Small Molecule Synthesis
Our small molecule team uses structure-based rational drug design to inform two primary projects, targeting malarial kinase PfCLK3 and GPR84.
Our small molecule team uses structure-based rational drug design to inform two primary projects, targeting malarial kinase PfCLK3 and GPR84.
Our malaria project focuses on kinase inhibitors of Plasmodium falciparum CLK3. We have shown that our hit compound, TCMDC-135051 has prophylactic, curative and transmission blocking potential 3D7 parasites. Our current approach works on optimizing this hit compound, namely through developing covalent inhibitors to improve potency and selectivity.
We also work with antagonists of GPR84 for therapeutic use in inflammatory diseases. We use medicinal chemistry strategies to develop structure-activity relationships and improve ADME properties.