Nongenomic Actions of Bile Acids. Synthesis and Preliminary Characterization of 23- and 6,23-Alkyl-Substituted Bile Acid Derivatives as Selective Modulators for the G-Protein Coupled Receptor TGR5

2007 ◽  
Vol 50 (18) ◽  
pp. 4265-4268 ◽  
Author(s):  
Roberto Pellicciari ◽  
Hiroyuki Sato ◽  
Antimo Gioiello ◽  
Gabriele Costantino ◽  
Antonio Macchiarulo ◽  
...  
Keyword(s):  
Bile Acid ◽  
Bile Acids ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
Preliminary Characterization ◽  
Bile Acid Derivatives ◽  
G Protein Coupled

scholarly journals Expression, purification, and characterization of the G protein-coupled receptor kinase GRK5.

1994 ◽  
Vol 269 (2) ◽  
pp. 1099-1105 ◽  
Author(s):  
P. Kunapuli ◽  
J.J. Onorato ◽  
M.M. Hosey ◽  
J.L. Benovic
Keyword(s):  
G Protein ◽  
Receptor Kinase ◽  
G Protein Coupled Receptor ◽  
Purification And Characterization ◽  
G Protein Coupled

scholarly journals Bile acids drive colonic secretion of glucagon-like-peptide 1 and peptide-YY in rodents

2019 ◽  
Vol 316 (5) ◽  
pp. G574-G584 ◽  
Author(s):  
Charlotte Bayer Christiansen ◽  
Samuel Addison Jack Trammell ◽  
Nicolai Jacob Wewer Albrechtsen ◽  
Kristina Schoonjans ◽  
Reidar Albrechtsen ◽  
...  
Keyword(s):  
Bile Acids ◽  
G Protein ◽  
Peptide Yy ◽  
Whole Body ◽  
Rat Colon ◽  
G Protein Coupled Receptor ◽  
L Cells ◽  
Glucagon Like Peptide ◽  
Glucagon Like Peptide 1 ◽  
G Protein Coupled

A large number of glucagon-like-peptide-1 (GLP-1)- and peptide-YY (PYY)-producing L cells are located in the colon, but little is known about their contribution to whole body metabolism. Since bile acids (BAs) increase GLP-1 and PYY release, and since BAs spill over from the ileum to the colon, we decided to investigate the ability of BAs to stimulate colonic GLP-1 and PYY secretion. Using isolated perfused rat/mouse colon as well as stimulation of the rat colon in vivo, we demonstrate that BAs significantly enhance secretion of GLP-1 and PYY from the colon with average increases of 3.5- and 2.9-fold, respectively. Furthermore, we find that responses depend on BA absorption followed by basolateral activation of the BA-receptor Takeda-G protein-coupled-receptor 5. Surprisingly, the apical sodium-dependent BA transporter, which serves to absorb conjugated BAs, was not required for colonic conjugated BA absorption or conjugated BA-induced peptide secretion. In conclusion, we demonstrate that BAs represent a major physiological stimulus for colonic L-cell secretion.NEW & NOTEWORTHY By the use of isolated perfused rodent colon preparations we show that bile acids are potent and direct promoters of colonic glucagon-like-peptide 1 and peptide-YY secretion. The study provides convincing evidence that basolateral Takeda-G protein-coupled-receptor 5 activation is mediating the effects of bile acids in the colon and thus add to the existing literature described for L cells in the ileum.

scholarly journals A G Protein-coupled Receptor Responsive to Bile Acids

2003 ◽  
Vol 278 (11) ◽  
pp. 9435-9440 ◽  
Author(s):  
Yuji Kawamata ◽  
Ryo Fujii ◽  
Masaki Hosoya ◽  
Masataka Harada ◽  
Hiromi Yoshida ◽  
...  
Keyword(s):  
Bile Acids ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

scholarly journals Characterization of Two Fly LGR (Leucine-Rich Repeat-Containing, G Protein-Coupled Receptor) Proteins Homologous to Vertebrate Glycoprotein Hormone Receptors: Constitutive Activation of Wild-Type Fly LGR1 But Not LGR2 in Transfected Mammalian Cells**This study was supported by NIH Grant HD-23273. The GenBank submission number for fly LGR2 is AF274591.

