Scientific Background

 
Professor Thue W. Schwartz and Dr. Christian E. Elling are internationally recognized pioneers in the characterization of the molecular mechanism of action of endogenous ligands and drugs on 7TM receptors. Their work originated in the 1980s, when Prof. Schwartz described different subtypes of NPY receptors, by designing the first truly subtype-selective ligands. In the early 1990s, Prof. Schwartzs laboratory took a leading role internationally in 7TM receptor molecular pharmacology by mapping the binding sites for the first non-peptide compounds.

Other contributions from Schwartz and Elling include characterization of the molecular mechanism of action of drugs and drug candidates in the substance P receptor and subsequently in several other receptor systems, including the angiotensin AT1 receptor (e.g. Lozartan and similar drugs). These and other structure-function studies have facilitated the understanding of the molecular recognition and action of agonists and antagonists and the possibility of activating or blocking the receptor not only at the binding site of the natural ligand, but also at other distinct sites. Exchange of binding sites not only for antagonists but also agonists with structurally well-defined metal-ion sites has provided a detailed insight into the molecular mechanisms of 7TM receptor activation, thus building the basis for development of small molecule agonists for this receptor family.