Protein Biochemistry and Analytics
The Protein Biochemistry and Analytics Group is composed of scientists from a diverse range of backgrounds and this is reflected in its activities. The Group is involved in all stages of the drug discovery process. Early on, new drug targets are cloned, expressed and purified. The recombinant proteins are then characterized using both biochemical and analytical tools. Extremely sensitive mass spectrometry techniques are routinely used to determine molecular masses of the protein targets with accuracies in the range of 1 ppb (part per billion).
The next phase of the process is the development of enzymatic and biophysical assays using reference compounds synthesized by the Medicinal Chemistry Group. State of the art instrumentation enables our researchers to perform kinetic analyses using microfluidic capillary devices and to execute thermodynamic studies using the most up to date calorimetry techniques.
After validation, the assays are ramped up to assess the activity of hits from HTS (high throughput screening), to assess the activity of compounds designed by rational drug design and to aid the SAR (structure activity relationship) in the hit to lead phase. This stage of the drug discovery process can involve the assessment of high numbers of compounds, which necessitates the high throughput capabilities of the Group’s instrumentation. Assay support continues throughout the lead optimisation phase of drug discovery until a development candidate is identified.
The Group also provides biology support during the drug discovery process. This can take the form of cell based assays in our anti-bacterial projects where MIC50 values are generated for a range of model and pathogenic organisms or knock down experiments to validate compound mode of action. Additional target validation data is also routinely generated for example; proteins that interact with our targets can be identified by mass spectrometry techniques. The Protein Biochemistry and Analytics Group’s involvement in ETC’s drug discovery process from start to finish position it at the core of the organization.