Endocrinology ◽  
2000 ◽  
Vol 141 (11) ◽  
pp. 4081-4090 ◽  
Author(s):  
Shinya Nishi ◽  
Sheau Yu Hsu ◽  
Karen Zell ◽  
Aaron J. W. Hsueh
Keyword(s):  
G Protein ◽  
Hormone Receptors ◽  
Coupling Mechanism ◽  
Leucine Rich Repeat ◽  
G Protein Coupled Receptor ◽  
Glycoprotein Hormone ◽  
Glycoprotein Hormone Receptors ◽  
Signaling Mechanisms ◽  
G Protein Coupled

Abstract The receptors for lutropin (LH), FSH, and TSH belong to the large G protein-coupled receptor (GPCR) superfamily and are unique in having a large N-terminal extracellular (ecto-) domain important for interactions with the large glycoprotein hormone ligands. Recent studies indicated the evolution of a large family of the leucine-rich repeat-containing, G protein-coupled receptors (LGRs) with at least seven members in mammals. Based on the sequences of mammalian glycoprotein hormone receptors, we have identified a new LGR in Drosophila melanogaster and named it as fly LGR2 to distinguish it from the previously reported fly LH/FSH/TSH receptor (renamed as fly LGR1). Genomic analysis indicated the presence of 10 exons in fly LGR2 as compared with 16 exons in fly LGR1. The deduced fly LGR2 complementary DNA (cDNA) showed 43 and 64% similarity to the fly LGR1 in the ectodomain and transmembrane region, respectively. Comparison of 12 LGRs from diverse species indicated that these proteins can be divided into three subfamilies and fly LGR1 and LGR2 belong to different subfamilies. Potential signaling mechanisms were tested in human 293T cells overexpressing the fly receptors. Of interest, fly LGR1, but not LGR2, showed constitutive activity as reflected by elevated basal cAMP production in transfected cells. The basal activity of fly LGR1 was further augmented following point mutations of key residues in the intracellular loop 3 or transmembrane VI, similar to those found in patients with familial male precocious puberty. The present study reports the cloning of fly LGR2 and indicates that the G protein-coupling mechanism is conserved in fly LGR1 as compared with the mammalian glycoprotein hormone receptors. The characterization of fly receptors with features similar to mammalian glycoprotein hormone receptors allows a better understanding of the evolution of this unique group of GPCRs and future elucidation of their ligand signaling mechanisms.

scholarly journals Identification and characterization of a G protein-coupled receptor homolog encoded by murine cytomegalovirus.

1997 ◽  
Vol 71 (2) ◽  
pp. 1521-1529 ◽  
Author(s):  
N J Davis-Poynter ◽  
D M Lynch ◽  
H Vally ◽  
G R Shellam ◽  
W D Rawlinson ◽  
...  
Keyword(s):  
G Protein ◽  
Murine Cytomegalovirus ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled ◽  
Identification And Characterization

Characterization of a G Protein-Coupled Receptor for Nicotinic Acid

2001 ◽  
Vol 59 (2) ◽  
pp. 349-357 ◽  
Author(s):  
Anna Lorenzen ◽  
Christina Stannek ◽  
Heidrun Lang ◽  
Viktor Andrianov ◽  
Ivars Kalvinsh ◽  
...  
Keyword(s):  
Nicotinic Acid ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

Characterization of G-Protein Coupled Receptor Modulators Using Homogeneous cAMP Assays

2012 ◽  
pp. 171-180 ◽  
Author(s):  
Daniel L. Bassoni ◽  
Qumber Jafri ◽  
Sunitha Sastry ◽  
Mahesh Mathrubutham ◽  
Tom S. Wehrman
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptor ◽  
Receptor Modulators ◽  
G Protein Coupled
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