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He then took a senior researcher position in Dusseldorf before moving to the University of Halle-Wittenberg as a full professor in His main interests are focussed on medicinal chemistry, computational chemistry and drug design Manfred Jung is Professor for Pharmaceutical and Medicinal Chemistry at the Albert-Ludwigs University of Freiburg Germany.

He obtained a Ph. Durst at the University of Ottawa Canada. In he started his own group at the Institute of Pharmaceutical Chemistry at the University of Munster and in he moved to Freiburg to his current position. His main research focus is the synthesis of enzyme inhibitors and in-vitro assay development in the field of histone modifying enzymes. Free Access. Tools Get online access For authors. Email or Customer ID. Forgot password?

Old Password. New Password. Password Changed Successfully Your password has been changed. Returning user. Arthritis Rheum. This paper provided early evidence of epigenetic alterations correlating with disease status in SLE and RA. Absher, D. Rakyan, V. Identification of type 1 diabetes-associated DNA methylation variable positions that precede disease diagnosis.

Mastronardi, F.

Epigenetics in Melanoma Development and Drug Resistance

Bos, S. Graves, M. Fukuhara, T. Lian, X. Lu, Q. Demethylation of the same promoter sequence increases CD70 expression in lupus T cells and T cells treated with lupus-inducing drugs. Jiang, H. Wang, Y. Kennedy, A. A novel upstream enhancer of FOXP3 , sensitive to methylation-induced silencing, exhibits dysregulated methylation in rheumatoid arthritis Treg cells. Li, Y. Diabetes Res. Hori, S. Control of regulatory T cell development by the transcription factor Foxp3.

Cribbs, A. Treg cell function in rheumatoid arthritis is compromised by CTLA-4 promoter methylation resulting in a failure to activate the indoleamine 2,3-dioxygenase pathway. Association between enhanced type I collagen expression and epigenetic repression of the FLI1 gene in scleroderma fibroblasts. Epigenetic repression of bone morphogenetic protein receptor II expression in scleroderma. Dees, C. Karouzakis, E. DNA hypomethylation in rheumatoid arthritis synovial fibroblasts.

Nakano, K. DNA methylome signature in rheumatoid arthritis. Tak, P. Rheumatoid arthritis and p how oxidative stress might alter the course of inflammatory diseases. Today 21 , 78—82 Ai, R. DNA methylome signature in early rheumatoid arthritis synoviocytes compared with longstanding rheumatoid arthritis synoviocytes. This paper describes emerging evidence for epigenetic changes becoming apparent early in RA disease progression. Calabrese, R.

Database construction and content

TET2 gene expression and 5-hydroxymethylcytosine level in multiple sclerosis peripheral blood cells. Acta , — Zhao, M. Hu, N. Zhang, P. Aberrant histone modification in peripheral blood B cells from patients with systemic sclerosis. Wada, T. Aberrant histone acetylation contributes to elevated interleukin-6 production in rheumatoid arthritis synovial fibroblasts.

Buckley, C. The resolution of inflammation. Sorm, F. Experimentia 20 , — Cellular differentiation, cytidine analogs and DNA methylation. Cell 20 , 85—93 Lu, L. Mechanism of 5-azacytidine-induced transfer RNA cytosinemethyltransferase deficiency. Cancer Res. Lee, T. Inhibition of protein synthesis in 5-azacytidine-treated HeLa cells.

Almstedt, M. Lal, G. Wu, C. The DNA methylation inhibitor 5-azacytidine increases regulatory T cells and alleviates airway inflammation in ovalbumin-sensitized mice. Allergy Immunol. Chan, M. Mangano, K. Zheng, Q. Dunn, J. Flow-dependent epigenetic DNA methylation regulates endothelial gene expression and atherosclerosis. Cao, Q. Endocrinology , — Guo, H.

Inhibiting cardiac allograft rejection with interleukin therapy combined with decitabine treatment in mice. Goodyear, O. Azacitidine augments expansion of regulatory T cells after allogeneic stem cell transplantation in patients with acute myeloid leukemia AML. Adair, S. Cancer Immunol. Dubovsky, J. Treatment of chronic lymphocytic leukemia with a hypomethylating agent induces expression of NXF2, an immunogenic cancer testis antigen. Wang, L. Decitabine enhances lymphocyte migration and function and synergizes with CTLA-4 blockade in a murine ovarian cancer model.

