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Novel Choline Kinase Inhibitors for Cancer Imaging and Therapy

Description:

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. 

 

Applications

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

 

Advantages

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

 

Inventor

Edward Delikatny 

Stage of Development

12 compounds synthesized and prototype compounds tested in vitro

In vivo studies performed on lead compound

Medicinal chemistry studies are underway

A number of in assays evaluating activity of ChoK based on 14C phosphorylation, magnetic resonance spectroscopy, nearinfrared optical imaging have been developed

 

Intellectual Property

Pending PCT application WO2014165216A1

 

Reference Media

Arlauckas, S. P., et.al. 2014. Mol. Cancer Ther. 13(9). 2149-58.

 

Kumar M., et.al. 2015. Mol. Cancer Ther. 14(4). 899-908.

 

Desired partnerships

• License

• Co-development 

 

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Patent Information:
For Information, Contact:
Linara Axanova
Associate Director, PSOM Licensing Group
University of Pennsylvania
axanova@upenn.edu
Inventors:
Edward Delikatny
Keywords:
Cancer