Picture: Interdisciplinary research yield new receptor targets and bioactive molecules for drug development
GPCRs account for 1/3rd of the approved drugs and 224 (56%) of the non-olfactory GPCRs have a yet untapped therapeutic potential (ref). The cluster for GPCR function and drug discovery identifies new receptor targets and bioactive molecules for drug development through interdisciplinary research:
Computational drug design
The Gloriam computational receptor biology group conducts computational drug design. The group combines ligand- and target-based methods (e.g. pharmacophores and ligand docking) to determine structure-activity relationships guiding the optimisation of ligand potency and selectivity. It has also designs peptide ligands with new properties such as increased solubility and secondary structure and metabolic stability.
The Ulven Free Fatty Acid Receptor Ligand Discovery group synthesises ligands with druggable properties for a range of metabolic GPCR targets. The separate Rexen Ulven group synthesises ligands for carboxylic acid receptors.
Molecular and in vivo pharmacology
The Bräuner-Osborne Molecular Pharmacology group identifies tool compounds to elucidate receptor function and nanobodies with therapeutic potential. The Jensen group identifies ligands for the serotonin 2A receptor (5-HT2A), which mediates the effect of recreational drugs, e.g. LSD and agents in clinical trials for treatment-resistant depression and anxiety. The Sheykhzade Vascular Physiology and Pharmacology group uncovers mechanisms responsible for ischemic heart disease, diabetes, and hypertension.