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RegenMD Accessing Protein Methyltransferase and Demethylase Enzymology Using Microfluidic Capillary Electrophoresis. July 28, 2010 at 9:13 AM Accessing Protein Methyltransferase and Demethylase Enzymology Using Microfluidic Capillary Electrophoresis. Chem Biol. 2010 Jul 30;17(7):695-704 Authors: Wigle TJ, Provencher LM, Norris JL, Jin J, Brown PJ, Frye SV, Janzen WP The discovery of small molecules targeting the >80 enzymes that add (methyltransferases) or remove (demethylases) methyl marks from lysine and arginine residues, most notably present in histone tails, may yield unprecedented chemotherapeutic agents and facilitate regenerative medicine. To better enable chemical exploration of these proteins, we have developed a highly quantitative microfluidic capillary electrophoresis assay to enable full mechanistic studies of these enzymes and the kinetics of their inhibition. This technology separates small biomolecules, i.e., peptides, based on their charge-to-mass ratio. Methylation, however, does not alter the charge of peptide substrates. To overcome this limitation, we have employed a methylation-sensitive endoproteinase strategy to separate methylated from unmethylated peptides. The assay was validated on a lysine methyltransferase (G9a) and a lysine demethylase (LSD1) and was employed to investigate the inhibition of G9a by small molecules. PMID: 20659682 [PubMed - as supplied by publisher]   Managing More than 300 Grants: CIRM's Thin Ice Question July 28, 2010 at 3:38 AM   This email was sent to regenmd@gmail.com.  Account Login Don't want to receive this feed any longer? Unsubscribe here This email was carefully delivered by Feed My Inbox. 230 Franklin Road Suite 814 Franklin, TN 37064