Chromatin proteins and modifications as drug targets

K Helin, D Dhanak - Nature, 2013 - nature.com
A plethora of groundbreaking studies have demonstrated the importance of chromatin-
associated proteins and post-translational modifications of histones, proteins and DNA (so …

Targeting transcription factors: promising new strategies for cancer therapy

JE Yeh, PA Toniolo, DA Frank - Current opinion in oncology, 2013 - journals.lww.com
Transcription factors are an important target for cancer therapy, both through direct
anticancer effects and immunomodulatory actions. Newly developed delivery systems that …

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

S Picaud, C Wells, I Felletar… - Proceedings of the …, 2013 - National Acad Sciences
Bromodomains have emerged as attractive candidates for the development of inhibitors
targeting gene transcription. Inhibitors of the bromo and extraterminal (BET) family recently …

BET bromodomains mediate transcriptional pause release in heart failure

P Anand, JD Brown, CY Lin, J Qi, R Zhang, PC Artero… - Cell, 2013 - cell.com
Heart failure (HF) is driven by the interplay between regulatory transcription factors and
dynamic alterations in chromatin structure. Pathologic gene transactivation in HF is …

Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening

LR Vidler, P Filippakopoulos, O Fedorov… - Journal of medicinal …, 2013 - ACS Publications
Bromodomains (BRDs) are epigenetic readers that recognize acetylated-lysine (KAc) on
proteins and are implicated in a number of diseases. We describe a virtual screening …

S6K2: the neglected S6 kinase family member

OE Pardo, MJ Seckl - Frontiers in oncology, 2013 - frontiersin.org
S6 kinase 2 (S6K2) is a member of the AGC kinases super-family. Its closest homolog,
S6K1, has been extensively studied along the years. However, due to the belief in the …

Small-molecule modulators for epigenetics targets.

S Knapp, H Weinmann - ChemMedChem, 2013 - europepmc.org
A capital conference: Influencing epigenetic mechanisms may be highly relevant for future
therapies of various diseases such as cancer, inflammation, and metabolic disorders …