PubAg

Main content area

You searched for: Subject "G-protein coupled receptors" Remove constraint Subject: "G-protein coupled receptors" Subject G-protein coupled receptors Remove constraint Subject: G-protein coupled receptors Subject agonists Remove constraint Subject: agonists
Start Over

Search

229  Search Results

« Previous | 1 - 20 of 229 |
Number of results to display per page

Search Results

1. Split luciferase-based assay for simultaneous analyses of the ligand concentration- and time-dependent recruitment of β-arrestin2

Author:
Littmann, Timo; Buschauer, Armin; Bernhardt, Günther
Source:
Analytical biochemistry 2019 v.573 pp. 8-16
ISSN:
0003-2697
Subject:
G-protein coupled receptors,   etc   ; adverse effects; agonists; cell membranes; drugs; ligands; luciferase; recycling; signal transduction;     Show all 9 Subjects
Abstract:
... Functional selectivity of agonists has gained increasing interest in G protein-coupled receptor (GPCR) research, e.g. due to expectations of drugs with reduced adverse effects. Different agonist-dependent GPCR conformations are conceived to selectively activate a balanced or imbalanced intracellular signalling response, involving e.g. different Gα subtypes, Gβγ-subunits and β-arrestins. To discrim ...
DOI:
10.1016/j.ab.2019.02.023

2. Angiotensin Analogs with Divergent Bias Stabilize Distinct Receptor Conformations

Author:
Wingler, Laura M.; Elgeti, Matthias; Hilger, Daniel; Latorraca, Naomi R.; Lerch, Michael T.; Staus, Dean P.; Dror, Ron O.; Kobilka, Brian K.; Hubbell, Wayne L.; Lefkowitz, Robert J.
Source:
Cell 2019 v.176 no.3 pp. 468-478.e11
ISSN:
0092-8674
Subject:
G-protein coupled receptors,   etc   ; G-proteins; agonists; angiotensin II; drugs; electron paramagnetic resonance spectroscopy; ligands; monitoring;     Show all 8 Subjects
Abstract:
... “Biased” G protein-coupled receptor (GPCR) agonists preferentially activate pathways mediated by G proteins or β-arrestins. Here, we use double electron-electron resonance spectroscopy to probe the changes that ligands induce in the conformational distribution of the angiotensin II type I receptor. Monitoring distances between 10 pairs of nitroxide labels distributed across the intracellular regio ...
DOI:
10.1016/j.cell.2018.12.005

3. Distinctive Activation Mechanism for Angiotensin Receptor Revealed by a Synthetic Nanobody

Author:
Wingler, Laura M.; McMahon, Conor; Staus, Dean P.; Lefkowitz, Robert J.; Kruse, Andrew C.
Source:
Cell 2019 v.176 no.3 pp. 479-490.e12
ISSN:
0092-8674
Subject:
G-protein coupled receptors,   etc   ; agonists; angiotensin II; antibodies; crystal structure; humans; models; renal function;     Show all 8 Subjects
Abstract:
... The angiotensin II (AngII) type 1 receptor (AT1R) is a critical regulator of cardiovascular and renal function and is an important model for studies of G-protein-coupled receptor (GPCR) signaling. By stabilizing the receptor with a single-domain antibody fragment (“nanobody”) discovered using a synthetic yeast-displayed library, we determined the crystal structure of active-state human AT1R bound ...
DOI:
10.1016/j.cell.2018.12.006

