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- Author:
- Guilin R. Ren; Jonas Folke; Frank Hauser; Shizhong Li; Cornelis J.P. Grimmelikhuijzen
- Source:
- Biochemical and biophysical research communications 2015 v.462 pp. 358-364
- ISSN:
- 0006-291X
- Subject:
- Drosophila melanogaster; G-protein coupled receptors; acetylcholine; agonists; amino acids; antagonists; arthropods; atropine; cholinergic receptors; genome; mammals; pharmacology
- Abstract:
- ... Muscarinic acetylcholine receptors (mAChRs) are G protein-coupled receptors (GPCRs) that are activated by the agonists acetylcholine and muscarine and blocked by several antagonists, among them atropine. In mammals five mAChRs (m1-m5) exist of which m1, m3, and m5 are coupled to members of the Gq/11 family and m2 and m4 to members of the Gi/0 family. We have recently shown that Drosophila melanoga ...
- DOI:
- 10.1016/j.bbrc.2015.04.141
- https://doi.org/10.1016/j.bbrc.2015.04.141
- Author:
- Chunling Li; Jingjing Xie; Zhigang Lu; Chen Chen; Yancun Yin; Renhui Zhan; Yi Fang; Xuemei Hu; Cheng Cheng Zhang
- Source:
- Biochemical and biophysical research communications 2015 v.465 pp. 47-52
- ISSN:
- 0006-291X
- Subject:
- G-protein coupled receptors; adenylate cyclase; adults; apoptosis; cell growth; databases; humans; myeloid leukemia; neoplasm cells; pathogenesis; patients; relapse
- Abstract:
- ... Acute myeloid leukemia (AML) is the most common adult acute leukemia. Despite treatment, the majority of the AML patients relapse within 5 years. In silico analysis of several available databases of AML patients showed that the expression of adenylate cyclase 7 (ADCY7) significantly inversely correlates with the overall survival of AML patients. To determine whether ADCY7 supports AML development, ...
- DOI:
- 10.1016/j.bbrc.2015.07.123
- PubMed:
- 26220344
- PubMed Central:
- PMC4554980
- https://doi.org/10.1016/j.bbrc.2015.07.123
- Author:
- Sung-Kuk Cho; Jung-Mi Choi; Jong-Mu Kim; Jae Youl Cho; Sung-Soo Kim; Sungyoul Hong; Haeyoung Suh-Kim; Young-Don Lee
- Source:
- Biochemical and biophysical research communications 2015 v.467 pp. 1063-1069
- ISSN:
- 0006-291X
- Subject:
- G-protein coupled receptors; extracellular matrix; glycoproteins; ligands; mice; mitogen-activated protein kinase; neurites; pertussis toxin; phosphatidylinositol 3-kinase; phosphorylation; postpartum period; precipitin tests; signal transduction; tau-protein kinase; transfection
- Abstract:
- ... Reelin, a large secreted extracellular matrix glycoprotein, plays a key role in neuronal migration during cortical development and promotes neuronal maturation. The signaling pathway regulating neuronal maturation in the postnatal period are relatively less well understood. In this study, we demonstrated that a heterotrimeric G protein, Go, is a novel target of Reelin-induced signaling to promote ...
- DOI:
- 10.1016/j.bbrc.2015.09.167
- https://doi.org/10.1016/j.bbrc.2015.09.167
- Author:
- Yingkai Sun; Jie Hong; Maopei Chen; Yingying Ke; Shaoqian Zhao; Wen Liu; Qinyun Ma; Juan Shi; Yaoyu Zou; Tinglu Ning; Zhiguo Zhang; Ruixin Liu; Jiqiu Wang; Guang Ning
- Source:
- Biochemical and biophysical research communications 2015 v.464 pp. 396-400
- ISSN:
- 0006-291X
- Subject:
- G-protein coupled receptors; body weight; energy; fasting; fatty acids; food intake; fuels; gene expression; genes; glucose; glucose transporters; heterozygosity; homozygosity; humans; lipid metabolism; mice; mutants; mutation; skeletal muscle; white adipose tissue
- Abstract:
- ... Leucine-rich repeat-containing G protein-coupled receptor 4 (Lgr4) is a newfound obese-associated gene. Previous study reveals that heterozygous mutation of Lgr4 correlates with decreased body weight in human. In our recent study, we demonstrate that Lgr4 ablation promotes browning of white adipose tissue and improves whole-body metabolic status. However little is known about its role in other met ...
- DOI:
- 10.1016/j.bbrc.2015.06.066
- https://doi.org/10.1016/j.bbrc.2015.06.066
- Author:
- Singh Rajesh; Ahalawat Navjeet; Murarka Rajesh K.
- Source:
- Journal of physical chemistry 2015 v.119 no.7 pp. 2806-2817
- ISSN:
- 1520-5207
- Subject:
- G-protein coupled receptors; G-proteins; agonists; anxiety; binding sites; brain; corticotropin-releasing hormone; crystal structure; crystallography; drugs; irritable bowel syndrome; metabolic diseases; models; molecular dynamics
- Abstract:
- ... G-protein-coupled receptors (GPCRs) constitute the largest family of membrane-bound proteins involved in translation of extracellular signals into intracellular responses. They regulate diverse physiological and pathophysiological processes, and hence, they are prime drug targets for therapeutic intervention. In spite of the recent advancements in membrane protein crystallography, limited informat ...
- DOI:
- 10.1021/jp509814n
- https://doi.org/10.1021/jp509814n
- Author:
- Chunyan Wu; Yaoyao Jia; Ji Hae Lee; Yeonji Kim; Sivakumar Sekharan; Victor S. Batista; Sung-Joon Lee
- Source:
- international journal of biochemistry & cell biology 2015 v.64 pp. 75-80
- ISSN:
- 1357-2725
- Subject:
- G-protein coupled receptors; cAMP-dependent protein kinase; calcium; cyclic AMP; genes; glycerol-3-phosphate acyltransferase; hepatocytes; ligands; metabolism; mitochondria; olfactory receptors; phosphorylation; tissues; triacylglycerols
- Abstract:
- ... Olfactory receptors (ORs) comprise the largest G protein-coupled receptor gene superfamily. Recent studies indicate that ORs are also expressed in non-olfactory organs, including metabolically active tissues, although their biological functions in these tissues are largely unknown. In this study, OR1A1 expression was detected in HepG2 liver cells. OR1A1 activation by (−)-carvone, a known OR1A1 lig ...
