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| 1 | Inhibition of histone deacetylase for the treatment of biliary tract cancer:A new effective pharmacological approach显示文摘瞄准:调查在试管内和在活体内治疗学的效果嘘胆道癌症上的一 deacetylase 禁止者 NVP-LAQ824 和 NVP-LBH589。方法:由 NVP-LAQ824 和 NVP-LBH589 的房间生长抑制是在由 MTT 试金的 7 根人的胆道癌症房间线的学习在试管内。另外, NVP-LBH589 的 anti-tumoral 效果在一个妄想的老鼠模型被学习。Anti-tumoral 药机制被为 MIB-1 为 acH4 和 p21 弄污 WAF-1/CIP-1, PARP 试金,房间周期分析, TUNEL 试金,和 immunhistochemistry 的免疫估计。结果:有两混合物的在试管内治疗显著地压制了所有癌症房间线的生长[吝啬的 IC50 ( 3 d ) 0.11 和 0.05 mumol/L ,分别地],并且与 nucleosomal 的 hyperacetylation 被联系嘘一 H4 , p21 WAF-1/CIP-1 的增加的表示, apoptosis ( PARP 劈开)感应,并且房间周期在 G2/M 逮捕检查点。在 28 d 以后, NVP-LBH589 显著地减少了在 66% 集体的肿瘤(胆汁管癌) 并且 87%( 胆囊癌症) 与安慰剂相比的在活体内,并且加强 gemcitabine 的功效。揭示的肿瘤标本的进一步的分析由 TUNEL 试金增加了 apoptosis 并且减少了房间增长(MIB-1 ) 。结论:我们的调查结果建议 NVP-LBH589 和 NVP-LAQ824 对人的胆道癌症是活跃的在试管内。另外, NVP-LBH589 表明了重要在活体内活动并且加强 gemcitabine 的功效。因此,为胆道癌症的治疗的这新药的进一步临床的评估被推荐。 | Thilo Bluethner Manuel Niederhagen Karel Caca Frederik Serr Helmut Witzigmann Christian Moebius Joachim Mossner Marcus Wiedmann | 2007 | World Journal of Gastroenterology2007，13，35： | 5 |
| 2 | Experimental treatment of pancreatic cancer with two novel histone deacetylase inhibitors显示文摘AIM:To investigate in vitro and in vivo treatment with histone deacetylase inhibitors NVP-LAQ824 and NVP-LBH589 in pancreatic cancer. METHODS:Cell-growth inhibition by NVP-LAQ824 and NVP-LBH589 was studied in vitro in 8 human pancreatic cancer cell lines using the 3-(4,5-dimethylthiazol-2-yl) -2,5-diphenyltetrazolium bromide(MTT) assay. In addition,the anti-tumoral effect of NVP-LBH589 was studied in a chimeric mouse model. Anti-tumoral activity of the drugs was assessed by immunoblotting for p21WAF-1,acH4,cell cycle analysis,TUNEL assay,and immunohistochemistry for MIB-1. RESULTS:In vitro treatment with both compounds significantly suppressed the growth of all cancer cell lines and was associated with hyperacetylation of nucleosomal histone H4,increased expression of p21WAF-1,cell cycle arrest at G2/M-checkpoint,and increased apoptosis. In vivo,NVP-LBH589 alone significantly reduced tumor mass and potentiated the efficacy of gemcitabine. Further analysis of the tumor specimens revealed slightly increased apoptosis and no significant reduction of cell proliferation.CONCLUSION:Our findings suggest that NVP-LBH589 and NVP-LAQ824 are active against human pancreatic cancer,although the precise mechanism of in vivo drug action is not yet completely understood. Therefore,further preclinical and clinical studies for the treatment of pancreatic cancer are recommended. | Martin Haefner Thilo Bluethner Manuel Niederhagen Christian Moebius Christian Wittekind Joachim Mossner Karel Caca Marcus Wiedmann | 2008 | World Journal of Gastroenterology2008，14，23： | 2 |
| 3 | Circulating selectin and immunogloblin-type adhesion molecules in acute ischemic stroke显示文摘 | Mossner R Motsch L | 1995 | Stroke1995，26，： | 1 |
| 4 | Characterization of diamond-like carbon by raman spectroscopy,XPS and optical constants 显示文摘 | Mossner C Grant P Tran H | 1998 | Thin Solid Films1998，317，： | 1 |
