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Journal of Receptor and Signal Transduction Research

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https://www.readbyqxmd.com/read/28292218/high-glucose-induces-alternative-activation-of-macrophages-via-pi3k-akt-signaling-pathway
#1
Jie Wang, Jingjing Liu, Yuying Wang, Minghui Lin, Wei Tian, Lingling Zhou, Xiaoyin Ye, Lihang Lin
OBJECTIVE: It has been proved that lactate-4.25% dialysate could result in peritoneal fibrosis by inducing alternative activation of macrophages in our previous study, but the mechanism of high glucose-induced alternative activation has not been elucidated. This study was, therefore, to investigate the mechanism by high glucose stimuli. METHODS: In this study, Raw264.7 (murine macrophage cell line) cells were cultured and stimulated by 4.25% glucose medium, and mannitol medium was used as osmotic pressure control...
March 15, 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/28279120/ccl11-promotes-angiogenic-activity-by-activating-the-pi3k-akt-pathway-in-huvecs
#2
Jun Young Park, Yeo Wool Kang, Byung Young Choi, Young Chul Yang, Byung Pil Cho, Won Gil Cho
CCR3, the receptor for CCL11, is expressed on the surface of immune cells and even on non-immune cells. CCL11-CCR3 interactions can promote cell migration and proliferation. In this study, we investigated the effect of CCL11 on angiogenesis in HUVECs and also examined the molecular mechanisms of this process. We found that CCL11 induced mRNA transcription and protein expression of CCR3 in HUVECs. Moreover, the scratch wound healing assay and MTS proliferation assay both demonstrated that CCL11 promotes endothelial cell migration and induces weak proliferation...
March 9, 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/28270026/manganese-and-cobalt-activate-zebrafish-ovarian-cancer-g-protein-coupled-receptor-1-but-not-gpr4
#3
Jun Negishi, Yuka Omori, Mami Shindo, Hayate Takanashi, Shiori Musha, Suminori Nagayama, Jun Hirayama, Hiroshi Nishina, Takashi Nakakura, Chihiro Mogi, Koichi Sato, Fumikazu Okajima, Yuta Mochimaru, Hideaki Tomura
Mammalian ovarian G-protein-coupled receptor 1 (OGR1) is activated by some metals in addition to extracellular protons and coupling to multiple intracellular signaling pathways. In the present study, we examined whether zebrafish OGR1, zebrafish GPR4, and human GPR4 (zOGR1, zGPR4, and hGPR4, respectively) could sense the metals and activate the intracellular signaling pathways. On one hand, we found that only manganese and cobalt of the tested metals stimulated SRE-promoter activities in zOGR1-overexpressed HEK293T cells...
March 7, 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/28270014/evidence-of-alterations-in-the-expression-of-orphan-receptors-gpr26-and-gpr39-due-to-the-etiology-of-the-metabolic-syndrome
#4
Rodrigo Romero-Nava, De-Shan Zhou, Noemí García, Armando Ruiz-Hernández, Yin-Chu Si, Fausto Sánchez-Muñoz, Fengyang Huang, Enrique Hong, Santiago Villafaña
AIMS: Metabolic syndrome (MS) is composed of several metabolic abnormalities that increase the risk of cardiovascular diseases and diabetes. Although there are treatments for the components of MS, this pathology maintains a high mortality, suggesting that there are other mechanisms in which orphan receptors such as GPR26 and GPR39 may be involved. For this reason, the aim of this work was to evaluate the expression of GPR26 and GPR39 orphan receptors in two models of MS (diet and genetics)...
March 7, 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/28264627/natural-polyphenolic-inhibitors-against-the-antiapoptotic-bcl-2
#5
Sharad Verma, Aditi Singh, Anchala Kumari, Chetna Tyagi, Sukriti Goyal, Salma Jamal, Abhinav Grover
The apoptotic mechanism is regulated by the BCL-2 family of proteins, such as BCL-2 or Bcl-xL, which block apoptosis while Bad, Bak, Bax, Bid, Bim or Hrk induce apoptosis. The overexpression of BCL-2 was found to be related to the progression of cancer and also providing resistance towards chemotherapeutic treatments. In the present study, we found that all polyphenols (apigenin, fisetin, galangin and luteolin) bind to the hydrophobic groove of BCL-2 and the interaction is stable throughout MD simulation run...
