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- Volume 19, Issue 28, 2013
Current Pharmaceutical Design - Volume 19, Issue 28, 2013
Volume 19, Issue 28, 2013
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Histone Acetylation: From Code to Web and Router Via Intrinsically Disordered Regions
More LessStructural changes of chromatin, which consists of nucleosomes and nucleosome-associated factors, lead to functional changes that are important determinants of eukaryotic gene regulation. These structural changes are regulated by modifications of histones and DNA, both of which are components of nucleosomes, as well as by replacement of histone variants and the actions of noncoding RNAs. In studies of chromatin Read More
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Histone Acetylation in Neurodevelopment
Authors: Antonio Contestabile and Silvia SintoniPost-translational modification of histones is a primary mechanism through which epigenetic regulation of DNA transcription does occur. Among these modifications, regulation of histone acetylation state is an important tool to influence gene expression. Epigenetic regulation of neurodevelopment contributes to the structural and functional shaping of the brain during neurogenesis and continues to impact on neu Read More
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Lysine Acetyltransferases CBP and p300 as Therapeutic Targets in Cognitive and Neurodegenerative Disorders
Authors: Luis M. Valor, Jose Viosca, Jose P. Lopez-Atalaya and Angel BarcoNeuropsychiatric pathologies, including neurodegenerative diseases and neurodevelopmental syndromes, are frequently associated with dysregulation of various essential cellular mechanisms, such as transcription, mitochondrial respiration and protein degradation. In these complex scenarios, it is difficult to pinpoint the specific molecular dysfunction that initiated the pathology or that led to the fatal cascade of event Read More
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Histone Post-translational Modifications to Target Memory-related Diseases
More LessEpigenetic mechanisms, i.e. the control gene of expression without changing DNA sequence, include DNA methylation, histone post-translational modifications (PTMs) and microRNAs (miRNAs). Aberrant epigenetic modifications are associated with several pathological conditions, including brain diseases, resulting from environmental causes, ageing or genetic factors. The role of histone PTMs, including acetylation, phospho Read More
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Phenylbutyrate is a Multifaceted Drug that Exerts Neuroprotective Effects and Reverses the Alzheimer´s Disease-like Phenotype of a Commonly Used Mouse Model
Authors: Mar Cuadrado-Tejedor, Ana L. Ricobaraza, Rosana Torrijo, Rafael Franco and Ana Garcia-Osta4-phenylbutyrate (PBA) is a histone deacetylase (HDAC) inhibitor whose efficacy in the Tg2576 mouse model of Alzheimer´s disease (AD) is correlated with decreased tau phosphorylation, clearance of intraneuronal Aβ and restoration of dendritic spine density in hippocampal CA1 pyramidal neurons. PBA is also a chemical chaperone that facilitates cell proteostasis. To determine the relative contributions of HDAC in Read More
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Histone Post-translational Modifications in Huntington’s and Parkinson’s Diseases
Authors: Luis Emiliano Pena-Altamira, Elisabetta Polazzi and Barbara MontiGene expression is controlled by several epigenetic mechanisms involving post-translational modification of histones (acetylation, phosphorylation and others). These mechanisms in the brain are not only important for normal function but also for the development of pathologies when their derangement does occur. The present review deals with post-translational modifications of histones in two neurodegenerative diseases Read More
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Histone Acetylation as a Potential Therapeutic Target in Motor Neuron Degenerative Diseases
Authors: Lutz Garbes, Markus Riessland and Brunhilde WirthAmong hereditary diseases, the group of motor neuron diseases (MNDs) includes some of the most devastating and rapidly progressive lethal conditions. Although degeneration of motor neurons is common to all of them, the phenotypic spectrum of MNDs is relatively broad and ranges from perinatal conditions like spinal muscular atrophy (SMA) to adult-onset diseases such as amyotrophic lateral sclerosis (ALS). While th Read More
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Potential Roles of HDAC Inhibitors in Mitigating Ischemia-induced Brain Damage and Facilitating Endogenous Regeneration and Recovery
Authors: Emily B. Fessler, Fairouz L. Chibane, Zhifei Wang and De-Maw ChuangIschemic stroke is a leading cause of death and disability worldwide, with few available treatment options. The pathophysiology of cerebral ischemia involves both early phase tissue damage, characterized by neuronal death, inflammation, and blood-brain barrier breakdown, followed by late phase neurovascular recovery. It is becoming clear that any promising treatment strategy must target multiple points in the evoluti Read More
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Factors Affecting Residual Platelet Aggregation in Prasugrel Treated Patients
