Volume 270,
Number 17,
Issue of April 28, pp. 9828-9832, 1995
©1995 by The American Society for Biochemistry and Molecular Biology, Inc.
Different
1-Adrenergic Receptor Sequences Required for Activating Different
G
Subunits of Gq Class of G Proteins
Dianqing
Wu
,
Huiping
Jiang
,
Melvin I.
Simon
In order to understand the specific interactions between
receptors and guanine nucleotide-binding regulatory protein (G
proteins), we attempted to delineate the
1B-adrenergic receptor
sequences involved in activation of the
subunits of the Gq class
of G proteins. A number of specific mutations were introduced into the
third inner loop of the receptor, and the mutants were tested for their
abilities to activate different G
subunits of the Gq class. Our
results indicate that the receptor sequences required for activating
G
q/11, G
14, or G
16 are different. The sequence extending
from residues Lys
to His
is
required for activation of G
q/11, but not for activation of
G
14 or G
16. Two segments in the third loop of the receptor
are required for activation of G
14: one is located at the N
terminus of the loop ending at residue Asn
, and the other
is located at the C terminus of the loop starting from residue
Ser
. The latter contains a BB XXB motif, which is
apparently critical for G
14 coupling, but not for G
16 or
G
q/11 coupling. Furthermore, the three amino acids stretch
(Tyr
to Val
) included in the N-terminal
segment is not only required for G
14 coupling, but also for
G
q/11 coupling. It may be involved to some extent in G
16
coupling as well.