| Assay Method Information | |
| | Dose response confirmation of DNMT1 inhibitors in a Fluorescent Molecular Beacon assay |
| Description: | Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1 R03 DA031091-01A1 Assay Provider: Dr. James Stivers, Johns Hopkins University, Baltimore, MD Hypermethylation of CpG dinucleotides in promoter regions of tumor suppressor genes by DNA 5-C-MTases is an important hallmark of human cancers [1-3]. Such reversible epigenetic silencing is a key pathway resulting in loss-of-function phenotypes that promote the growth of many cancers. Examples of genes that have undergone hypermethylation-induced silencing include the genes encoding the cell cycle regulator proteins pIS and p16, the pro-apoptotic effector gene Apaf-1, the mismatch DNA repair gene MLH1, and GSTP1 that codes for the phase 2 enzyme glutathione S-transferase [1, 2, 4-9]. Thus, inhibitors of MTase enzymes have the demonstrated potent |
| Affinity data for this assay | |
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