| 5 | Hereditary chronic pancreatitis显示文摘 | Teich N Mossner J | 2008 | Best Pract Res Clin Gastroenterol2008，221，： | 1 |
| 6 | Brain-derived neurotrophic factor V66M polymorphism in childhoodonset obsessivecompulsive disorder 显示文摘 | MOSSNER R WALITZA S LESCH K P | 2005 | Int J Neuropsychopharmacol2005，8，1： | 1 |
| 7 | Role of hypertriglyceridemia in the pathogenesis of experimental acute pancreatitis in rats显示文摘 | Kimura W Mossner J | 1996 | Int J Pacreatol1996，20，3： | 1 |
| 8 | Effects of stem design and material properties on stresses in hip endoprostheses显示文摘 | Rohlmann A Mossner V Bergmann G | 1987 | J Biomed Eng1987，9，1： | 1 |
| 9 | Oligosaccharide reprocessing and recycling of a cell surface glycoprotein in cultured rat hepatocytes 显示文摘 | Kreisel W Hildebrand H Mossner W | 1993 | Biol Chem Hoppe-Seyler1993，374，： | 1 |
| 10 | Myelodysplastic cells in patients reprogram mesenchymal stromal cells to establish a transplantable stem cell niche disease unit 显示文摘 | Medyouf H Mossner M Jann JC | 2014 | Cell Stem Cell2014，14，6： | 1 |
| 11 | Promoter polymorphisms of the genes encoding tumor necrosis factor-alpha and interleukin beta are associated with different subtypes of psoriasis character ized by early and late disease onset显示文摘 | Reich K Mossner R Konig IR | 2002 | J Invest Dermatol2002，118，1： | 1 |
| 12 | Serotonin transporter function is modulated by brain-derived neurotrophic factor (BDNF) but not nerve growth factor (NGF) 显示文摘 | Mossner R Daniel S Albert D | 2000 | Neurochem Int2000，36，3： | 1 |
| 13 | Changes in incidence and prevalence of acute and chronic pancreatitis in Germany显示文摘 | SECKNUS R MOSSNER J | 2000 | Chirurg2000，71，3： | 1 |
| 14 | Functional serotonin 1A receptor variant influences treatment response to atypical antipsychotics in schizophrenia显示文摘 | MOssner R Schuhmacher A Kuhn KU | 2009 | Pharmacogenet Genomics2009，19，1： | 1 |
| 15 | Promoter polymorphisms of the genes encoding tumor necrosis factor-alpha and interleukin beta are associated with different subtypes of psoriasis character ized by early and late disease onset 显示文摘 | Reich K Mossner R Konig IR | 2002 | J Invest Dermatol2002，118，1： | 1 |
| 16 | Role of hypertriglyceridemia in the pathogenesis of experimental acute pancreatitis in rats显示文摘 | Mossner J | 1996 | Int J pancreatol1996，20，3： | 1 |
| 17 | Circulating selectin -amt immunoglobulin - type adhesion molecules in acute ischemic stroke显示文摘 | Fassbender K Mossner R Motsch L | 1995 | Stroke1995，26，8： | 1 |
| 18 | Allelic variation of serotonin transporter expression is associated with depression in Parkinson's disease显示文摘 | Mossner R Henneberg A Schmitt A | 2001 | Mol Psychiatry2001，6，： | 1 |
| 19 | Variations in the genes encoding the peroxisome proliferator-activated receptors α and γ in psoriasis 显示文摘 | Mossner R Kaiser R Matern P | 2004 | Arch Dermatol Res2004，296，1： | 1 |
| 20 | Promotor polymorphisms of the genes encoding tumor necrosis factor-alpha and interleukin- lbets are associated with different stubtypes of proriasis character- ized by early and late disease onset显示文摘 | Reich K Mossner R koning IR | 2002 | J Invest Dematol2002，118，1： | 1 |
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