- DOI:
- 10.1016/j.biocel.2015.03.008
- https://doi.org/10.1016/j.biocel.2015.03.008
- Author:
- Hannah M. Stoveken; Alexander G. Hajduczok; Lei Xu; Gregory G. Tall
- Source:
- Proceedings of the National Academy of Sciences of the United States of America 2015 v.112 no.19 pp. 6194-6199
- ISSN:
- 0027-8424
- Subject:
- G-protein coupled receptors; adhesion; agonists; neoplasms; synthetic peptides
- Abstract:
- ... The large class of adhesion G protein-coupled receptors (aGPCRs) bind extracellular matrix or neighboring cell-surface ligands to regulate organ and tissue development through an unknown activation mechanism. We examined aGPCR activation using two prototypical aGPCRs, GPR56 and GPR110. Active dissociation of the noncovalently bound GPR56 or GPR110 extracellular domains (ECDs) from the respective s ...
- DOI:
- 10.1073/pnas.1421785112
- PubMed:
- 25918380
- PubMed Central:
- PMC4434738
- https://doi.org/10.1073/pnas.1421785112
- Author:
- Cheng-Chih Hsiao; Kerstin Keysselt; Hsin-Yi Chen; Doreen Sittig; Jörg Hamann; Hsi-Hsien Lin; Gabriela Aust
- Source:
- international journal of biochemistry & cell biology 2015 v.65 pp. 197-208
- ISSN:
- 1357-2725
- Subject:
- DNA; G-protein coupled receptors; adhesion; alternative splicing; apoptosis; blood serum; caspases; cell viability; enzyme inhibition; global positioning systems; neoplasm cells; proteolysis; tissues; tumor necrosis factors
- Abstract:
- ... The Adhesion G protein-coupled receptor (GPCR) CD97/ADGRE5 is induced, upregulated, and/or biochemically modified in various malignancies, compared to the corresponding normal tissues. As tumor cells are generally more resistant to apoptosis, we here studied the ability of CD97 to regulate tumor cell survival under apoptotic conditions. Stable overexpression of wild-type CD97 reduced serum starvat ...
- DOI:
- 10.1016/j.biocel.2015.06.007
- https://doi.org/10.1016/j.biocel.2015.06.007
- Author:
- M. Zandawala; Z. Hamoudi; A. B. Lange; I. Orchard
- Source:
- Insect molecular biology 2015 v.24 no.2 pp. 264-276
- ISSN:
- 0962-1075
- Subject:
- Chagas disease; G-protein coupled receptors; RNA interference; Rhodnius prolixus; adipokinetic hormone; adults; carbohydrates; complementary DNA; corpora cardiaca; disease vectors; double-stranded RNA; fat body; flight; gonadotropin-releasing hormone; hemolymph; insects; lipid content; males; mammals; neuropeptides; nucleotide sequences; proline; quantitative polymerase chain reaction
- Abstract:
- ... Neuropeptides and their G protein‐coupled receptors are widespread throughout Metazoa and in several cases, clear orthologues can be identified in both protostomes and deuterostomes. One such neuropeptide is the insect adipokinetic hormone (AKH), which is related to the mammalian gonadotropin‐releasing hormone. AKH has been studied extensively and is known to mobilize lipid, carbohydrates and prol ...
- DOI:
- 10.1111/imb.12157
- https://doi.org/10.1111/imb.12157
- Author:
- Klara R. Klein; Kathleen M. Caron
- Source:
- Cellular and molecular life sciences 2015 v.72 no.16 pp. 3115-3126
- ISSN:
- 1420-682X
- Subject:
- G-protein coupled receptors; endothelial cells; humans; lymphatic system
- Abstract:
- ... Over the past decade, we have begun to appreciate that the lymphatic vascular system does more than simply return plasma back into the circulatory system and, in fact, contributes to a wide variety of normal and disease states. For this reason, much research has been devoted to understanding how lymphatic vessels form and function, with a particular interest in which molecules contribute to lympha ...
- DOI:
- 10.1007/s00018-015-1921-3
- https://doi.org/10.1007/s00018-015-1921-3
- Author:
- Henry J. Pownall; Corina Rosales; Baiba K. Gillard; Antonio M. Gotto
- Source:
- Nutrients 2015 v.7 no.3 pp. 1992-2000
- ISSN:
- 2072-6643
- Subject:
- G-protein coupled receptors; G-proteins; acetates; adipose tissue; alcohols; blood lipids; cardioprotective effect; cardiovascular diseases; energy metabolism; glucose; ligands; lipoproteins; mechanistic models; metabolites; risk factors
- Abstract:
- ... Numerous studies have shown that cardiovascular disease is lower among alcohol consumers than among nonconsumers. Many of the metabolic effects of alcohol are mediated by its terminal metabolite, acetate, which has reported insulinemic properties. There have been few rational metabolic targets that underly its cardioprotective effects until it was reported that acetate, the terminal product of alc ...
- DOI:
- 10.3390/nu7031992
- PubMed:
- 25793631
- PubMed Central:
- PMC4377895
- https://doi.org/10.3390/nu7031992
- Author:
- Zhao-shun Yuan; Yang-zhao Zhou; Xiao-bo Liao; Jia-wen Luo; Kang-jun Shen; Ye-rong Hu; Lu Gu; Jian-ming Li; Chang-ming Tan; He-ming Chen; Xin-min Zhou
- Source:
- Amino acids 2015 v.47 no.12 pp. 2475-2482
- ISSN:
- 0939-4451
- Subject:
- G-protein coupled receptors; alkaline phosphatase; calcification; dose response; humans; mineralization; mitogen-activated protein kinase; phosphatidylinositol 3-kinase; protective effect; signal transduction; transcription factors
- Abstract:
- ... Aortic valve calcification (AVC), which used to be recognized as a passive and irreversible process, is now widely accepted as an active and regulated process characterized by osteoblastic differentiation of aortic valve interstitial cells (AVICs). Apelin, the endogenous ligand for G-protein-coupled receptor APJ, was found to have protective cardiovascular effects in several studies. However, the ...
- DOI:
- 10.1007/s00726-015-2020-3
- PubMed:
- 26142632
- PubMed Central:
- PMC4633450
- https://doi.org/10.1007/s00726-015-2020-3
13. Association of GPR126 gene polymorphism with adolescent idiopathic scoliosis in Chinese populations
- Author:
- Ji-Feng Xu; Guang-hai Yang; Xiao-Hong Pan; Shui-Jun Zhang; Chen Zhao; Bin-Song Qiu; Hai-Feng Gu; Jian-Fei Hong; Li Cao; Yu Chen; Bing Xia; Qin Bi; Ya-Ping Wang
- Source:
- Genomics 2015 v.105 pp. 101-107
- ISSN:
- 0888-7543
- Subject:
- case-control studies; etiology; messenger RNA; alternative splicing; scoliosis; haplotypes; phenotype; G-protein coupled receptors; linkage disequilibrium; gene expression; pathogenesis; genotyping; adolescents; patients; genetic variation; exons; introns; single nucleotide polymorphism; China
- Abstract:
- ... Idiopathic scoliosis is the most common pediatric spinal deformity affecting 1% to 3% of the population, and adolescent idiopathic scoliosis (AIS) accounts for approximately 80% of these cases; however, the etiology and pathogenesis of AIS are still uncertain. The current study aims to identify the relationship between G protein-coupled receptor 126 (GPR126) gene and AIS predisposition, to identif ...