4. Targeting the relaxin/insulin-like family peptide receptor 1 and 2 with small molecule compounds

Author:
Ng, Hooi Hooi; Esteban-Lopez, Maria; Agoulnik, Alexander I.
Source:
Molecular and cellular endocrinology 2019 v.487 pp. 40-44
ISSN:
0303-7207
Subject:
G-protein coupled receptors,   etc   ; liver cirrhosis; cardiovascular diseases; intravenous injection; drugs; muscles; ligands; peptide receptors; relaxin; agonists; half life;     Show all 11 Subjects
Abstract:
... The peptide hormone relaxin has beneficial roles in several organs through its action on its cognate G protein-coupled receptor, RXFP1. Relaxin administration is limited to intravenous, subcutaneous, intramuscular, or spinal injection. Another drawback of peptide-based therapy is the short half-life, which requires continuous delivery of the drug to achieve efficient concentration in target organs ...
DOI:
10.1016/j.mce.2018.12.013

5. Exploring receptor selectivity of the chimeric relaxin family peptide R3/I5 by incorporating unnatural amino acids

Author:
Wang, Jia-Hui; Hu, Meng-Jun; Zhang, Lei; Shao, Xiao-Xia; Lv, Cai-Hong; Liu, Ya-Li; Xu, Zeng-Guang; Guo, Zhan-Yun
Source:
Biochimie 2018 v.154 pp. 77-85
ISSN:
0300-9084
Subject:
G-protein coupled receptors,   etc   ; agonists; amino acids; antagonists; peptides; relaxin;     Show all 6 Subjects
Abstract:
... Relaxin family peptides perform a variety of biological functions by activating four G protein-coupled receptors, namely RXFP1−4. Our recent study demonstrated that selectivity of the chimeric relaxin family peptide R3/I5 towards the homologous RXFP3 and RXFP4 can be modulated by replacement of the highly conserved nonchiral B23Gly or B24Gly with some natural l-amino acids. To investigate the mech ...
DOI:
10.1016/j.biochi.2018.08.003

6. Uncovering kappa-opioid receptor agonist-induced PAK1/2 phosphorylation by quantitative phosphoproteomics

Author:
Wu, Jianhong; Jiang, Qinghui; Zhu, Hongwen; Zhou, Yanting; Lu, Dayun; Liu, Xing; Chen, Xiangling; Chen, Jie; Wang, Yujun; Liu, Jinggen; Song, Rentao; Huang, Ruimin; Zhou, Hu
Source:
Biochemical and biophysical research communications 2019 v.516 no.1 pp. 320-326
ISSN:
0006-291X
Subject:
G-protein coupled receptors,   etc   ; actin; agonists; cognition; cytoskeleton; diuresis; immune system; ligands; neurons; nociception; phosphorylation; phosphotransferases (kinases); prediction; proteomics; signal transduction; therapeutics;     Show all 16 Subjects
Abstract:
... Kappa-opioid receptor (KOR) is a member of G-protein coupled receptors (GPCRs) expressed in serotonergic neurons and neuronal terminals. The involvement of KOR ligands in nociception, diuresis, emotion, cognition, and immune system has been extensively studied. Omics-based methods are preferable to understand the signaling cascade after KOR activation in a systematic manner. In this study, an in-d ...
DOI:
10.1016/j.bbrc.2019.06.111

7. CPI-17-mediated contraction of vascular smooth muscle is essential for the development of hypertension in obese mice

Author:
Sun, Jie; Tao, Tao; Zhao, Wei; Wei, Lisha; She, Fan; Wang, Pei; Li, Yeqiong; Zheng, Yanyan; Chen, Xin; Wang, Wei; Qiao, Yanning; Zhang, Xue-Na; Zhu, Min-Sheng
Source:
Journal of genetics and genomics 2019 v.46 no.3 pp. 109-118
ISSN:
1673-8527
Subject:
G-protein coupled receptors,   etc   ; agonists; animal disease models; blood pressure; calcium; high fat diet; hypertension; mice; muscles; mutants; obesity; protein kinase C; signal transduction; smooth muscle;     Show all 14 Subjects
Abstract:
... Several factors have been implicated in obesity-related hypertension, but the genesis of the hypertension is largely unknown. In this study, we found a significantly upregulated expression of CPI-17 (C-kinase-potentiated protein phosphatase 1 inhibitor of 17 kDa) and protein kinase C (PKC) isoforms in the vascular smooth muscles of high-fat diet (HFD)-fed obese mice. The obese wild-type mice showe ...
DOI:
10.1016/j.jgg.2019.02.005

