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Approaches to drug target deconvolution in the kinetoplastids

There is a severe lack of robustly validated drug targets in the kinetoplastids leaving our drug discovery programs heavily reliant upon phenotypic screening in order to identify effective start points for drug discovery. However, the down-stream development and optimisation of phenotypically-active compounds is hindered by lack of information regarding their mechanism(s) of action and the molecular target(s). With this in mind, the Mode of Action Group was established to address this specific issue. The group is focused on carrying out drug target deconvolution studies in the kineoplastids, utilising a matrix of established and new methodologies in the fields of high-throughput genetics, cell biology/biochemistry and chemical proteomics. The value of these diverse approaches will be discussed and two specific target identification studies will be described in detail.

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