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International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors.
- B. Fredholm, A. IJzerman, K. Jacobson, K. Klotz, J. Linden
- BiologyPharmacological reviews
- 1 December 2001
Experiments with receptor antagonists and mice with targeted disruption of adenosine A(1), A(2A), and A(3) expression reveal roles for these receptors under physiological and particularly pathophysiological conditions.
The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist
The crystal structure of the human A2A adenosine receptor is determined, in complex with a high-affinity subtype-selective antagonist, ZM241385, to 2.6 angstrom resolution and suggests a role for ZM 241385 in restricting the movement of a tryptophan residue important in the activation mechanism of the class A receptors.
International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B)
- S. Offermanns, S. Colletti, T. Lovenberg, G. Semple, A. Wise, A. IJzerman
- Biology, ChemistryPharmacological Reviews
- 1 June 2011
The aim of this article is to give an overview on the discovery and pharmacological characterization of HCAs, and to introduce an International Union of Basic and Clinical Pharmacology (IUPHAR)-recommended nomenclature for this receptor family.
Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions
The high-resolution structure of a stabilized version of the human A2Aadenosine receptor (A2AAR) reveals the position of about 60 internal waters, which suggests an almost continuous channel in the GPCR and can explain the allosteric effects of Na+ on ligand binding and how cholesterol may contribute to G PCR stabilization.
International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors—An Update
- B. Fredholm, A. IJzerman, K. Jacobson, J. Linden, C. Müller
- Biology, MedicinePharmacological Reviews
- 1 March 2011
In the 10 years since our previous International Union of Basic and Clinical Pharmacology report on the nomenclature and classification of adenosine receptors, no developments have led to major…
Allosteric modulation of G-protein-coupled receptors
An overview of allosteric modulators enhancing or diminishing the effects of (endogenous) agonists or antagonists on a variety of G-protein-coupled receptors such as muscarinic, α-adrenergic, serotoninergic, dopaminergic, adenosine, metabotropic glutamate and Ca2+ receptors is presented.
Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation.
Involvement of Asn-293 in stereospecific agonist recognition and in activation of the beta 2-adrenergic receptor.
- K. Wieland, H. Zuurmond, C. Krasel, A. IJzerman, M. Lohse
- Biology, ChemistryProceedings of the National Academy of Sciences…
- 20 August 1996
Data indicate a relationship between stereospecificity and intrinsic activity of agonists and suggest that Asn-293 is important for both properties of the agonist-receptor interaction.
Suramin analogues as subtype-selective G protein inhibitors.
The results show that it is possible to design G protein inhibitors that target the effector binding site on the alpha subunits, and selected suramin is selective for recombinant Gsalpha-s and recombinant Go alpha.
Structure of CC Chemokine Receptor 2 with Orthosteric and Allosteric Antagonists
The present structure of CCR2 in a ternary complex with an orthosteric and allosteric (CCR2-RA-[R]) antagonist suggests diverse pocket epitopes that can be exploited to overcome obstacles in drug design.