Histone deacetylases (HDACs): evolution, specificity, role in transcriptional complexes, and pharmacological actionability

G Milazzo, D Mercatelli, G Di Muzio, L Triboli… - Genes, 2020 - mdpi.com
Histone deacetylases (HDACs) are evolutionary conserved enzymes which operate by
removing acetyl groups from histones and other protein regulatory factors, with functional …

Epidrug repurposing: discovering new faces of old acquaintances in cancer therapy

M Montalvo-Casimiro, R González-Barrios… - Frontiers in …, 2020 - frontiersin.org
Gene mutations are strongly associated with tumor progression and are well known in
cancer development. However, recently discovered epigenetic alterations have shown the …

Target engagement and drug residence time can be observed in living cells with BRET

MB Robers, ML Dart, CC Woodroofe… - Nature …, 2015 - nature.com
The therapeutic action of drugs is predicated on their physical engagement with cellular
targets. Here we describe a broadly applicable method using bioluminescence resonance …

Ribosomal elongation of cyclic γ-amino acids using a reprogrammed genetic code

T Katoh, H Suga - Journal of the American Chemical Society, 2020 - ACS Publications
Because γ-amino acids generally undergo rapid self-cyclization upon esterification on the
carboxyl group, for example, γ-aminoacyl-tRNA, there are no reports of the ribosomal …

Cytotoxicity mediated by histone deacetylase inhibitors in cancer cells: mechanisms and potential clinical implications

DS Schrump - Clinical Cancer Research, 2009 - AACR
Aberrant expression of epigenetic regulators of gene expression contributes to initiation and
progression of cancer. During recent years, considerable research efforts have focused on …

[HTML][HTML] Natural compound histone deacetylase inhibitors (HDACi): synergy with inflammatory signaling pathway modulators and clinical applications in cancer

H Losson, M Schnekenburger, M Dicato, M Diederich - Molecules, 2016 - mdpi.com
The remarkable complexity of cancer involving multiple mechanisms of action and specific
organs led researchers Hanahan and Weinberg to distinguish biological capabilities …

S-adenosylhomocysteine hydrolase inhibition by 3-deazaneplanocin A analogues induces anti-cancer effects in breast cancer cell lines and synergy with both histone …

A Hayden, PWM Johnson, G Packham… - Breast cancer research …, 2011 - Springer
Epigenetic abnormalities including abnormal histone methyltransferase activity contribute to
breast cancer pathogenesis. An example is over expression of the polycomb repressive …

Differential response of cancer cells to HDAC inhibitors trichostatin A and depsipeptide

J Chang, DS Varghese, MC Gillam, M Peyton… - British journal of …, 2012 - nature.com
Background: Over the last decade, several drugs that inhibit class I and/or class II histone
deacetylases (HDACs) have been identified, including trichostatin A, the cyclic depsipeptide …

Real-time imaging of histone H4K12–specific acetylation determines the modes of action of histone deacetylase and bromodomain inhibitors

T Ito, T Umehara, K Sasaki, Y Nakamura, N Nishino… - Chemistry & biology, 2011 - cell.com
Histone acetylation constitutes an epigenetic mark for transcriptional regulation. Here we
developed a fluorescent probe to visualize acetylation of histone H4 Lys12 (H4K12) in living …

Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets

MGJ Baud, T Leiser, P Haus, S Samlal… - Journal of medicinal …, 2012 - ACS Publications
Psammaplin A (11c) is a marine metabolite previously reported to be a potent inhibitor of two
classes of epigenetic enzymes: histone deacetylases and DNA methyltransferases. The …