Carola Tilgmann, Piero Pollesello, Martti Ovaska, Juha Kaivola, Jarmo Pystynen, Eija Tiainen, Marjo Yliperttula, Arto Annila and Jouko Levijoki Discovery and Structural Characterization of a Phospholamban-Binding Cyclic Peptide and Design of Novel Inhibitors of Phospholamban Chemical Biology & Drug Design 81
Article first published online: 6 JUN 2012 | DOI: 10.1111/j.1747-0285.2012.01409.x
Molecules able to interfere with the inhibitory activity of phospholamban (PLB) on SERCA2a were discovered. PLB was used as target for a phage display peptide library screening. The cyclic peptide C-Y-W-E-L-EW-L-P-C-A was found to bind to PLB and interfere with its activity. Its structure was determined and a model of this interaction with PLB was built. A pharmacophore was defined and used for the design of small molecules. Examples of such molecules were synthesized and characterized as phospholamban inhibitors.
Complete the form below and we will send an e-mail message containing a link to the selected article on your behalf