- DOI:
- 10.1016/j.ygeno.2014.11.009
- https://doi.org/10.1016/j.ygeno.2014.11.009
- Author:
- Dyan MacWilliam; Peter Arensburger; Jason Higa; Xinping Cui; Michael E. Adams
- Source:
- Insect biochemistry and molecular biology 2015 v.62 pp. 154-167
- ISSN:
- 0965-1748
- Subject:
- G-protein coupled receptors; Manduca sexta; avoidance behavior; behavior change; calcium channels; chloride channels; gene expression; gene expression regulation; genes; imagos; insect larvae; insects; instars; molting; neurosecretory system; sequence analysis; sleep
- Abstract:
- ... During the transition from feeding to molting, larval insects undergo profound changes in behavior and patterns of gene expression regulated by the neuroendocrine system. For some species, a distinctive characteristic of molting larvae is presence of a quiescent state sometimes referred to as “molt-sleep”. Here, observations of 4th instar Manduca sexta larvae indicate the molting period involves a ...
- DOI:
- 10.1016/j.ibmb.2015.01.012
- https://doi.org/10.1016/j.ibmb.2015.01.012
- Author:
- Shin-ichi Terawaki; Rina Matsubayashi; Kanako Hara; Tatsuki Onozuka; Toshiyuki Kohno; Kaori Wakamatsu
- Source:
- Biochemical and biophysical research communications 2015 v.463 pp. 64-69
- ISSN:
- 0006-291X
- Subject:
- G-protein coupled receptors; G-proteins; acetylcholine; cholinergic receptors; glycine (amino acid); guanine; guanine nucleotide exchange factors; nerve tissue
- Abstract:
- ... Muscarinic acetylcholine receptors (mAChRs) are G-protein coupled receptors (GPCRs) that are activated by acetylcholine released from parasympathetic nerves. The mAChR family comprises 5 subtypes, m1–m5, each of which has a different coupling selectivity for heterotrimeric GTP-binding proteins (G-proteins). m4 mAChR specifically activates the Gi/o family by enhancing the guanine nucleotide exchang ...
- DOI:
- 10.1016/j.bbrc.2015.05.018
- https://doi.org/10.1016/j.bbrc.2015.05.018
- Author:
- Mitsuru Hattori; Takeaki Ozawa
- Source:
- RSC advances 2015 v.5 no.17 pp. 12655-12663
- ISSN:
- 2046-2069
- Subject:
- G-protein coupled receptors; bioluminescence; drugs; energy transfer; gene expression; high-throughput screening methods; monitoring; screening; second messengers; therapeutics
- Abstract:
- ... G protein-coupled receptors (GPCRs) play crucial roles in numerous physiological and disorder-related processes. Because GPCRs are regarded as a target of many therapeutics, various methods for their analyses have been developed and applied for high-throughput screening of large chemical libraries. As a complement to the traditional analysis of second messengers and gene expression, direct monitor ...
- DOI:
- 10.1039/c4ra14979c
- https://doi.org/10.1039/c4ra14979c
- Author:
- William S. Powell; Joshua Rokach
- Source:
- Biochimica et biophysica acta 2015 v.1851 no.4 pp. 340-355
- ISSN:
- 1388-1981
- Subject:
- G-protein coupled receptors; antagonists; arachidonic acid; asthma; biosynthesis; cell proliferation; cytochrome P-450; diabetes; eosinophils; lipid peroxidation; metabolites; metastasis; neoplasm cells; neoplasms; oxidation; peroxisome proliferator-activated receptors; prostaglandin synthase; protective effect; therapeutics
- Abstract:
- ... Arachidonic acid can be oxygenated by a variety of different enzymes, including lipoxygenases, cyclooxygenases, and cytochrome P450s, and can be converted to a complex mixture of oxygenated products as a result of lipid peroxidation. The initial products in these reactions are hydroperoxyeicosatetraenoic acids (HpETEs) and hydroxyeicosatetraenoic acids (HETEs). Oxoeicosatetraenoic acids (oxo-ETEs) ...
- DOI:
- 10.1016/j.bbalip.2014.10.008
- PubMed:
- 25449650
- PubMed Central:
- PMC5710736
- https://doi.org/10.1016/j.bbalip.2014.10.008
- Author:
- Daniel G. Isom; Henrik G. Dohlman
- Source:
- Proceedings of the National Academy of Sciences of the United States of America 2015 v.112 no.18 pp. 5702-5707
- ISSN:
- 0027-8424
- Subject:
- G-protein coupled receptors; bacteria; epinephrine; neurotransmitters; norepinephrine; scientists
- Abstract:
- ... Seven-transmembrane receptors (7TMRs) have evolved in prokaryotes and eukaryotes over hundreds of millions of years. Comparative structural analysis suggests that these receptors may share a remote evolutionary origin, despite their lack of sequence similarity. Here we used structure-based computations to compare 221 7TMRs from all domains of life. Unexpectedly, we discovered that these receptors ...
- DOI:
- 10.1073/pnas.1417888112
- PubMed:
- 25902551
- PubMed Central:
- PMC4426463
- https://doi.org/10.1073/pnas.1417888112
- Author:
- Jillian L. Rourke; Helen J. Dranse; Christopher J. Sinal
- Source:
- Molecular and Cellular Endocrinology 2015 v.417 pp. 36-51
- ISSN:
- 0303-7207
- Subject:
- G-protein coupled receptors; adenocarcinoma; chemotaxis; energy; genes; immunity; ligands; lymphocytes; mitogen-activated protein kinase; signal transduction; transcription factors; transcriptional activation
- Abstract:
- ... Chemerin is an adipose-derived hormone that regulates immunity and energy homesotasis. To date, all known chemerin functions have been attributed to activation of the G protein-coupled receptor chemokine-like receptor-1 (CMKLR1). Chemerin is also the only known ligand for a second receptor, G protein-coupled receptor-1 (GPR1), whose signaling and function remains unknown. This study investigated t ...
