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Journal of Receptor and Signal Transduction Research

A Sudha, P Srinivasan, V Kanimozhi, K Palanivel, B Kadalmani
The aim of this study was to find the efficacy of 5-hydroxy 3',4',7-trimethoxyflavone (HTMF), a flavonoid compound isolated from the medicinal plant Lippia nodiflora, in inhibiting the proliferation and inducing apoptosis in human breast cancer cell line MCF-7. The anti-proliferative effect of the compound HTMF was confirmed using MTT cytotoxicity assay. Increased apoptotic induction by HTMF was demonstrated by acridine orange/ethidium bromide (AO/EtBr) and Hoechst 33258 staining studies. The phosphatidylserine translocation, an early feature of apoptosis and DNA damage were revealed through AnnexinV-Cy3 staining and comet assay...
May 8, 2018: Journal of Receptor and Signal Transduction Research
Penghua Li, Jiale Peng, Yeheng Zhou, Yaping Li, XingYong Liu, LiangLiang Wang, ZhiLi Zuo
Human Coagulation Factor IXa (FIXa), specifically inhibited at the initiation stage of the blood coagulation cascade, is an excellent target for developing selective and safe anticoagulants. To explore this inhibitory mechanism, 86 FIXa inhibitors were selected to generate pharmacophore models and subsequently SAR models. Both best pharmacophore model and ROC curve were built through the Receptor-Ligand Pharmacophore Generation module. CoMFA model based on molecular docking and PLS factor analysis methods were developed...
May 4, 2018: Journal of Receptor and Signal Transduction Research
Fereshteh Shiri, Maryam Salahinejad, Rahmatollah Dijoor, Massoud Nejati-Yazdinejad
Pathogenic Gram-negative bacteria are responsible for nearly half of the serious human infections. Hologram quantitative structure-activity relationships (HQSAR), comparative molecular field analysis (CoMFA), and comparative molecular similarity index analysis (CoMSIA) were implemented on a group of 32 of potent Gram-negative LpxC inhibitors. The most effective HQSAR model was obtained using atoms, bonds, donor, and acceptor as fragment distinction. The cross-validated correlation coefficient (q2 ), non-cross-validated correlation coefficient (r2 ), and predictive correlation coefficient (r2 Pred ) for test set of HQSAR model were 0...
April 6, 2018: Journal of Receptor and Signal Transduction Research
Harmit S Ranhotra
The eukaryotic nuclear receptors (NRs) super-family of transcriptional factors include the estrogen-related receptors (ERRs) that have diverse roles in control of cellular energy balance, general metabolism, growth and development, immunity etc. Mouse knock-out models of specific ERR isoforms (ERRα, ERRβ and ERRγ) exhibit defects in several phenotypic traits. Newer findings indicate important roles of ERRs in the regulation of brown adipocyte tissue mitochondrial oxidative functions as well as metabolic control in association with hypoxia-inducible factors during cellular hypoxic state...
April 5, 2018: Journal of Receptor and Signal Transduction Research
Gustavo Nieto-Alamilla, Juan Escamilla-Sánchez, María-Cristina López-Méndez, Anayansi Molina-Hernández, Agustín Guerrero-Hernández, José-Antonio Arias-Montaño
In stably-transfected human neuroblastoma SH-SY5Y cells, we have compared the effect of activating two isoforms of 445 and 365 amino acids of the human histamine H3 receptor (hH3 R445 and hH3 R365 ) on [35 S]-GTPγS binding, forskolin-induced cAMP formation, depolarization-induced increase in the intracellular concentration of Ca2+ ions ([Ca2+ ]i) and depolarization-evoked [3  H]-dopamine release. Maximal specific binding (Bmax ) of [3  H]-N-methyl-histamine to cell membranes was 953 ± 204 and 555 ± 140 fmol/mg protein for SH-SY5Y-hH3 R445 and SH-SY5Y-hH3 R365 cells, respectively, with similar dissociation constants (Kd , 0...
March 20, 2018: Journal of Receptor and Signal Transduction Research
Ganesan Mahendran, Ramachandran Vijayan
Anxiety represents a public health problem consistently found to be the most prevalent class of mental disorders among people of all ages. Xanthones possess many biological properties, including neuroprotective, antioxidant or antidepressant-like. In this study, we aimed to investigate anxiolytic-like antidepressant and anticonvulsant properties of isolated xanthones from Swertia corymbosa. We evaluated anxiolytic-like activity of compounds 1-3 in the mouse elevated plus maze (EPM) and open field test (OF)...
April 2018: Journal of Receptor and Signal Transduction Research
Rohini Agrawal, Virendra Nath, Harish Kumar, Vipin Kumar
Cardiometabolic syndrome (CMetS) is a consolidation of metabolic disorders characterized by insulin resistance, dyslipidemia and hypertension. Curcumin, a natural bioactive compound, has been shown to possess notable anti-oxidant activity and it has also been included as a super natural herb in the super natural herbs database. Most of the beneficial effects of Curcumin are possibly due to activation of the nuclear receptor, peroxisome proliferator-activated receptor gamma (PPARγ). The present study investigates molecular interactions of curcumin with PPARγ protein through molecular docking and molecular dynamics (MD) simulation studies...