Identification of factors affecting platelet reactivity (PR) and high PR (HPR) or high platelet inhibition (HPI) rates while on prasugrel maintenance dose (MD) might be helpful in avoiding ischemic or bleeding complications. We retrospectively analyzed all patients (n=233) treated in our institution between April 2010 and November 2012 who had platelet function assessment pre-prasugrel and following prasugrel 10 mg Read More
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Targets for Anti-metastatic Drug Development
Authors: Anna-Maria Stock, Gabriele Troost, Bernd Niggemann, Kurt S. Zanker and Frank EntschladenWith a constant focus on the primary tumor, the current approaches in drug development in oncology yield dismal results. However over 90 percent of cancer deaths today are due to metastasis formation and yet there is no anti-metastatic drug on the market. Tumor cell migration is the essential prerequisite for invasion and metastasis formation. It is regulated by signal substances in terms of the grade of activity and in t Read More
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Cell-free DNA: Characteristics, Detection and its Applications in Myocardial Infarction
Authors: Rongrong Jing, Ming Cui, Huimin Wang and Shaoqing JuMuch attention has been focused on cell-free DNA (cf-DNA) and its levels in the plasma, serum and body fluids of pregnant women and patients with cancer or autoimmune disease, and those with severe trauma; however, knowledge of its biology and relationship with myocardial infarction (MI) is still at an early stage. This paper introduces general aspects of the nomenclature, structure, function, release mechanisms and m Read More
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New Strategy for High Throughput Screening of Anti-Influenza Virus M2 Ion Channel Inhibitors
Authors: Chufang Li, Yan Long, Zuoxian Lin, Yanling Jie, Yajuan Xiao, Lingzhi Yang, Juanjuan Sun, Yizhong Ren, Ling Chen and Zhiyuan LiSince the recent emergence of swine and avian flu, there has been a sense of urgency to discover new anti-influenza drugs. In this study, a stable cell line with M2 ion channel/ enhanced Green fluorescent protein (EGFP) co-expression was established in order to develop an EGFP-based high-throughput assay for screening M2 ion channel inhibitors. This assay directly monitors the proton conductivity of the M2 ion channel by Read More
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Novel Insights into Biased Agonism at G Protein-Coupled Receptors and their Potential for Drug Design
Authors: Maria Marti-Solano, Ramon Guixa-Gonzalez, Ferran Sanz, Manuel Pastor and Jana SelentG-protein coupled receptors (GPCRs) are the most important class of current pharmacological targets. However, it is now widely acknowledged that their regulation is more complex than previously thought: the evidence that GPCRs can couple to several effector pathways, and the existence of biased agonists able to activate them differentially, has introduced a new level of complexity in GPCR drug research. Considering bias re Read More
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Volumes & issues
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Volume 31 (2025)
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Volume 30 (2024)
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Volume 29 (2023)
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Volume 28 (2022)
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Volume 27 (2021)
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Volume 26 (2020)
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Volume 25 (2019)
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Volume 24 (2018)
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Volume 23 (2017)
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Volume 22 (2016)
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Volume 21 (2015)
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Volume 20 (2014)
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Volume 19 (2013)
- Issue 42
- Issue 41
- Issue 40
- Issue 39
- Issue 38
- Issue 37
- Issue 36
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- Issue 31
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- Issue 27
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- Issue 19
- Issue 18
- Issue 17
- Issue 16
- Issue 15
- Issue 28
- Issue 14
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- Issue 12
- Issue 11
- Issue 10
- Issue 9
- Issue 8
- Issue 7
- Issue 6
- Issue 5
- Issue 4
- Issue 3
- Issue 2
- Issue 1
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Volume 18 (2012)
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Volume 17 (2011)
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Volume 16 (2010)
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Volume 15 (2009)
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Volume 14 (2008)
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Volume 13 (2007)
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Volume 12 (2006)
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Volume 11 (2005)
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Volume 10 (2004)
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Volume 9 (2003)
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Volume 8 (2002)
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Volume 7 (2001)
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Volume 6 (2000)
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