- DOI:
- 10.1016/j.mce.2015.09.002
- https://doi.org/10.1016/j.mce.2015.09.002
20. Calcium-sensing receptor in the T lymphocyte enhanced the apoptosis and cytokine secretion in sepsis
- Author:
- Chun-li Wu; Qiu-yue Wu; Jing-jing Du; Jing-ya Zeng; Ting-ting Li; Chang-qing Xu; Yi-hua Sun
- Source:
- Molecular Immunology 2015 v.63 pp. 337-342
- ISSN:
- 0161-5890
- Subject:
- G-protein coupled receptors; T-lymphocytes; Western blotting; apoptosis; enzyme-linked immunosorbent assay; flow cytometry; interleukin-4; mitogen-activated protein kinase; phosphorylation; protein synthesis; rats; secretion; sepsis (infection); signal transduction; transcription factor NF-kappa B; tumor necrosis factor-alpha
- Abstract:
- ... Calcium-sensing receptor (CaSR) is a member of the G protein-coupled receptor superfamily that existed in lymphocytes and promoted cytokine secretion. Lymphocytes are also involved in sepsis. However, the role of CaSR in lymphocytes in sepsis is unclear. In this study, we want to examine whether the CaSR in lymphocytes in sepsis is involved in the cytokine secretions and apoptosis and make clear t ...
- DOI:
- 10.1016/j.molimm.2014.08.007
- https://doi.org/10.1016/j.molimm.2014.08.007
- Author:
- Fuxuan Wang; Shu Xiao; Yang Zhang; Yuehuan Zhang; Ying Liu; Yan Yan; Zhiming Xiang; Ziniu Yu
- Source:
- Fish & shellfish immunology 2015 v.47 no.2 pp. 1015-1023
- ISSN:
- 1050-4648
- Subject:
- Crassostrea; G-protein coupled receptors; active sites; angiogenesis; cell viability; complementary DNA; cytoplasm; gene overexpression; heat shock response; heat stress; larval development; messenger RNA; metabolism; molecular cloning; oysters; pathogens; protein-serine-threonine kinases; quantitative polymerase chain reaction; reporter genes; signal transduction; temperature; tissues; transcription (genetics); transcription factor NF-kappa B
- Abstract:
- ... G-protein-coupled receptors (GPCRs) are the largest class of cell-surface receptors and play crucial roles in virtually every organ system. As one of the major downstream effectors of GPCRs, Akt can acquire information from the receptors and coordinate intracellular responses for many signaling pathways, through which the serine/threonine kinase masters numerous aspects of biological processes, su ...
- DOI:
- 10.1016/j.fsi.2015.11.009
- https://doi.org/10.1016/j.fsi.2015.11.009
22. Changes in protein expression of pacific oyster Crassostrea gigas exposed in situ to urban sewage
- Author:
- Fabrício Flores-Nunes; Tânia Gomes; Rui Company; Roberta R. M. Moraes; Silvio T. Sasaki; Satie Taniguchi; Márcia C. Bicego; Cláudio M. R. Melo; Afonso C. D. Bainy; Maria J. Bebianno
- Source:
- Environmental science and pollution research international 2015 v.22 no.22 pp. 17267-17279
- ISSN:
- 0944-1344
- Subject:
- Crassostrea gigas; DNA damage; G-protein coupled receptors; apoptosis; biomarkers; cell cycle; coasts; cytoskeleton; ecotoxicology; effluents; farming systems; immune system; oyster culture; oysters; proteomics; sewage; signal transduction; ubiquitination
- Abstract:
- ... The composition and concentration of substances in urban effluents are complex and difficult to measure. These contaminants elicit biological responses in the exposed organisms. Proteomic analysis is a powerful tool in environmental toxicology by evidencing alterations in protein expression due to exposure to contaminants and by providing a useful framework for the development of new potential bio ...
- DOI:
- 10.1007/s11356-014-3821-8
- https://doi.org/10.1007/s11356-014-3821-8
23. Characterization of a tyramine receptor type 2 from hemocytes of rice stem borer, Chilo suppressalis
- Author:
- Shun-Fan Wu; Gang Xu; Gong-Yin Ye
- Source:
- Journal of insect physiology 2015 v.75 pp. 39-46
- ISSN:
- 0022-1910
- Subject:
- Chilo suppressalis; G-protein coupled receptors; Malpighian tubules; Western blotting; agonists; calcium; complementary DNA; dopamine; dose response; fat body; hemocytes; humans; immune response; immunohistochemistry; insect physiology; insects; invertebrates; kidneys; larvae; ligands; median effective concentration; messenger RNA; midgut; nerve tissue; octopamine; sequence homology; serotonin; tyramine
- Abstract:
- ... Calcium acts as a second messenger in many cell types, including insect hemocytes. Intracellular calcium level has a definite role in innate and adaptive immune signaling. Biogenic amines such as octopamine (OA), tyramine (TA), dopamine (DA) and serotonin (5-HT) play various important physiological roles in insects by activating distinct G-protein-coupled receptors (GPCRs) that share a putative se ...
- DOI:
- 10.1016/j.jinsphys.2015.03.004
- https://doi.org/10.1016/j.jinsphys.2015.03.004
- Author:
- Yutaka Suzuki; Satoshi Haga; Daiki Katoh; Kyoung-ha So; Ki-choon Choi; U-suk Jung; Hong-gu Lee; Kazuo Katoh; Sang-gun Roh
- Source:
- Biochemical and biophysical research communications 2015 v.466 pp. 283-288
- ISSN:
- 0006-291X
- Subject:
- G-protein coupled receptors; adipocytes; adiponectin; casein; cattle; chemoattractants; chemokines; epithelial cells; fatty acids; gene expression; gene expression regulation; genes; glucose; hepatocytes; insulin; insulin resistance; mammary glands; milk synthesis; prolactin; somatotropin; tumor necrosis factor-alpha
- Abstract:
- ... Chemerin is a chemoattractant cytokine (chemokine) produced by adipocytes and hepatocytes; it regulates insulin sensitivity and adipocyte differentiation. The objective of this study was to investigate the effect of chemerin on the expression of genes related to lactogenesis and the regulators of chemerin signaling in a bovine mammary epithelial cell line (MAC-T). Two types of chemerin receptors, ...
- DOI:
- 10.1016/j.bbrc.2015.08.105
- https://doi.org/10.1016/j.bbrc.2015.08.105
- Author:
- Rui Fang; Juan Su; Lucheng Zheng; Mengmeng Jin; Yuanlong Hou; Zhiyu Ma; Tingting Guo; Shenzheng Zhu; Xueli Ma; Ejlal Ahmed; Zhihai Lei
- Source:
- Research in veterinary science 2015 v.101 pp. 106-116
- ISSN:
- 0034-5288
- Subject:
- G-protein coupled receptors; brain; complementary DNA; energy metabolism; gene expression; immunohistochemistry; messenger RNA; molecular cloning; neuropeptides; protein synthesis; reverse transcriptase polymerase chain reaction; sequence analysis; swine; tissues
- Abstract:
- ... Neuropeptide W (NPW), a novel hypothalamic peptide, is an endogenous ligand for the orphan G protein-coupled receptors GPR7 (NPBWR1) and GPR8 (NPBWR2). Although several studies have implicated NPW in the regulation of feeding and energy metabolism in many species, the precise physiological function of NPW in pigs remains unclear. In this study, we cloned and sequenced NPW, GPR7, and GPR8 cDNA from ...
