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Articles
Balancing Histone/Protein Acetylation: Gene Regulation and Cancer Therapy
A highly sophisticated mechanism organizes the 2-meter long human genome within a 6-μm wide nucleus. Up to 10,000-fold of compaction of the chromatin is achieved during mitosis, allowing faithful seg...
Min-Hao Kuo
LSI Volume 7 Article 1
Keywords: Acetylations, Anaerobic, Apoptosis, Biochemistry, Cancer, Catalysis, Cell division, Cell proliferation, Chromatin immunoprecipitation, Clinical, DNA replication, Degradations, Environmental, Enzymology, Gene expression, Genetic, Genetics, Hormones, Immunoprecipitation, Indicators, Mass spectrometry, Metal organic frameworks, Methylations, Microarray Analysis, Molecular biology, Phase transitions, Phosphorylations, Recombination, Substitutions, Transcription
Carcinogenesis and Epigenetics
Cancer research has revealed that the classical model of carcinogenesis, a three step process consisting of initiation, promotion, and progression, is not complete. The expansion of the carcinogenesi...
Vicki Caligur
BioFiles 2008, 3.5, 18.
Keywords: Acetylations, Adhesion, Alkylations, Apoptosis, Cancer, Carcinogens, Cell division, Cell proliferation, Cell signaling, DNA microarrays, Drug discovery, Environmental, Epigenetics, Gene expression, Genetic, Hormones, Metabolism, Methylations, Microarray Analysis, Mutagens, PAGE, Recombination, Reductions, Transcription, transformation
Histone Modification and Chromatin Remodeling
Gene expression is governed by complex mechanisms including transcription factor binding to DNA and coordinated changes in chromatin structure. The primary protein components of chromatin are the his...
Savita Bagga, PhD.
BioFiles v7 n3, 2012, 10–16
Keywords: Acetylations, Amplification, Cancer, Cell culture, Chromatin immunoprecipitation, Cloning, DNA purification, Diseases, Gene expression, Immunoprecipitation, Indicators, Methylations, Microarray Analysis, PAGE, Polymerase chain reaction, Polymerase chain reaction - quantitative, Polymorphisms, Purification, Sequencing, Transcription, Whole genome amplification
Papers
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Survival Motor Neuron Gene 2 Silencing By DNA Methylation Correlates With Spinal Muscular Atrophy Disease Severity And Can Be Bypassed By Histone Deacetylase Inhibition. Hauke, J., et al. Hum. Mol. Genet. 18, 304-17, (2009)
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A Positive Regulatory Role For The MSin3A-HDAC Complex In Pluripotency Through Nanog And Sox2. Baltus, G.A., et al. J. Thorac. Cardiovasc. Surg. 284, 6998-7006, (2009)
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Effects Of Levetiracetam And Valproate On Reproductive Endocrine Function Studied In Human Ovarian Follicular Cells. Taubøll, E., et al. Epilepsia 50, 1868-74, (2009)
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Novel Functional Residues In The Core Domain Of Histone H2B Regulate Yeast Gene Expression And Silencing And Affect The Response To DNA Damage. Kyriss, M.N., et al. Mol. Cell. Biol. 30, 3503-18, (2010)
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Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides. Antonello Mai et al J. Med. Chem. 48, 3344-53, (2005)
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Azolylchromans as a novel scaffold for anticonvulsant activity. Saeed Emami et al Bioorg. Med. Chem. Lett. 16, 1803-6, (2006)
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Chemical genetics reveals a complex functional ground state of neural stem cells Diamandis, P., et. al. Nat. Chem. Biol. 3(5), 268-273, (2007)
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Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential. Dennis J Pelletier et al J. Chem. Inf. Model. 47, 1196-205, (2007)
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Anticonvulsant activity of some xanthone derivatives. Henryk Marona et al Bioorg. Med. Chem. 16, 7234-44, (2008)
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Synthesis and anticonvulsant activities of N-benzyl (2R)-2-acetamido-3-oxysubstituted propionamide derivatives. Pierre Morieux et al Bioorg. Med. Chem. 16, 8968-75, (2008)
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Synthesis and CNS depressant activity of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. Varsha Jatav et al Eur. J. Med. Chem. 43, 135-41, (2008)
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CNS depressant and anticonvulsant activities of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. Varsha Jatav et al Eur. J. Med. Chem. 43, 1945-54, (2008)
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Lacosamide isothiocyanate-based agents: novel agents to target and identify lacosamide receptors. Ki Duk Park et al J. Med. Chem. 52, 6897-911, (2009)
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Synthesis and potential anticonvulsant activity of new N-3-substituted 5,5-cyclopropanespirohydantoins. Qifeng Zhu et al Eur. J. Med. Chem. 44, 296-302, (2009)
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Synthesis, anticonvulsant and CNS depressant activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea. Sushil K Kashaw et al Eur. J. Med. Chem. 44, 4335-43, (2009)