8. Chemoattractant receptors activate, recruit and capture G proteins for wide range chemotaxis

Author:
Miyanaga, Yukihiro; Kamimura, Yoichiro; Kuwayama, Hidekazu; Devreotes, Peter N.; Ueda, Masahiro
Source:
Biochemical and biophysical research communications 2018 v.507 no.1-4 pp. 304-310
ISSN:
0006-291X
Subject:
G-protein coupled receptors,   etc   ; Dictyostelium; G-proteins; agonists; chemoattractants; chemotaxis; ligands;     Show all 7 Subjects
Abstract:
... The wide range sensing of extracellular signals is a common feature of various sensory cells. Eukaryotic chemotactic cells driven by GPCRs and their cognate G proteins are one example. This system endows the cells directional motility towards their destination over long distances. There are several mechanisms to achieve the long dynamic range, including negative regulation of the receptors upon li ...
DOI:
10.1016/j.bbrc.2018.11.029

9. Delta opioid receptors recycle to the membrane after sorting to the degradation path

Author:
Charfi, Iness; Abdallah, Khaled; Gendron, Louis; Pineyro, Graciela
Source:
Cellular and molecular life sciences 2018 v.75 no.12 pp. 2257-2271
ISSN:
1420-682X
Subject:
G-protein coupled receptors,   etc   ; agonists; analgesics; binding proteins; cell membranes; endosomes;     Show all 6 Subjects
Abstract:
... Soon after internalization delta opioid receptors (DOPrs) are committed to the degradation path by G protein-coupled receptor (GPCR)-associated binding protein. Here we provide evidence that this classical post-endocytic itinerary may be rectified by downstream sorting decisions which allow DOPrs to regain to the membrane after having reached late endosomes (LE). The LE sorting mechanism involved ...
DOI:
10.1007/s00018-017-2732-5

10. Single-molecule force spectroscopy study of interactions between angiotensin II type 1 receptor and different biased ligands in living cells

Author:
Li, Wenhui; Xu, Jiachao; Kou, Xiaolong; Zhao, Rong; Zhou, Wei; Fang, Xiaohong
Source:
Analytical and bioanalytical chemistry 2018 v.410 no.14 pp. 3275-3284
ISSN:
1618-2642
Subject:
G-protein coupled receptors,   etc   ; agonists; angiotensin II; dissociation; energy; ligands; quantitative analysis; signal transduction; spectroscopy;     Show all 9 Subjects
Abstract:
... Angiotensin II type 1 receptor (AT1R), a typical G protein-coupled receptor, plays a key role in regulating many cardiovascular functions. Different ligands can bind with AT1R to selectively activate either G protein (Gq) or β-arrestin (β-arr) pathway, or both pathways, but the molecular mechanism is not clear yet. In this work, we used, for the first time, atomic force microscopy-based single mol ...
DOI:
10.1007/s00216-018-0956-3

11. O-GlcNAc Engineering of GPCR Peptide-Agonists Improves Their Stability and in Vivo Activity

Author:
Levine, Paul M.; Balana, Aaron T.; Sturchler, Emmanuel; Koole, Cassandra; Noda, Hiroshi; Zarzycka, Barbara; Daley, Eileen J.; Truong, Tin T.; Katritch, Vsevolod; Gardella, Thomas J.; Wootten, Denise; Sexton, Patrick M.; McDonald, Patricia; Pratt, Matthew R.
Source:
Journal of the American Chemical Society 2019 v.141 no.36 pp. 14210-14219
ISSN:
1520-5126
Subject:
G-protein coupled receptors,   etc   ; agonists; amino acids; blood serum; calcium; engineering; glucagon-like peptide 1; glucose; glycosylation; half life; molecular models; mutagenesis; parathyroid hormone; peptides; protein secretion; proteolysis; therapeutics;     Show all 17 Subjects
Abstract:
... Peptide agonists of GPCRs and other receptors are powerful signaling molecules with high potential as biological tools and therapeutics, but they are typically plagued by instability and short half-lives in vivo. Nature uses protein glycosylation to increase the serum stability of secreted proteins. However, these extracellular modifications are complex and heterogeneous in structure, making them ...
DOI:
10.1021/jacs.9b05365

