BIOT 216 |
| We have been investigating the conjugation of photosensitizing agents for the photodynamic therapy of cancer to certain peptide sequences in order to improve their specific delivery to targeted cells and organelles. The peptide signaling sequences investigated include cell penetrating peptides (CPP) and nuclear or mitochondria localization sequences (NLS, MLS). Our studies show that conjugates of photosensitizers to CPP or NLS/MLS peptides have enhanced photoactivity in vitro compared with the non-conjugated photosensitizers. The biological efficacy of the conjugates depends on the nature and sequence of the amino acids, the porphyrin peripheral substituents, the linker, their conformation(s) in aqueous solutions, amphiphilic character and metabolic stability. We will report our most recent results on the synthesis and properties of photosensitizer conjugates to one or more linear bifunctional peptide(s) composed of CPP and NLS or MLS peptide chains. Their uptake, subcellular localization, phototoxicity and enzymatic stability were investigated in human carcinoma HEp2 cells. |
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Biophysical and Biomolecular Symposium: Targeted Delivery of Proteins & Nucleotides
3:00 PM-5:20 PM, Wednesday, August 22, 2007 BCEC -- 106, Oral
Division of Biochemical Technology |