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Journal of Receptor and Signal Transduction Research

Anshita Gupta, Chanchal Deep Kaur, Shailendra Saraf, Swarnlata Saraf
Targeted drug delivery through folate receptor (FR) has emerged as a most biocompatible, target oriented, and non-immunogenic cargoes for the delivery of anticancer drugs. FRs are highly overexpressed in many tumor cells (like ovarian, lung, breast, kidney, brain, endometrial, and colon cancer), and targeting them through conjugates bearing specific ligand with encapsulated nanodrug moiety is undoubtedly, a promising approach toward tumor targeting. Folate, being an endogenous ligand, can be exploited well to affect various cellular events occurring during the progress of tumor, in a more natural and definite way...
January 17, 2017: Journal of Receptor and Signal Transduction Research
Nasser S M Ismail, Heba S A Elzahabi, Peter Sabry, Fady N Baselious, Andrew Samy AbdelMalak, Fady Hanna
Structure-based pharmacophores were generated and validated using the bioactive conformations of different co-crystallized enzyme-inhibitor complexes for allosteric palm-1 and thumb-2 inhibitors of NS5B. Two pharmacophore models were obtained, one for palm-1 inhibitors with sensitivity = 0.929 and specificity = 0.983, and the other for thumb-2 inhibitors with sensitivity = 1 and specificity = 0.979. In addition, a quantitative structure activity relationship (QSAR) models were developed based on using the values of different scoring functions as descriptors predicting the activity on both allosteric binding sites (palm-1 and thumb-2)...
November 9, 2016: Journal of Receptor and Signal Transduction Research
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...
November 9, 2016: Journal of Receptor and Signal Transduction Research
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)...
November 3, 2016: Journal of Receptor and Signal Transduction Research
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...
November 3, 2016: Journal of Receptor and Signal Transduction Research
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...
November 3, 2016: Journal of Receptor and Signal Transduction Research
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)...
November 3, 2016: Journal of Receptor and Signal Transduction Research
Neha Nagpal, Sukriti Goyal, Jaspreet Kaur Dhanjal, Liu Ye, Sunil C Kaul, Renu Wadhwa, Rupesh Chaturvedi, Abhinav Grover
INTRODUCTION: Cancer is one of the leading causes of mortality worldwide that requires attention in terms of extensive study and research. Eradication of mortalin-p53 interaction that leads to the inhibition of transcriptional activation or blocking of p53 from functioning as a suppressor and induction of nuclear translocation of p53 can prove to be one of the useful approaches for cancer management. RESULTS: In this study, we used structure-based approach to target the p53-binding domain of mortalin in order to prevent mortalin-p53 complex formation...
February 2017: Journal of Receptor and Signal Transduction Research
I-Shu Chen, Chiang-Ting Chou, Yuan-Yuarn Liu, Chia-Cheng Yu, Wei-Zhe Liang, Chun-Chi Kuo, Pochuen Shieh, Daih-Huang Kuo, Fu-An Chen, Chung-Ren Jan
Minoxidil is clinically used to prevent hair loss. However, its effect on Ca(2+) homeostasis in prostate cancer cells is unclear. This study explored the effect of minoxidil on cytosolic-free Ca(2+) levels ([Ca(2+)]i) and cell viability in PC3 human prostate cancer cells. Minoxidil at concentrations between 200 and 800 μM evoked [Ca(2+)]i rises in a concentration-dependent manner. This Ca(2+) signal was inhibited by 60% by removal of extracellular Ca(2+). Minoxidil-induced Ca(2+) influx was confirmed by Mn(2+)-induced quench of fura-2 fluorescence...
February 2017: Journal of Receptor and Signal Transduction Research
Peng Hu, Xun Xia, Qiang Xuan, Bao Yu Huang, Si Yan Liu, Dong Dong Zhang, Guang Mei Jiang, Yao Xu, Yuan Han Qin
The initiation and progression of renal interstitial fibrosis (RIF) is a complicated process in which many factors may play an activate role. Among these factors, C-type natriuretic peptide (CNP) is an endothelium-derived hormone and acts in a local, paracrine fashion to regulate vascular smooth muscle tone and proliferation. In this study, we established a rat model of unilateral ureteral obstruction (UUO). CNP expression tends to be higher immediately after ligation and declined at later time points, occurring predominantly in tubular epithelial cells...
February 2017: Journal of Receptor and Signal Transduction Research
Rajan Kumar Pandey, Bajarang Vasant Kumbhar, Shyam Sundar, Ambarish Kunwar, Vijay Kumar Prajapati
Visceral leishmaniasis (VL) is the most fatal form of leishmaniasis and it affects 70 countries worldwide. Increasing drug resistant for antileishmanial drugs such as miltefosine, sodium stibogluconate and pentamidine has been reported in the VL endemic region. Amphotericin B has shown potential antileishmanial activity in different formulations but its cost of treatment and associated nephrotoxicity have limited its use by affected people living in the endemic zone. To control the VL infection in the affected countries, it is necessary to develop new antileishmanial compounds with high efficacy and negligible toxicity...
February 2017: Journal of Receptor and Signal Transduction Research
Mahesh Ramalingam, Sung-Jin Kim
Parkinson's disease (PD) is the second most common neurodegenerative disorder after Alzheimer's disease (AD) associated with mitochondrial dysfunction mediated by oxidative stress. Astrocytes regulate neuronal function via the modulation of synaptic transmission and plasticity, secretion of growth factors, uptake of neurotransmitters, and regulation of extracellular ion concentrations and metabolic support of neurons. Therefore, this study was undertaken to investigate the mechanism of action of insulin on a 1-methyl-4-phenylpyridinium (MPP(+))-induced toxicity of events associated in cell viability and toxicity to the expression profile of cell signaling pathway proteins and genes in rat C6 glial cells...
