Novel compounds allowing for optical detection and targeting of choline kinases for cancer treatment.
Problem
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.
Solution
The Delikatny lab at UPenn 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.
diagnostic: fluorescent detection of ChoK in animal models of cancer and human patients
therapeutic: inhibition of ChoK in ChoK overexpressing tumors
measurement of response to therapy in ChoK overexpressing tumors
tumor imaging agent that could be used for intraoperative imaging during cancer surgeries
Lower toxicity and higher selectivity compared to existing ChoK inhibitors
Fluorescence in the NIR range is suitable for detection of ChoK in vivo
Fluorescence in the NIR range has lower light scattering interference from hemoglobin, fat and water
Quantitative detection of ChoK reflecting tumor aggressiveness
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activity
delikatny
novel
cancer
cancers
kinase
inhibitors
tumor
chok
choline
