Bromodomain and extra-terminal motif inhibitors: a review of preclinical and clinical advances in cancer therapy

A Alqahtani, K Choucair, M Ashraf… - Future science …, 2019 - Taylor & Francis
Histone lysine acetylation is critical in regulating transcription. Dysregulation of this process
results in aberrant gene expression in various diseases, including cancer. The …

[HTML][HTML] Bromodomain and extraterminal proteins as novel epigenetic targets for renal diseases

JL Morgado-Pascual, S Rayego-Mateos… - Frontiers in …, 2019 - frontiersin.org
Epigenetic mechanisms, especially DNA methylation and histone modifications, are
dynamic processes that regulate the gene expression transcriptional program in normal and …

Therapeutic epigenetic reprogramming of trained immunity in myeloid cells

RM Rodriguez, B Suarez-Alvarez, C Lopez-Larrea - Trends in Immunology, 2019 - cell.com
Infiltrating and tissue-resident myeloid cells are essential regulators of innate and adaptive
immunity. During inflammation, and in response to microbial products, these cells can adapt …

Discovery of Benzo[cd]indol-2(1H)-ones and Pyrrolo[4,3,2-de]quinolin-2(1H)-ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for …

F Jiang, Q Hu, Z Zhang, H Li, H Li… - Journal of medicinal …, 2019 - ACS Publications
The bromodomain and extra-terminal domain (BET) family of proteins are readers which
specifically recognize histone-acetylated lysine residues. Each BET bromodomain protein …

CD109 regulates the inflammatory response and is required for the pathogenesis of rheumatoid arthritis

G Song, T Feng, RU Zhao, Q Lu, Y Diao… - Annals of the …, 2019 - ard.bmj.com
Objective The aim of this study was to investigate the role of CD109 in rheumatoid arthritis
(RA) fibroblast-like synoviocytes (FLSs) and to evaluate its potential as a therapeutic target …

Toward normalization of the tumor microenvironment for cancer therapy

J Zheng, P Gao - Integrative cancer therapies, 2019 - journals.sagepub.com
The tumor microenvironment (TME) is a complex ecosystem, including blood vessels,
immune cells, fibroblasts, extracellular matrix, cytokines, hormones, and so on. The TME …

[HTML][HTML] BET bromodomain inhibitors suppress inflammatory activation of gingival fibroblasts and epithelial cells from periodontitis patients

A Maksylewicz, A Bysiek, KB Lagosz… - Frontiers in …, 2019 - frontiersin.org
BET bromodomain proteins are important epigenetic regulators of gene expression that bind
acetylated histone tails and regulate the formation of acetylation-dependent chromatin …

Clinical candidates modulating protein-protein interactions: The fragment-based experience

D Valenti, S Hristeva, D Tzalis, C Ottmann - European Journal of Medicinal …, 2019 - Elsevier
Protein-protein interactions (PPIs) cover a very wide range of biological functions and
consequently have become one of the favourite targets for new therapeutic strategies. PPIs …

The next‐generation BET inhibitor, PLX51107, delays melanoma growth in a CD8‐mediated manner

DA Erkes, CO Field, C Capparelli… - Pigment cell & …, 2019 - Wiley Online Library
Epigenetic agents such as bromodomain and extra‐terminal region inhibitors (BETi) slow
tumor growth via tumor intrinsic alterations; however, their effects on antitumor immunity …

Small molecule and pooled CRISPR screens investigating IL17 signaling identify BRD2 as a novel contributor to keratinocyte inflammatory responses

PF Slivka, CL Hsieh, A Lipovsky, SD Pratt… - ACS Chemical …, 2019 - ACS Publications
Interleukin-17A (IL17A) plays a critical role in the development of numerous autoimmune
diseases, including psoriasis. The clinical success of IL17A neutralizing biologics in …