Kadoch, C. Biochemistry 55 , — Su, I. Polycomb group protein Ezh2 controls actin polymerization and cell signaling. He, S. The histone methyltransferase Ezh2 is a crucial epigenetic regulator of allogeneic T-cell responses mediating graft-versus-host disease. The polycomb repressive complex 2 governs life and death of peripheral T cells. Yang, X. EZH2 is crucial for both differentiation of regulatory T cells and T effector cell expansion. Tough, D. Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review Fang, T.

Histone H3 lysine 9 di-methylation as an epigenetic signature of the interferon response. Gregoretti, I. Molecular evolution of the histone deacetylase family: functional implications of phylogenetic analysis. Bantscheff, M. Khan, O. HDAC inhibitors in cancer biology: emerging mechanisms and clinical applications. Lobera, M. Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group. Cantley, M. Inflammopharmacology 21 , — Hu, E. Identification of novel isoform-selective inhibitors within class i histone deacetylases.

Jochems, J. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology 39 , — Schlimme, S. Carbamate prodrug concept for hydroxamate HDAC inhibitors. ChemMedChem 6 , — Greer, C. Histone deacetylases positively regulate transcription through the elongation machinery.


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Cell Rep. Grabiec, A. Histone deacetylase inhibitors suppress rheumatoid arthritis fibroblast-like synoviocyte and macrophage IL-6 production by accelerating mRNA decay. Leoni, F. The antitumor histone deacetylase inhibitor suberoylanilide hydroxamic acid exhibits antiinflammatory properties via suppression of cytokines. USA 99 , — Early evidence of the ability of HDAC inhibition to modulate cytokine production and inflammation. The histone deacetylase inhibitor ITF reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo.

Li, S.


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Specific inhibition of histone deacetylase 8 reduces gene expression and production of proinflammatory cytokines in vitro and in vivo. Mishra, N. Inhibition of histone deacetylase 6 improves long-term survival in a lethal septic model. Trauma Acute Care Surg. Histone deacetylase inhibition by sodium valproate regulates polarization of macrophage subsets. DNA Cell Biol. Wang, B. Butyrate inhibits functional differentiation of human monocyte-derived dendritic cells. Frikeche, J. Impact of valproic acid on dendritic cells function. Immunobiology , — Brogdon, J.

Histone deacetylase activities are required for innate immune cell control of Th1 but not Th2 effector function. Bosisio, D. Blocking T H polarizing cytokines by histone deacetylase inhibitors in vitro and in vivo. Leukocyte Biol. Su, R. Epigenetic regulation of established human type 1 versus type 2 cytokine responses. Allergy Clin. Arbez, J. Histone deacetylase inhibitor valproic acid affects plasmacytoid dendritic cells phenotype and function.

Tao, R. Deacetylase inhibition promotes the generation and function of regulatory T cells. Waibel, M. Manipulation of B-cell responses with histone deacetylase inhibitors. Chung, Y. A therapeutic strategy uses histone deacetylase inhibitors to modulate the expression of genes involved in the pathogenesis of rheumatoid arthritis. Choi, J. Trichostatin A attenuates airway inflammation in mouse asthma model. Allergy 35 , 89—96 Hartman, H. Histone deacetylase regulates trypsin activation, inflammation, and tissue damage in acute pancreatitis in mice.

Introduction

Marumo, T. Histone deacetylase modulates the proinflammatory and -fibrotic changes in tubulointerstitial injury. Renal Physiol. Zhao, T. Zhang, L. Histone deacetylase inhibitors attenuate acute lung injury during cecal ligation and puncture-induced polymicrobial sepsis. World J. Camelo, S. Transcriptional therapy with the histone deacetylase inhibitor trichostatin A ameliorates experimental autoimmune encephalomyelitis.

Glauben, R. Regna, N. Reddy, P. Histone deacetylase inhibitor suberoylanilide hydroxamic acid reduces acute graft-versus-host disease and preserves graft-versus-leukemia effect. USA , — Joosten, L. Inhibition of HDAC activity by ITF ameliorates joint inflammation and prevents cartilage and bone destruction in experimental arthritis. Lewis, E. Histone hyperacetylation is associated with amelioration of experimental colitis in mice. Nishida, K. Hsieh, I. Preclinical anti-arthritic study and pharmacokinetic properties of a potent histone deacetylase inhibitor MPT0G Cell Death Dis.