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Synthesis and anticonvulsant activities of (R)-N-(4'-substituted)benzyl 2-acetamido-3-methoxypropionamides. Christophe Salomé et al J. Med. Chem. 53, 1288-305, (2010)
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Merging the Structural Motifs of Functionalized Amino Acids and α-Amino amides: Compounds with Significant Anticonvulsant Activities Salome, C.; et al. J. Med. Chem. 53, 3756-3771, (2010)
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Novel semicarbazones based 2,5-disubstituted-1,3,4-oxadiazoles: one more step towards establishing four binding site pharmacophoric model hypothesis for anticonvulsant activity. Harish Rajak et al Bioorg. Med. Chem. Lett. 20, 4168-72, (2010)
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Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. Francisco J Prado-Prado et al Bioorg. Med. Chem. 18, 2225-31, (2010)
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Developing structure-activity relationships for the prediction of hepatotoxicity. Nigel Greene et al Chem. Res. Toxicol. 23, 1215-22, (2010)
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Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening. Nadeem Siddiqui et al Eur. J. Med. Chem. 45, 1536-43, (2010)
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N'-[(5-chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)methylene] 2/4-substituted hydrazides: synthesis and anticonvulsant activity. Darpan Kaushik et al Eur. J. Med. Chem. 45, 3943-9, (2010)
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Design & synthesis of 2-(substituted aryloxy)-5-(substituted benzylidene)-3-phenyl-2,5-dihydro-1H-[1,2,4] triazin-6-one as potential anticonvulsant agents. Darpan Kaushik et al Eur. J. Med. Chem. 45, 3960-9, (2010)
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Synthesis and anticonvulsant activity of N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives. Xianran He et al Eur. J. Med. Chem. 45, 5870-7, (2010)
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Neural computational prediction of oral drug absorption based on CODES 2D descriptors. A Guerra et al Eur. J. Med. Chem. 45, 930-40, (2010)
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A predictive ligand-based Bayesian model for human drug-induced liver injury. Sean Ekins et al Drug Metab. Dispos. 38, 2302-8, (2010)
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Primary amino acid derivatives: substitution of the 4'-N'-benzylamide site in (R)-N'-benzyl 2-amino-3-methylbutanamide, (R)-N'-benzyl 2-amino-3,3-dimethylbutanamide, and (R)-N'-benzyl 2-amino-3-methoxypropionamide provides potent anticonvulsants with pain-attenuating properties. Amber M King et al J. Med. Chem. 54, 6417-31, (2011)
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Defining the Structural Parameters That Confer Anticonvulsant Activity by the Site-by-Site Modification of (R)-N'-Benzyl 2-Amino-3-methylbutanamide A. M. King, et al., J. Med. Chem. 54, 6432-6442, (2011)
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Imidazolylchromanone oxime ethers as potential anticonvulsant agents: Anticonvulsive evaluation in PTZ-kindling model of epilepsy and SAR study. Saeed Emami et al Bioorg. Med. Chem. Lett. 21, 655-9, (2011)
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Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. Xian-Qing Deng et al Eur. J. Med. Chem. 46, 2955-63, (2011)
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Design & synthesis of N'-[substituted] pyridine-4-carbohydrazides as potential anticonvulsant agents. Laxmi Tripathi et al Eur. J. Med. Chem. 46, 509-18, (2011)
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Design and synthesis of 2-(1, 3-dioxoisoindolin-2-yl)-N-(4-oxo-2-substitutedthiazolidin-3-yl) acetamide derivatives as potential anticonvulsant agents. Anna Pratima G Nikalje et al Eur. J. Med. Chem. 46, 5448-55, (2011)
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Design and synthesis of novel 7-aminoquinazoline derivatives: Antitumor and anticonvulsant activities. Adel S El-Azab et al Bioorg. Med. Chem. Lett. 22, 1879-85, (2012)
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Synthesis and anticonvulsant evaluation of some new 2,3,8-trisubstituted-4(3H)-quinazoline derivatives. Adel S El-Azab et al Bioorg. Med. Chem. Lett. 22, 327-33, (2012)
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Design, synthesis and anticonvulsant evaluation of novel N-(4-substituted phenyl)-2-[4-(substituted) benzylidene]-hydrazinecarbothio amides. Laxmi Tripathi et al Eur. J. Med. Chem. 47, 153-66, (2012)
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Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-yl)-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones. Xianran He et al Eur. J. Med. Chem. 48, 338-46, (2012)
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Modelling of the pharmacodynamic interaction between phenytoin and sodium valproate. Della Paschoa, O.E., et al. Br. J. Pharmacol. 125, 1610-1616, (1998)
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Cholinergic stimulation of early growth response-1 DNA binding activity requires protein kinase C and mitogen-activated protein kinase kinase activation and is inhibited by sodium valproate in SH-SY5Y cells. Grimes, C.A. and Jope, R.S. J. Neurochem. 73, 1384-1392, (1999)
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Merck 14,9913