The microtubule dysregulation is associated with many diseases including cancer and neurodegenerative diseases such as Alzheimer’s Disease, Parkinson’s Disease, and ALS, making them an important diagnostic and therapeutic target. PET is a non-invasive molecular imaging technique currently used for in vivo imaging. Although this imaging technique is powerful, imaging the brain is challenging because the radiotracers used must be capable of crossing the blood-brain barrier (BBB). There are currently no PET tracers available for the in vivo imaging of microtubules in the brain. However, scientists, led by Professor J. John Mann, at the Columbia University Medical Center developed a radiolabeled microtubule binding agent that enables positron emission tomography (PET) imaging of microtubules in the brain for diagnosis and treatment monitoring of tumours and neurological disease.

Microtubules (MTs) are highly abundant throughout the cytoskeleton, and their dysfunction is implicated in the pathogenesis of malignancies, various neurodegenerative disorders, and brain injuries. This innovative development can satisfy a big demand of CNS-penetrating PET tracer for in vivo microtubule imaging. It identifies high-affinity microtubule-binding agents that can be radiolabeled with carbon-11 (11C) or fluorine-18 (18F). These agents are small enough to penetrate the BBB and are used for radiolabeling microtubules in the central nervous system (CNS) and other parts of the body. These radiolabeled microtubule binding agents enable live in vivo PET and single photon emission computed tomography (SPECT) imaging that can be used to look at tumours, neuropsychiatric, and neurodegenerative disorders.

[11C]MPC-6827 was synthesized and shown to cross the BBB and distribute rapidly to multiple brain regions in imaging studies. These agents can be applied in PET or SPECT diagnostic imaging and treatment monitoring not only of brain tumours but of neurodegenerative diseases including Alzheimer’s or Parkinson’s disease. Furthermore, such non-invasive method provides diagnosis and treatment monitoring of traumatic brain injury, psychiatric disorders, and other microtubule-associated diseases in the brain and peripheral body parts. In addition, the other application of this technique is that it can help to quantitate the disease progression and remission.