 |
PDBsum entry 6lml
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Signaling protein
|
PDB id
|
|
|
|
6lml
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
 |
Contents |
 |
|
|
|
|
|
|
|
|
|
|
|
224 a.a.
|
|
|
|
|
|
|
|
|
|
|
306 a.a.
|
|
|
|
|
|
|
|
|
|
|
33 a.a.
|
|
|
|
|
|
|
|
|
|
|
232 a.a.
|
|
|
|
|
|
|
|
|
|
|
29 a.a.
|
|
|
|
|
|
|
|
|
|
|
395 a.a.
|
|
|
|
|
|
|
|
|
|
References listed in PDB file
|
|
|
Key reference
|
|
|
Title
|
|
Structural basis of gs and gi recognition by the human glucagon receptor.
|
|
|
Authors
|
|
A.Qiao,
S.Han,
X.Li,
Z.Li,
P.Zhao,
A.Dai,
R.Chang,
L.Tai,
Q.Tan,
X.Chu,
L.Ma,
T.S.Thorsen,
S.Reedtz-Runge,
D.Yang,
M.W.Wang,
P.M.Sexton,
D.Wootten,
F.Sun,
Q.Zhao,
B.Wu.
|
|
|
Ref.
|
|
Science, 2020,
367,
1346-1352.
[DOI no: ]
|
|
|
PubMed id
|
|
|
|
|
|
Abstract
|
|
|
Class B G protein-coupled receptors, an important class of therapeutic targets,
signal mainly through the Gs class of heterotrimeric G proteins,
although they do display some promiscuity in G protein binding. Using
cryo-electron microscopy, we determined the structures of the human glucagon
receptor (GCGR) bound to glucagon and distinct classes of heterotrimeric G
proteins, Gs or Gi1 These two structures adopt a similar
open binding cavity to accommodate Gs and Gi1 The
Gs binding selectivity of GCGR is explained by a larger interaction
interface, but there are specific interactions that affect Gi more
than Gs binding. Conformational differences in the receptor
intracellular loops were found to be key selectivity determinants. These
distinctions in transducer engagement were supported by mutagenesis and
functional studies.
|
|
|
|
|
|
|
