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2009 MAY 18 ... containing a triple-hemimethylated CpG motive as a recognition sequence for the human methyltransferase Dnmt1," scientists in Munich, Germany report.
"The DNA strands ... carry within these CpG islands dC(F) building blocks that function as mechanism-based inhibitors of the analyzed methyltransferases. In addition, we replaced the phosphodiester ...
2009 OCT 19 ... made at Epizyme in evolving a robust pipeline of first-in-class inhibitors of histone methyltransferase (HMT) enzymes involved in cancer," said Epizyme chief executive officer Kazumi ...
2009 JUN 15 ... will have their tumor tissue assessed for methylation of the MGMT (methylguanine-DNA methyltransferase) gene promoter. This gene promoter acts as a controlling element in the expression of ... is the first in a new class of investigational anti-cancer therapies called integrin inhibitors having reached Phase III development. These are thought to work by targeting tumor cells ...
2009 JUL 27 ... (Molecular Modeling and Molecular Dynamics Studies of Hydralazine with Human DNA Methyltransferase 1. Chemmedchem, 2009;4(5):792-799). For additional information, contact N. ... of DNA methylation. Despite the different scaffolds of other non-nucleoside DNMT inhibitors such as procaine and procainamide, the current modeling work reveals that these drugs ...
2009 JUN 8 ... "Mixed lineage leukemia (MLL) is a histone methyltransferase that activates gene transcription and associates with menin. In multiple endocrine ... the MLL promoter region and used small interfering RNA for MLL and specific inhibitors for signal transduction pathways. A strong correlation between MILL and p27(Kip1) mRNA ...
2009 JUL 27 ... is a potent inhibitor of S-adenosylhomocysteine hydrolase, which regulates cellular methyltransferase activity. In the present study, we sought to determine the effect of c3Ado on vascular ... "This was accompanied by an increased expression of the cyclin-dependent kinase inhibitors p21(WAF1/Cip1), p27(Kip1), a decreased expression of G1/S phase cyclins, and a lack of ...
2009 OCT 5 ... cells. However, treatment of cells with inhibitors of histone deacetylase (HDAC) and DNA methyltransferase (DNMT) enzymes indicated that epigenetic mechanisms are involved in the down-regulation ...
2009 JUN 29 ... in human malignancies. In this article, we report that parthenolide 1) inhibits DNA methyltransferase 1 (DNMT1) with an IC50 of 3.5 mc M, possibly through alkylation of the proximal thiolate ... to be a hallmark of various tumors. Modulation of DNA methylation with DNA methylation inhibitors has been shown to result in cancer cell differentiation or apoptosis and represents a ...
2009 AUG 17 ... methoxy derivatives catalyzed by the soluble or membrane-bound form of the catechol-O-methyltransferase (COMT)," scientists in Homburg, Germany report. "As all three compounds ... enantiomers. Furthermore, the catecholic metabolites were identified to be uncompetitive inhibitors of the sCOMT localized in HLC.." Meyer and colleagues published their ...
2009 AUG 24 ... "Betaine-homocysteine S-methyltransferase (BHMT) catalyzes the transfer of a methyl group from betaine to L-homocysteine, yielding ... dimethylglycine and L-methionine. In this study, we prepared a new series of BHMT inhibitors," scientists in Prague, Czech Republic report. "The inhibitors were ...
2009 JUN 29 ... Fresh data on acute myeloid leukemia are presented in the report 'The DNA methyltransferase inhibitors azacitidine, decitabine and zebularine exert differential effects on cancer gene ...
2009 AUG 17 ... expression were observed in clinical sarcomas. Importantly, histone deacetylase and DNA methyltransferase inhibitors were able to induce more ubiquitous expression levels of cancer-germline antigens in ...
2009 JUL 13 ... agents on 5-FU cytotoxicity." "We investigated the effect of a DNA methyltransferase (DNMT) inhibitor, zebularine (Zeb), on the chemosensitivity of 5-FU and cisplatin (CDDP) ... investigated due to potential harmful effects in the clinical application of DNMT inhibitors." Suzuki and colleagues published their study in Cancer Chemotherapy and ...
2009 NOV 16 ... for enzyme catalysis. In the adrenaline-synthesizing enzyme PNMT (phenylethanolamine N-methyltransferase), minor changes in substituents can convert substrates into inhibitors." ...
2009 AUG 17 ... show that DZNep acts through a different pathway than 5-aza-2'-deoxycytidine, a DNA methyltransferase inhibitor. These observations give us interesting insight into how chromatin structure ... of drugs that target these processes is therefore important for cancer therapy. Inhibitors of DNA methylation and histone deacetylation have been approved by the Food and Drug ...
2009 NOV 2 ... the loss of chromosomes 1p and 19q and the epigenetic silencing of the methylguanine-DNA methyltransferase (MGMT) gene," wrote J. Ruiz and colleagues, Wake Forest University. The ... establish the role of newer targeted therapies including small-molecule tyrosine kinase inhibitors in patients with newly diagnosed and recurrent LGG." Ruiz and colleagues ...
2009 JUN 29 ... PARP inhibitors alone and in combination with non-cytotoxic concentrations of DNA methyltransferase inhibitor, 5' aza-2'-deoxycytidine and/or the histone deacetylase inhibitor, MS275,. ...
2009 AUG 3 ... 5-azacytidine, epigenetic therapies have been added to the anticancer armamentarium. DNA methyltransferase (DNMT) inhibitors such as 5-aza-2'-deoxycytidine or 5-azacytidine have been approved in ...
2009 JUN 29 ... include concomitant treatment with inhibitors of dopa decarboxylase (DDC) and catechol-O-methyltransferase (COMT) to prolong the peripheral levodopa half-life and increase CNS bioavailability. ...
