Chemical Biology – Developing and Testing New Probes and Therapies

Chemical biology involves the use of small molecules to study and affect living systems and can be used to solve complex biological problems such as understanding the mechanisms of disease, the regulation of biological pathways and the roles of different biomolecules in controlling cellular function. Chemical Biology at McMaster

Chemical biology research in the Valliant Research Group involves developing and testing radiolabelled probes that bind biomarkers associated with diseases like cancer.  The group evaluates compounds in cells and pre-clinical models using the latest assay and imaging technologies.  The ultimate aim is to find compounds that can be translated in into human clinical trials through the CPDC.

An example of development programs is:

RADIOLABELLED INSULIN – A TARGET WITH WIDESPREAD IMPACT

Human insulin is a polypeptide involved in the breakdown and storage of sugars. Insulin dysregulation is associated with a number of diseases: diabetes, cancer, obesity and heart failure. Consequently, a labeled form of insulin would aid in the understanding of the role of the hormone in various diseases, and it could become a tool for early disease detection and monitoring the impact of targeted therapies.

The Valliant Research Group has reported on the development of PET and SPECT probes for imaging insulin biodistribution and biochemistry.  This work involves developing ways to link isotopes to the 1B position of the hormone, without impacting the biological activity, and testing the resulting probe on various models. (See J. Med. Chem. 2010 57, 3678-3686 and J. Med. Chem. 2014, 53, 2612-2621)

Human_Insulin
The amino acid sequence of insulin. The disulfide bonds are shown as dark lines.

 

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