Tumor imaging by means of proteolytic activation of cell-penetrating peptides
Howard Hughes Medical Institute · University of California San Diego
Abstract
We have devised and tested a new strategy for selectively delivering molecules to tumor cells. Cellular association of polyarginine-based, cell-penetrating peptides (CPPs) is effectively blocked when they are fused to an inhibitory domain made up of negatively charged residues. We call these fusions activatable CPPs (ACPPs) because cleavage of the linker between the polycationic and polyanionic domains, typically by a protease, releases the CPP portion and its attached cargo to bind to and enter cells. Association with cultured cells typically increases 10-fold or more upon linker cleavage. In mice xenografted with human tumor cells secreting matrix metalloproteinases 2 and 9, ACPPs bearing a…
Citation impact
- FWCI
- 7.71
- Percentile
- 100%
- References
- 45
Authors
6- TJTao Jiang
Howard Hughes Medical Institute, University of California San Diego
- ESEmilia S. Olson
Howard Hughes Medical Institute, University of California San Diego
- QTQuyen T. Nguyen
Howard Hughes Medical Institute, University of California San Diego
- MRM. Roy
Howard Hughes Medical Institute, University of California San Diego
- PAPatricia A. Jennings
Howard Hughes Medical Institute, University of California San Diego
Topics & keywords
- Linker
- Proteases
- Cleavage (geology)
- Protease
- In vivo
- Matrix metalloproteinase
- Chemistry
- Extracellular matrix
- Good health and well-being