Synthesis of a novel series of thiazole-based histone acetyltransferase inhibitors.

[1]  P. Casali,et al.  Combinatorial H3K9acS10ph histone modification in IgH locus S regions targets 14-3-3 adaptors and AID to specify antibody class-switch DNA recombination. , 2013, Cell reports.

[2]  K. Capaccione,et al.  The Notch signaling pathway as a mediator of tumor survival. , 2013, Carcinogenesis.

[3]  Jian Luo,et al.  Small-Molecule Inhibitors of Acetyltransferase p300 Identified by High-Throughput Screening Are Potent Anticancer Agents , 2013, Molecular Cancer Therapeutics.

[4]  C. De Monte,et al.  Synthesis and Selective Human Monoamine Oxidase B Inhibition of Heterocyclic Hybrids Based on Hydrazine and Thiazole Scaffolds , 2013, Archiv der Pharmazie.

[5]  S. Carradori,et al.  3-methylcyclohexanone thiosemicarbazone: determination of E/Z isomerization barrier by dynamic high-performance liquid chromatography, configuration assignment and theoretical study of the mechanisms involved by the spontaneous, acid and base catalyzed processes. , 2012, Journal of chromatography. A.

[6]  J. Torchia,et al.  Cellular GCN5 Is a Novel Regulator of Human Adenovirus E1A-Conserved Region 3 Transactivation , 2012, Journal of Virology.

[7]  A. Riggs,et al.  Acetylated STAT3 is crucial for methylation of tumor-suppressor gene promoters and inhibition by resveratrol results in demethylation , 2012, Proceedings of the National Academy of Sciences.

[8]  W. Sippl,et al.  Small Molecule Inhibitors of Histone Acetyltransferases as Epigenetic Tools and Drug Candidates , 2012, Archiv der Pharmazie.

[9]  K. Jeong,et al.  Histone deacetylases 1, 6 and 8 are critical for invasion in breast cancer. , 2011, Oncology reports.

[10]  P. Filetici,et al.  Epigenetic regulation in cancer development. , 2011, Frontiers in bioscience.

[11]  Danny Reinberg,et al.  Chromatin higher-order structures and gene regulation. , 2011, Current opinion in genetics & development.

[12]  H. Haisma,et al.  Isothiazolones; thiol-reactive inhibitors of cysteine protease cathepsin B and histone acetyltransferase PCAF. , 2011, Organic & biomolecular chemistry.

[13]  H. Kikuchi,et al.  GCN5 Regulates the Superoxide-Generating System in Leukocytes Via Controlling gp91-phox Gene Expression , 2011, The Journal of Immunology.

[14]  H. Yoshikawa,et al.  Comparative Studies of Genome-Wide Maps of Nucleosomes between Deletion Mutants of elp3 and hos2 Genes of Saccharomyces cerevisiae , 2011, PloS one.

[15]  J. Denu,et al.  Catalytic activation of histone acetyltransferase Rtt109 by a histone chaperone , 2010, Proceedings of the National Academy of Sciences.

[16]  A. Mai,et al.  Chemogenomic profiling of the cellular effects associated with histone H3 acetylation impairment by a quinoline-derived compound. , 2010, Genomics.

[17]  S. Carradori,et al.  Synthesis, stereochemical separation, and biological evaluation of selective inhibitors of human MAO-B: 1-(4-arylthiazol-2-yl)-2-(3-methylcyclohexylidene)hydrazines. , 2010, Journal of medicinal chemistry.

[18]  Ruben Abagyan,et al.  Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. , 2010, Chemistry & biology.

[19]  M. Fujita,et al.  Novel heart failure therapy targeting transcriptional pathway in cardiomyocytes by a natural compound, curcumin. , 2010, Circulation journal : official journal of the Japanese Circulation Society.

[20]  P. Filetici,et al.  Tuning acetylated chromatin with HAT inhibitors: A novel tool for therapy , 2010, Epigenetics.

