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 …

Bromodomain inhibitors and cancer therapy: From structures to applications

M Pérez-Salvia, M Esteller - Epigenetics, 2017 - Taylor & Francis
Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes
that are “writers,”“erasers,” or “readers” of histone modification marks are common …

HDL in the 21st century: a multifunctional roadmap for future HDL research

A Rohatgi, M Westerterp, A Von Eckardstein… - Circulation, 2021 - Am Heart Assoc
Low high-density lipoprotein cholesterol (HDL-C) characterizes an atherogenic dyslipidemia
that reflects adverse lifestyle choices, impaired metabolism, and increased cardiovascular …

Epigenetics-targeted drugs: Current paradigms and future challenges

W Dai, X Qiao, Y Fang, R Guo, P Bai, S Liu… - … and Targeted Therapy, 2024 - nature.com
Epigenetics governs a chromatin state regulatory system through five key mechanisms: DNA
modification, histone modification, RNA modification, chromatin remodeling, and non-coding …

Dysfunctional HDL in diabetes mellitus and its role in the pathogenesis of cardiovascular disease

RAK Srivastava - Molecular and cellular biochemistry, 2018 - Springer
Coronary artery disease, the leading cause of death in the developed and developing
countries, is prevalent in diabetes mellitus with 68% cardiovascular disease (CVD)-related …

Targeting epigenetic DNA and histone modifications to treat kidney disease

M Fontecha-Barriuso, D Martin-Sanchez… - Nephrology dialysis …, 2018 - academic.oup.com
Epigenetics refers to heritable changes in gene expression patterns not caused by an
altered nucleotide sequence, and includes non-coding RNAs and covalent modifications of …

Selective BET inhibitor RVX‐208 ameliorates periodontal inflammation and bone loss

M Sun, N Clayton, S Alam, N Asmussen… - Journal of Clinical …, 2023 - Wiley Online Library
Aim To determine the effects of RVX‐208, a selective bromodomain and extra‐terminal
domain (BET) inhibitor targeting bromodomain 2 (BD2), on periodontal inflammation and …

Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and …

KK Ray, SJ Nicholls, HD Ginsberg, JO Johansson… - American Heart …, 2019 - Elsevier
Background After an acute coronary syndrome (ACS), patients with diabetes remain at high
risk for additional cardiovascular events despite use of current therapies. Bromodomain and …

Bromodomains in protozoan parasites: evolution, function, and opportunities for drug development

V Jeffers, C Yang, S Huang… - … and Molecular Biology …, 2017 - Am Soc Microbiol
Parasitic infections remain one of the most pressing global health concerns of our day,
affecting billions of people and producing unsustainable economic burdens. The rise of drug …

Inhibition of bromodomain and extraterminal domain (BET) proteins by JQ1 unravels a novel epigenetic modulation to control lipid homeostasis

C Tonini, M Colardo, B Colella… - International journal of …, 2020 - mdpi.com
The homeostatic control of lipid metabolism is essential for many fundamental physiological
processes. A deep understanding of its regulatory mechanisms is pivotal to unravel …