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Journal of Receptor and Signal Transduction Research

Thangesweran Ayakannu, Anthony H Taylor, Justin C Konje
The lack of good diagnostic/prognostic biomarkers and the often late presentation of endometrial cancer (EC) hinders the amelioration of the morbidity and mortality rates associated with this primarily estrogen-driven disease, a disease that is becoming more prevalent in the population. Previous studies on the expression of the classical cannabinoid receptors, CB1 and CB2, suggest these could provide good diagnostic/prognostic biomarkers for EC but those observations have been contradictory. In this study, we sought to resolve the inconsistency of CB1 and CB2 expression levels in different EC studies...
December 20, 2018: Journal of Receptor and Signal Transduction Research
Gopinadh Bhyrapuneni, Jagadeesh Babu Thentu, Veera Raghava Choudary Palacharla, Nageswararao Muddana, Raghupathi Reddy Aleti, Devender Reddy Ajjala, Ramakrishna Nirogi
Unbound drug concentration in the brain would be the true exposure responsible for specific target occupancy. Drug exposures from preclinical are total concentrations of those over/underestimate the clinical dose projection. With the application of mass spectrometry, the current work proposes a definite measure of test drug exposures at serotonin-2A occupancy. The 5-HT2A occupancy of antagonist in the rat brain has determined with non-radiolabeled tracer MDL-100,907 at an optimized dose (3 µg/kg) and treatment time (30 min)...
August 2018: Journal of Receptor and Signal Transduction Research
Noor Saba Khan, Rashi Verma, Dibyabhaba Pradhan, Arnab Nayek, Rajabrata Bhuyan, Tanmaya Kumar Sahu, Arun Kumar Jain
Wealth of structural data on theurapeutic targets in complex with monoclonal antibodies (mAbs) and advances in molecular modeling algorithms present exciting opportunities in the field of novel biologic design. Interleukin 23 (IL23), a well-known drug target for autoimmune diseases, in complex with mAb 7G10 offers prospect to design potent lead antibodies by traversing the complete epitope-paratope interface. Herein, key interactions aiding antibody-based neutralization in IL23-7G10 complex are resolute through PyMOL, LigPlot+ , Antibody i-Patch, DiscoTope and FoldX...
August 2018: Journal of Receptor and Signal Transduction Research
Kaori Fukushima, Shiho Otagaki, Kaede Takahashi, Kanako Minami, Kaichi Ishimoto, Nobuyuki Fukushima, Kanya Honoki, Toshifumi Tsujiuchi
Lysophosphatidic acid (LPA) is a simple biological lipid and mediates several biological functions with LPA receptors (LPA1 to LPA6 ). In the present study, to assess whether LPA receptors promote cell-invasive activity of pancreatic cancer cells, highly invasion PANC-R9 cells were established from PANC-1 cells, using Matrigel-coated Cell Culture Insert. The cell-invasive activity of PANC-R9 cells was shown to be approximately 15 times higher than that of PANC-1 cells. LPAR1 expression level was markedly elevated in PANC-R9 cells in comparison with PANC-1 cells, while LPAR3 expression level was reduced...
August 2018: Journal of Receptor and Signal Transduction Research
Kranthi Kumar Konidala, Uma Devi Bommu, Neeraja Pabbaraju
In this study, binding efficiency of new pyrrolopyrimidine structural analogs against human vascular endothelial growth factor receptor-2 (VEGFR-2) were elucidated using integrated in silico methods. Optimized high-resolution model of VEGFR-2 was generated and adopted for structure-based virtual screening approaches. Pyrrolopyrimidine inhibitor (CP15) associated compounds were screened from PubChem database and subjected to virtual screening and comparative docking methods against the receptor ligand-binding domain...
August 2018: Journal of Receptor and Signal Transduction Research
Eltayeb E M Eid, Faizul Azam, Mahmoud Hassan, Ismail M Taban, Mohammad A Halim
Breast cancer is the most frequent malignancy among females worldwide. Estrogen receptor (ER) mediate important pathophysiological signaling pathways induced by estrogens, and is regarded as a promising target for the treatment of breast cancer. Zerumbone (2,6,9,9-tetramethylcycloundeca-2,6,10-trien-1-one; ZER), a chemical constituent present in the Zingiber zerumbet is known to exhibit anti-breast cancer activity by modulating several proteins to induce apoptosis. Medicinal chemists usually exploit lead compounds of natural origin to develop molecules with improved pharmacological properties...
August 2018: Journal of Receptor and Signal Transduction Research
Xianchun Sun, Yan Zhang, Bingshu Li, Haiyan Yang
The metastasis-associated gene 1 (MTA1) has previously been recognized as an oncogene, and abnormal MTA1 expression has been related to progression of numerous cancer types to the metastasis stage. However, the function of MTA1 in the regulation of pancreatic cancer progression and metastasis remains unclear. Western blot analysis was adopted to determine the expression of MTA1 in pancreatic cancer tissues and corresponding near normal tissues. Steady clone with MTA1-overexpression and MTA1-inhibitionweregenerated via lentivirus technology in BxPc-3 cells...
