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 bromodomains …

Histone H3 lysine 9 di-methylation as an epigenetic signature of the interferon response

…, A Stienen, S Dewell, MS Chen, I Rioja… - Journal of Experimental …, 2012 - rupress.org
Effective antiviral immunity depends on the ability of infected cells or cells triggered with
virus-derived nucleic acids to produce type I interferon (IFN), which activates transcription of …

Potential novel biomarkers of disease activity in rheumatoid arthritis patients: CXCL13, CCL23, transforming growth factor α, tumor necrosis factor receptor superfamily …

I Rioja, FJ Hughes, CH Sharp… - … : Official Journal of …, 2008 - Wiley Online Library
Objective To determine whether the plasma levels of a range of inflammatory proteins have
utility as biomarkers of disease activity in rheumatoid arthritis (RA) patients. Methods Plasma …

Epigenetic regulation of T cell memory: recalling therapeutic implications

DF Tough, I Rioja, LK Modis, RK Prinjha - Trends in immunology, 2020 - cell.com
Memory T cells possess functional differences from naïve T cells that powerfully contribute
to the efficiency of secondary immune responses. These abilities are imprinted during the …

Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11

DF Tough, HD Lewis, I Rioja… - British journal of …, 2014 - Wiley Online Library
The properties of a cell are determined both genetically by the DNA sequence of its genes
and epigenetically through processes that regulate the pattern, timing and magnitude of …

GSK789: a selective inhibitor of the first bromodomains (BD1) of the bromo and extra terminal domain (BET) proteins

…, A Phillipou, RK Prinjha, I Rioja… - Journal of Medicinal …, 2020 - ACS Publications
Pan-bromodomain and extra terminal (BET) inhibitors interact equipotently with all eight
bromodomains of the BET family of proteins. They have shown profound efficacy in vitro and in …

The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes

…, N Smithers, RC Furze, L Gordon, G Drewes, I Rioja… - …, 2014 - pubs.rsc.org
Herein we describe the design and synthesis of a dual active histone deacetylase (HDAC)/bromodomain
and extra terminal (BET) small molecule tool inhibitor, DUAL946 (1). Exploiting …

[HTML][HTML] Epigenetic modulation of type-1 diabetes via a dual effect on pancreatic macrophages and β cells

…, SM Clardy, K Hattori, P Mander, K Lee, I Rioja… - Elife, 2014 - elifesciences.org
10.7554/eLife.04631.001 Epigenetic modifiers are an emerging class of anti-tumor drugs,
potent in multiple cancer contexts. Their effect on spontaneously developing autoimmune …

[HTML][HTML] Cohesin couples transcriptional bursting probabilities of inducible enhancers and promoters

…, C Whilding, D Dormann, S Marguerat, I Rioja… - Nature …, 2022 - nature.com
Innate immune responses rely on inducible gene expression programmes which, in contrast
to steady-state transcription, are highly dependent on cohesin. Here we address …

[HTML][HTML] Combined noncanonical NF-κB agonism and targeted BET bromodomain inhibition reverse HIV latency ex vivo

…, LI James, G Wu, P Zuck, I Rioja… - The Journal of …, 2022 - Am Soc Clin Investig
Latency reversal strategies for HIV cure using inhibitor of apoptosis protein (IAP) antagonists
(IAPi) induce unprecedented levels of latent reservoir expression without immunotoxicity …