Implementing a novel approach to high-throughput screening of membrane transport proteins as potential drug targets

Lead Applicant

Prof. S.A. Baldwin

Project Summary

Membrane proteins represent >50% of current drug targets and so are of intense interest both to the pharmaceutical industry and to academia. IMB at Leeds has a high profile in this area, examples of current research include diversity-oriented synthesis of inhibitors of human neuronal glutamate transporters for potential treatment of stroke and crystallisation and structure-determination of a bacterial homologue of the intestinal peptide transporter PepT1, an important route of drug delivery in humans. However, a key rate-limiting step in screening potential drugs is the need for cumbersome and expensive assays using radiolabelled substrates. A novel alternative approach recently introduced commercially by Iongate exploits the electrogenic nature of transport to measure this in a label-free, high-throughput (HTP) manner. The PSF award will enable introduction of this technology to multiple users at Leeds  and will allow vital preliminary data to be obtained not only to support research project applications to funding agencies.