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The human epidermal growth factor receptor (EGFR) is a ~180 kDa transmembrane glycoprotein that contains an extracellular domain, a transmembrane domain and an intracellular tyrosine kinase domain. We have recently prepared porphyrin-, phthalocyanine- and boron BODIPY-peptide conjugates that target the extracellular domain of EGFR. These compounds are promising theranostic agents for the diagnosis and treatment of cancers that overexpress EGFR, including breast, ovarian, prostate, and colorectal cancers.1-4 We will present our recent studies on the preparation of these photosensitizer-peptide conjugates and investigations of their EGFR-targeting ability using surface plasmon resonance, molecular modeling, cell culture assays, and animal studies.
References
1. B. G. Ongarora, K. R. Fontenot, X. Hu, I. Sehgal, S. D. Jois and M. G. H. Vicente. Journal of Medicinal Chemistry 2012, 55, 3725-3738.
2. K. R. Fontenot, B. G. Ongarora, L. E. LeBlanc, Z. Zhou, S. D. Jois and M. G. H. Vicente. Journal of Porphyrins and Phthalocyanines 2016, 20, 352-366.
3. N. Zhao, T. M. Williams, Z. Zhou, F. R. Fronczek, M. Sibrian-Vazquez, S. D. Jois and M. G. H. Vicente. Bioconjugate Chemistry 2017, 28, 1566–1579.
4. T. M. Williams, R. Sable, S. Singh, M. G. H. Vicente and S. D. Jois. Chemical Biology & Drug Design 2018, 91, 605-619.
Acknowledgements: The authors thank the US National Institutes of Health and the US National Science Foundation for supporting this research.
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