Histone deacetylases (HDACs): evolution, specificity, role in transcriptional complexes, and pharmacological actionability
Histone deacetylases (HDACs) are evolutionary conserved enzymes which operate by
removing acetyl groups from histones and other protein regulatory factors, with functional …
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 …
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 …
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 …
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 …
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
The remarkable complexity of cancer involving multiple mechanisms of action and specific
organs led researchers Hanahan and Weinberg to distinguish biological capabilities …
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 …
Epigenetic abnormalities including abnormal histone methyltransferase activity contribute to
breast cancer pathogenesis. An example is over expression of the polycomb repressive …
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 …
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 …
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 …
classes of epigenetic enzymes: histone deacetylases and DNA methyltransferases. The …