12. A Forward Chemical Genetic Screen Reveals Gut Microbiota Metabolites That Modulate Host Physiology

Author:
Chen, Haiwei; Nwe, Phu-Khat; Yang, Yi; Rosen, Connor E.; Bielecka, Agata A.; Kuchroo, Manik; Cline, Gary W.; Kruse, Andrew C.; Ring, Aaron M.; Crawford, Jason M.; Palm, Noah W.
Source:
Cell 2019 v.177 no.5 pp. 1217-1231.e18
ISSN:
0092-8674
Subject:
G-protein coupled receptors,   etc   ; G-proteins; agonists; amine oxidase (flavin-containing); bacteria; blood-brain barrier; enzyme inhibitors; essential amino acids; histamine; histidine; humans; intestinal microorganisms; metabolites; metabolome; phenethylamine; poisoning;     Show all 16 Subjects
Abstract:
... The intestinal microbiota produces tens of thousands of metabolites. Here, we used host sensing of small molecules by G-protein coupled receptors (GPCRs) as a lens to illuminate bioactive microbial metabolites that impact host physiology. We screened 144 human gut bacteria against the non-olfactory GPCRome and identified dozens of bacteria that activated both well-characterized and orphan GPCRs, i ...
DOI:
10.1016/j.cell.2019.03.036

13. Number and brightness analysis to study spatio-temporal distribution of the angiotensin II AT1 and the endothelin-1 ETA receptors: Influence of ligand binding

Author:
Planes, Nadir; Digman, Michelle A.; Vanderheyden, Patrick P.M.L.; Gratton, Enrico; Caballero-George, Catherina
Source:
Biochimica et biophysica acta 2019 v.1863 no.5 pp. 917-924
ISSN:
0304-4165
Subject:
G-protein coupled receptors,   etc   ; agonists; angiotensin II; antagonists; antihypertensive agents; dyes; endothelins; energy transfer; fluorescence; heart failure; hypertension; hypertrophy; ligands; oligomerization; pathogenesis; plasma membrane; protein aggregates; spatial distribution; stroke;     Show all 19 Subjects
Abstract:
... The angiotensin II AT1 and the endothelin 1 ETA receptors play a crucial role in the pathogenesis of cardiovascular diseases like hypertension, heart failure, stroke, pulmonary hypertension, and cardiac hypertrophy. Both receptors are members of the rhodopsion-like superfamily of G protein-coupled receptors which can exist as monomers, dimers, and higher order aggregates.Recently, oligomerization ...
DOI:
10.1016/j.bbagen.2019.03.004

14. Protective Effects of Omega-3 Fatty Acids in Cancer-Related Complications

Author:
Freitas, Raquel D. S.; Campos, Maria M.
Source:
Nutrients 2019 v.11 no.5
ISSN:
2072-6643
Subject:
G-protein coupled receptors,   etc   ; agonists; analgesic effect; cell structures; clinical nutrition; diet therapy; guidelines; inflammation; metabolism; metabolites; neoplasms; omega-3 fatty acids; pain; patients; polyunsaturated fatty acids; protective effect;     Show all 16 Subjects
Abstract:
... Omega-3 polyunsaturated fatty acids (PUFAs) are considered immunonutrients and are commonly used in the nutritional therapy of cancer patients due to their ample biological effects. Omega-3 PUFAs play essential roles in cell signaling and in the cell structure and fluidity of membranes. They participate in the resolution of inflammation and have anti-inflammatory and antinociceptive effects. Addit ...
DOI:
10.3390/nu11050945