- DOI:
- 10.1016/j.rvsc.2015.06.001
- https://doi.org/10.1016/j.rvsc.2015.06.001
- Author:
- Matthias B. Van Hiel; Hans Peter Vandersmissen; Paul Proost; Jozef Vanden Broeck
- Source:
- Peptides 2015 v.68 pp. 83-90
- ISSN:
- 0196-9781
- Subject:
- Drosophila melanogaster; G-protein coupled receptors; fat body; females; fruit flies; genetic vectors; genome; imagos; larvae; males; mammals; midgut; open reading frames; plasmids; relaxin; tissue distribution; transmembrane proteins
- Abstract:
- ... Leucine-rich repeat containing G protein-coupled receptors (LGRs) comprise a cluster of transmembrane proteins, characterized by the presence of a large N-terminal extracellular domain. This receptor group can be classified into three subtypes. Belonging to the subtype C LGRs are the mammalian relaxin receptors LGR7 (RXFP1) and LGR8 (RXFP2), which mediate important reproductive and other processes ...
- DOI:
- 10.1016/j.peptides.2014.07.014
- https://doi.org/10.1016/j.peptides.2014.07.014
- Author:
- Ji-Hye Yun; Kuglae Kim; Youngjin Jung; Jae-Hyun Park; Hyun-Soo Cho; Weontae Lee
- Source:
- Biochemical and biophysical research communications 2015 v.456 pp. 116-121
- ISSN:
- 0006-291X
- Subject:
- G-protein coupled receptors; Spodoptera frugiperda; energy; gel chromatography; homeostasis; humans; lysozyme; melting point; mutants; obesity; solubility; thermal stability
- Abstract:
- ... G protein-coupled receptors (GPCRs) represent the largest family of transmembrane signaling proteins, and they are considered major targets of approximately half of all therapeutic agents. Human melanocortin-4 receptor (hMC4R) plays an important role in the control of energy homeostasis, and its mutants are directly related to severe human obesity. Here, we describe optimized protocols for the hig ...
- DOI:
- 10.1016/j.bbrc.2014.11.044
- https://doi.org/10.1016/j.bbrc.2014.11.044
- Author:
- Matthias Hillenbrand; Christian Schori; Jendrik Schöppe; Andreas Plöückthun
- Source:
- Proceedings of the National Academy of Sciences of the United States of America 2015 v.112 no.11 pp. E1181
- ISSN:
- 0027-8424
- Subject:
- G-protein coupled receptors; G-proteins; drugs; markets; mutants
- Abstract:
- ... Agonist binding to G-protein–coupled receptors (GPCRs) triggers signal transduction cascades involving heterotrimeric G proteins as key players. A major obstacle for drug design is the limited knowledge of conformational changes upon agonist binding, the details of interaction with the different G proteins, and the transmission to movements within the G protein. Although a variety of different GPC ...
- DOI:
- 10.1073/pnas.1417573112
- PubMed:
- 25733868
- PubMed Central:
- PMC4371982
- https://doi.org/10.1073/pnas.1417573112
- Author:
- Gene A. Morrill; Adele B. Kostellow; Raj K. Gupta
- Source:
- Biochemical and biophysical research communications 2015 v.459 pp. 36-41
- ISSN:
- 0006-291X
- Subject:
- Dionaea muscipula; G-protein coupled receptors; Homo sapiens; Markov chain; calcium; crystallography; gamma-aminobutyric acid; glutamic acid; ion channels; lipids; monitoring; neural networks; neurotransmitters; plasma membrane
- Abstract:
- ... The extracellular Ca2+ sensing receptor (CaSR) belongs to Class C G-protein-coupled receptors (GPCRs) which include receptors for amino acids, γ-aminobutyric acid and glutamate neurotransmitters. CaSR has been described as having an extended sequence containing a Ca2+ binding pocket within an extracellular amino (N)-terminal domain, called a Venus Fly Trap (VFT) module. CaSR is thought to consist ...
- DOI:
- 10.1016/j.bbrc.2015.02.049
- https://doi.org/10.1016/j.bbrc.2015.02.049
- Author:
- M. Rasmussen; M. Leander; S. Ons; R. Nichols
- Source:
- Peptides 2015 v.71 pp. 259-267
- ISSN:
- 0196-9781
- Subject:
- Anopheles gambiae; Bombyx mori; Drosophila melanogaster; G-protein coupled receptors; Rhodnius prolixus; Tribolium castaneum; adipokinetic hormone; ligands; neuropeptides; peptide receptors; tyrosine
- Abstract:
- ... Peptides may act through G protein-coupled receptors to influence cardiovascular performance; thus, delineating mechanisms involved in signaling is a molecular-based strategy to influence health. Molecular switches, often represented by conserved motifs, maintain a receptor in an inactive state. However, once the switch is broken, the transmembrane regions move and activation occurs. The molecular ...
- DOI:
- 10.1016/j.peptides.2015.07.012
- https://doi.org/10.1016/j.peptides.2015.07.012
- Author:
- Edward S. Chambers; Douglas J. Morrison; Gary Frost
- Source:
- Proceedings of the Nutrition Society 2015 v.74 no.3 pp. 328-336
- ISSN:
- 1475-2719
- Subject:
- G-protein coupled receptors; acetates; adipocytes; adipose tissue; animal models; appetite; biochemical pathways; dietary fiber; digestive system; energy intake; epithelium; feeding behavior; fermentation; free fatty acids; glucagon-like peptide 1; glucose; homeostasis; humans; leptin; obesity; propionic acid; ruminants; tyrosine; weight control
- Abstract:
- ... In recent years, there has been a renewed interest in the role of dietary fibre in obesity management. Much of this interest stems from animal and human studies which suggest that an increased intake of fermentable fibre can suppress appetite and improve weight management. A growing number of reports have demonstrated that the principal products of colonic fermentation of dietary fibre, SCFA, cont ...
- DOI:
- 10.1017/S0029665114001657
- PubMed:
- 25497601
- https://doi.org/10.1017/S0029665114001657
- Author:
- Jill E. Chrencik; Christopher B. Roth; Masahiko Terakado; Haruto Kurata; Rie Omi; Yasuyuki Kihara; Dora Warshaviak; Shinji Nakade; Guillermo Asmar-Rovira; Mauro Mileni; Hirotaka Mizuno; Mark T. Griffith; Caroline Rodgers; Gye Won Han; Jeffrey Velasquez; Jerold Chun; Raymond C. Stevens; Michael A. Hanson
- Source:
- Cell 2015 v.161 pp. 1633-1643
- ISSN:
- 0092-8674
- Subject:
- G-protein coupled receptors; antagonists; crystal structure; extracellular space; humans; ligands; lipids; molecular dynamics; sphingosine; therapeutics
- Abstract:
- ... Lipid biology continues to emerge as an area of significant therapeutic interest, particularly as the result of an enhanced understanding of the wealth of signaling molecules with diverse physiological properties. This growth in knowledge is epitomized by lysophosphatidic acid (LPA), which functions through interactions with at least six cognate G protein-coupled receptors. Herein, we present thre ...
