Design and synthesis of subtype-selective agonists for metabotropic glutamate receptors
The metabotropic glutamate receptors (mGluRs) are divided into three groups, named group I-III. Within each group a number of receptor subtypes are found and these display a high degree of sequence homology. Notably mGlu2 and mGlu3 (group II) show a high degree of sequence homology, nevertheless, we have discovered competitive agonists, which display full selectivity for mGlu2 over mGlu3. Was it all planned for by in silico studies - or did we just get lucky?
Recently published work on the topic: J. Med. Chem., 2016, 59, 914–924