The P2Y/P2X divide: How it began

摘要: Abstract Extracellular purine and pyrimidine nucleotides produce their pharmacological effects through P2 receptors. These were first named by Geoff Burnstock in an extensive review 1978. They then subdivided into P2X P2Y purinoceptors Kennedy 1985, based on applying criteria to data generated functional studies smooth muscle tissues. Several other subtypes, P2T, P2Z, P2U P2D subsequently identified the following years, again using criteria. The number identity of subtypes clarified simplified cloning seven ATP-sensitive ligand-gated ion channel subunits eight adenine and/or uracil nucleotide-sensitive G protein-coupled receptors from 1993 onwards. former all classified as members receptor family latter family. More recently, high resolution imaging tertiary quaternary structures several has provided a much greater understanding how where agonists antagonists bind this leads changes conformation activity. In addition, medicinal chemistry produced variety subtype-selective antagonists, some which are now clinical use. This progress success is testimony foresight, intelligence, enthusiasm drive Burnstock, who led field forward throughout his scientific life.