Faculty Opinions recommendation of Structural basis of GABAB receptor-Gi protein coupling.

2021 ◽  
Author(s):  
Patrick Sexton
Keyword(s):  
Gabab Receptor ◽  
Structural Basis ◽  
Protein Coupling ◽  
Gi Protein

scholarly journals Structural basis of GABAB receptor–Gi protein coupling

Nature ◽  
2021 ◽  
Author(s):  
Cangsong Shen ◽  
Chunyou Mao ◽  
Chanjuan Xu ◽  
Nan Jin ◽  
Huibing Zhang ◽  
...  
Keyword(s):  
G Protein ◽  
Transmembrane Domain ◽  
Gabab Receptor ◽  
Transmembrane Helix ◽  
Active Form ◽  
Binding Mode ◽  
Structural Basis ◽  
Intracellular Loop ◽  
Protein Activation ◽  
Gi Protein

AbstractG-protein-coupled receptors (GPCRs) have central roles in intercellular communication1,2. Structural studies have revealed how GPCRs can activate G proteins. However, whether this mechanism is conserved among all classes of GPCR remains unknown. Here we report the structure of the class-C heterodimeric GABAB receptor, which is activated by the inhibitory transmitter GABA, in its active form complexed with Gi1 protein. We found that a single G protein interacts with the GB2 subunit of the GABAB receptor at a site that mainly involves intracellular loop 2 on the side of the transmembrane domain. This is in contrast to the G protein binding in a central cavity, as has been observed with other classes of GPCR. This binding mode results from the active form of the transmembrane domain of this GABAB receptor being different from that of other GPCRs, as it shows no outside movement of transmembrane helix 6. Our work also provides details of the inter- and intra-subunit changes that link agonist binding to G-protein activation in this heterodimeric complex.

scholarly journals Structural basis of the activation of the CC chemokine receptor 5 by a chemokine agonist

2020 ◽  
Author(s):  
Polina Isaikina ◽  
Ching-Ju Tsai ◽  
Nikolaus Dietz ◽  
Filip Pamula ◽  
Anne Grahl ◽  
...  
Keyword(s):  
Chemokine Receptor ◽  
Chemokine Receptors ◽  
Binding Mode ◽  
Activation Mechanism ◽  
Structural Basis ◽  
Cc Chemokine ◽  
Gi Protein ◽  
Agonist And Antagonist ◽  
Cc Chemokine Receptor 5 ◽  
Chemokine Receptor 5

AbstractThe human CC chemokine receptor 5 (CCR5) is a G protein-coupled receptor (GPCR) that plays a major role in inflammation and is involved in the pathology of cancer, HIV, and COVID-19. Despite its significance as a drug target, the activation mechanism of CCR5, i.e. how chemokine agonists transduce the activation signal through the receptor, is yet unknown. Here, we report the cryo-EM structure of wild-type CCR5 in an active conformation bound to the chemokine super-agonist [6P4]CCL5 and the heterotrimeric Gi protein. The structure provides the rationale for the sequence-activity relation of agonist and antagonist chemokines. The N-terminus of agonist chemokines pushes onto an aromatic connector that transmits activation to the canonical GPCR microswitch network. This activation mechanism differs significantly from other CC chemokine receptors that bind shorter chemokines in a shallow binding mode and have unique sequence signatures and a specialized activation mechanism.One-sentence summaryThe structure of CCR5 in complex with the chemokine agonist [6P4]CCL5 and the heterotrimeric Gi protein reveals its activation mechanism

Structural Basis of GABAB Receptor Regulation and Signaling

2020 ◽  
Author(s):  
Thorsten Fritzius ◽  
Michal Stawarski ◽  
Shin Isogai ◽  
Bernhard Bettler
Keyword(s):  
Gabab Receptor ◽  
Structural Basis ◽  
Receptor Regulation

Structural basis of receptor/G protein coupling selectivity studied with muscarinic receptors as model systems

Life Sciences ◽  
1997 ◽  
Vol 60 (13-14) ◽  
pp. 1007-1014 ◽  
Author(s):  
Jürgen Wess ◽  
Jie Liu ◽  
Nathalie Blin ◽  
June Yun ◽  
Christian Lerche ◽  
...  
Keyword(s):  
G Protein ◽  
Muscarinic Receptors ◽  
Model Systems ◽  
Structural Basis ◽  
G Protein Coupling ◽  
Protein Coupling

scholarly journals Gi protein coupling to adenosine A1-A2A receptor heteromers in human brain caudate nucleus

2010 ◽  
pp. no-no ◽  
Author(s):  
Vicent Casadó ◽  
Sergio Barrondo ◽  
Milena Spasic ◽  
Luis F. Callado ◽  
Josefa Mallol ◽  
...  
Keyword(s):  
Human Brain ◽  
Caudate Nucleus ◽  
Protein Coupling ◽  
Receptor Heteromers ◽  
A2a Receptor ◽  
Adenosine A1 ◽  
Gi Protein

scholarly journals GABAB2 Is Essential for G-Protein Coupling of the GABAB Receptor Heterodimer

2001 ◽  
Vol 21 (20) ◽  
pp. 8043-8052 ◽  
Author(s):  
Melanie J. Robbins ◽  
Andrew R. Calver ◽  
Alexander K. Filippov ◽  
Warren D. Hirst ◽  
Robert B. Russell ◽  
...  
Keyword(s):  
G Protein ◽  
Gabab Receptor ◽  
G Protein Coupling ◽  
Protein Coupling
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