Novel receptor concepts
- Laura Heitman
G protein-coupled receptors (GPCRs) constitute an important protein family of drug targets. Many drugs have been developed over the years for a range of diseases, varying from increased stomach acid secretion to depression, from asthma and high blood pressure to migraine. Today, it is estimated that approximately half of the marketed medicines act through members of this protein class.
The current dogma present in many standard textbooks of pharmacology and medicine is that such drugs can either be agonists, activating the receptor, or antagonists, blocking the receptor, both occupying, at least partly, the same ligand binding site on the receptor. Recent findings, however, now point to novel concepts of drug action. In our division of Medicinal Chemistry we are very interested in such novel concepts and their relevance for adenosine and other receptors.