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Vol. 55, Issue 5, 910-920, May 1999
Centre National de la Recherche Scientifique, Unité Propre de
Recherche 9023, Montpellier, France
We have cloned new 5-Hydroxytryptamine 4 (5-HT4) receptor splice variants from mouse
(m5-HT4(e)R and m5-HT4(f)R), rat
(r5-HT4(e)R), and human brain tissue
(h5-HT4(e)R) which differ, as do the previously described
5-HT4 receptor variants, in the length and composition of
their intracellular C termini after the common splicing site (L358).
These new variants have a unique C-terminal sequence made of two PV
repeats and are only expressed in brain tissue. All of the
5-HT4 receptor splice variants have a high constitutive activity when expressed at low and physiological densities (<500 fmol/mg protein). At similar density, they showed a much higher constitutive activity than the native and the mutated
2-adrenergic receptors. The constitutive activity of the
new splice variants with short C-terminal sequences
(m5-HT4(e)R and m5-HT4(f)R) was higher than
that of the long C-terminal sequence variants (m5-HT4(a)R and m5-HT4(b)R). This may indicate that the short variants
have a higher capacity for isomerization from the inactive to the
active conformation. Moreover, we further identified a sequence within the C-terminal tail upstream of L358, rich in serine and threonine residues, that played a crucial role in maintaining 5-HT4R
under its inactive conformation.
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