April 2018: Journal of Receptor and Signal Transduction Research
Chang-Jun Zheng, Li-Li Yang, Jun Liu, Lei Zhong
BACKGROUND: The research of G protein-coupled receptors (GPCRs) is a promising strategy for drug discovery. In cancer therapy, there is a need to discover novel agents that can inhibit proliferation and induce apoptosis in cancer cells. JTC-801 is a novel GPCR antagonist with the function of reversing pain and anxiety symptoms. This study aims to investigate the antitumor effects of JTC-801 on human osteosarcoma cells (U2OS) and elucidate the underlying mechanism. MATERIALS AND METHODS: The Cell Counting Kit-8 assay was used to detect the viability of U2OS cells treated with JTC-801 in vitro...
April 2018: Journal of Receptor and Signal Transduction Research
Ignacio Miro Estruch, Laura H J de Haan, Diana Melchers, René Houtman, Jochem Louisse, John P Groten, Ivonne M C M Rietjens
Estrogen receptor alpha (ERα) and retinoic acid receptors (RARs) play important and opposite roles in breast cancer growth. While exposure to ERα agonists such as 17β-estradiol (E2 ) is related to proliferation, RAR agonists such as all-trans retinoic acid (AtRA) induce anti-proliferative effects. Although crosstalk between these pathways has been proposed, the molecular mechanisms underlying this interplay are still not completely unraveled. The aim of this study was to evaluate the effects of AtRA on ERα-mediated signaling in the ERα positive cell lines MCF7/BUS and U2OS-ERα-Luc to investigate some of the possible underlying modes of action...
April 2018: Journal of Receptor and Signal Transduction Research
W R Williams
Purine nucleotides transduce cell membrane receptor responses and modulate ion channel activity. This is accomplished through conformational change in the structure of nucleotides and cell membrane associated proteins. The aim of this study is to enhance our understanding of nucleotide dependence in regard to signal transduction events, drug action and pharmacological promiscuity. Nucleotides and ligand structures regulating Gα protein subunits, voltage- and ligand-gated ion channels are investigated for molecular similarity using a computational program...
April 2018: Journal of Receptor and Signal Transduction Research
Song Mao, Li Fang, Fen Liu, Siqiong Jiang, Liangxia Wu, Jianhua Zhang
Chronic kidney diseases (CKD), a common outcome of various kidney diseases, cause a series of refractory complications, which lead to great economic burdens on patients. The clinical outcomes of CKD depend on various factors, including metabolic disorders. Leptin, a peptide hormone, produced in adipose tissues, plays an important role in regulating food consumption and energy expenditure. Leptin also influences the immune system and hematopoiesis. Increased leptin status is observed in CKD, leptin deficiency attenuates the immune response in nephritis...
April 2018: Journal of Receptor and Signal Transduction Research
Srilata Ballu, Ramesh Itteboina, Sree Kanth Sivan, Vijjulatha Manga
Filamentous temperature-sensitive protein Z (FtsZ) is a protein encoded by the FtsZ gene that assembles into a Z-ring at the future site of the septum of bacterial cell division. Structurally, FtsZ is a homolog of eukaryotic tubulin but has low sequence similarity; this makes it possible to obtain FtsZ inhibitors without affecting the eukaryotic cell division. Computational studies were performed on a series of substituted 3-arylalkoxybenzamide derivatives reported as inhibitors of FtsZ activity in Staphylococcus aureus...
February 2018: Journal of Receptor and Signal Transduction Research
Kaede Takahashi, Kaori Fukushima, Shiho Otagaki, Kaichi Ishimoto, Kanako Minami, Nobuyuki Fukushima, Kanya Honoki, Toshifumi Tsujiuchi
Lysophosphatidic acid (LPA) is a simple physiological lipid and exhibits a variety of cellular responses via the activation of G protein-coupled transmembrane LPA receptors (LPA receptor-1 (LPA1) to LPA6). The aim of our study was to investigate effects of LPA receptors on soft agar colony formation in colon cancer cells treated with anticancer drugs. DLD1 cells were treated with fluorouracil (5-FU) or cisplatin (CDDP) for at least six months (DLD-5FU and DLD-CDDP cells, respectively). LPAR1 gene expression was markedly elevated in DLD-5FU cells...