Inhibiting histone deacetylase 1 suppresses both inflammation and bone loss in arthritis. Rheumatology 54 , — Nakamura, T. Schroeder, T. Histone deacetylase inhibitors promote osteoblast maturation. Bone Miner. Histone deacetylase inhibitors suppress inflammatory activation of rheumatoid arthritis patient synovial macrophages and tissue. Gillespie, J. Histone deacetylases are dysregulated in rheumatoid arthritis and a novel histone deacetylase 3-selective inhibitor reduces interleukin-6 production by peripheral blood mononuclear cells from rheumatoid arthritis patients.

Furlan, A. Pharmacokinetics, safety and inducible cytokine responses during a phase 1 trial of the oral histone deacetylase inhibitor ITF givinostat. Choi, S. Histone deacetylase inhibition regulates inflammation and enhances Tregs after allogeneic hematopoietic cell transplantation in humans. Bodar, E. Effects of the histone deacetylase inhibitor ITF in autoinflammatory syndromes.

Vojinovic, J. Safety and efficacy of an oral histone deacetylase inhibitor in systemic-onset juvenile idiopathic arthritis. First evidence of clinical efficacy for HDAC inhibition in patients with juvenile arthritis. Kong, S. The class III histone deacetylase sirtuin 1 in immune suppression and its therapeutic potential in rheumatoid arthritis. Genomics 40 , — Gao, X. Immunomodulatory activity of resveratrol: suppression of lymphocyte proliferation, development of cell-mediated cytotoxicity, and cytokine production.

Zou, T. Sharma, S. Xuzhu, G. Resveratrol modulates murine collagen-induced arthritis by inhibiting Th17 and B-cell function. Shindler, K. Oral resveratrol reduces neuronal damage in a model of multiple sclerosis. Dittenhafer-Reed, K. Catalysis and mechanistic insights on sirtuin activation. ChemBioChem 12 , — Hubbard, B. Evidence for a common mechanism of SIRT1 regulation by allosteric activators. Jia, Y.

Ichikawa, T. Sirtuin 1 activator SRT suppresses inflammation in an ovalbumin-induced mouse model of asthma. Respirology 18 , — Hoffmann, E. Pharmacokinetics and tolerability of SRT, a first-in-class small molecule activator of SIRT1, after single and repeated oral administration in man. Libri, V. Filippakopoulos, P. The bromodomain interaction module. Chung, C. Small molecule bromodomain inhibitors: extending the druggable genome.

Targeting epigenetics for cancer therapy

Barda, S. Expression of BET genes in testis of men with different spermatogenic impairments. Jang, M. Cell 19 , — Anand, P. BET bromodomains mediate transcriptional pause release in heart failure. Zhang, W. Lamonica, J. Bromodomain protein Brd3 associates with acetylated GATA1 to promote its chromatin occupancy at erythroid target genes.

USA , E—E Huang, B. Shi, J. Disrupting the interaction of BRD4 with diacetylated twist suppresses tumorigenesis in basal-like breast cancer. Cancer Cell 25 , — Nicodeme, E. Suppression of inflammation by a synthetic histone mimic. References and are the first disclosures of BET inhibitors and their function in regulating inflammation. Selective inhibition of BET bromodomains. Noel, J. Cancer Ther.

Epigenetic targets in the diagnosis and treatment of prostate cancer

Mirguet, O. Zhang, G. Fish, P. Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. Khmelnitsky, Y. In vitro biosynthesis, isolation, and identification of predominant metabolites of 2- 4- 2-hydroxyethoxy -3,5-dimethylphenyl -5,7-dimethoxyquinazolin-4 3 H -one RVX Ran, X. Dittmann, A. ACS Chem. Gacias, M. Selective chemical modulation of gene transcription favors oligodendrocyte lineage progression. Belkina, A.

Barrett, E. Wienerroither, S. Regulation of NO synthesis, local inflammation, and innate immunity to pathogens by BET family proteins. Meng, S. BET inhibitor JQ1 blocks inflammation and bone destruction. Dental Res. Qiao, Y. Immunity 39 , — Chan, C. BET bromodomain inhibition suppresses transcriptional responses to cytokine-Jak-STAT signaling in a gene-specific manner in human monocytes.

Toniolo, P. Bandukwala, H. Describes the first demonstration that BET bromodomain inhibition can modulate T H 1 cell differentiation and pathogenicity. Mele, D. BET bromodomain inhibition suppresses T H mediated pathology.

The double bromodomain protein Brd2 promotes B cell expansion and mitogenesis. Stanlie, A. Chromatin reader Brd4 functions in Ig class switching as a repair complex adaptor of nonhomologous end-joining.