The sequencing of the human genome has provided a ‘parts list’ of the human inventory comprising potential therapeutic targets for the pharmaceutical and biotechnology industry. In order to cope with this huge number of targets we introduced a new theoretical conception of protein structural biology (meta-structure) that can be used for protein sequence-to-function annotation and drug design. A hallmark of our research is the integrative application of this novel conception and sophisticated NMR spectroscopy directed towards a better understanding of fundamental biological processes. Finally, as much of protein function is predicated on dynamics, we are developing novel methodological approaches that combine biochemistry, bioorganic chemistry and NMR spectroscopy to unravel the microscopic details of functionally important protein plasticity.