[21]  E. Cho,et al.  Association of Global Levels of Histone Modifications with Recurrence-Free Survival in Stage IIB and III Esophageal Squamous Cell Carcinomas , 2010, Cancer Epidemiology, Biomarkers & Prevention.

[22]  H. Haisma,et al.  Reactivity of isothiazolones and isothiazolone-1-oxides in the inhibition of the PCAF histone acetyltransferase. , 2009, European journal of medicinal chemistry.

[23]  H. Haisma,et al.  Histone acetyl transferases as emerging drug targets. , 2009, Drug discovery today.

[24]  M. Giacca,et al.  GCN5-dependent acetylation of HIV-1 integrase enhances viral integration , 2009, Retrovirology.

[25]  S. Agrawal,et al.  Inhibition of Lysine Acetyltransferase KAT3B/p300 Activity by a Naturally Occurring Hydroxynaphthoquinone, Plumbagin* , 2009, The Journal of Biological Chemistry.

[26]  L. Altucci,et al.  Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases. , 2009, Bioorganic & medicinal chemistry letters.

[27]  S. Carradori,et al.  A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl)hydrazone. , 2009, Journal of medicinal chemistry.

[28]  Kyung-Chul Choi,et al.  Epigallocatechin-3-gallate, a histone acetyltransferase inhibitor, inhibits EBV-induced B lymphocyte transformation via suppression of RelA acetylation. , 2009, Cancer research.

[29]  H. Haisma,et al.  Inhibition of the PCAF histone acetyl transferase and cell proliferation by isothiazolones. , 2009, Bioorganic & medicinal chemistry.

[30]  Y. Zou,et al.  Positive roles of SAS2 in DNA replication and transcriptional silencing in yeast , 2008, Nucleic acids research.

[31]  S. Carradori,et al.  High-performance liquid chromatographic separation of enantiomers and diastereomers of 2-methylcyclohexanone thiosemicarbazone, and determination of absolute configuration and configurational stability. , 2007, Journal of chromatography. A.

[32]  T. Kundu,et al.  Specific inhibition of p300-HAT alters global gene expression and represses HIV replication. , 2007, Chemistry & biology.

[33]  J. Murguía,et al.  Yeast on drugs: Saccharomyces cerevisiae as a tool for anticancer drug research , 2007, Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico.

[34]  D. Tindall,et al.  Androgen deprivation increases p300 expression in prostate cancer cells. , 2007, Cancer research.

[35]  L. Verdone,et al.  H4 acetylation does not replace H3 acetylation in chromatin remodelling and transcription activation of Adr1‐dependent genes , 2006, Molecular microbiology.

[36]  L. Altucci,et al.  Small-molecule inhibitors of histone acetyltransferase activity: identification and biological properties. , 2006, Journal of medicinal chemistry.

[37]  A. Khar,et al.  Biological effects of curcumin and its role in cancer chemoprevention and therapy. , 2006, Anti-cancer agents in medicinal chemistry.

[38]  Andrew J. Bannister,et al.  Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity , 2005, Molecular Cancer Therapeutics.

[39]  Udaykumar Ranga,et al.  Curcumin, a Novel p300/CREB-binding Protein-specific Inhibitor of Acetyltransferase, Represses the Acetylation of Histone/Nonhistone Proteins and Histone Acetyltransferase-dependent Chromatin Transcription* , 2004, Journal of Biological Chemistry.

[40]  Athanassios Giannis,et al.  Design, synthesis, and biological evaluation of a small-molecule inhibitor of the histone acetyltransferase Gcn5. , 2004, Angewandte Chemie.

[41]  K. Imai,et al.  Synergistic Effect of Histone Deacetylase Inhibitors FK228 and m-Carboxycinnamic Acid Bis-Hydroxamide with Proteasome Inhibitors PSI and PS-341 against Gastrointestinal Adenocarcinoma Cells , 2004, Clinical Cancer Research.

[42]  Tapas K. Kundu,et al.  Small Molecule Modulators of Histone Acetyltransferase p300* , 2003, Journal of Biological Chemistry.

[43]  R. Roeder,et al.  HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. , 2000, Molecular cell.