Bromodomains: Structure, function and pharmacology of inhibition

E Ferri, C Petosa, CE McKenna - Biochemical pharmacology, 2016 - Elsevier
Bromodomains are epigenetic readers of histone acetylation involved in chromatin
remodeling and transcriptional regulation. The human proteome comprises 46 …

Bromodomain and extra-terminal (BET) family proteins: New therapeutic targets in major diseases

B Padmanabhan, S Mathur, R Manjula, S Tripathi - Journal of biosciences, 2016 - Springer
The bromodomains and extra-terminal domain (BET) family proteins recognize acetylated
chromatin through their bromodomains (BDs) and help in regulating gene expression. BDs …

Structure-guided design of IACS-9571, a selective high-affinity dual TRIM24-BRPF1 bromodomain inhibitor

WS Palmer, G Poncet-Montange, G Liu… - Journal of medicinal …, 2016 - ACS Publications
The bromodomain containing proteins TRIM24 (tripartite motif containing protein 24) and
BRPF1 (bromodomain and PHD finger containing protein 1) are involved in the epigenetic …

Discovery and characterization of GSK2801, a selective chemical probe for the bromodomains BAZ2A and BAZ2B

P Chen, A Chaikuad, P Bamborough… - Journal of medicinal …, 2016 - ACS Publications
Bromodomains are acetyl-lysine specific protein interaction domains that have recently
emerged as a new target class for the development of inhibitors that modulate gene …

Epigenetic stress responses induce muscle stem-cell ageing by Hoxa9 developmental signals

S Schwoerer, F Becker, C Feller, AH Baig, U Koeber… - Nature, 2016 - nature.com
The functionality of stem cells declines during ageing, and this decline contributes to ageing-
associated impairments in tissue regeneration and function. Alterations in developmental …

The bromodomain: a new target in emerging epigenetic medicine

SG Smith, MM Zhou - ACS chemical biology, 2016 - ACS Publications
The bromodomain (BrD) is a conserved protein modular domain found in many chromatin-
and transcription-associated proteins that has the ability to recognize acetylated lysine …

Immunomodulatory drugs target IKZF1-IRF4-MYC axis in primary effusion lymphoma in a cereblon-dependent manner and display synergistic cytotoxicity with BRD4 …

R Gopalakrishnan, H Matta, B Tolani, T Triche Jr… - Oncogene, 2016 - nature.com
Primary effusion lymphoma (PEL) is an aggressive type of non-Hodgkin lymphoma localized
predominantly in body cavities. Kaposi's sarcoma-associated herpes virus (KSHV) is the …

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia

S Picaud, K Leonards, JP Lambert, O Dovey… - Science …, 2016 - science.org
Bromodomains (BRDs) have emerged as compelling targets for cancer therapy. The
development of selective and potent BET (bromo and extra-terminal) inhibitors and their …

Discovery of a chemical tool inhibitor targeting the bromodomains of TRIM24 and BRPF

J Bennett, O Fedorov, C Tallant… - Journal of Medicinal …, 2016 - ACS Publications
TRIM24 is a transcriptional regulator as well as an E3 ubiquitin ligase. It is overexpressed in
diverse tumors, and high expression levels have been linked to poor prognosis in breast …

Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological …

X Xue, Y Zhang, Z Liu, M Song, Y Xing… - Journal of Medicinal …, 2016 - ACS Publications
The discovery of inhibitors of bromodomain and extra terminal domain (BET) has achieved
great progress, and at least seven inhibitors have progressed into clinical trials for the …