August 2018: Journal of Receptor and Signal Transduction Research
Chris S Breivogel, John M McPartland, Bhavita Parekh
PURPOSE: Previous studies have found non-CB1 non-CB2 G-protein-coupled receptors in rodents that are activated by the aminoalkylindole cannabinoid agonist WIN55212-2. This work obtained evidence for the presence or absence of similar receptors in the brains of other mammals, birds and amphibians. MATERIALS AND METHODS: Antagonism of the stimulation of [35 S]GTPγS binding by WIN55212-2 and CP55940 was assessed in multiple CNS regions of rat and canine, and in whole brain membranes from shrew, pigeon, frog and newt...
August 2018: Journal of Receptor and Signal Transduction Research
Sergey Menzikov
The Cl- /[Formula: see text]-ATPase from the plasma membranes of animal brains is an ATP-consuming Cl- -transporting ATPase P-type that is structurally coupled to GABAA receptors. The aim of work was to study the GABA effect on Cl- transport across liposomal membranes by the reconstituted ATPase under various conditions (i.e. in the absence and in the presence of ATP in the incubation medium). We reconstituted the affinity-purified enzyme in the liposomes with a fluorescent dye for Cl- . The Cl- -transport in proteoliposomes was evaluated from variations in fluorescence...
August 2018: Journal of Receptor and Signal Transduction Research
Amrutha Nisthul A, Archana P Retnakumari, Shabna A, Ruby John Anto, C Sadasivan
De novo lipogenesis (DNL) by upregulation of fatty acid synthase (FASN) is an important metabolic alteration of cancer cells. FASN is over-expressed in several cancers and is often associated with a high risk of recurrence and poor prognosis. Differential expression of FASN in cancer cells and their normal counterparts leads to the impression that FASN can be an attractive druggable target in cancer therapy. Present study focuses on identification of inhibitors against FASN ketoacyl synthase (KS) domain from Asinex Biodesign compound database using in silico tools...
August 2018: Journal of Receptor and Signal Transduction Research
Shehnaz Fatima, Subhash Mohan Agarwal
EGFR is an important drug target in cancer. However, the ineffectiveness of first generation inhibitors due to the occurrence of a secondary mutation (T790M) results in the relapse of the disease. Identification of reversible inhibitors against T790M/L858R double mutants (TMLR) thus is a foremost requirement. In this study, various 2 D and 3 D Quantitative Structure-Activity Relationship models were built for amino-pyrimidine compounds with their known biological activity against TMLR mutants. The model developed using multiple linear regression statistical method via stepwise forward-backward variable selection technique showed the best results in terms of internal and external predictivity...
August 2018: Journal of Receptor and Signal Transduction Research
Kaori Fukushima, Kaede Takahashi, Mirai Kusaka, Kaichi Ishimoto, Kanako Minami, Shiho Otagaki, Nobuyuki Fukushima, Kanya Honoki, Toshifumi Tsujiuchi
Free fatty acid (FFA) receptors belong to a member of G-protein-coupled receptors. GPCR 120 (GPR120) and GPR40 are identified as FFA receptors and activated via the binding of long- and medium-chain FFAs. The aim of this study was to assess the effects of GPR120 and GPR40 on cell motility and growth in breast cancer cells treated with tamoxifen (TAM). MCF-7 cells were continuously treated with TAM for approximately 6 months. The expression level of GPR40 gene was markedly higher in the long-term TAM treated (MCF-TAM) cells than in MCF-7 cells...
August 2018: Journal of Receptor and Signal Transduction Research
Trinath Daggupati, Rishika Pamanji, Suneetha Yeguvapalli
Glycogen synthase kinase-3β (GSK3β) has been reported for its impact on multitude biological processes from cell proliferation to apoptosis. The increase in the ratio of active/inactive GSK3β is the major factor associated in the etiology of several psychiatric diseases, diabetes, muscle hypertrophy, neurodegenerative diseases, and some cancers. These findings made GSK3β a promising therapeutic target, and the interest in the discovery, synthesis of novel drugs to effectively attenuate its function with probably no side effects has been increasing in the chronology of GSK3β drug discovery...
