1,019 results match your criteria Journal of Receptors and Signal Transduction[Journal]


Cannabinoid receptor expression in estrogen-dependent and estrogen-independent endometrial cancer.

J Recept Signal Transduct Res 2018 Dec 20:1-8. Epub 2018 Dec 20.

a Reproductive Sciences Section, Department of Cancer Studies and Molecular Medicine , University of Leicester , Leicester , UK.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1531890DOI Listing
December 2018
1 Read

A definite measure of occupancy exposures, seeking with non-radiolabeled in vivo 5-HT2A receptor occupancy and in vitro free fractions.

J Recept Signal Transduct Res 2018 Aug;38(4):359-366

a Discovery Research, Suven Life Sciences Ltd , Hyderabad , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1531888DOI Listing

Analysis of interleukin 23 and 7G10 interactions for computational design of lead antibodies against immune-mediated inflammatory diseases.

J Recept Signal Transduct Res 2018 Aug 1;38(4):327-334. Epub 2018 Nov 1.

a Biomedical Informatics Centre , ICMR-National Institute of Pathology , New Delhi , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1511729DOI Listing
August 2018
2.277 Impact Factor

Promotion of cell-invasive activity through the induction of LPA receptor-1 in pancreatic cancer cells.

J Recept Signal Transduct Res 2018 Aug 5;38(4):367-371. Epub 2018 Nov 5.

a Division of Molecular Oncology, Department of Life Science, Faculty of Science and Engineering , Kindai University , Higashiosaka , Osaka , Japan.

Lysophosphatidic acid (LPA) is a simple biological lipid and mediates several biological functions with LPA receptors (LPA to LPA). 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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1531889DOI Listing

In silico insights into the identification of potential novel angiogenic inhibitors against human VEGFR-2: a new SAR-based hierarchical clustering approach.

J Recept Signal Transduct Res 2018 Aug 5;38(4):372-383. Epub 2018 Nov 5.

a Department of Zoology, Division of Molecular Physiology , Sri Venkateswara University , Tirupati , India.

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. Read More

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https://www.tandfonline.com/doi/full/10.1080/10799893.2018.1
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http://dx.doi.org/10.1080/10799893.2018.1531891DOI Listing
August 2018
8 Reads

Zerumbone binding to estrogen receptors: an in-silico investigation.

J Recept Signal Transduct Res 2018 Aug 5;38(4):342-351. Epub 2018 Nov 5.

d Division of Computer-aided Drug Design , The Red-Green Research Center , BICCB , Dhaka , Bangladesh.

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. Read More

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https://www.tandfonline.com/doi/full/10.1080/10799893.2018.1
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http://dx.doi.org/10.1080/10799893.2018.1531886DOI Listing
August 2018
20 Reads
2.277 Impact Factor

MTA1 promotes the invasion and migration of pancreatic cancer cells potentially through the HIF-α/VEGF pathway.

J Recept Signal Transduct Res 2018 Aug 5;38(4):352-358. Epub 2018 Nov 5.

b Department of Emergency , Yantaishan Hospital , Yantai , Shandong , China.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1531887DOI Listing
August 2018
7 Reads

Investigation of non-CB, non-CB WIN55212-2-sensitive G-protein-coupled receptors in the brains of mammals, birds, and amphibians.

J Recept Signal Transduct Res 2018 Aug 31;38(4):316-326. Epub 2018 Oct 31.

a Department of Pharmaceutical Sciences , Campbell University College of Pharmacy & Health Sciences , Buies Creek , NC , USA.

Purpose: Previous studies have found non-CB non-CB 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 [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. Read More

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https://www.tandfonline.com/doi/full/10.1080/10799893.2018.1
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http://dx.doi.org/10.1080/10799893.2018.1494743DOI Listing
August 2018
1 Read

Dual character of GABA action on Cl-transport by the reconstituted Cl/[Formula: see text]-ATPase from rat brain.

Authors:
Sergey Menzikov

J Recept Signal Transduct Res 2018 Aug 27;38(4):307-310. Epub 2018 Sep 27.

a Institute of General Pathology and Pathological Physiology , Moscow , Russia.

