Genetic and Epigenetic Drug Targets in Myelodysplastic Syndromes

2016 ◽  
Vol 22 (999) ◽  
pp. 1-1
Author(s):  
Karmen Stankov ◽  
Sunčica Stankov ◽  
Jasmina Katanić
Keyword(s):  
Myelodysplastic Syndromes ◽  
Drug Targets ◽  
Epigenetic Drug

INSIDE INDUSTRY

2012 ◽  
Vol 16 (07) ◽  
pp. 54-57
Keyword(s):  
Drug Targets ◽  
Next Generation ◽  
Support Design ◽  
Energy Investment ◽  
Packaging Technology ◽  
Cell Therapies ◽  
National Geographic ◽  
Lead Compounds ◽  
Sartorius Stedim Biotech ◽  
Epigenetic Drug

German biotech innovator Altona Diagnostics launches BioNexus-certified regional hub in Malaysia: ADT Biotech Sdn Bhd. FEI launches "Explore the Unseen" image contest in partnership with National Geographic. BIO applauds Representative Kaptur's Energy Investment Act of 2012. Cytori to utilize Sistemic's SistemQC™ to strengthen understanding of mechanisms & support design of Next-Generation Cell Therapies. Bosch packaging technology and Sartorius Stedim Biotech introduce PreVAS. CellCentric and ZoBio enter into partnership to develop lead compounds against epigenetic drug targets.

scholarly journals Genome-bound enzymes as epigenetic drug targets in cancer

Epigenomics ◽  
2019 ◽  
Vol 11 (13) ◽  
pp. 1463-1467
Author(s):  
Karol Bomsztyk ◽  
Yuliang Wang
Keyword(s):  
Drug Targets ◽  
Epigenetic Drug

scholarly journals Molecular Structure, Binding Affinity, and Biological Activity in the Epigenome

2020 ◽  
Vol 21 (11) ◽  
pp. 4134 ◽  
Author(s):  
Balázs Zoltán Zsidó ◽  
Csaba Hetényi
Keyword(s):  
Molecular Structure ◽  
Biological Activity ◽  
Binding Affinity ◽  
Drug Targets ◽  
New Drugs ◽  
Titration Calorimetry ◽  
Activity Data ◽  
Theoretical Approaches ◽  
Emerging Trends ◽  
Epigenetic Drug

Development of valid structure–activity relationships (SARs) is a key to the elucidation of pathomechanisms of epigenetic diseases and the development of efficient, new drugs. The present review is based on selected methodologies and applications supplying molecular structure, binding affinity and biological activity data for the development of new SARs. An emphasis is placed on emerging trends and permanent challenges of new discoveries of SARs in the context of proteins as epigenetic drug targets. The review gives a brief overview and classification of the molecular background of epigenetic changes, and surveys both experimental and theoretical approaches in the field. Besides the results of sophisticated, cutting edge techniques such as cryo-electron microscopy, protein crystallography, and isothermal titration calorimetry, examples of frequently used assays and fast screening techniques are also selected. The review features how different experimental methods and theoretical approaches complement each other and result in valid SARs of the epigenome.

scholarly journals Next-generation of selective histone deacetylase inhibitors

RSC Advances ◽  
2019 ◽  
Vol 9 (34) ◽  
pp. 19571-19583 ◽  
Author(s):  
Feifei Yang ◽  
Na Zhao ◽  
Di Ge ◽  
Yihua Chen
Keyword(s):  
Cancer Treatment ◽  
Histone Deacetylase ◽  
Histone Deacetylases ◽  
Drug Targets ◽  
Histone Deacetylase Inhibitors ◽  
Next Generation ◽  
Epigenetic Drug

Histone deacetylases (HDACs) are clinically validated epigenetic drug targets for cancer treatment.

