New therapeutics for Type 2 diabetes

Type 2 diabetes (T2D) is becoming a global epidemic that presents a major challenge to healthcare systems worldwide. Current therapies for T2D fail in the long term and there is an urgent need to develop new drugs with novel modes of action. We are working to develop inhibitors of an enzyme (protein kinase C epsilon, or PKCe) known to play key roles in both β-cell failure and insulin resistance. Using fragment-based and high-throughput screening we have identified a number of compounds that bind to the target enzyme. A small peptide is also able to inhibit PKCe activation. In this project, we will elaborate these small molecule and/or peptides hits into potent inhibitors using medicinal chemistry optimisation and structure-based drug design, and subsequently test these in cell-based and animal models of T2D.

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