Thirty years of HDAC inhibitors: 2020 insight and hindsight
It is now 30 years since the first report of a potent zinc-dependent histone deacetylase
(HDAC) inhibitor appeared. Since then, five HDAC inhibitors have received regulatory …
(HDAC) inhibitor appeared. Since then, five HDAC inhibitors have received regulatory …
Recent developments of HDAC inhibitors: Emerging indications and novel molecules
AD Bondarev, MM Attwood, J Jonsson… - British journal of …, 2021 - Wiley Online Library
The histone deacetylase (HDAC) enzymes, a class of epigenetic regulators, are historically
well established as attractive therapeutic targets. During investigation of trends within …
well established as attractive therapeutic targets. During investigation of trends within …
Lysine acetylation goes global: from epigenetics to metabolism and therapeutics
Post-translational acetylation of lysine residues has emerged as a key regulatory
mechanism in all eukaryotic organisms. Originally discovered in 1963 as a unique …
mechanism in all eukaryotic organisms. Originally discovered in 1963 as a unique …
Glioblastoma: Current status, emerging targets, and recent advances
Glioblastoma (GBM) is a highly malignant brain tumor characterized by a heterogeneous
population of genetically unstable and highly infiltrative cells that are resistant to …
population of genetically unstable and highly infiltrative cells that are resistant to …
[PDF][PDF] Chromatin repressive complexes in stem cells, development, and cancer
A Laugesen, K Helin - Cell stem cell, 2014 - cell.com
The chromatin environment is essential for the correct specification and preservation of cell
identity through modulation and maintenance of transcription patterns. Many chromatin …
identity through modulation and maintenance of transcription patterns. Many chromatin …
[HTML][HTML] Common stemness regulators of embryonic and cancer stem cells
C Hadjimichael, K Chanoumidou… - World journal of stem …, 2015 - ncbi.nlm.nih.gov
Pluripotency of embryonic stem cells (ESCs) and induced pluripotent stem cells is regulated
by a well characterized gene transcription circuitry. The circuitry is assembled by ESC …
by a well characterized gene transcription circuitry. The circuitry is assembled by ESC …
Induction of LIFR confers a dormancy phenotype in breast cancer cells disseminated to the bone marrow
Breast cancer cells frequently home to the bone marrow, where they may enter a dormant
state before forming a bone metastasis. Several members of the interleukin-6 (IL-6) cytokine …
state before forming a bone metastasis. Several members of the interleukin-6 (IL-6) cytokine …
The sphingosine 1-phosphate receptor modulator fingolimod as a therapeutic agent: Recent findings and new perspectives
A Huwiler, U Zangemeister-Wittke - Pharmacology & therapeutics, 2018 - Elsevier
The immunomodulatory drug fingolimod (FTY720, Gilenya R) was approved for oral
treatment of relapsing-remitting multiple sclerosis, due to its impressive efficacy and good …
treatment of relapsing-remitting multiple sclerosis, due to its impressive efficacy and good …
[HTML][HTML] Roles of histone deacetylases and inhibitors in anticancer therapy
Histones are the main structural proteins of eukaryotic chromatin. Histone acetylation/
deacetylation are the epigenetic mechanisms of the regulation of gene expression and are …
deacetylation are the epigenetic mechanisms of the regulation of gene expression and are …
PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes
We have identified a proteolysis targeting chimera (PROTAC) of class I HDACs 1, 2 and 3.
The most active degrader consists of a benzamide HDAC inhibitor, an alkyl linker, and the …
The most active degrader consists of a benzamide HDAC inhibitor, an alkyl linker, and the …