- DOI:
- 10.1016/j.cell.2015.06.002
- PubMed:
- 26091040
- PubMed Central:
- PMC4476059
- https://doi.org/10.1016/j.cell.2015.06.002
33. Cyclic AMP concentrations in dendritic cells induce and regulate Th2 immunity and allergic asthma
- Author:
- Jihyung Lee; Tae Hoon Kim; Fiona Murray; Xiangli Li; Sara S. Choi; David H. Broide; Maripat Corr; Jongdae Lee; Nicholas J. G. Webster; Paul A. Insel; Eyal Raz
- Source:
- Proceedings of the National Academy of Sciences of the United States of America 2015 v.112 no.5 pp. 1529-1534
- ISSN:
- 0027-8424
- Subject:
- CD4-positive T-lymphocytes; G-protein coupled receptors; adenosine monophosphate; asthma; cell differentiation; cyclic AMP; dendritic cells; humans; immunity; inflammation; mice
- Abstract:
- ... The inductive role of dendritic cells (DC) in Th2 differentiation has not been fully defined. We addressed this gap in knowledge by focusing on signaling events mediated by the heterotrimeric GTP binding proteins Gαs, and Gαi, which respectively stimulate and inhibit the activation of adenylyl cyclases and the synthesis of cAMP. We show here that deletion of Gnas , the gene that encodes Gαs in mou ...
- DOI:
- 10.1073/pnas.1417972112
- PubMed:
- 25605931
- PubMed Central:
- PMC4321256
- https://doi.org/10.1073/pnas.1417972112
- Author:
- Allison M. Churcher; Peter C. Hubbard; João Pedro Marques; Adelino V. M. Canário; Mar Huertas
- Source:
- Molecular ecology 2015 v.24 no.4 pp. 822-834
- ISSN:
- 0962-1083
- Subject:
- Anguilla anguilla; G-protein coupled receptors; eel; epithelium; freshwater; gene expression regulation; genes; high-throughput nucleotide sequencing; males; odor compounds; phylogeny; reproduction; seawater; sexual maturity; signal transduction
- Abstract:
- ... Vertebrate genomes encode a diversity of G protein‐coupled receptor (GPCR) that belong to large gene families and are used by olfactory systems to detect chemical cues found in the environment. It is not clear however, if individual receptors from these large gene families have evolved roles that are specific to certain life stages. Here, we used deep sequencing to identify differentially expresse ...
- DOI:
- 10.1111/mec.13065
- https://doi.org/10.1111/mec.13065
- Author:
- A. K. Tiwari; J. Yui; Pooja; S. Aggarwal; T. Yamasaki; L. Xie; N. Chadha; Y. Zhang; M. Fujinaga; Y. Shimoda; K. Kumata; A. K. Mishra; M. Ogawa; M.-R. Zhang
- Source:
- RSC advances 2015 v.5 no.25 pp. 19752-19759
- ISSN:
- 2046-2069
- Subject:
- G-protein coupled receptors; binding capacity; biological assessment; brain; carbon dioxide; circadian rhythm; fluorescence; human serum albumin; image analysis; ligands; liver; longitudinal studies; mice; pharmacology; positron-emission tomography; radioactivity; rats; serotonin; sleep
- Abstract:
- ... The 5-HT₇ receptor is a recently cloned G-protein-coupled receptor (GPCR) that is important in regulating sleep, depression, and circadian rhythms. However, the potential pathophysiological roles of 5-HT₇ have not been fully elucidated, and no 5-HT₇ positron emission tomography (PET) radioligands are available, thus limiting imaging studies of this receptor in humans. Here, we present the radiosyn ...
- DOI:
- 10.1039/c4ra15833d
- https://doi.org/10.1039/c4ra15833d
- Author:
- Ihara Masaru; Inoue Asuka; Hanamoto Seiya; Zhang Han; Aoki Junken; Tanaka Hiroaki
- Source:
- Environmental Science & Technology 2015 v.49 no.3 pp. 1903-1911
- ISSN:
- 1520-5851
- Subject:
- G-protein coupled receptors; acetylcholine; aquatic environment; aquatic organisms; bioactive properties; cannabinoids; dopamine; histamine; humans; risk; serotonin; transforming growth factor alpha; vasopressin; wastewater
- Abstract:
- ... Although pharmaceuticals are generally found at very low levels in aquatic environments, concern about their potential risks to humans and aquatic species has been raised because they are designed to be biologically active. To resolve this concern, we must know whether the biological activity of pharmaceuticals can be detected in waters. Nearly half of all marketed pharmaceuticals act by binding t ...
- DOI:
- 10.1021/es505349s
- https://doi.org/10.1021/es505349s
- Author:
- Mayu Kasubuchi; Sae Hasegawa; Takero Hiramatsu; Atsuhiko Ichimura; Ikuo Kimura
- Source:
- Nutrients 2015 v.7 no.4 pp. 2839-2849
- ISSN:
- 2072-6643
- Subject:
- G-protein coupled receptors; acetates; butyrates; diabetes; dietary fiber; energy; epigenetics; fermentation; gene expression; histone deacetylase; intestinal microorganisms; intestines; metabolites; obesity; propionic acid; short chain fatty acids; signal transduction; tissues
- Abstract:
- ... During feeding, the gut microbiota contributes to the host energy acquisition and metabolic regulation thereby influencing the development of metabolic disorders such as obesity and diabetes. Short-chain fatty acids (SCFAs) such as acetate, butyrate, and propionate, which are produced by gut microbial fermentation of dietary fiber, are recognized as essential host energy sources and act as signal ...
- DOI:
- 10.3390/nu7042839
- PubMed:
- 25875123
- PubMed Central:
- PMC4425176
- https://doi.org/10.3390/nu7042839
- Author:
- Taro Horiba; Masahiro Katsukawa; Moeko Mita; Ryuichiro Sato
- Source:
- Biochemical and biophysical research communications 2015 v.463 pp. 846-852
- ISSN:
- 0006-291X
- Subject:
- Citrus; G-protein coupled receptors; adipocytes; bile; bioactive properties; blood glucose; diet; dose response; glycosylation; hemoglobin; hyperglycemia; hypertrophy; limonoids; mice; muscles; obesity; peroxisome proliferator-activated receptors; reporter genes; tissue weight; transcription (genetics); white adipose tissue
- Abstract:
- ... Obacunone is a limonoid that is predominantly found in Citrus. Although various biological activities of limonoids have been reported, little is known about the beneficial effects of obacunone on metabolic disorders. In the present study, we examined the effects of dietary obacunone supplementation on obese KKAy mice, to clarify the function of obacunone in metabolic regulation. Mice were pair-fed ...
