CBB1003, a lysine-specific demethylase 1 inhibitor, suppresses colorectal cancer cells growth through down-regulation of leucine-rich repeat-containing G-protein-coupled receptor 5 expression

2014 ◽  
Vol 141 (1) ◽  
pp. 11-21 ◽  
Author(s):  
Hung-Chih Hsu ◽  
Yi-Shiuan Liu ◽  
Kai-Chi Tseng ◽  
Tsai-Sheng Yang ◽  
Chien-Yuh Yeh ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Cancer Cells ◽  
G Protein ◽  
Leucine Rich Repeat ◽  
G Protein Coupled Receptor ◽  
Down Regulation ◽  
Lysine Specific Demethylase ◽  
Colorectal Cancer Cells ◽  
G Protein Coupled

The G Protein–Coupled Receptor GPR30 Mediates the Nontranscriptional Effect of Estrogen on the Activation of PI3K/Akt Pathway in Endometrial Cancer Cells

2013 ◽  
Vol 23 (1) ◽  
pp. 52-59 ◽  
Author(s):  
Xin Ge ◽  
Ruixia Guo ◽  
Yuhuan Qiao ◽  
Yancai Zhang ◽  
Jia Lei ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Endometrial Cancer ◽  
Cancer Cells ◽  
G Protein ◽  
Akt Pathway ◽  
G Protein Coupled Receptor ◽  
Down Regulation ◽  
Phosphorylated Akt ◽  
Ishikawa Cells ◽  
G Protein Coupled

ObjectiveThe goal of this study was to investigate the effect of G protein–coupled receptor 30 (GPR30) on the activation of PI3K/Akt pathway induced by E2 in endometrial cancer cells.Methods and materialsImmunohistochemistry was performed to determine the location and expression of GPR30, estrogen receptors (ERs), Akt, and phosphorylated Akt. We also investigated the expression of GPR30, ERs, and the level of phosphorylation of Akt induced by E2 in endometrial cancer cells, Ishikawa cells, and HEC-1A cells. We down-regulated the expression of GPR30 in endometrial cancer cell lines by transfection with shGPR30-pGFP-V-RS, a GPR30 antisense expression vector. The cells were then subjected to a proliferation assay. Immunoprecipitation assay was performed to determine whether GPR30 directly bind to PI3K. The stable transfected cells resuspension of 100 μL (5 × 106 cells) was injected subcutaneously into the right flank of athymic mice to perform xenograft tumor formation assays.ResultsE2 stimulated cell proliferation and induced GPR30 expression and PI3K/Akt pathway activation in endometrial cancer cells, Ishikawa cells, and HEC-1A cells, whereas the expression of ERs remained unchangeable. Down-regulation of GPR30 decreased the phosphorylation of Akt and reduced cell proliferation, and GPR30 did not bind to PI3K. Down-regulation of GPR30 significantly inhibited the tumor growth of HEC-1A cells in athymic nude mice.ConclusionsThese findings suggest that GPR30 mediates the nontranscriptional effect of estrogen on the activation of PI3K/Akt pathway in endometrial cancer cells.

scholarly journals Overexpression of leucine-rich repeat-containing G protein-coupled receptor 5 in colorectal cancer

2010 ◽  
Vol 101 (7) ◽  
pp. 1731-1737 ◽  
Author(s):  
Hiroshi Uchida ◽  
Ken Yamazaki ◽  
Mariko Fukuma ◽  
Taketo Yamada ◽  
Tetsu Hayashida ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
G Protein ◽  
Leucine Rich Repeat ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

Leucine-rich repeat-containing G protein-coupled receptor 5 expression in ductular reactions after chemotherapy for metastatic colorectal cancer

2013 ◽  
Vol 43 (1) ◽  
pp. 84-90 ◽  
Author(s):  
Susumu Saigusa ◽  
Koji Tanaka ◽  
Yuji Toiyama ◽  
Kohei Matsushita ◽  
Mikio Kawamura ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Metastatic Colorectal Cancer ◽  
G Protein ◽  
Leucine Rich Repeat ◽  
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.

Leucine-rich repeat-containing G-protein-coupled receptor 8 in the rat brain: Enrichment in thalamic neurons and their efferent projections

Neuroscience ◽  
2008 ◽  
Vol 156 (2) ◽  
pp. 319-333 ◽  
Author(s):  
K. Sedaghat ◽  
P.-J. Shen ◽  
D.I. Finkelstein ◽  
J.M. Henderson ◽  
A.L. Gundlach
Keyword(s):  
Rat Brain ◽  
G Protein ◽  
Leucine Rich Repeat ◽  
G Protein Coupled Receptor ◽  
Thalamic Neurons ◽  
Efferent Projections ◽  
G Protein Coupled
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