August 2018: Journal of Receptor and Signal Transduction Research
Gopinadh Bhyrapuneni, Jagadeesh Babu Thentu, Abdul Rasheed Mohammed, Raghupathi Reddy Aleti, Nagasurya Prakash Padala, Devender Reddy Ajjala, Ramakrishna Nirogi
The use of liquid chromatography coupled with mass spectrometry (LC-MS/MS) is advantageous in in-vivo receptor occupancy assays at pre-clinical drug developmental stages. Relatively, its application is effective in terms of high throughput, data reproducibility, sensitivity, and sample processing. In this perspective, we have evaluated the use of FTC-146 as a non-radiolabelled tracer to determine the sigma-1 receptor occupancy of test drugs in mice brain. Further, the brain and plasma exposures of test drug were determined at their corresponding occupancies...
August 2018: Journal of Receptor and Signal Transduction Research
Sanjay K Choubey, Jeyaraman Jeyakanthan
Histone deacetylase 2 (HDAC2) is an emerging target of Alzheimer's disease. Four featured pharmacophore model (ADRR) with one H-bond acceptor (A), one H-bond donor (D), and two aromatic rings (R) was generated using experimentally reported compounds, ((E-5[3-benzenesulfonamido) phenyl]-N-hydroxypent-2-en-4-ynamide)) and (N'-hydroxy-N-phenyloctanediamide) with IC50 values of 0.16 ± 0.11 nM and 62 ± 0.15 nM, respectively. Quantum Polarized Ligand Docking and Binding Free Energy calculation was performed for the top three identified leads RH01652, JFD02573, and HTS00800 from HitFinder database...
June 2018: Journal of Receptor and Signal Transduction Research
Mingdong Yu, Baohui Su, Xiaoxia Zhang
OBJECTIVES: Here, using rat model, we investigated the roles of gardenoside in the chronic constriction injury (CCI) of the ischiadic nerve. METHODS: Bennett and Xie's unilateral sciatic nerve CCI model was used in this study. A total of 60 rats were divided into control group (CN), sham group (Sham), CCI group, and gardenoside administrated CCI group. An aliquot of 5 mL gardenoside solution was administrated through gavage once per day for 14 d. Mechanical withdrawal threshold (MWT) and the thermal withdrawal latency (TWL) were detected...
June 2018: Journal of Receptor and Signal Transduction Research
Tuyen N M Hua, Jun Namkung, Ai N H Phan, Vu T A Vo, Min-Kyu Kim, Yangsik Jeong, Jong-Whan Choi
CONTEXT: The metabolic function of peroxisome proliferator-activated receptor gamma (PPARγ) in lung cancer remains unclear. OBJECTIVES: To determine the relationship of PPARγ on ALDH1A3-induced lipid peroxidation to inhibit lung cancer cell growth. MATERIALS AND METHODS: In silico analysis using microarray dataset was performed to screen the positive correlation between PPARγ and all ALDH isoforms. NUBIscan software and ChIP assay were used to identify the binding sites (BSs) of PPARγ on ALDH1A3 promoter...
June 2018: Journal of Receptor and Signal Transduction Research
Angel Jemima Ebenezer, Kavya Prasad, Sanjana Rajan, Elden Berla Thangam
CONTEXT: Mast cell (MC) activation through H4R releases various inflammatory mediators which are associated with allergic asthma. OBJECTIVES: To investigate the siRNA-mediated gene silencing effect of H4R on human mast cells (HMCs) functions and the activation of stress-activated protein kinases (SAPK)/jun amino-terminal kinases (JNK) signaling pathways for the release of ineterleukin-1β (IL-1β) in HMCs. MATERIALS AND METHODS: H4R expression was analyzed by RT-PCR and western blotting in human mast cell line-1 (HMC-1) cells and H4RsiRNA transfected cells...
June 2018: Journal of Receptor and Signal Transduction Research
Sharanya C S, Arun K G, Vijaytha V, Sabu A, Haridas M
Methyl gallate was purified, by lipoxygenase (LOX) inhibitory activity-guided method since its alleged anti-inflammatory property, from Bergenia ligulata (Wall), a plant used in the traditional, Ayurvedic system of medicine extensively. The LOX inhibitory property of methyl gallate was studied by enzyme kinetics, isothermal titration calorimetry and molecular docking followed by molecular simulation studies. The wet-laboratory experiments and in silico studies showed complete agreement, and promise of methyl gallate as a drug-lead molecular scaffold for anti-inflammatory therapy, based on LOX inhibition...
June 2018: Journal of Receptor and Signal Transduction Research
K G Arun, C S Sharanya, C Sadasivan
Adenosine deaminase (ADA) is one of the major enzymes involved in purin metabolism, it has a significant role in cell growth and differentiation. Over-activity of ADA has been noticed in some pathology, like malignancy and inflammation and makes it an attractive target for the development of drugs for such diseases. In the present study, ADA inhibitory activity of morin, a bioactive flavonoid, was assessed through computational and biophysical methods. The enzyme kinetics data showed that morin is a competitive inhibitor of ADA...
June 2018: Journal of Receptor and Signal Transduction Research
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