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Adenosine receptors as therapeutic targets
TLDR
Recent advances in the understanding of the roles of the various adenosine receptor subtypes, and in the development of selective and potent ligands, have brought the goal of therapeutic application of adenosines receptor modulators considerably closer. Expand
Structure of an Agonist-Bound Human A2A Adenosine Receptor
TLDR
The molecule UK-432097 is defined as a “conformationally selective agonist” capable of receptor stabilization in a specific active-state configuration and sheds light on G protein–coupled receptor activation. Expand
Structure of the human P2Y12 receptor in complex with an antithrombotic drug
TLDR
The 2.6 Å resolution crystal structure of human P2Y12R in complex with a non-nucleotide reversible antagonist, AZD1283, reveals a distinct straight conformation of helix V, which sets P2y12R apart from all other known class A GPCR structures. Expand
Agonist-bound structure of the human P2Y12 receptor
TLDR
The agonist-bound P2Y12R structure answers long-standing questions surrounding P2y12R–agonist recognition, and reveals interactions with several residues that had not been reported to be involved in agonist binding. Expand
Two disparate ligand-binding sites in the human P2Y1 receptor
In response to adenosine 5′-diphosphate, the P2Y1 receptor (P2Y1R) facilitates platelet aggregation, and thus serves as an important antithrombotic drug target. Here we report the crystal structuresExpand
Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors.
TLDR
A series of symmetric aryl diisothiocyanate derivatives are synthesized and their ability to inhibit phospholipase C (PLC) activity induced by activation of five subtypes of recombinant P2Y receptors is examined. Expand
Structure-Based Discovery of A2A Adenosine Receptor Ligands
TLDR
Whether novel chemotypes may be discovered for the A2A adenosine receptor, based on complementarity to its recently determined structure, is explored, with high hit rates and affinities at least partly reflect the bias of commercial libraries toward GPCR-like chemotypes. Expand
Identification by Site-directed Mutagenesis of Residues Involved in Ligand Recognition and Activation of the Human A3 Adenosine Receptor*
TLDR
Several residues of the human A3 adenosine receptor within transmembrane domains 3 and 6 and the second extracellular loop, which have been predicted by previous molecular modeling to be involved in the ligand recognition, were mutated, indicating that Trp243 was critical for receptor activation. Expand
Identification of essential residues involved in the allosteric modulation of the human A(3) adenosine receptor.
TLDR
The results were interpreted using a rhodopsin-based molecular model of the A(3)AR to suggest multiple binding modes of the allosteric modulators. Expand
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
TLDR
Following sequence-based secondary-structure prediction, complete models of all the human P2Y receptors by homology to rhodopsin were constructed and new recognition elements were identified to further define the P2 Y1 binding site and related these to other P2y receptor subtypes. Expand
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