scholarly journals Molecular determinants of inactivation and G protein modulation in the intracellular loop connecting domains I and II of the calcium channel  1A subunit

1997 ◽  
Vol 94 (4) ◽  
pp. 1512-1516 ◽  
Author(s):  
S. Herlitze ◽  
G. H. Hockerman ◽  
T. Scheuer ◽  
W. A. Catterall
Keyword(s):  
Calcium Channel ◽  
G Protein ◽  
Intracellular Loop ◽  
Molecular Determinants

scholarly journals Scanning mutagenesis of the I-II loop of the Cav2.2 calcium channel identifies residues Arginine 376 and Valine 416 as molecular determinants of voltage dependent G protein inhibition

2010 ◽  
Vol 3 (1) ◽  
pp. 6 ◽  
Author(s):  
Hugo W Tedford ◽  
Alexandra E Kisilevsky ◽  
Lucienne B Vieira ◽  
Diego Varela ◽  
Lina Chen ◽  
...  
Keyword(s):  
Calcium Channel ◽  
G Protein ◽  
Protein Inhibition ◽  
Molecular Determinants ◽  
Voltage Dependent

Molecular Determinants in the Second Intracellular Loop of the 5-Hydroxytryptamine-1A Receptor for G-Protein Coupling

2006 ◽  
Vol 69 (5) ◽  
pp. 1518-1526 ◽  
Author(s):  
Neena Kushwaha ◽  
Shannon C. Harwood ◽  
Ariel M. Wilson ◽  
Miles Berger ◽  
Laurence H. Tecott ◽  
...  
Keyword(s):  
G Protein ◽  
Intracellular Loop ◽  
G Protein Coupling ◽  
Protein Coupling ◽  
Molecular Determinants

scholarly journals The Intracellular Loop between Domains I and II of the B-Type Calcium Channel Confers Aspects of G-Protein Sensitivity to the E-Type Calcium Channel

1997 ◽  
Vol 17 (4) ◽  
pp. 1330-1338 ◽  
Author(s):  
Karen M. Page ◽  
Gary J. Stephens ◽  
Nicholas S. Berrow ◽  
Annette C. Dolphin
Keyword(s):  
Calcium Channel ◽  
G Protein ◽  
Intracellular Loop

scholarly journals Intracellular Loop 2 Peptides of the Human 5HT1a Receptor are Differential Activators of Gi

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Brian Hall ◽  
Carley Squires ◽  
Keith K. Parker
Keyword(s):  
G Protein ◽  
Pharmacological Intervention ◽  
Intracellular Camp ◽  
Intracellular Loop ◽  
Peptide Mimics ◽  
G Protein Coupling ◽  
5Ht1a Receptor ◽  
Protein Coupling ◽  
Loop Region ◽  
Loop 2

Peptide mimics of intracellular loop 2 (ic2) of the human 5HT1a receptor have been studied with respect to their ability to inhibit agonist binding via interference with receptor-G-protein coupling. These peptides give shallow concentration-effect relationships. Additionally, these peptides have been studied with respect to their ability to trigger the signal transduction system of this Gi-coupled receptor. Two signaling parameters have been quantified: concentration of intracellular cAMP and changes in incorporation into the G protein of a stable analog of GTP. In both cases, peptide mimics near midloop of ic2 actually show agonist activity with efficacy falling off toward both loop termini near TM 3 and TM 4. Previous results have suggested that the loop region near the TM3/ic2 interface is primarily responsible for receptor-G-protein coupling, while the current result emphasizes the mid-ic2 loop region's ability to activate the G protein following initial coupling. A limited number of peptides from the receptor's TM5/ic3 loop vicinity were also studied regarding agonist inhibition and G-protein activation. These peptides provide additional evidence that the human 5HT1a receptor, TM5/ic3 loop region, is involved in both coupling and activation actions. Overall, these results provide further information about potential pharmacological intervention and drug development with respect to the human 5HT1a receptor/G-protein system. Finally, the structural evidence generated here provides testable models pending crystallization and X-ray analysis of the receptor.

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