All Outputs (6)

Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A) (2010)
Journal Article
van Veldhoven, J. P. D., Blad, C. C., Artsen, C. M., Klopman, C., Wolfram, D. R., Abdelkadir, M. J., …IJzerman, A. P. (2011). Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A). Bioorganic and Medicinal Chemistry, 21(9), 2736-2739. https://doi.org/10.1016/j.bmcl.2010.11.091

Nicotinic acid (niacin) has been used for decades as an antidyslipidemic drug in man. Its main target is the hydroxy-carboxylic acid receptor HCA2 (GPR109A), a G protein-coupled receptor. Other acids and esters such as methyl fumarate also interact w... Read More about Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A).

Characterization of [3H]LUF5834: A novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor (2010)
Journal Article
Lane, J. R., Klaasse, E., Lin, J., van Bruchem, J., Beukers, M. W., & Ijzerman, A. P. (2010). Characterization of [3H]LUF5834: A novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor. Biochemical Pharmacology, 80(8), 1180-1189. https://doi.org/10.1016/j.bcp.2010.06.041

The adenosine A(1) receptor is a promising therapeutic target for neurological disorders such as cognition deficits and is involved in cardiovascular preconditioning. Classically adenosine receptor agonists were all derivatives of adenosine, and thou... Read More about Characterization of [3H]LUF5834: A novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor.

Hybrid ortho/allosteric ligands for the adenosine A(1) receptor (2010)
Journal Article
Narlawar, R., Lane, J. R., Doddareddy, M., Lin, J., Brussee, J., & Ijzerman, A. P. (2010). Hybrid ortho/allosteric ligands for the adenosine A(1) receptor. Journal of Medicinal Chemistry, 53(8), 3028-3037. https://doi.org/10.1021/jm901252a

Many G protein-coupled receptors (GPCRs), including the adenosine A(1) receptor (A(1)AR), have been shown to be allosterically modulated by small molecule ligands. So far, in the absence of structural information, the exact location of the allosteric... Read More about Hybrid ortho/allosteric ligands for the adenosine A(1) receptor.

Structure-Based Discovery of Novel Chemotypes for Adenosine A2A Receptor Antagonists (2010)
Journal Article
Katritch, V., Jaakola, V., Lane, J. R., Lin, J., Ijzerman, A. P., Yeager, M., …Abagyan, R. (2010). Structure-Based Discovery of Novel Chemotypes for Adenosine A2A Receptor Antagonists. Journal of Medicinal Chemistry, 53(4), 1799-1809. https://doi.org/10.1021/jm901647p

The recent progress in crystallography of G-protein coupled receptors opens an unprecedented venue for structure-based GPCR drug discovery. To test efficiency of the structure-based approach, we performed molecular docking and virtual ligand screenin... Read More about Structure-Based Discovery of Novel Chemotypes for Adenosine A2A Receptor Antagonists.

Ligand binding and subtype selectivity of the human A(2A) adenosine receptor: identification and characterization of essential amino acid residues (2010)
Journal Article
Jaakola, V., Lane, J. R., Lin, J. Y., Katritch, V., Ijzerman, A. P., & Stevens, R. C. (2010). Ligand binding and subtype selectivity of the human A(2A) adenosine receptor: identification and characterization of essential amino acid residues. Journal of Biological Chemistry, 285(17), 13032-13044. https://doi.org/10.1074/jbc.M109.096974

The crystal structure of the human A(2A) adenosine receptor bound to the A(2A) receptor-specific antagonist, ZM241385, was recently determined at 2.6-A resolution. Surprisingly, the antagonist binds in an extended conformation, perpendicular to the p... Read More about Ligand binding and subtype selectivity of the human A(2A) adenosine receptor: identification and characterization of essential amino acid residues.

A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization (2010)
Journal Article
van der Horst, E., Peironcely, J. E., Ijzerman, A. P., Beukers, M. W., Lane, J. R., van Vlijmen, H. W. T., …Bender, A. (2010). A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization. BMC Bioinformatics, 11, Article 316. https://doi.org/10.1186/1471-2105-11-316

BACKGROUND:G protein-coupled receptors (GPCRs) represent a family of well-characterized drug targets with significant therapeutic value. Phylogenetic classifications may help to understand the characteristics of individual GPCRs and their subtypes. P... Read More about A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization.