G protein-coupled adenosine (P1) and P2Y receptors: ligand design and receptor interactions.

ABSTRACT: The medicinal chemistry and pharmacology of the four subtypes of adenosine receptors (ARs) and the eight subtypes of P2Y receptors (P2YRs, activated by a range of purine and pyrimidine mono- and dinucleotides) has recently advanced significantly leading to selective ligands. X-ray crystallographic structures of both agonist- and antagonist-bound forms of the A(2A)AR have provided unprecedented three-dimensional detail concerning molecular recognition in the binding site and the conformational changes in receptor activation. It is apparent that this ubiquitous cell signaling system has implications for understanding and treating many diseases. ATP and other nucleotides are readily released from intracellular sources under conditions of injury and organ stress, such as hypoxia, ischemia, or

SUBMITTER: Jacobson KA 

PROVIDER: S-EPMC3360101 | biostudies-literature | 2012 Sep

REPOSITORIES: biostudies-literature