunity serves as the rapid and first-line defense against invading pathogens, and
this process can be regulated at various levels, including epigenetic mechanisms. The …

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation

O Gilan, I Rioja, K Knezevic, MJ Bell, MM Yeung… - Science, 2020 - science.org
The two tandem bromodomains of the BET (bromodomain and extraterminal domain)
proteins enable chromatin binding to facilitate transcription. Drugs that inhibit both …

Small airway-on-a-chip enables analysis of human lung inflammation and drug responses in vitro

KH Benam, R Villenave, C Lucchesi, A Varone… - Nature …, 2016 - nature.com
Here we describe the development of a human lung'small airway-on-a-chip'containing a
differentiated, mucociliary bronchiolar epithelium and an underlying microvascular …

[HTML][HTML] A cancer vaccine-mediated postoperative immunotherapy for recurrent and metastatic tumors

T Wang, D Wang, H Yu, B Feng, F Zhou… - Nature …, 2018 - nature.com
Vaccines to induce effective and sustained antitumor immunity have great potential for
postoperative cancer therapy. However, a robust cancer vaccine simultaneously eliciting …

Targeting bromodomains: epigenetic readers of lysine acetylation

P Filippakopoulos, S Knapp - Nature reviews Drug discovery, 2014 - nature.com
Lysine acetylation is a key mechanism that regulates chromatin structure; aberrant
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …

[HTML][HTML] The mechanisms behind the therapeutic activity of BET bromodomain inhibition

J Shi, CR Vakoc - Molecular cell, 2014 - cell.com
The bromodomain and extraterminal (BET) protein Brd4 recruits transcriptional regulatory
complexes to acetylated chromatin. While Brd4 is considered to be a general transcriptional …

[HTML][HTML] BET bromodomain inhibition promotes anti-tumor immunity by suppressing PD-L1 expression

H Zhu, F Bengsch, N Svoronos, MR Rutkowski… - Cell reports, 2016 - cell.com
Restoration of anti-tumor immunity by blocking PD-L1 signaling through the use of
antibodies has proven to be beneficial in cancer therapy. Here, we show that BET …

Phase 1 study of molibresib (GSK525762), a bromodomain and extra-terminal domain protein inhibitor, in NUT carcinoma and other solid tumors

SA Piha-Paul, CL Hann, CA French… - JNCI Cancer …, 2020 - academic.oup.com
Background Bromodomain and extra-terminal domain proteins are promising epigenetic
anticancer drug targets. This first-in-human study evaluated the safety, recommended phase …

Lung-on-a-chip: the future of respiratory disease models and pharmacological studies

J Shrestha, S Razavi Bazaz… - Critical reviews in …, 2020 - Taylor & Francis
Abstract Recently, organ-on-a-chip models, which are microfluidic devices that mimic the
cellular architecture and physiological environment of an organ, have been developed and …