Development of [18F]Maleimide-Based Glycogen Synthase Kinase-3β Ligands for Positron Emission Tomography Imaging for Positron Emission Tomography Imaging

Novel 18F-labeled GSK3β inhibitors that can cross the blood brain barrier.


Dysregulation of Glycogen Synthase Kinase 3β (GSK3β) is associated with several neurodegenerative diseases, such as Parkinson’s, Alzheimer's and Huntington's. Therefore, development of a selective GSK3β PET tracer would enable both, early detection of its aberrant activity and facilitate therapeutic drug discovery. However, efforts to develop a potent tracer has remained unsuccessful due to either poor penetration of the blood-brain-barrier (BBB) and/ or short half life of traditional radio-label conjugate, 11C, used as a radio-label.

Technology Overview:

Researchers at Stony Brook University have developed novel 18F radiolabeled GSK3β inhibitors. 18F radiolabeling offer several advantages to these inhibitors:


Long half life (t1/2 = 109.7m) which eliminates the reliance on in-house cyclotron thus facilitating wide spread use.

Better spatial resolution and image quality due to short range positron emission. Additionally, these compounds are highly potent (IC50 = 1.7nM) and have been demonstrated to cross BBB in rodents (Figure 1.).

Further Details:


Hu et al. ACS Medicinal Chemistry Letters, 8, 287-292, 2017


Longer t1/2 of 18F ( vs traditional 11C) labeled tracers

Demonstrated brain penetration

Improved spatial resolution and image quality

High potency


- Medical Imaging

- Diagnostics 

- Therapeutics



Intellectual Property Summary:

Patent application submitted

Stage of Development:

PCT application covering compositions and methods of use (PCT/US18/13446).

Licensing Potential:

Licensing Status:

Additional Information:

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Please note, header image is purely illustrative. Source: SciBiograph, Wikimedia Commons, CC BY-SA 4.0, edited.

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