February 2018: Journal of Receptor and Signal Transduction Research
Fabián Meza-Cuenca, J M L Medina-Contreras, Patrick Mailloux-Salinas, Luis A Bautista-Hernández, Beatríz Buentello-Volante, Alfredo Domínguez-López, Yonathan Garfias, P Valentín Correa-López, Víctor M Bautista de Lucio, Guadalupe Bravo
INTRODUCTION/AIMS: In recent years, it has been shown that free fatty acids receptors (FFAR) of whose function in the cell surface plays a significant role in the regulation of cell function and nutrition as well are activated by various endogenous ligands, but mainly by fatty acids. Within FFAR of our interest are GPR 41, 43 and 120. The functions of these receptors are varied and dependent on the tissue where they are. The activation and signaling of these receptors, FFAR, are involved in many physiological processes, and currently the target of many drugs in metabolic disorders like obesity, diabetes and atherosclerosis...
February 2018: Journal of Receptor and Signal Transduction Research
Uma Devi Bommu, Kranthi Kumar Konidala, Rishika Pamanji, Suneetha Yeguvapalli
The observable mutated isoforms of epidermal growth factor receptor (EGFR) are important considerable therapeutic benchmarks in moderating the non-small cell lung cancer (NSCLC). Recently, quinazoline-based ATP competitive inhibitors have been developed against the EGFR; however, these imply the mutation probabilities, which contribute to the discovery of high probable novel inhibitors for EGFR mutants. Therefore, SAR-based bioactivity analysis, molecular docking and computational toxicogenomics approaches were performed to identify and evaluate new analogs of gefitinib against the ligand-binding domain of the EGFR double-mutated model...
February 2018: Journal of Receptor and Signal Transduction Research
Pingping Dong, Fengmei Hao, Shufeng Dai, Lin Tian
This study aimed to investigate the anti-cervical cancer effects of everolimus (Eve) and paclitaxel (Pac) when used alone or in combination. Human cervical cancer cells HeLa and SiHa were divided into four group: Blank control group (control), everolimus group (Eve), paclitaxel group (Pac) and combined therapy group (Eve + Pac). The cell viability was detected by CCK-8 assay and the cell cloning ability was detected by clonegenic assay. Flow cytometry was used to detect cell apoptosis. Meanwhile, the expression of phosphatidylinositol 3-kinase (PI3K), protein kinase B (AKT), mammalian target of rapamycin (mTOR) and their phosphorylated proteins were studied by western blot...
February 2018: Journal of Receptor and Signal Transduction Research
Fereshteh Shiri, Somayeh Pirhadi, Azita Rahmani
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) have gained a definitive place due to their unique antiviral potency, high specificity and low toxicity in antiretroviral combination therapies which are used to treat HIV. To design more specific HIV-1 inhibitors, 218 diverse non-nucleoside reverse transcriptase inhibitors with their EC50 values were collected. Then, different types of molecular descriptors were calculated. Also, genetic algorithm (GA) and enhanced replacement methods (ERM) were used as the variable selection approaches to choose more relevant features...
February 2018: Journal of Receptor and Signal Transduction Research
Mostafa Khedri, Khalil Abnous, Houshang Rafatpanah, Mohammad Ramezani
Programmed cell death-1 (PD1) is an inhibitory receptor expressed on the activated T and B cells. Binding of PD1 to its ligands, PD-L1 and PD-L2 has led to deliver an inhibitory signal into the activated T cells. Recently, blocking PD1/PD-L1 pathway has emerged as a new treatment paradigm across a broad spectrum of malignancies. Remarkable clinical responses of monoclonal antibodies specific for PD-1 or its ligands in patients with many different types of cancer, attracted several pharmaceutical companies and researchers to investigate the agents that block PD1/PD-L1 signal...
February 2018: Journal of Receptor and Signal Transduction Research
Ning Su, Chaoxing Xiao, Yi Wei, Qiuye Kou, Zongpei Jiang
Macrophages can be alternatively activated by TGF-β1 and high-ambient glucose, in which the role of Smad2 and the crosstalk between ERK and Smad2 pathways are not fully understood. The activation of ERK and Smad2 pathways and the expression of arginase-1 were detected by Western blot. The role of Smad2 and the relationship between ERK and Smad2 pathways were investigated by using biochemical inhibitors. The protein of arginase-1 was significantly overexpressed in RAW264.7 cells stimulated by TGF-β1 and high-ambient glucose, which can be partially blocked by not only U0126 (ERK inhibitor) but also SB431542 (Smad2 inhibitor)...
February 2018: Journal of Receptor and Signal Transduction Research
Radka Moravcova, Barbora Melkes, Jiri Novotny
OBJECTIVES: Extensive research has been dedicated to elucidating the mechanisms of signal transduction through different G protein-coupled receptors (GPCRs). However, relatively little is known about the regulation of receptor movement within the cell membrane upon ligand binding. In this study we focused our attention on the thyrotropin-releasing hormone (TRH) receptor that typically couples to Gq/11 proteins. METHODS: We monitored receptor diffusion in the plasma membrane of HEK293 cells stably expressing yellow fluorescent protein (YFP)-tagged TRH receptor (TRHR-YFP) by fluorescence recovery after photobleaching (FRAP)...
February 2018: Journal of Receptor and Signal Transduction Research
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