Multimodal HDAC Inhibitors with Improved Anticancer Activity

2017 ◽  
Vol 18 (1) ◽  
pp. 39-56 ◽  
Author(s):  
Rainer Schobert ◽  
Bernhard Biersack
Keyword(s):  
Anticancer Activity ◽  
Histone Deacetylases ◽  
Drug Targets ◽  
Hdac Inhibitors ◽  
Hydroxamic Acids ◽  
Zinc Binding ◽  
Tumor Aggressiveness ◽  
Epigenetic Drug ◽  
Intrinsic Drug Resistance ◽  
Derivatives Of

Histone deacetylases (HDACs) play a significant role in the proliferation and dissemination of cancer and represent promising epigenetic drug targets. The HDAC inhibitor vorinostat featuring a zinc-binding hydroxamate fragment was already clinically approved. However, HDAC inhibitors containing hydroxamic acids are often hampered by acquired or intrinsic drug resistance and may lead to enhanced tumor aggressiveness. In order to overcome these drawbacks of hydroxamate HDAC inhibitors, a series of multimodal derivatives of this compound class, including such with different zinc-binding groups, was recently developed and showed promising anticancer activity. This review provides an overview of the chemistry and pleiotropic anticancer modes of action of these conceptually new HDAC inhibitors.

scholarly journals Epigenetic mechanisms in schizophrenia

2014 ◽  
Vol 16 (3) ◽  
pp. 405-417 ◽  
Keyword(s):  
Genome Organization ◽  
Drug Targets ◽  
Therapeutic Potential ◽  
Regulatory Mechanisms ◽  
Pharmacological Treatments ◽  
Major Psychiatric Disorder ◽  
Metabolic Genes ◽  
Epigenetic Drug ◽  
And Function ◽  
Genome Scale

Schizophrenia is a major psychiatric disorder that lacks a unifying neuropathology, while currently available pharmacological treatments provide only limited benefits to many patients. This review will discuss how the field of neuroepigenetics could contribute to advancements of the existing knowledge on the neurobiology and treatment of psychosis. Genome-scale mapping of DMA methylation, histone modifications and variants, and chromosomal loopings for promoter-enhancer interactions and other epigenetic determinants of genome organization and function are likely to provide important clues about mechanisms contributing to dysregulated expression of synaptic and metabolic genes in schizophrenia brain, including the potential links to the underlying genetic risk architecture and environmental exposures. In addition, studies in animal models are providing a rapidly increasing list of chromatin-regulatory mechanisms with significant effects on cognition and complex behaviors, thereby pointing to the therapeutic potential of epigenetic drug targets in the nervous system.

scholarly journals Resveratrol and Related Compounds as Antioxidants With an Allosteric Mechanism of Action in Epigenetic Drug Targets

2013 ◽  
pp. 1-13 ◽  
Author(s):  
H. FARGHALI ◽  
N. KUTINOVÁ CANOVÁ ◽  
N. LEKIĆ
Keyword(s):  
Drug Targets ◽  
Molecular Mechanisms ◽  
High Capacity ◽  
Basic Research ◽  
Clinical Results ◽  
Allosteric Mechanism ◽  
Epigenetic Drug ◽  
Allosteric Mechanisms ◽  
Amp Activated Protein Kinase ◽  
Related Compounds

The present review is intended to focus on naturally occurring cytoprotective agents such as resveratrol (trans-3,4’,5-trihydroxystilbene) and other related compounds, probably with similar molecular mechanisms of action and high capacity to find applications in medical fields. Several physiological aspects have been ascribed to resveratrol and similar compounds. Resveratrol, among others, has been recently described as a silent information regulator T1 (SIRT1) activator that increases AMP-activated protein kinase (AMPK) phosphorylation and reduces the oxidative damage biomarkers during aging in laboratory settings. The reports on resveratrol and other SIRT1 activators from various sources are encouraging. The pharmacological strategies for modulation of sirtuins by small molecules through allosteric mechanisms should gain a greater momentum including human research. Resveratrol and resveratrol-like molecules seem to fulfill the requirement of a new horizon in drug research since these molecules cover a growing research means as antioxidants with allosteric mechanism in epigenetic drug targets. However, one should keep in mind the challenges of extrapolation of basic research into clinical results. Overall, the issue of sirtuins in biology and disease provides an insight on therapeutic potentials of sirtuin-based therapeutics and demonstrates the high complexity of drug-targeting these modalities for human applications.

Sign in / Sign up

Export Citation Format

Share Document