March 6, 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27829319/effect-of-different-concentrations-of-oxygen-on-expression-of-sigma-1-receptor-and-superoxide-dismutases-in-human-colon-adenocarcinoma-cell-lines
#6
Michał Skrzycki, Hanna Czeczot, Magdalena Mielczarek-Puta, Dagmara Otto-Ślusarczyk, Wojciech Graboń
CONTEXT: Tumor cells due to distance from capillary vessels exist in different oxygenation conditions (anoxia, hypoxia, normoxia). Changes in cell oxygenation lead to reactive oxygen species production and oxidative stress. Sigma 1 receptor (Sig1R) is postulated to be stress responding agent and superoxide dismutases (SOD1 and SOD2) are key antioxidant enzymes. It is possible that they participate in tumor cells adaptation to different concentrations of oxygen. OBJECTIVE: Evaluation of Sig1R, SOD1, and SOD2 expression in different concentrations of oxygen (1%, 10%, 21%) in colon adenocarcinoma cell lines...
June 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27808000/regulation-of-dendritic-cell-function-by-insulin-igf-1-pi3k-akt-signaling-through-klotho-expression
#7
Nguyen Thi Xuan, Nguyen Huy Hoang, Vu Phuong Nhung, Nguyen Thuy Duong, Nguyen Hai Ha, Nong Van Hai
Insulin or insulin-like growth factor 1 (IGF-1) promotes the activation of phosphoinositide 3 kinase (PI3K)/Akt signaling in immune cells including dendritic cells (DCs), the most potent professional antigen-presenting cells for naive T cells. Klotho, an anti-aging protein, participates in the regulation of the PI3K/Akt signaling, thus the Ca(2+)-dependent migration is reduced in klotho-deficient DCs. The present study explored the effects of insulin/IGF-1 on DC function through klotho expression. To this end, the mouse bone marrow cells were isolated and cultured with GM-CSF to attain bone marrow-derived DCs (BMDCs)...
June 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27807998/discovery-and-pharmacological-effects-of-a-novel-gpr142-antagonist
#8
Michiko Murakoshi, Harumi Kuwabara, Miyuki Nagasaki, Yu Mei Xiong, Jeff D Reagan, Hiroaki Maeda, Futoshi Nara
GPR142 is a G-protein-coupled receptor (GPCR), whose most potent and efficacious ligand has been reported as being the natural amino acid l-tryptophan. GPR142 is highly expressed in pancreatic β-cells and immune cells, suggesting the receptor may play a role in the pathogenesis and development of diabetes or inflammatory diseases. In a previous report, we developed GPR142 agonists as insulin secretagogues. In this report, we show the discovery of a selective, potent small-molecule GPR142 antagonist, CLP-3094, and its pharmacological characteristics...
June 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27807997/adenosine-receptors-expression-in-cardiac-fibroblasts-of-patients-with-left-ventricular-dysfunction-due-to-valvular-disease
#9
Silvia Del Ry, Manuela Cabiati, Veronica Della Latta, Stefania Zimbone, Mariarita Natale, Pietro Enea Lazzerini, Francesco Diciolla, Pier Leopoldo Capecchi, Franco Laghi-Pasini, Maria Aurora Morales
CONTEXT: Adenosine restores tissue homeostasis through the interaction with its membrane receptors (AR) expressed on fibroblasts, endothelial cells, smooth muscle cells and leukocytes, but their modulation is still not fully understood. OBJECTIVE: To evaluate whether changes in the transcriptomic profiling of adenosine receptors (AR) occur in cardiac fibroblasts (CF) of patients (pts) with LV dysfunction due to valvular disease (V). The secondary aim was to compare in the same pts the results obtained at cardiac level with those found in circulating leukocytes...
June 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27807993/effect-of-h4r-antagonist-n-2-aminoethyl-5-chloro-1h-indol-2-carboxamides-and-5-chloro-2-piperazin-1-ylmethyl-1h-benzimidazole-on-histamine-and-4-methylhistamine-induced-mast-cell-response
#10
Gomathi Nagarajan, Vairamani Mariappanadar, Muthu Tamizh, Ilango Kaliappan, Berla Thangam Elden
CONTEXT: The histamine plays a decisive role in acute and chronic inflammatory responses and is regulated through its four types of distinct receptors designated from H1 to H4. Recently histamine 4 receptor (H4R) antagonists have been reported to possess various pharmacological effects against various allergic diseases. OBJECTIVE: To investigate the inhibitory effect of N-(2-aminoethyl)-5-chloro-1H-indol-2-carboxamide (Compound A) and 5-chloro-2-(piperazin-1-ylmethyl)-1H-benzimidazole (Compound L) on H4R-mediated calcium mobilization, cytokine IL-13 production, ERK1/2, Akt and NF-κB activation in human mastocytoma cells-1 (HMC-1)...