15. N-arachidonoyl glycine, another endogenous agonist of GPR55

Author:
Console-Bram, Linda; Ciuciu, Sandra M.; Zhao, Pingwei; Zipkin, Robert E.; Brailoiu, Eugen; Abood, Mary E.
Source:
Biochemical and biophysical research communications 2017
ISSN:
0006-291X
Subject:
G-protein coupled receptors,   etc   ; acids; agonists; amino acids; antagonists; calcium;     Show all 6 Subjects
Abstract:
... Interest in lipoamino acids as endogenous modulators of G-protein coupled receptors has escalated due to their involvement in a variety of physiologic processes. In particular, a role for these amino acid conjugates has emerged in the endocannabinoid system. The study presented herein investigated the effects of N-arachidonoyl glycine (NAGly) on a candidate endocannabinoid receptor, GPR55. Our nov ...
DOI:
10.1016/j.bbrc.2017.07.038
PubMed:
28698140
PubMed Central:
PMC5576593

16. Development of a novel ligand binding assay for relaxin family peptide receptor 3 and 4 using NanoLuc complementation

Author:
Hu, Meng-Jun; Shao, Xiao-Xia; Li, Hao-Zheng; Nie, Wei-Han; Wang, Jia-Hui; Liu, Ya-Li; Xu, Zeng-Guang; Guo, Zhan-Yun
Source:
Amino acids 2018 v.50 no.8 pp. 1111-1119
ISSN:
0939-4451
Subject:
G-protein coupled receptors,   etc   ; agonists; automation; bioluminescence; humans; ligands; peptide receptors; peptides; plasma membrane; relaxin; sortase A; washing;     Show all 12 Subjects
Abstract:
... Relaxin family peptides perform a variety of biological functions by binding and activating relaxin family peptide receptor 1–4 (RXFP1–4), four A-class G protein-coupled receptors. In the present work, we developed a novel ligand binding assay for RXFP3 and RXFP4 based on NanoLuc complementation technology (NanoBiT). A synthetic ligation version of the low-affinity small complementation tag (SmBiT ...
DOI:
10.1007/s00726-018-2588-5

17. Quantification of receptor activation by oxytocin and vasopressin in endocytosis-coupled bioluminescence reduction assay using nanoKAZ

Author:
Kii, Isao; Hirahara-Owada, Shino; Yamaguchi, Masataka; Niwa, Takashi; Koike, Yuka; Sonamoto, Rie; Ito, Harumi; Takahashi, Kayo; Yokoyama, Chihiro; Hayashi, Takuya; Hosoya, Takamitsu; Watanabe, Yasuyoshi
Source:
Analytical biochemistry 2018 v.549 pp. 174-183
ISSN:
0003-2697
Subject:
G-protein coupled receptors,   etc   ; agonists; antagonists; arginine vasopressin; behavior disorders; bioluminescence; brain; calcium; endocytosis; luciferase; neurotransmitters; oxytocin; signal transduction; triazoles;     Show all 14 Subjects
Abstract:
... Oxytocin (OXT) and arginine vasopressin (AVP) are structurally similar neuropeptide hormones that function as neurotransmitters in the brain, and have opposite key roles in social behaviors. These peptides bind to their G protein-coupled receptors (OXTR and AVPRs), inducing calcium ion-dependent signaling pathways and endocytosis of these receptors. Because selective agonists and antagonists for t ...
DOI:
10.1016/j.ab.2018.04.001

