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Discovery of a Selective Histone Deacetylase 6 Degrader (HDAC6 PROTAC) with a Short and Rigid Linker Demonstrating Sustained Knockdown of HDAC6 <i>In Vivo</i>. [PDF]

ACS Med Chem Lett
Ripa L, Cassani C, Hughes G, Ranieri B, Ullah V, Zambelloni R, Andreasson T, Collins M, Lindberg B, Llinas A, Pehrson R, Barylyuk K, Johansson J, Ek M, Gunnarsson A, Jung B, Lundqvist S, Novén A, Sandmark J, Åstrand A.   +19 more
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Histone deacetylase inhibitors

European Journal of Medicinal Chemistry, 2005
AbstractFor Abstract see ChemInform Abstract in Full Text.
BRESSI JEROME C, GANGLOFF ANTHONY R, KWOK LILY   +2 more
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Histone deacetylases

Current Opinion in Pharmacology, 2003
Post-translational modification of the histones of chromatin has a fundamental role in regulating gene expression. Enzymes involved in these epigenetic events include histone deacetylases (class I and class II), which can be inhibited by a structurally diverse group of small molecules.
Paul A, Marks, Thomas, Miller, Victoria M, Richon   +2 more
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Histone Deacetylase Inhibitors

ChemInform, 2003
AbstractFor Abstract see ChemInform Abstract in Full Text.
Thomas A, Miller, David J, Witter, Sandro, Belvedere   +2 more
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Assays for Histone Deacetylases

Current Topics in Medicinal Chemistry, 2009
Epigenetics is defined as heritable changes in gene expression, i.e. the presentation of a certain phenotype, without alterations to the genetic code. This is a central phenomenon in developmental biology but also for the pathogenesis of a variety of diseases, e.g. for cancer in the case of silencing of tumor suppressor proteins.
Hauser, Alexander-Thomas, Jung, Manfred, Jung, Mira   +2 more
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Histone deacetylase in neuropathology

2021
Neuroepigenetics, a new branch of epigenetics, plays an important role in the regulation of gene expression. Neuroepigenetics is associated with holistic neuronal function and helps in formation and maintenance of memory and learning processes. This includes neurodevelopment and neurodegenerative defects in which histone modification enzymes appear to ...
Rohan, Gupta, Rashmi K, Ambasta, Pravir, Kumar   +2 more
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HISTONE DEACETYLASE INHIBITORS

2004
The base sequence of DNA provides the genetic code for proteins. The regulation of expression or suppression of gene transcription is largely determined by the structure of the chromatin--referred to as epigenetic gene regulation (Agalioti et al., 2002; Jenuwein and Allis, 2001; Richards and Elgin, 2002; Spotswood and Turner, 2002; Zhang and Reinberg ...
JOEL SIMON, MARSON CHARLES, SAVY PASCAL
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Histone Deacetylases

2008
Deacetylation of histones is required for gene regulation and cell cycle progression and the mediators, the histone deacetylases, are being vigorously pursued as drug targets for cancer chemotherapy. The deacetylases are also potential drug targets against infectious diseases and genome sequencing revealed proteins of this class in each of three ...
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Histone deacetylases and atherosclerosis

Atherosclerosis, 2015
Atherosclerosis is the most common pathological process that leads to cardiovascular diseases, a disease of large- and medium-sized arteries that is characterized by a formation of atherosclerotic plaques consisting of necrotic cores, calcified regions, accumulated modified lipids, smooth muscle cells (SMCs), endothelial cells, leukocytes, and foam ...
Xia-xia, Zheng, Tian, Zhou, Xin-An, Wang, Xiao-hong, Tong, Jia-wang, Ding   +4 more
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