June 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27649896/correction-to-evidence-of-a-m1-muscarinic-gpcr-homolog-in-unicellular-eukaryotes-featuring-acanthamoeba-spp-bioinformatics-3d-modelling-and-experimentations
#11
(no author information available yet)
No abstract text is available yet for this article.
June 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27608133/a-systems-biology-approach-for-elucidating-the-interaction-of-curcumin-with-fanconi-anemia-fanc-g-protein-and-the-key-disease-targets-of-leukemia
#12
David Mahato, Dipayan Samanta, Sudit S Mukhopadhyay, R Navanietha Krishnaraj
Fanconi anemia (FA) is an autosomal recessive disorder with a high risk of malignancies including acute myeloid leukemia and squamous cell carcinoma. There is a constant search out of new potential therapeutic molecule to combat this disorder. In most cases, patients with FA develop haematological malignancies with acute myeloid leukemia and acute lymphoblastic leukemia. Identifying drugs which can efficiently block the pathways of both these disorders can be an ideal and novel strategy to treat FA. The curcumin, a natural compound obtained from turmeric is an interesting therapeutic molecule as it has been reported in the literature to combat both FA as well as leukemia...
June 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27607834/pharmacophore-modeling-3d-qsar-and-in-silico-adme-prediction-of-n-pyridyl-and-pyrimidine-benzamides-as-potent-antiepileptic-agents
#13
Ruchi Malik, Pakhuri Mehta, Shubham Srivastava, Bhanwar Singh Choudhary, Manish Sharma
Biological mechanism attributing mutations in KCNQ2/Q3 results in benign familial neonatal epilepsy (BFNE), a rare form of epilepsy and thus neglected. It offers a potential target for antiepileptic drug discovery. In the present work, a pharmacophore-based 3D-QSAR model was generated for a series of N-pyridyl and pyrimidine benzamides possessing KCNQ2/Q3 opening activity. The pharmacophore model generated contains one hydrogen bond donor (D), one hydrophobic (H), and two aromatic rings (R). They are the crucial molecular write-up detailing predicted binding efficacy of high affinity and low affinity ligands for KCNQ2/Q3 opening activity...
June 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27601178/evidence-of-a-m1-muscarinic-gpcr-homolog-in-unicellular-eukaryotes-featuring-acanthamoeba-spp-bioinformatics-3d-modelling-and-experimentations
#14
Abdul Mannan Baig, H R Ahmad
Acetylcholine affects the target cellular function via muscarinic and nicotinic cholinergic receptors that are seen to exist in humans. Both the cholinergic receptors are G-protein coupled receptors (GPCRs) that perform cardinal functions in humans. Anti-muscarinic drugs, particularly the ones that target M1 subtype (mAChR1), have consistently shown to kill unicellular pathogenic eukaryotes like Acanthamoeba spp. As the M1 receptor subtype has not been reported to be expressed in the above protist, the presence of an ancient form of the M1 muscarinic receptor was inferred...
June 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27485399/novel-virtual-lead-identification-in-the-discovery-of-hematopoietic-cell-kinase-hck-inhibitors-application-of-3d-qsar-and-molecular-dynamics-simulation
#15
Rohit Bavi, Raj Kumar, Shailima Rampogu, Yongseong Kim, Yong Jung Kwon, Seok Ju Park, Keun Woo Lee
High level of hematopoietic cell kinase (Hck) is associated with drug resistance in chronic myeloid leukemia. Additionally, Hck activity has also been connected with the pathogenesis of HIV-1 and chronic obstructive pulmonary disease. In this study, three-dimensional (3D) QSAR pharmacophore models were generated for Hck based on experimentally known inhibitors. A best pharmacophore model, Hypo1, was developed with high correlation coefficient (0.975), Low RMS deviation (0.60) and large cost difference (49.31), containing three ring aromatic and one hydrophobic aliphatic feature...
