Transcriptome analysis identifies genes with enriched expression in the mouse central extended amygdala
Biological and pharmacological roles of HCA receptors.
Random mutagenesis of the human adenosine A2B receptor followed by growth selection in yeast. Identification of constitutively active and gain of function mutations.
The large number of receptor mutants created in yeast suggests that the wild-type (wt) human A2B receptor itself is rather silent, which may explain the low affinity of agonists for this receptor.
G protein-coupled receptors for energy metabolites as new therapeutic targets
The functions of these metabolite-sensing GPC receptors in physiology and disease are summarized, and the emerging pharmacological agents that are being developed to target these GPCRs for the treatment of metabolic disorders are discussed.
ZM241385, DPCPX, MRS1706 Are Inverse Agonists with Different Relative Intrinsic Efficacies on Constitutively Active Mutants of the Human Adenosine A2B Receptor
- Qilan Li, K. Ye, M. Beukers
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 February 2007
This study describes the first description of inverse agonists for the human adenosine A2B receptor and discovered two highly constitutively active mutants whose basal activity could not be reversed by any of the three compounds.
Novel 3,6,7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A).
- C. Blad, J. V. van Veldhoven, A. IJzerman
- Chemistry, BiologyJournal of Medicinal Chemistry
- 27 March 2012
Interestingly, some of the compounds were found to increase the efficacy of the endogenous ligand 3-hydroxybutyrate and enhance its potency almost 10-fold, suggesting that the pyrazolopyrimidines may have therapeutic value when given alone.
Putative role of the adenosine A3 receptor in the antiproliferative action of N6-(2-isopentenyl)adenosine
- C. Blad, J. K. von Frijtag Drabbe Künzel, A. IJzerman
- Biology, ChemistryPurinergic Signalling Purinergic Signalling
- 1 July 2011
The antiproliferative effects of the naturally occurring nucleoside IPA are at least in part mediated by the A3R, as demonstrated on human and rat tumor cell lines LNCaP and N1S1.
Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A).
ZM 241385 , DPCPX , MRS 1706 Are Inverse Agonists with Different Relative Intrinsic Efficacies on Constitutively Active Mutants of the Human Adenosine A 2 B Receptor
This study is the first description of inverse agonists for the human adenosine A2B receptor and the use of receptor mutants with varying levels of constitutive activity enabled us to determine the relative intrinsic efficacy of these inverse agonist compounds.
Effects of pyrazole partial agonists on HCA2‐mediated flushing and VLDL‐triglyceride levels in mice
Two partial agonists for HCA2, LUF 6281 and LUF6283 are evaluated with respect to their anti‐dyslipidaemic potential and cutaneous flushing effect.