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Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
- M. Ruat, E. Traiffort, J. Schwartz
- BiologyProceedings of the National Academy of Sciences…
- 15 September 1993
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.
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
- H. Lim, R. V. van Rijn, Ping Ling, R. Bakker, R. Thurmond, R. Leurs
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 September 2005
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.
A novel rat serotonin (5-HT6) receptor: molecular cloning, localization and stimulation of cAMP accumulation.
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.
The histamine H3 receptor: from gene cloning to H3 receptor drugs
- R. Leurs, R. Bakker, H. Timmerman, I. D. Esch
- Biology, MedicineNature Reviews Drug Discovery
- 1 February 2005
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.
Constitutive Signaling of the Human Cytomegalovirus-encoded Chemokine Receptor US28*
The data suggest that a high level of constitutive activity might be a more general characteristic of viral G protein-coupled receptors and that human cytomegalovirus might exploit this G Protein-Coupled receptor property to modulate the homeostasis of infected cells via the early gene product US28.
Identification of rat H3 receptor isoforms with different brain expression and signaling properties.
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.
Pharmacological modulation of chemokine receptor function
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.
Molecular pharmacological aspects of histamine receptors.
Human cytomegalovirus-encoded chemokine receptor US28 promotes tumorigenesis
- D. Maussang, D. Verzijl, M. Smit
- BiologyProceedings of the National Academy of Sciences
- 29 August 2006
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.
The human cytomegalovirus-encoded chemokine receptor US28 promotes angiogenesis and tumor formation via cyclooxygenase-2.
The development of HCMV-related proliferative diseases may partially be ascribed to the ability of US28 to activate COX-2, a key mediator of inflammatory diseases and major determinant in several forms of cancer.