Angiotensin II and Angiotensin IV Mimetics

The research interests encompass a range of protein targets of pharmaceutical relevance, including proteases and G-protein coupled receptors (GPCRs). One of the primary themes is to identify novel and selective low molecular weight ligands for these targets. New strategies are developed for both the design and for the synthesis of small, drug-like molecules. Lead compounds are optimized using computer-aided techniques and are preferentially synthesized using new efficient transition metal-catalyzed reactions developed in our laboratory. Considerable efforts have in particular been devoted to the development of new robust and useful palladium-catalyzed C-C bond forming reactions and novel equipment for microwave and/or flow synthesis.

Research is conducted to identify novel ligands that interfere with proteins in the renin/angiotensin system. The first drug-like selective and potent angiotensin II, type II receptor (AT2R) agonist (M24/C21) was discovered in our laboratory. M24/C21 has been extensively studied in vivo and is currently undergoing clinical evaluation.

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