R. Leurs

Publications562
h-index74
Citations19,980
Highly Influential Citations906
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Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
TLDR
Northern blot and in situ hybridization analyses showed the 5-HT7 transcripts to be expressed in discrete areas of the limbic brain (e.g., pyramidal hippocampus cells, tenia tecta, amygdaloid, or mammillary nuclei), suggesting that the receptor mediates serotoninergic controls in functions like mood, learning, or neuroendocrine and vegetative behaviors. Expand
Evaluation of Histamine H1-, H2-, and H3-Receptor Ligands at the Human Histamine H4 Receptor: Identification of 4-Methylhistamine as the First Potent and Selective H4 Receptor Agonist
TLDR
Interestingly, 4-methylhistamine is identified as a high-affinity H4R ligand that has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes, of major importance for future studies to unravel the physiological roles of the H 4R. Expand
A novel rat serotonin (5-HT6) receptor: molecular cloning, localization and stimulation of cAMP accumulation.
TLDR
Cloned a rat cDNA encoding a functional serotonin receptor (5-HT6), its coding sequence corresponds to a glycoprotein of 436 amino acids displaying significant homology with other cloned monoaminergic receptors, e.g., various serotonin receptors. Expand
The histamine H3 receptor: from gene cloning to H3 receptor drugs
TLDR
relevant information on this target protein is discussed and the development of various H3 receptor agonists and antagonists are described, and their effects in preclinical animal models are described. Expand
Molecular pharmacological aspects of histamine receptors.
TLDR
The description of pharmacological tools for the H1, H2 and H3 receptor, including the recent cloning of the receptor genes, and their respective signal transduction mechanisms are described. Expand
Identification of rat H3 receptor isoforms with different brain expression and signaling properties.
TLDR
The identification of these new H3 receptor isoforms and their specific signaling properties adds a new level of complexity to the understanding of the role of histamine, and the H3 receptors in brain function. Expand
Human cytomegalovirus-encoded chemokine receptor US28 promotes tumorigenesis
TLDR
The studies reveal that expression of US28 induces a proangiogenic and transformed phenotype by up-regulating the expression of vascular endothelial growth factor and enhancing cell growth and cell cycle progression, indicating the importance of constitutive receptor activity in the early onset of tumor development. Expand
Molecular and biochemical pharmacology of the histamine H4 receptor
TLDR
The historical developments and the molecular and biochemical pharmacology of the H4 receptor and its role in immune function are summarized. Expand
H1‐antihistamines: inverse agonism, anti‐inflammatory actions and cardiac effects
This review addresses novel concepts of histamine H1‐receptor function and attempts to relate them to the anti‐inflammatory effects of H1‐antihistamines. Furthermore, the molecular mechanisms… Expand
Pharmacological modulation of chemokine receptor function
TLDR
An overview of the evidence supporting modulation of this intriguing receptor family by a range of ligands, including small molecules, peptides and antibodies is given. Expand
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