International symposium on G-protein-coupled receptors (GPCRs), TRP (ion) channels and lipid signalling - GPCR-Helsinki 2010.

摘要

G-protein-coupled receptors (GPCRs) are the major signalling entities for extracellular signalling molecules in intra-organism communication and chemosensation. GPCR functions have been known to the scientific world since the first seminal work of Langley and Loewi, among others, on the pharmacology and physiology, in the late 19th and early 20th century. With the refined pharmacological and biochemical methods, receptors and G-proteins could be specifically analysed, but the molecular isolation and finally exact molecular identification of the receptors, G-proteins and effectors was first initiated in the 1980s. Actually, as Robert Lefkowitz recollects, even that - for us obvious - fact that receptors or G-proteins exist as distinct molecular entities, was still in the 1970s doubted by many prominent scientists in the field (Lefkowitz 2007). The genomic and protein work and functional studies have since then revealed hundreds of GPCRs - with still quite a few without a known ligand - and almost 30 different Ga-subunits, together with a wide range of different downstream targets. GPCRs have also been suggested and shown to interact with and signal via other proteins than heterotrimeric G-proteins (Ritter & Hall 2009). Finally, GPCRs have risen to become the medically most important drug target.