Laura Heitman Group
GPCR, allosteric modulation, target binding kinetics, small molecules
In the Heitman group, we combine different expertise and research domains, such as molecular biology, pharmacology, organic and computational chemistry. We have selected G protein-coupled receptors (GPCRs), a superfamily of membrane-bound proteins, as study objects, as many drugs act via these. Although it is clear that GPCRs also have a role in cancer, little is known about the mechanisms they are involved in, and thus how to best target them (at a receptor-level). Using this membrane protein class, our research focus is on so called “Novel receptor concepts”, with the ultimate aim to make medicines work better. Two such concepts are ‘Allosteric modulation’ and ‘Drug-target binding kinetics’, which can both lead to so-called insurmountable antagonism, i.e. antagonists that cannot be disrupted/counteracted by high local concentrations of the endogenous receptor agonist that is often causal to the disease state. This includes endogenous agonists for GPCRs involved in cancer, and thus these “novel receptor concepts” are potentially highly valuable for drug discovery in this disease area.