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 GABA 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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1494741DOI Listing
August 2018
7 Reads

In silico screening for identification of fatty acid synthase inhibitors and evaluation of their antiproliferative activity using human cancer cell lines.

J Recept Signal Transduct Res 2018 Aug 26;38(4):335-341. Epub 2018 Sep 26.

a Department of Biotechnology and Microbiology , Kannur University , Kannur , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1511730DOI Listing
August 2018
6 Reads

Unraveling structural requirements of amino-pyrimidine T790M/L858R double mutant EGFR inhibitors: 2D and 3D QSAR study.

J Recept Signal Transduct Res 2018 Aug 11;38(4):299-306. Epub 2018 Sep 11.

a Bioinformatics Division , ICMR-National Institute of Cancer Prevention and Research , Noida , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1494740DOI Listing
August 2018
3 Reads

Induction of GPR40 positively regulates cell motile and growth activities in breast cancer MCF-7 cells.

J Recept Signal Transduct Res 2018 Aug 15;38(4):311-315. Epub 2018 Aug 15.

a Division of Molecular Oncology, Department of Life Science, Faculty of Science and Engineering , Kindai University , Higashiosaka , Osaka , Japan.

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). Read More

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https://www.tandfonline.com/doi/full/10.1080/10799893.2018.1
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http://dx.doi.org/10.1080/10799893.2018.1494742DOI Listing
August 2018
15 Reads

In silico screening and identification of potential GSK3β inhibitors.

J Recept Signal Transduct Res 2018 Aug 27;38(4):279-289. Epub 2018 Jun 27.

a Department of Zoology , Sri Venkateswara University , Tirupati , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1478854DOI Listing
August 2018
5 Reads

Molecular dynamics and quantum chemistry-based approaches to identify isoform selective HDAC2 inhibitor - a novel target to prevent Alzheimer's disease.

J Recept Signal Transduct Res 2018 Jun 22;38(3):266-278. Epub 2018 Jun 22.

a Structural Biology and Bio-computing Lab, Department of Bioinformatics , Alagappa University , Karaikudi , India.

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 IC values of 0.16 ± 0. Read More

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http://dx.doi.org/10.1080/10799893.2018.1476541DOI Listing
June 2018
4 Reads

Gardenoside suppresses the pain in rats model of chronic constriction injury by regulating the P2X3 and P2X7 receptors.

J Recept Signal Transduct Res 2018 Jun 22;38(3):198-203. Epub 2018 Jun 22.

a Department of the Spine Surgery II , Weifang People Hospital , Weifang , PR China.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1468782DOI Listing
June 2018
3 Reads

Assessment of sigma-1 receptor occupancy in mice with non-radiolabelled FTC-146 as a tracer.

J Recept Signal Transduct Res 2018 Aug 18;38(4):290-298. Epub 2018 Jun 18.

a Discovery Research Suven Life Sciences Ltd , Hyderabad , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1478855DOI Listing
August 2018
3 Reads

PPARgamma-mediated ALDH1A3 suppression exerts anti-proliferative effects in lung cancer by inducing lipid peroxidation.

J Recept Signal Transduct Res 2018 Jun 6;38(3):191-197. Epub 2018 Jun 6.

a Department of Biochemistry, Wonju College of Medicine , Yonsei University , Wonju , South Korea.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1468781DOI Listing
June 2018
9 Reads

Silencing of H4R inhibits the production of IL-1β through SAPK/JNK signaling in human mast cells.

J Recept Signal Transduct Res 2018 Jun 4;38(3):204-212. Epub 2018 Jun 4.

a Department of Biotechnology, School of Bioengineering , SRM University , Kattankulathur , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1468783DOI Listing
June 2018
5 Reads

Designing of enzyme inhibitors based on active site specificity: lessons from methyl gallate and its lipoxygenase inhibitory profile.

J Recept Signal Transduct Res 2018 Jun 30;38(3):256-265. Epub 2018 May 30.

a Inter University Centre for Bioscience and Department of Biotechnology & Microbiology , Kannur University , Thalassery Campus , Palayad, India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1478856DOI Listing
June 2018
3 Reads

Computational and experimental validation of morin as adenosine deaminase inhibitor.

