Novel compounds allowing for optical detection and targeting of Choline Kinases for cancer treatment.
Choline Kinase (ChoK) deregulation is associated with oncogenesis and tumor progression in a number of human cancers, including glioblastoma, breast, and lung cancers. In breast cancer, elevated ChoK activity is correlated with histological tumor grade, resistance to antiestrogen therapies, and poor prognosis. Overexpression of ChoK alone is sufficient to induce malignant transformation.
The Delikatny Lab at the University of Pennsylvania has developed and synthetized novel cancer theranostics – therapeutics that can also serve as diagnostics – molecules based on ChoK Inhibitors. These small fluorescent molecules used at low doses can be effective as agents to image the status of tumor choline metabolism, at higher doses they can serve as inhibitors of tumor growth.