Graeme Milligan

TL;DR: It is shown that the mGluR2 interacts through specific transmembrane helix domains with the 2AR, a member of an unrelated G-protein-coupled receptor family, to form functional complexes in brain cortex that may be involved in the altered cortical processes of schizophrenia.

TL;DR: It is demonstrated that heteromerization of adenosine A1 receptors and A2A receptors allowsAdenosine to exert a fine-tuning modulation of glutamatergic neurotransmission and that chronic caffeine treatment leads to modifications in the function of the A1R–A2AR heteromer that could underlie the strong tolerance to the psychomotor effects of caffeine.

TL;DR: The functional and pharmacological properties of GPCR oligomers are reviewed and some guidelines for the application of discrete direct screening and high-throughput screening approaches to the discovery of receptor-heteromer selective compounds are provided.

TL;DR: Key questions that remain to be addressed effectively include the prevalence and relevance of these in native tissues and the implications of heterodimerization for pharmacology and, potentially, for drug design.

TL;DR: The generation of chimeras between different α‐subunits defined the role of different sections of the primary/secondary sequence and crystal structures and cocrystals with interacting proteins have given detailed understanding of their molecular structure and basis of function.