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Publication : Cloning of the mouse 5-HT6 serotonin receptor and mutagenesis studies of the third cytoplasmic loop.

First Author  Kohen R Year  2001
Journal  Brain Res Mol Brain Res Volume  90
Issue  2 Pages  110-7
PubMed ID  11406289 Mgi Jnum  J:70063
Mgi Id  MGI:2136133 Doi  10.1016/s0169-328x(01)00090-0
Citation  Kohen R, et al. (2001) Cloning of the mouse 5-HT(6) serotonin receptor and mutagenesis studies of the third cytoplasmic loop. Brain Res Mol Brain Res 90(2):110-7
abstractText  We have cloned the mouse 5-HT(6) serotonin receptor and examined structure-function relationships in the C-terminal end of the third cytoplasmic (CIII) loop, introducing point mutations by site-directed mutagenesis at positions 264 to 268. We examined the ability of 5-HT(6) wild type and receptor mutants to activate a cAMP responsive reporter gene when transiently expressed in JEG-3 or COS-7 cells. The wild type 5-HT(6) receptor showed strong constitutive activity even when expressed at very low levels and which increased in proportion to the amount of receptor cDNA transfected. Three of the five mutants investigated (K264I, K267A and A268R) showed reduction in constitutive activity compared to wild type. These data suggest that constitutive activity may be important to 5-HT(6) 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-HT(6) receptor.
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