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'Frontiers in Medicinal Chemistry 2009' was organized as a joint German-Swiss meeting at the University of Heidelberg. It covered the areas of kinases and nuclear hormone receptors, inflammatory diseases, atherosclerosis and neuropsychiatry. Special sessions were dedicated to new technologies in nanomedicine, proteomics and drug targeting. A session on highlights in medicinal chemistry completed the program. The lectures covered a broad range of interdisciplinary topics including molecular design and lead optimization programs, development and application of new technologies in proteomics, drug delivery & chemical synthesis.