- DOI:
- 10.1016/j.bbrc.2015.06.022
- https://doi.org/10.1016/j.bbrc.2015.06.022
- Author:
- Youngjoo Yun; Dong Kyun Kim; Min-Duk Seo; Kyeong-Man Kim; Ka Young Chung
- Source:
- Biochemical and biophysical research communications 2015 v.457 pp. 50-57
- ISSN:
- 0006-291X
- Subject:
- G-protein coupled receptors; arrestins; deuterium; mass spectrometry; mutants
- Abstract:
- ... Arrestins have important roles in G protein-coupled receptor (GPCR) signaling including desensitization of GPCRs and G protein-independent signaling. There have been four arrestins identified: arrestin1, arrestin2 (e.g. β-arrestin1), arrestin3 (e.g. β-arrestin2), and arrestin4. β-Arrestin1 and β-arrestin2 are ubiquitously expressed and regulate a broad range of GPCRs, while arrestin1 and arrestin4 ...
- DOI:
- 10.1016/j.bbrc.2014.12.079
- https://doi.org/10.1016/j.bbrc.2014.12.079
- Author:
- Aiysha Thompson; Venkateswarlu Kanamarlapudi
- Source:
- Molecular and Cellular Endocrinology 2015 v.413 pp. 66-77
- ISSN:
- 0303-7207
- Subject:
- G-protein coupled receptors; cyclic AMP; drugs; glucagon-like peptide 1; humans; insulin secretion; mutation; noninsulin-dependent diabetes mellitus; plasma membrane
- Abstract:
- ... The glucagon-like peptide-1 (GLP-1) receptor (GLP-1R), an important drug target in the treatment of type 2 diabetes, is a G-protein coupled receptor (GPCR) that mediates insulin secretion by GLP-1. The N-terminus controls GLP-1R biosynthetic trafficking to the cell surface but the C-terminus involvement in that trafficking is unknown. The aim of this study was to identify distinct regions within t ...
- DOI:
- 10.1016/j.mce.2015.06.012
- https://doi.org/10.1016/j.mce.2015.06.012
- Author:
- Daniel Morales-González; Ernesto Flores-Martínez; Roberto Zamora-Bustillos; Reginaldo Rivera-Reyes; Jesús Emilio Michel-Morfín; Víctor Landa-Jaime; Andrés Falcón; Manuel B. Aguilar
- Source:
- Peptides 2015 v.68 pp. 25-32
- ISSN:
- 0196-9781
- Subject:
- Conus; G-protein coupled receptors; amino acids; coasts; complementary DNA; conotoxins; disulfide bonds; drug design; ion channels; muscles; neurotransmitters; nicotinic receptors; peptides; post-translational modification; predators; reverse transcriptase polymerase chain reaction; signal peptide; snails; toxins; transporters
- Abstract:
- ... Conus marine snails (∼500 species) are tropical predators that use venoms mainly to capture prey and defend themselves from predators. The principal components of these venoms are peptides that are known as “conotoxins” and generally comprise 7–40 amino acid residues, including 0–5 disulfide bridges and distinct posttranslational modifications. The most common molecular targets of conotoxins are v ...
- DOI:
- 10.1016/j.peptides.2015.02.002
- https://doi.org/10.1016/j.peptides.2015.02.002
- Author:
- Laurent Rouméas; Jean-Paul Humbert; Séverine Schneider; Christelle Doebelin; Isabelle Bertin; Martine Schmitt; Jean-Jacques Bourguignon; Frédéric Simonin; Frédéric Bihel
- Source:
- Peptides 2015 v.71 pp. 156-161
- ISSN:
- 0196-9781
- Subject:
- G-protein coupled receptors; agonists; antagonists; kisspeptin; ligands; mammals; prolactin
- Abstract:
- ... Mammalian RF-amide peptides including RF-amide-related peptides-1 and -3, neuropeptides AF and FF, Prolactin releasing peptides, Kisspeptins and RFa peptides are currently considered endogenous peptides for the GPCRs NPFF1R, NPFF2R, GPR10, GPR54 and GPR103, respectively. While NPFF1R and NPFF2R displayed high affinity for all the RF-amide peptides, GPR10, GPR54 and GPR103 only bind their cognate l ...
- DOI:
- 10.1016/j.peptides.2015.07.016
- https://doi.org/10.1016/j.peptides.2015.07.016
- Author:
- Arif U. Hasan; Koji Ohmori; Kumi Konishi; Junsuke Igarashi; Takeshi Hashimoto; Kazuyo Kamitori; Fuminori Yamaguchi; Ikuko Tsukamoto; Toru Uyama; Yasuhiro Ishihara; Takahisa Noma; Masaaki Tokuda; Masakazu Kohno
- Source:
- Molecular and Cellular Endocrinology 2015 v.406 pp. 10-18
- ISSN:
- 0303-7207
- Subject:
- G-protein coupled receptors; adipocytes; angiogenesis; chromatin; eicosapentaenoic acid; gene expression; genes; inflammation; insulin resistance; luciferase; messenger RNA; peroxisome proliferator-activated receptors; precipitin tests; promoter regions; transfection; vascular endothelial growth factor A
- Abstract:
- ... Vascular endothelial growth factor-A (VEGF-A) released from adipocytes promotes angiogenesis; and thereby ameliorates the local hypoxia-induced adipose inflammation and insulin resistance. Here, we newly found that eicosapentaenoic acid (EPA) upregulated both mRNA expression and release of VEGF-A in mature 3T3-L1 adipocytes. Silencing mRNA of G-protein coupled receptor 120 (GPR120) and specific in ...
- DOI:
- 10.1016/j.mce.2015.02.012
- https://doi.org/10.1016/j.mce.2015.02.012
- Author:
- Davy Baudelet; Christophe Furman; Alina Ghinet; Xavier Dezitter; Sahil Adriouch; Frédéric Capet; Tiphaine Rogez-Florent; Philippe Gautret; Benoit Rigo; Régis Millet; Claude Vaccher; Emmanuelle Lipka
- Source:
- Journal of Chromatography B 2015 v.986-987 pp. 35-43
- ISSN:
- 1570-0232
- Subject:
- Alzheimer disease; G-protein coupled receptors; adenosine triphosphate; antagonists; capillary electrophoresis; cyclodextrins; cytotoxicity; detection limit; enantiomers; high performance liquid chromatography; humans; inhibitory concentration 50; ischemia; ligands; medicinal properties; neoplasms; neurodegenerative diseases; stereoisomerism; supercritical fluid chromatography
- Abstract:
- ... The P2X receptors are seven-transmembrane domain G protein-coupled receptors and the 7 subtypes of P2X receptors identified in humans, and named P2X1 to P2X7, are channel receptors whose endogenous ligand is ATP. New antagonists of the P2X7 receptor were developed, since this purinergic receptor was highlighted to be involved in many diseases such as different types of pain, cancer, ischemia, neur ...
