Cloning, Characterization, and Chromosomal Localization of a Human 5‐HT6 Serotonin Receptor

@article{Kohen1996CloningCA,
  title={Cloning, Characterization, and Chromosomal Localization of a Human 5‐HT6 Serotonin Receptor},
  author={Ruth Kohen and Mark A. Metcalf and Naseem Khan and Teresa Druck and Kay Huebner and Jean E. Lachowicz and Herbert Y. Meltzer and David R. Sibley and Bryan L. Roth and Mark W. Hamblin},
  journal={Journal of Neurochemistry},
  year={1996},
  volume={66}
}
Abstract: We describe the cloning and characterization of a human 5‐HT6 serotonin receptor. The open reading frame is interrupted by two introns in positions corresponding to the third cytoplasmic loop and the third extracellular loop. The human 5‐HT6 cDNA encodes a 440‐amino‐acid polypeptide whose sequence diverges significantly from that published for the rat 5‐HT6 receptor. Resequencing of the rat cDNA revealed a sequencing error producing a frame shift within the open reading frame. The… 
Identification of a human 5-HT6 receptor variant produced by alternative splicing.
TLDR
Experiments performed using a degenerate PCR approach from human caudate cDNA revealed a 5-HT6 receptor clone with a 289 bp deletion of the region coding for transmembrane IV through the third intracellular loop and a truncated protein containing 10 unique amino acids at its carboxyl end.
Creation, expression, and characterization of a constitutively active mutant of the human serotonin 5‐HT6 receptor
TLDR
It is concluded that the S267K mutation renders the 5‐ HT6 receptor constitutively active and that clozapine is an inverse agonist at the mutant 5‐HT6 receptor.
Cloning of the mouse 5-HT6 serotonin receptor and mutagenesis studies of the third cytoplasmic loop.
TLDR
The data suggest that constitutive activity may be important to 5-HT6 receptor activity in vivo and that, unlike some other G-protein coupled receptors, alteration in the BBXXB CIII-loop motif reduces rather than further activates basal activity of the murine 5- HT6 receptor.
Assignment of the human serotonin 4 receptor gene (HTR4) to the long arm of chromosome 5 (5q31-q33).
TLDR
The chromosomal localization of the human 5-HT4 receptor gene (HTR4) is reported by the analysis of somatic cell hybrids using monochromosomal hybrid cell lines of the NIGMS Mapping Panel 2 to localized the HTR4 gene to human chromosome 5.
Characterization of 5-ht6 receptor and expression of 5-ht6 mRNA in the rat brain during ontogenetic development
TLDR
The hypothesis that 5-ht6 receptors may correspond to an important target for atypical antipsychotics and reveal an original pharmacological profile for this receptor is confirmed and its role in the early growth process involving the serotonergic system is suggested.
Differences in the central nervous system distribution and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling.
TLDR
Molecular modeling of the receptor and docking of selective and nonselective compounds was undertaken to elucidate the ligand receptor interactions and predicted the binding pocket was predicted to be different in the mouse compared with rat and human 5-HT6 receptors.
Novel polymorphism in the 5′-upstream region of the human 5-HT6 receptor gene and schizophrenia
TLDR
The results suggest that the 5-HT6 receptor gene polymorphism does not confer increased susceptibility to schizophrenia.
Cloning and Functional Expression of an Aplysia 5-HT Receptor Negatively Coupled to Adenylate Cyclase
TLDR
The cloning of a cDNA coding for an Aplysia G-protein-coupled 5-HT receptor (5-HTap1) is reported, whose deduced amino acid sequence resembles those of the 5- HT1 receptor subfamily.
The Putative 5‐ht6 Receptor: Localization and Function
TLDR
Work detailing the cloning and characterization of the recombinant 5‐ht6 receptor, its distribution and evidence for functional responses mediated by naturally occurring 5‐HT6 receptors is reviewed.
Function and distribution of three rat 5-hydroxytryptamine7 (5-HT7) receptor isoforms produced by alternative splicing
TLDR
While all three known 5-HT7 receptor isoforms in the rat are functionally competent, any functionally important differences between the three isoforms are not likely to involve differences in ligand binding or gross differences in adenylate cyclase coupling.
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