SYNTHESIS AND EVALUATION OF MULTIVALENT LIGANDS TARGETING MELANOMA

picture of Kara Saunders presenting his/her poster: SYNTHESIS AND EVALUATION OF MULTIVALENT LIGANDS TARGETING MELANOMA

Kara Saunders , Kevin Nguyen, Nabila Brabez, Victor J. Hruby

SYNTHESIS AND EVALUATION OF MULTIVALENT LIGANDS TARGETING MELANOMA

Melanoma, the most aggressive form of skin cancer, consists of mutated cells marked by overexpression of the melanocortin 1 receptor (MC1R) on the cellular surface, a G-protein coupled receptor (GPCR). GPCR’s are an ideal family of receptors for drug targeting because of their prevalence in the human body and because of their ability to ultimately generate a cellular response when a ligand is bound to the receptor. Targeting of these receptors via multivalent interactions allows for a method leading to earlier detection and a drug delivery mechanism to be used as specific treatment. Previous research has shown that binding affinity of the ligands increases with valency of the multimeric ligands. In this study, we aim to use multivalent interactions to create a ligand highly selective for the MC1R receptor. Synthesis of the multivalent ligands (bivalent, trivalent, hexavalent, etc.) includes a scaffold to which all melanotropin (MSH sequences) ligands are attached with a linker. In vivo studies are done by attachment of a fluorescent probe, Cy5 rather than radioactive labeling. Results from the assays indicate binding affinity at lower concentrations for the trivalent ligands as opposed to bivalent and monovalent ligands. Funding for this project is provided by Office of the Provost.

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