Rose Bengal-Amphiphilic Peptide Conjugate for Enhanced Photodynamic Therapy of Malignant Melanoma

Simanpreet Kaur Dhillon, Simon Porter, Nermeen Rizk, Yingjie Sheng, Thomas McKaig, Kathryn Burnett, Bronagh White, Heather Nesbitt, Rubeta N. Matin, Anthony P. McHale, Bridgeen Callan, J Callan

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Malignant melanoma is an aggressive skin cancer with poor survival outcomes for patients diagnosed at an advanced stage. While targeted serine/threonine-protein kinase B-Raf (BRAF) and immune checkpoint inhibitors have improved survival outcomes for a proportion of these patients, response rates remain variable. There is a need, therefore, for more effective treatments to bolster the options available for melanoma patients. In this manuscript, we covalently attached Rose Bengal (RB) to the amphipathic peptide (AMP) C(KLAKLAK)2 and determined the effectiveness of the resulting RB-C(KLAKLAK)2 conjugate as a photodynamic therapy (PDT) sensitizer. RB-C(KLAKLAK)2-mediated PDT treatment of subcutaneous B16-F10-Luc2 tumors in C57 mice resulted in lesions that were 479% smaller at the end of the study than animals treated with RB-mediated PDT. The synergistic effect between RB and C(KLAKLAK)2 has been attributed to the AMP sensitizing cells to reactive oxygen species (ROS), making them more susceptible to ROS-induced oxidative stress.
Original languageEnglish
Pages (from-to)1328-1336
Number of pages9
JournalJournal of Medicinal Chemistry
Volume63
Issue number3
Early online date15 Jan 2020
DOIs
Publication statusPublished - 13 Feb 2020

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