Visualization of anti-cancer targeted drug delivery using NIR fluorescent switchable reporters

Gary Gellerman, Chemical Sciences, Ariel, Ariel, Israel (garyg@ariel.ac.il)
Leonid Patsenker, Chemical Sciences, Ariel, Ariel, Israel

Visualization of a drug delivery is an essential topic in effective monitoring of drug release. It is especially important requirement in the targeted drug delivery (TDD) for securing the release of the drug at the target and for further optimization of drug conjugation method.  This research aims to provide a new approach for designing novel theranostic tools — peptide drug conjugates for targeted therapy of cancer. These conjugates, having a dimension of about 5 nm, comprise an anticancer drug linked biodegradably to a novel near-infrared dye — switchable reporter (SFR is in the non-fluorescent “Off” form), conjugated with a cancer-specific peptide. Peptide carrier is specific to the overexpressed receptors in solid tumors, providing receptor specific mediated drug delivery. Cleavage of the biodegradable linker in targeted cancer cells results in the release of drug and the increase of the SFR fluorescence intensity (“On” form).

Such an approach will provide a NIR light controlled, targeted therapy of cancer cells, reduced side-effects, and fluorescence monitoring.

1. A. Rozovsky, L. Patsenker, G. Gellerman. Bifunctional reactive pentamethine cyanine dyes for biomedical applications. Dyes & Pigments (2019), 162, 18-25.
2. E. Ragozina, A. Hesin, A. Bazylevich, H. Tuchinsky, A. Bovina, M.A. Firer, M.Y. Sherman, G. Gellerman. New somatostatin-drug conjugates for effective targeting pancreatic cancer.  Bioorganic & Medicinal Chemistry 26 (2018) 3825–3836.
3. M. Bokan, K. Bondar, V. Marks, G. Gellerman, L. Patsenker. Switchable Phenolo-Cyanine Reporters for Fluorescence-Based Targeted Drug Delivery Monitoring. Dyes & Pigments 159 (2018) 18–27.

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Abstract Reference & Short Personal Biography of Presenting Author

Prof. Gary Gellerman received his Ph.D degre from Tel Aviv University in Organic Chemistry in 1994. After completing his doctorate, Prof. Gellerman engaged in research in the field of drug development in pharmaceutical companies. In 2005 he received a position in Ariel University as a senior Lecturer in department of Biological Chemistry. Since 2015, Professor Gellerman holds a deanship of the Faculty of Natural Sciences. His main research interests are: drug design and targeted drug delivery.