Poster Presentation 11th Australian Peptide Conference 2015

Cell-penetrating Phylomer peptides can successfully deliver the dominant-negative Myc mutant Omomyc and induce apoptosis in breast cancer cells  (#179)

Nadia Milech 1 , Heique Bogdawa 1 , Paula Cunningham 1 , Yew-Foon Tan 1 , Scott Winslow 1 , Emanuela Ferrari 1 , Ferrer Ong 1 , Maria Kerfoot 1 , Brooke Longville 1 , Susanna Juraja 1 , Mark Anastasas 1 , Clinton Hall 1 , Shane Stone 1 , Marie Scobie 1 , Rob Dewhurst 1 , Laura Florez 1 , Karen Kroeger 2 , Anabel Sorolla Bardaji 3 , Edina Wang 3 , Pilar Blancafort 3 , Katrin Hoffmann 1 , Richard Hopkins 2 , Paul Watt 2
  1. Telethon Institute for Child Health Research, Subiaco, WA, Australia
  2. Phylogica, Subaico, Western Australia, Australia
  3. Harry Perkins Research Institute, Nedlands, WA, Australia

Phylomers are a class of peptides derived from fragments of biodiverse microbial genomes. The vast majority of cell-penetrating peptides (CPPs) identified to date are inefficient at intracellular delivery, as they often remain trapped within the endosomal compartment.  This inefficiency has limited the feasibility of intracellular biologics. We have used Phylomer libraries to identify new CPPs for the delivery of macromolecules and nanoparticles into cells. Here we assess the ability of these novel cell-penetrating Phylomer peptides to deliver a functional cargo, Omomyc. The dominant-negative Omomyc is a c-Myc-derived basic, helix-loop-helix, leucine zipper (bHLHZip) mutant that is able to dimerize with c-Myc. Therefore, Omomyc competes with the formation of c-Myc/MAX complex and supresses transcription activation. The overexpression of Myc is involved in many types of human malignancies and in vivo overexpression of Omomyc strongly inhibits Myc-induced oncogenesis. However, Omomyc alone does not efficiently cross the cell membrane. Therefore, to achieve delivery of the Omomyc payload into breast cancer cells, we have produced a recombinant Phylomer-Omomyc fusion protein. We demonstrate that this Phylomer-Omomyc fusion effectively induces apoptosis in triple negative, drug resistant breast cancer cells and is more potent than Omomyc itself.