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 …

[HTML][HTML] Therapeutic targets for cardiac fibrosis: from old school to next-gen

JG Travers, CA Tharp, M Rubino… - The Journal of clinical …, 2022 - Am Soc Clin Investig
Cardiovascular diseases remain the leading cause of death worldwide, with pathological
fibrotic remodeling mediated by activated cardiac myofibroblasts representing a unifying …

[HTML][HTML] Histone acetyltransferases CBP/p300 in tumorigenesis and CBP/p300 inhibitors as promising novel anticancer agents

Q Chen, B Yang, X Liu, XD Zhang, L Zhang, T Liu - Theranostics, 2022 - ncbi.nlm.nih.gov
The histone acetyltransferases CBP and p300, often referred to as CBP/p300 due to their
sequence homology and functional overlap and co-operation, are emerging as critical …

EP300 Selectively Controls the Enhancer Landscape of MYCN-Amplified Neuroblastoma

AD Durbin, T Wang, VK Wimalasena, MW Zimmerman… - Cancer discovery, 2022 - AACR
Gene expression is regulated by promoters and enhancers marked by histone H3 lysine 27
acetylation (H3K27ac), which is established by the paralogous histone acetyltransferases …

Targeting hepatic glucose metabolism in the treatment of type 2 diabetes

AK Rines, K Sharabi, CDJ Tavares… - Nature reviews Drug …, 2016 - nature.com
Type 2 diabetes mellitus is characterized by the dysregulation of glucose homeostasis,
resulting in hyperglycaemia. Although current diabetes treatments have exhibited some …

Prostaglandin‐cytokine crosstalk in chronic inflammation

C Yao, S Narumiya - British journal of pharmacology, 2019 - Wiley Online Library
Chronic inflammation underlies various debilitating disorders including autoimmune,
neurodegenerative, vascular and metabolic diseases as well as cancer, where aberrant …

[HTML][HTML] Targeted degradation of the enhancer lysine acetyltransferases CBP and p300

R Vannam, J Sayilgan, S Ojeda, B Karakyriakou… - Cell chemical …, 2021 - cell.com
The enhancer factors CREB-binding protein (CBP) and p300 (also known as KAT3A and
KAT3B) maintain gene expression programs through lysine acetylation of chromatin and …

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 …

Current development of CBP/p300 inhibitors in the last decade

ZX He, BF Wei, X Zhang, YP Gong, LY Ma… - European Journal of …, 2021 - Elsevier
CBP/p300, functioning as histone acetyltransferases and transcriptional co-factors,
represents an attractive target for various diseases, including malignant tumor. The …

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 …