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 …

Epigenetic tools (The Writers, The Readers and The Erasers) and their implications in cancer therapy

S Biswas, CM Rao - European journal of pharmacology, 2018 - Elsevier
Addition of chemical tags on the DNA and modification of histone proteins impart a distinct
feature on chromatin architecture. With the advancement in scientific research, the key …

A non-canonical SWI/SNF complex is a synthetic lethal target in cancers driven by BAF complex perturbation

BC Michel, AR D'Avino, SH Cassel, N Mashtalir… - Nature cell …, 2018 - nature.com
Mammalian SWI/SNF chromatin remodelling complexes exist in three distinct, final-form
assemblies: canonical BAF (cBAF), PBAF and a newly characterized non-canonical complex …

Iterative design and optimization of initially inactive proteolysis targeting chimeras (PROTACs) identify VZ185 as a potent, fast, and selective von Hippel–Lindau (VHL) …

V Zoppi, SJ Hughes, C Maniaci, A Testa… - Journal of medicinal …, 2018 - ACS Publications
Developing PROTACs to redirect the ubiquitination activity of E3 ligases and potently
degrade a target protein within cells can be a lengthy and unpredictable process, and it …

Lysine acetylation goes global: from epigenetics to metabolism and therapeutics

I Ali, RJ Conrad, E Verdin, M Ott - Chemical reviews, 2018 - ACS Publications
Post-translational acetylation of lysine residues has emerged as a key regulatory
mechanism in all eukaryotic organisms. Originally discovered in 1963 as a unique …

DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic-and acquired-degrader resistance

M Schröder, M Renatus, X Liang, F Meili… - Nature …, 2024 - nature.com
Targeted protein degradation (TPD) mediates protein level through small molecule induced
redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal …

Degradation of the BAF complex factor BRD9 by heterobifunctional ligands

D Remillard, DL Buckley, J Paulk… - Angewandte Chemie …, 2017 - Wiley Online Library
The bromodomain‐containing protein BRD9, a subunit of the human BAF (SWI/SNF)
nucleosome remodeling complex, has emerged as an attractive therapeutic target in cancer …

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 …

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 …

Glioma tumor suppressor candidate region gene 1 (GLTSCR1) and its paralog GLTSCR1-like form SWI/SNF chromatin remodeling subcomplexes

A Alpsoy, EC Dykhuizen - Journal of Biological Chemistry, 2018 - ASBMB
The mammalian SWI/SNF chromatin remodeling complex is a heterogeneous collection of
related protein complexes required for gene regulation and genome integrity. It contains a …