February 2017: Journal of Receptor and Signal Transduction Research
Fengyun Wang, Yang Liu, Zhenyu Bi
OBJECTIVES: We aimed to study the antitumor effects of the PPARγ agonist pioglitazone on human retinoblastoma. METHODS: The effects of pioglitazone on cell proliferation and apoptosis of the human retinoblastoma Y79 cells were investigated by MTT assay and Hoechst 33258 staining assay. The apoptosis related protein levels were detected by western blot. Inflammationary factors analysis was evaluated by western blot and ELISA. The effect of pioglitazone on nuclear factor-kappa B (NF-κB)-dependent reporter gene transcription induced by LPS was analyzed by NF-κB-luciferase assay...
February 2017: Journal of Receptor and Signal Transduction Research
K Anbarasu, S Jayanthi
Estrogen receptor-α (ERα) is expressed more in patients with breast cancer and its level correlated with endocrine resistance. LMTK3 is reported as breast cancer target with regulation of estrogen receptor-α (ERα) through phosphorylation. In this computational study, structure-based inhibitor screening was performed on human LMTK3 using ZINC database. ATP-binding cavity with critical residues involved in the LMTK3 phosphorylation was used as target site for the screening. From the large ligand library, the best compounds were screen with three-phase virtual screening methods in Dockblaster, AutoDock Vina and AutoDock, respectively...
February 2017: Journal of Receptor and Signal Transduction Research
Pallavi Mohanty, Sonika Bhatnagar
The focal adhesion targeting (FAT) domain of focal adhesion kinase (FAK) exists in monomeric closed (c) or arm exchanged (ae) dimeric state. FAT interaction with Grb2 necessitates an intermediate open (o) state that interacts with Grb2 and activates signaling pathways leading to pathological cardiac hypertrophy. Targeted molecular dynamics (TMD) simulation was carried out in order to capture the structure of the intermediate formed by opening of Helix1 (H1) from monomeric cFAT leading to the formation of monomeric aeFAT...
February 2017: Journal of Receptor and Signal Transduction Research
Esin Sakallı Çetin, Mustafa Nazıroğlu, Bilal Çiğ, İshak Suat Övey, Pınar Aslan Koşar
BACKGROUND: In breast cancers, calcium signaling is a main cause of proliferation and apoptosis of breast cancer cells. Although previous studies have implicated the transient receptor potential vanilloid 1 (TRPV1) cation channel, the synergistic inhibition effects of selenium (Se) and cisplatin in cancer and the suppression of ongoing apoptosis have not yet been investigated in MCF-7 breast cancer cells. This study investigates the anticancer properties of Se through TRPV1 channel activity in MCF-7 breast cancer cell line cultures when given alone or in combination with cisplatin...
February 2017: Journal of Receptor and Signal Transduction Research
Robert Büttner, Alexander Berndt, Christina Valkova, Petra Richter, Alexander Korn, Christian Kosan, Claus Liebmann
INTRODUCTION: Receptors of the ErbB family belong to the key players in cancer development and are targets of several therapeutic approaches. Their functional dependency on the tumor microenvironment, especially on CAFs is albeit still poorly understood. Our objective was to investigate the impact of CAF secretome on ErbB receptor expression and signaling behavior in OSCC. METHODS: Stimulation of PE/CA-PJ15 OSCC cells with conditioned media of TGF-β1-activated fibroblasts was used as model system for CAF to cancer cell communication...
February 2017: Journal of Receptor and Signal Transduction Research
Shuzhen Li, Shuo Chen, Weiwei Yang, Lin Liao, Shanshan Li, Jiali Li, Yaqin Zheng, Daling Zhu
Allicin is a natural effective organosulfur compound isolated from garlic, which possesses many beneficial properties, such as antibacterial, anti-inflammatory, antimicrobial, hypotensive and hypolipidemic. In the present study, we investigated the effects and the underlying mechanisms of allicin on isolated mesenteric arteries (MAs). We examined MAs relaxation induced by allicin on rat-isolated mesenteric artery (MA) rings, the KATP channels with patch, and the expression of Kir6.1 and SUR2B with western blotting and NO production with Diaminofluorescein-FM diacetate (DAF-FMDA) in rat mesenteric artery smooth muscle cells (MASMCs)...
February 2017: Journal of Receptor and Signal Transduction Research
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December 2016: Journal of Receptor and Signal Transduction Research
Ya-Han Huang, Yeu-Shiuan Su, Chung-Jen Chang, Wei-Hsin Sun
Proton-sensing G-protein-coupled receptors (GPCRs; OGR1, GPR4, G2A, TDAG8), with full activation at pH 6.4 ∼ 6.8, are important to pH homeostasis, immune responses and acid-induced pain. Although G2A mediates the G13-Rho pathway in response to acid, whether G2A activates Gs, Gi or Gq proteins remains debated. In this study, we examined the response of this fluorescence protein-tagged OGR1 family to acid stimulation in HEK293T cells. G2A did not generate detectable intracellular calcium or cAMP signals or show apparent receptor redistribution with moderate acid (pH ≥ 6...
December 2016: Journal of Receptor and Signal Transduction Research
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