June 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27485292/calcium-induced-conformational-changes-of-thrombospondin-1-signature-domain-implications-for-vascular-disease
#16
Akanksha Gupta, Rahul Agarwal, Ashutosh Singh, Sonika Bhatnagar
CONTEXT: Thrombospondin1 (TSP1) participates in numerous signaling pathways critical for vascular physiology and disease. The conserved signature domain of thrombospondin 1 (TSP1-Sig1) comprises three epidermal growth factor (EGF), 13 calcium-binding type 3 thrombospondin (T3) repeats, and one lectin-like module arranged in a stalk-wire-globe topology. TSP1 is known to be present in both calcium-replete (Holo-) and calcium-depleted (Apo-) state, each with distinct downstream signaling effects...
June 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27485180/mir-128-promoted-adipogenic-differentiation-and-inhibited-osteogenic-differentiation-of-human-mesenchymal-stem-cells-by-suppression-of-vegf-pathway
#17
Wen Zhang, Chen Yao, Zhanying Wei, Qirong Dong
CONTEXT: MicroRNA-128 (miR-128), a brain-enriched microRNA, has been reported to participate in the regulation of cell differentiation, but its potential roles in adipogenic and osteogenic differentiation of human mesenchymal stem cells (hMSCs) have not been addressed. OBJECTIVE: The study was conducted to investigate the effects and mechanism of miR-128 on adipogenic and osteogenic differentiation of hMSCs. MATERIALS AND METHODS: Morphology of hMSCs, lipid droplets and calcium nodules were observed and photographed by LSM microscopy...
June 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27485024/cellular-and-molecular-mechanisms-of-acute-exposure-to-sulfur-mustard-a-systematic-review
#18
REVIEW
Mohammad Reza Nourani, Hamideh Mahmoodzadeh Hosseini, Sadegh Azimzadeh Jamalkandi, Abbas Ali Imani Fooladi
CONTEXT: Mustard gas (e.g. sulfur mustard (SM)) has been used as a chemical agent in several battles and is still a potential worldwide menace. Besides local absorption, particularly in the skin, eyes and lungs, systemic spread of the agent also has detrimental effects on gonads, bone marrow and nervous system. Moreover, chronic exposure of SM to respiratory system causes death. Inducing oxidative stress, and disturbing DNA and tissue repair systems, inflammation and cell death signaling pathways have been introduced as molecular mechanisms of the injury...
April 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27401208/cholest-4-en-3-one-attenuates-tgf-%C3%AE-responsiveness-by-inducing-tgf-%C3%AE-receptors-degradation-in-mv1lu-cells-and-colorectal-adenocarcinoma-cells
#19
Chun-Lin Chen, Deng-Chyang Wu, Min-Yun Liu, Ming-Wei Lin, Hung-Tu Huang, Yaw-Bin Huang, Li-Chai Chen, Yu-Yu Chen, Jih-Jung Chen, Pei-Hua Yang, Yu-Chen Kao, Pei-Yu Chen
PURPOSE: The transforming growth factor-beta (TGF-β) pathway is an important in the initiation and progression of cancer. Due to a strong association between an elevated colorectal cancer risk and increase fecal excretion of cholest-4-en-3-one, we aim to determine the effects of cholest-4-en-3-one on TGF-β signaling in the mink lung epithelial cells (Mv1Lu) and colorectal cancer cells (HT29) in vitro. METHODS: The inhibitory effects of cholest-4-en-3-one on TGF-β-induced Smad signaling, cell growth inhibition, and the subcellular localization of TGF-β receptors were investigated in epithelial cells using a Western blot analysis, luciferase reporter assays, DNA synthesis assay, confocal microscopy, and subcellular fractionation...
April 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27401115/assessment-of-cell-line-competence-for-studies-of-pharmacological-gpr30-modulation
#20
Cátia Sousa, Madalena Ribeiro, Ana Teresa Rufino, Alcino Jorge Leitão, Alexandrina Ferreira Mendes
CONTEXT/OBJECTIVE: Cell lines used to study the role of the G protein-coupled receptor 30 (GPR30) or G protein-coupled estrogen receptor (GPER) as a mediator of estrogen responses have yielded conflicting results. This work identified a simple assay to predict cell line competence for pharmacological studies of GPR30. MATERIALS AND METHODS: The phosphorylation or expression levels of ERK1/2, Akt, c-Fos and eNOS were evaluated to assess GPR30 activation in response to known agonists (17β-estradiol and G-1) in MCF-7 and T-47D breast cancer cell lines and in bovine aortic endothelial cells...
April 2017: Journal of Receptor and Signal Transduction Research
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