Novel pH Selective, Highly Lytic Peptides Based on a Chimeric Influenza Hemagglutinin Peptide/Cell Penetrating Peptide Motif.

Delivery of macromolecular cargos such as siRNA to the cytosol after endocytosis remains a critical challenge. Numerous approaches including viruses, lipid nanoparticles, polymeric constructs, and various peptide-based approaches have yet to yield a general solution to this delivery issue. In this manuscript, we describe our efforts to design novel endosomolytic peptides that could be used to facilitate the release of cargos from a late endosomal compartment.

Development of a fluorescence polarization binding assay for folate receptor.

Folate receptor (FR) has been actively investigated for targeted delivery of therapeutics into cancer cells because this receptor is selectively and highly expressed in carcinomas. Because FR rapidly cycles between the cell surface and cytoplasm, folic acid conjugated to a therapeutic agent can drive targeted therapeutic delivery to cancer cells. We prepared a novel fluorescent ligand Cy5-folate and used it to develop a fluorescence polarization (FP) FR binding assay to determine the binding affinities of FR-targeted molecules.

Development of a fluorescence polarization binding assay for asialoglycoprotein receptor.

Asialoglycoprotein receptor (ASGP-R) has been actively investigated for targeted delivery of therapeutic agents into hepatocytes because this receptor is selectively and highly expressed in liver and has a high internalization rate. Synthetic cluster glycopeptides (e.g.