- DOI:
- 10.1016/j.jchromb.2015.02.001
- https://doi.org/10.1016/j.jchromb.2015.02.001
- Author:
- Simona Francia; Lucia Silvotti; Filippo Ghirardi; François Catzeflis; Riccardo Percudani; Roberto Tirindelli
- Source:
- Genome Biology and Evolution 2015 v.7 no.1 pp. 272-285
- Subject:
- Cricetidae; G-protein coupled receptors; databases; ligands; major histocompatibility complex; mice; neurons; peptides; pheromones; phylogeny
- Abstract:
- ... The vomeronasal organ (VNO) is an olfactory structure for the detection of pheromones. VNO neurons express three groups of unrelated G-protein-coupled receptors. Type-2 vomeronasal receptors (V2Rs) are specifically localized in the basal neurons of the VNO and are believed to sense protein pheromones eliciting specific reproductive behaviors. In murine species, V2Rs are organized into four familie ...
- DOI:
- 10.1093/gbe/evu283
- PubMed:
- 25539725
- PubMed Central:
- PMC4316634
- https://doi.org/10.1093/gbe/evu283
- Author:
- Arunkumar Krishnan; Arshi Mustafa; Markus Sällman Almén; Robert Fredriksson; Michael J. Williams; Helgi B. Schiöth
- Source:
- Molecular phylogenetics and evolution 2015 v.91 pp. 27-40
- ISSN:
- 1055-7903
- Subject:
- Drosophila melanogaster; G-protein coupled receptors; arthropods; eyes; multigene family; phylogeny; signal transduction; vertebrates
- Abstract:
- ... Heterotrimeric G proteins perform a crucial role as molecular switches controlling various cellular responses mediated by G protein-coupled receptor (GPCR) signaling pathway. Recent data have shown that the vertebrate-like G protein families are found across metazoans and their closest unicellular relatives. However, an overall evolutionary hierarchy of vertebrate-like G proteins, including gene f ...
- DOI:
- 10.1016/j.ympev.2015.05.009
- https://doi.org/10.1016/j.ympev.2015.05.009
- Author:
- Camille Meslin; Colette Desert; Isabelle Callebaut; Anis Djari; Christophe Klopp; Frédérique Pitel; Sophie Leroux; Pascal Martin; Pascal Froment; Edith Guilbert; Florence Gondret; Sandrine Lagarrigue; Philippe Monget
- Source:
- Genome Biology and Evolution 2015 v.7 no.5 pp. 1332-1348
- Subject:
- DNA; G-protein coupled receptors; adipose tissue; amino acids; chickens; domestication; evolution; free fatty acids; gene conversion; gene dosage; gene expression; genes; intestines; linkage groups; lipid metabolism; mononuclear leukocytes; obesity; quantitative polymerase chain reaction; risk; sequence homology; splenocytes; testes
- Abstract:
- ... Free fatty acid receptors (FFAR) belong to a family of five G-protein coupled receptors that are involved in the regulation of lipid metabolism, so that their loss of function increases the risk of obesity. The aim of this study was to determine the expansion of genes encoding paralogs of FFAR2 in the chicken, considered as a model organism for developmental biology and biomedical research. By est ...
- DOI:
- 10.1093/gbe/evv072
- PubMed:
- 25912043
- PubMed Central:
- PMC4453067
- https://doi.org/10.1093/gbe/evv072
- Author:
- Claudio N. Cavasotto; Damián Palomba
- Source:
- Chemical communications 2015 v.51 no.71 pp. 13576-13594
- ISSN:
- 1364-548X
- Subject:
- G-protein coupled receptors; crystallography; drugs; flowering; humans; ligands; models; prospective studies; quantitative structure-activity relationships; site-directed mutagenesis; therapeutics
- Abstract:
- ... With >800 members in humans, the G protein-coupled receptor (GPCR) super-family is the target for more than 30% of the marketed drugs. The recent boom in GPCR crystallography has enabled the solution of ∼30 different GPCR structures, which boosted the identification and optimization of novel modulators and new chemical entities through structure-based strategies. However, the number of available s ...
- DOI:
- 10.1039/c5cc05050b
- https://doi.org/10.1039/c5cc05050b
- Author:
- Thangaraj Sindhu; Pappu Srinivasan
- Source:
- RSC advances 2015 v.5 no.19 pp. 14202-14213
- ISSN:
- 2046-2069
- Subject:
- G-protein coupled receptors; G-proteins; Gibbs free energy; agonists; binding properties; computer simulation; diabetes; human cell lines; hydrogen bonding; lipid bilayers; metabolic syndrome; molecular dynamics; new drugs; obesity
- Abstract:
- ... TGR5, a G-protein coupled receptor, acts as a promising target for the treatment of diabetes, obesity and metabolic syndromes. Understanding the activation of TGR5, the structural conformation and the mode of mechanism upon binding with agonists is crucial for the development of new drugs. In the absence of experimental data, homology modeling was performed to predict the structure of TGR5. Molecu ...
- DOI:
- 10.1039/c4ra16617e
- https://doi.org/10.1039/c4ra16617e
- Author:
- Samar El-Kholy; Flora Stephano; Yong Li; Anita Bhandari; Christine Fink; Thomas Roeder
- Source:
- Cell and tissue research 2015 v.361 no.3 pp. 669-684
- ISSN:
- 0302-766X
- Subject:
- Drosophila melanogaster; G-protein coupled receptors; epinephrine; fruit flies; heart; imagos; invertebrates; larvae; memory; monoamines; muscles; mushroom bodies; norepinephrine; octopamine; promoter regions; skeletal muscle; tyramine
- Abstract:
- ... The monoamines octopamine and tyramine, which are the invertebrate counterparts of epinephrine and norepinephrine, transmit their action through sets of G protein-coupled receptors. Four different octopamine receptors (Oamb, Octß1R, Octß2R, Octß3R) and 3 different tyramine receptors (TyrR, TyrRII, TyrRIII) are present in the fruit fly Drosophila melanogaster. Utilizing the presumptive promoter reg ...
- DOI:
- 10.1007/s00441-015-2137-4
- https://doi.org/10.1007/s00441-015-2137-4
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