18. Effect and mechanism of psoralidin on promoting osteogenesis and inhibiting adipogenesis

Author:
Cao, Hui-juan; Li, Cai-rong; Wang, Lin-ying; Ziadlou, Reihane; Grad, Sibylle; Zhang, Yan; Cheng, Yan; Lai, Yu-xiao; Yao, Xin-sheng; Alini, Mauro; Qin, Ling; Wang, Xin-luan
Source:
Phytomedicine 2019 v.61 pp. 152860
ISSN:
0944-7113
Subject:
G-protein coupled receptors,   etc   ; Cullen corylifolium; G-proteins; adipocytes; adipogenesis; agonists; alkaline phosphatase; antagonists; beta catenin; bone formation; bone marrow; calcium; coumestrol; enzyme activity; estradiol; estrogen receptors; gene expression regulation; glycogen synthase kinases; mesenchymal stromal cells; messenger RNA; mineralization; non-specific serine/threonine protein kinase; oils; osteocalcin; osteoporosis; postmenopause; protein synthesis; tau-protein kinase;     Show all 28 Subjects
Abstract:
... Psoralidin (PL), a prenylated coumestrol, is isolated from Psoralea corylifolia L. (Fabaceae), which is frequently used for treatment of osteoporosis.This study was designed to investigate the dual effects and potential mechanism of PL on promoting osteogenesis and inhibiting adipogenesis.Bone marrow mesenchymal stem cells (BMSCs) were used to investigate the effect of PL on stimulating osteogenes ...
DOI:
10.1016/j.phymed.2019.152860

19. Protease-activated receptor 2 (PAR2) upregulates granulocyte colony stimulating factor (G-CSF) expression in breast cancer cells

Author:
Carvalho, Érika; Hugo de Almeida, Vitor; Rondon, Araci M.R.; Possik, Patricia A.; Viola, João P.B.; Monteiro, Robson Q.
Source:
Biochemical and biophysical research communications 2018 v.504 no.1 pp. 270-276
ISSN:
0006-291X
Subject:
G-protein coupled receptors,   etc   ; G-proteins; agonists; antagonists; breast neoplasms; cell lines; databases; gene overexpression; granulocyte colony-stimulating factor; metastasis; neoplasm cells; neutrophils; secretion;     Show all 13 Subjects
Abstract:
... Protease-activated receptor 2 (PAR2) is a G-protein coupled receptor which is activated upon cleavage of its N-terminal region. PAR2 has been associated with many aspects regarding tumor progression, such as the production of pro-tumoral cytokines. Granulocyte colony-stimulating factor (G-CSF) is a cytokine essential to neutrophil production and maturation, and it is often overexpressed in tumors. ...
DOI:
10.1016/j.bbrc.2018.08.169

20. Entry from the Lipid Bilayer: A Possible Pathway for Inhibition of a Peptide G Protein-Coupled Receptor by a Lipophilic Small Molecule

Author:
Bokoch, Michael P.; Jo, Hyunil; Valcourt, James R.; Srinivasan, Yoga; Pan, Albert C.; Capponi, Sara; Grabe, Michael; Dror, Ron O.; Shaw, David E.; DeGrado, William F.; Coughlin, Shaun R.
Source:
Biochemistry 2018 v.57 no.39 pp. 5748-5758
ISSN:
1520-4995
Subject:
G-protein coupled receptors,   etc   ; agonists; antagonists; crystal structure; dissociation; drugs; ligands; lipid bilayers; lipids; lipophilicity; molecular dynamics; peptides; rhodopsin; simulation models; solvents; thrombin;     Show all 16 Subjects
Abstract:
... The pathways that G protein-coupled receptor (GPCR) ligands follow as they bind to or dissociate from their receptors are largely unknown. Protease-activated receptor-1 (PAR1) is a GPCR activated by intramolecular binding of a tethered agonist peptide that is exposed by thrombin cleavage. By contrast, the PAR1 antagonist vorapaxar is a lipophilic drug that binds in a pocket almost entirely occlude ...
DOI:
10.1021/acs.biochem.8b00577