scholarly journals FTY720 (Gilenya) Phosphate Selectivity of Sphingosine 1-Phosphate Receptor Subtype 1 (S1P1) G Protein-coupled Receptor Requires Motifs in Intracellular Loop 1 and Transmembrane Domain 2

2011 ◽  
Vol 286 (35) ◽  
pp. 30513-30525 ◽  
Author(s):  
William J. Valentine ◽  
Virginia I. Godwin ◽  
Daniel A. Osborne ◽  
Jianxiong Liu ◽  
Yuko Fujiwara ◽  
...  
Keyword(s):  
G Protein ◽  
Transmembrane Domain ◽  
Receptor Subtype ◽  
G Protein Coupled Receptor ◽  
Intracellular Loop ◽  
Sphingosine 1 Phosphate ◽  
G Protein Coupled

Effects ofN- andC-terminal addition of oligolysines or native loop residues on the biophysical properties of transmembrane domain peptides from a G-protein coupled receptor

2006 ◽  
Vol 12 (12) ◽  
pp. 808-822 ◽  
Author(s):  
Patricia Cano-Sanchez ◽  
Beatrice Severino ◽  
V. V. Sureshbabu ◽  
Joe Russo ◽  
Tatsuya Inui ◽  
...  
Keyword(s):  
G Protein ◽  
Transmembrane Domain ◽  
Biophysical Properties ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

scholarly journals Expression and biophysical analysis of two double-transmembrane domain-containing fragments from a yeast G protein-coupled receptor

Biopolymers ◽  
2008 ◽  
Vol 90 (2) ◽  
pp. 117-130 ◽  
Author(s):  
Leah S. Cohen ◽  
Boris Arshava ◽  
Racha Estephan ◽  
Jacqueline Englander ◽  
Heejung Kim ◽  
...  
Keyword(s):  
G Protein ◽  
Transmembrane Domain ◽  
G Protein Coupled Receptor ◽  
Biophysical Analysis ◽  
G Protein Coupled

scholarly journals Mechanism of β-arrestin recruitment by the μ-opioid G protein-coupled receptor

2020 ◽  
Vol 117 (28) ◽  
pp. 16346-16355 ◽  
Author(s):  
Amirhossein Mafi ◽  
Soo-Kyung Kim ◽  
William A. Goddard
Keyword(s):  
Side Effects ◽  
G Protein ◽  
Three Dimensional ◽  
G Protein Signaling ◽  
Protein Signaling ◽  
G Protein Coupled Receptor ◽  
Intracellular Loop ◽  
Cytoplasmic Region ◽  
Gi Protein ◽  
G Protein Coupled

Agonists to the μ-opioid G protein-coupled receptor (μOR) can alleviate pain through activation of G protein signaling, but they can also induce β-arrestin activation, leading to such side effects as respiratory depression. Biased ligands to μOR that induce G protein signaling without inducing β-arrestin signaling can alleviate pain while reducing side effects. However, the mechanism for stimulating β-arrestin signaling is not known, making it difficult to design optimum biased ligands. We use extensive molecular dynamics simulations to determine three-dimensional (3D) structures of activated β-arrestin2 stabilized by phosphorylated μOR bound to the morphine and D-Ala2,N-MePhe4, Gly-ol]-enkephalin (DAMGO) nonbiased agonists and to the TRV130 biased agonist. For nonbiased agonists, we find that the β-arrestin2 couples to the phosphorylated μOR by forming strong polar interactions with intracellular loop 2 (ICL2) and either the ICL3 or cytoplasmic region of transmembrane (TM6). Strikingly, Gi protein makes identical strong bonds with these same ICLs. Thus, the Gi protein and β-arrestin2 compete for the same binding site even though their recruitment leads to much different outcomes. On the other hand, we find that TRV130 has a greater tendency to bind the extracellular portion of TM2 and TM3, which repositions TM6 in the cytoplasmic region of μOR, hindering β-arrestin2 from making polar anchors to the ICL3 or to the cytosolic end of TM6. This dramatically reduces the affinity between μOR and β-arrestin2.

scholarly journals Transduction of Multiple Effects of Sphingosine 1-Phosphate (S1P) on T Cell Functions by the S1P1 G Protein-Coupled Receptor

2003 ◽  
Vol 171 (7) ◽  
pp. 3500-3507 ◽  
Author(s):  
Glenn Dorsam ◽  
Markus H. Graeler ◽  
Christine Seroogy ◽  
Yvonne Kong ◽  
Julia K. Voice ◽  
...  
Keyword(s):  
T Cell ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
Cell Functions ◽  
Sphingosine 1 Phosphate ◽  
G Protein Coupled

scholarly journals Sphingosine 1-Phosphate-induced Cell Rounding and Neurite Retraction Are Mediated by the G Protein-coupled Receptor H218

1999 ◽  
Vol 274 (8) ◽  
pp. 4626-4632 ◽  
Author(s):  
James R. Van Brocklyn ◽  
Zhenxing Tu ◽  
Lisa C. Edsall ◽  
Richard R. Schmidt ◽  
Sarah Spiegel
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptor ◽  
Cell Rounding ◽  
Neurite Retraction ◽  
Sphingosine 1 Phosphate ◽  
G Protein Coupled
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