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J. Biol. Chem., Vol. 276, Issue 31, 28667-28675, August 3, 2001
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From the School of Animal and Microbial Sciences, University of
Reading, Whiteknights, Reading, Berkshire RG6 6AJ, United Kingdom and
the § Department of Pharmacology and Toxicology, West
Virginia University, Morgantown, West Virginia 26506-9223
The D2 dopamine receptor
has been expressed in Sf21 insect cells together with the G
proteins Go and Gi2, using the
baculovirus system. Expression levels of receptor and G protein (
Agonist Regulation of D2 Dopamine Receptor/G Protein
Interaction
EVIDENCE FOR AGONIST SELECTION OF G PROTEIN SUBTYPE*
,
,
, and 
subunits) in the two preparations were similar as shown by
binding of [3H]spiperone and quantitative Western blot,
respectively. For several agonists, binding data were fitted best by a
two-binding site model in either preparation, showing interaction of
expressed receptor and G protein. For some agonists, binding to the
higher affinity site was of higher affinity in
D2/Go than in the
D2/Gi2 preparation. Some agonists exhibited
binding data that were best fitted by a two-binding site model in
D2/Go and a one-binding site model in
D2/Gi2. Therefore, receptor/G protein
interaction seemed to be stronger in the D2/Go
preparation. Agonist stimulation of [35S]GTPS
(guanosine 5'-3-O-(thio)triphosphate) binding in the two preparations also gave evidence for higher affinity
D2/Go interaction. In the
D2/Go preparation, agonist stimulation of
[35S]GTPS binding occurred at higher potency for
several agonists, and a higher stimulation (relative to dopamine) was
achieved in D2/Go compared with
D2/Gi2. Some agonists were able to stimulate [35S]GTPS binding in the D2/Go
preparation but not in D2/Gi2. The extent of
D2 receptor selectivity for Go over
Gi2 is therefore dependent on the agonist used, and thus
agonists may stabilize different conformations of the receptor with
different abilities to couple to and activate G proteins.
*
This work was supported by a BBSRC studentship (to Y. C.)
and National Science Foundation Grant MCB-9870839 (to S. G. G.).The costs of publication of this
article were defrayed in part by the
payment of page charges. The article
must therefore be hereby marked
"advertisement" in
accordance with 18 U.S.C. Section
1734 solely to indicate this fact.
Present address: School of Biomedical Sciences, Queens Medical
Centre, Nottingham, NG7 2UH, UK.
¶
To whom correspondence should be addressed. Tel.:
44-118-931-8015; Fax: 44-118-931-6537; E-mail:
P.G.Strange@rdg.ac.uk.
Copyright © 2001 by The American Society for Biochemistry and Molecular Biology, Inc.
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