Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 136 for “"HDAC"”.
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Development Of Elisa-Based Hdac Activity Assay For Identification Of Isoform Selective Hdac Inhibitors
… drugs that inhibit histone deacetylase (HDAC) proteins. HDACs are histone modifying enzymes that regulate transcription of genes. Aberrant recruitment of HDACs to the transcription factors leads to tumor onset and growth. Because of their potential anti-cancer therapeutic interest, …
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An improved synthesis of the HDAC inhibitor trichostatin A
<p>Histone deacetylase inhibitors (HDIs) have found a wide variety of medicinal uses and are most noted for their specific apoptotic action towards cancer cells. Several hydroxamate HDIs have since been moved on to phase 1 and 2 clinical drug trials, with one having already been approved for …
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Isoform-Selective HDAC Inhibition for the Treatment of Lupus Nephritis
… to contribute to disease. Histone deacetylases (HDACs) are a class of enzymes that hydrolyze the lysine bound acetyl group in both histone and non-histone proteins thereby altering protein structure and function. While the use of pan-HDAC inhibitors has proven to be effective for the treatment of …
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Targeting Histone Deacetylases (Hdac) For The Treatment of Soft Tissue Sarcoma
<p><strong>Targeting Histone deacetylases (HDAC) for the </strong><strong>treatment of genetically complex soft tissue sarcoma</strong></p> <p>Histone deactylase inhibitors (HDACi) are a new class of anticancer therapeutics; however, little is known about HDACi or the individual contribution of …
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Development Of Novel Radiotracers For Pet Imaging Of Hdac-Mediated Epigenetic Regulation
… transferases (HATs) and histone deacetylases (HDACs), respectively. To date, the vast majority of studies on epigenetic regulation have been conducted in cell cultures and tissue samples using conventional methodologies of molecular and cellular biology, which contain inherent limitations for …
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Integration of class 1 HDAC inhibitors into current treatments for prostate cancer
… regulators, including histone deacetylases (HDAC), are commonly mutated and highly expressed in cancer, representing attractive clinical targets. Although five HDAC inhibitors (HDACi) have been FDA approved for myelodysplastic syndromes, evaluation of pan-HDACi in CaP clinical trials as …
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Genomic Analysis of Chemo-Resistance to HDAC inhibitor in Gastric Cancer cells
Histone deacetylase inhibitors (HDACis) are a promising class of anticancer epigenetic drugs, however, molecular factors influencing the responses of individual tumors to HDACi therapies remain obscure. Here, we sought to identify genes associated with HDACi resistance in gastric cancer. Treating a …
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Entwicklung eines HTS-geeigneten Enzymtests für Histondeacetylasen zur Entwicklung von HDAC-Inhibitoren
… die entscheidende Rolle der Histondeacetylasen (HDAC) bei der Pathogenese von bestimmten Tumoren erkannt und diese folgerichtig als wichtiges molekulares Zielenzym eingestuft. Die Entwicklung von selektiven und hoch potenten Inhibitoren für diese Enzyme wurde damit zum erklärten Ziel der …
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Dual mTOR/HDAC Inhibition: Preclinical Development of a Novel Breast Cancer Therapy
… controlled by intracellular histone deacetylase (HDAC) activity as well. In fact, HDAC inhibitors that have been implemented into clinical practice are capable of overcoming resistance to HER2 and ER targeted therapeutics, in part by inducing the degradation of oncogenic transcripts. Given this …
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CYCLIZATION-BASED SITE-SELECTIVE N-TERMINAL CYSTEINE CONJUGATION, PEPTIDE STAPLING AND HISTONE DEACETYLASE (HDAC) PROBING
… the real-time activity of histone deacetylases (HDACs).
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Delineating mechanisms which underlie differential cell fates induced by p53 activation and HDAC inhibition in colorectal cancer
… of nuclear Class-I Histone deacetylases (HDACi) is effective in enhancing p53- dependent apoptotic cell death in multiple models of CRC. Interestingly, despite a notable switch in phenotype from cell cycle arrest to cell death, few changes in the mRNA and protein expression of …
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Ligandi ibridi Sigma-HDAC come potenziale trattamento terapeutico per il melanoma uveale: design, sintesi e valutazione biologica
… alcune isoforme dell’enzima istone deacetilasi (HDAC), come potenziali target per il trattamento del melanoma uveale. Come riportato in letteratura, i recettori σ sono presenti a livello uveale (iride e corpo ciliare) e, come abbiamo riportato in recenti studi preliminari, alcuni ligandi …
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HDAC inhibition results in suppression of FOXM1 and genes associated with poor prognosis prostate cancer through p53 dependent and independent mechanisms
… also known to be suppressed by p53. <br/><br/>HDACi are an emerging class of epigenetic modifying anti-cancer agents that we hypothesise will enhance p53 mediated cell death, whilst also altering patterns of gene expression to target p53-dependent and independent vulnerabilities in PCa. Using …
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Development of chemical inducers of dimerization for screening competitive histone deactelyase inhibitors
<p>Histone Deacetylase (HDAC) proteins are transcriptional regulators that affect histone proteins, which are involved in packaging of DNA into chromosomes. HDACs have been linked to the proliferation of cancer through their role in transcriptional regulation. Due to these findings, HDAC inhibitors …
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The structural requirements of histone deacetylase (hdac) inhibitors: suberoylanilide hydroxamic acid (saha) analogues modified at c3, c6, and c7 positions enhance selectivity
<p>Histone deacetylase (HDAC) proteins are targets for drug design towards the treatment of cancers since overexpression of HDAC is linked to cancer. Several HDAC inhibitors, including the FDA approved drug suberoylanilide hydroxamic acid (SAHA, Vorinostat), have cleared clinical trials and emerged …
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Histone deacetylase inhibitors as novel neuroprotective agents in in vitro and in vivo models of Parkinson’s disease
Histone deacetylases (HDAC) shift the balance towards chromatin condensation and silence gene expression. Aberrant recruitment of HDACs to alter transcription suggests the use of HDAC inhibitors (HDAC-Is) as potential therapeutic candidates for neurodegenerative disorders such as Parkinson’s …
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Identification of substrate-selective histone deacetylases and their inhibitors that mediate HER2 transcript stability
… include the utilization of histone deacetylase (HDAC) inhibitors. It has been observed that HDAC inhibitors can induce the rapid decay of oncogenic transcripts such as the HER2 mRNA, though the mechanism underlying this process remains undefined. Earlier observations in our lab led to speculation …
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Untersuchungen zur Assoziation des transkriptionellen Repressors Snail aus Drosophila melanogaster mit den Korepressoren CtBP und HDAC1
… (HAT) bzw. Histon-Deacetylasen (HDAC) reversibel modifiziert werden. Histon-Acetylierung destabilisiert vermutlich die Chromatinstruktur und ermöglicht so, dass Transkriptionsfaktoren und/oder die generelle RNA-Polymerase II Transkriptionsmaschinerie an Zielgene binden und deren …
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The Role of Histone Deacetylases in Cytokine Regulation in Human Gestational Tissues
… little is known about histone deacetylases (HDACs) in the placenta and membranes. The overall aim of this research was to investigate the role of histone deacetylases in cytokine regulation in human gestational tissues. HDAC expression was characterised in term placental, amnion and …
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Investigation of the Role of Histone Acetylation in Hippocampus-Dependent Memory Formation
… pharmacologically blocking histone deacetylases (HDAC) enhances long-term memory formation. Memory enhancement by HDAC inhibitors requires the interaction between the transcription factor CREB and CBP, suggesting that these two processes converge at functionally relevant target genes. As reviewed …
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