J Recept Signal Transduct Res 2018 Jun 29;38(3):240-245. Epub 2018 May 29.

a Department of Biotechnology and Microbiology , Kannur University, Thalassery Campus , Kannur , Kerala , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1476543DOI Listing

Pharmacophore modeling, molecular docking and molecular dynamics studies on natural products database to discover novel skeleton as non-purine xanthine oxidase inhibitors.

J Recept Signal Transduct Res 2018 Jun 29;38(3):246-255. Epub 2018 May 29.

a College of Chemical Engineering , Sichuan University of Science and Engineering , Zigong , China.

Gout is a common inflammatory arthritis caused by the deposition of urate crystals within joints. It is increasingly in prevalence during the past few decades as shown by the epidemiological survey results. Xanthine oxidase (XO) is a key enzyme to transfer hypoxanthine and xanthine to uric acid, whose overproduction leads to gout. Read More

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http://dx.doi.org/10.1080/10799893.2018.1476544DOI Listing
June 2018
4 Reads

Atom-based 3D-QSAR, induced fit docking, and molecular dynamics simulations study of thieno[2,3-b]pyridines negative allosteric modulators of mGluR5.

J Recept Signal Transduct Res 2018 Jun 28;38(3):225-239. Epub 2018 May 28.

a Department of Bioinformatics, Computer Aided Drug Design and Molecular Modeling Lab , Alagappa University , Karaikudi , India.

Atom-based three dimensional-quantitative structure-activity relationship (3D-QSAR) model was developed on the basis of 5-point pharmacophore hypothesis (AARRR) with two hydrogen bond acceptors (A) and three aromatic rings for the derivatives of thieno[2,3-b]pyridine, which modulates the activity to inhibit the mGluR5 receptor. Generation of a highly predictive 3D-QSAR model was performed using the alignment of predicted pharmacophore hypothesis for the training set (R = 0.84, SD = 0. Read More

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http://dx.doi.org/10.1080/10799893.2018.1476542DOI Listing
June 2018
5 Reads

Antiproliferative and apoptosis-induction studies of 5-hydroxy 3',4',7-trimethoxyflavone in human breast cancer cells MCF-7: an in vitro and in silico approach.

J Recept Signal Transduct Res 2018 Jun 8;38(3):179-190. Epub 2018 May 8.

c Department of Animal Science, School of Life Sciences , Bharathidasan University , Tiruchirappalli , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1468780DOI Listing
June 2018
1 Read

Discovery of FIXa inhibitors by combination of pharmacophore modeling, molecular docking, and 3D-QSAR modeling.

J Recept Signal Transduct Res 2018 Jun 4;38(3):213-224. Epub 2018 May 4.

b State Key Laboratory of Phytochemistry and Plant Resources in West China , Kunming Institute of Botany, Chinese Academy of Sciences , Kunming , PR China.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1468784DOI Listing
June 2018
1 Read

Neuropharmacological and molecular docking studies of xanthones from Swertia corymbosa.

J Recept Signal Transduct Res 2018 Apr;38(2):166-177

b School of Life Sciences , Jawaharlal Nehru University , New Delhi , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1458875DOI Listing
April 2018
5 Reads

An explorative study on potent Gram-negative specific LpxC inhibitors: CoMFA, CoMSIA, HQSAR and molecular docking.

J Recept Signal Transduct Res 2018 Apr 6;38(2):151-165. Epub 2018 Apr 6.

a Department of Chemistry , University of Zabol , Zabol , Iran.

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. Read More

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https://www.tandfonline.com/doi/full/10.1080/10799893.2018.1
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http://dx.doi.org/10.1080/10799893.2018.1457052DOI Listing
April 2018
5 Reads

The estrogen-related receptors in metabolism and cancer: newer insights.

J Recept Signal Transduct Res 2018 Apr 5;38(2):95-100. Epub 2018 Apr 5.

a Department of Biochemistry , St. Edmund's College , Shillong , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1456552DOI Listing
April 2018
3 Reads

Differential expression and signaling of the human histamine H receptor isoforms of 445 and 365 amino acids expressed in human neuroblastoma SH-SY5Y cells.

J Recept Signal Transduct Res 2018 Apr 20;38(2):141-150. Epub 2018 Mar 20.

a Departamento de Fisiología, Biofísica y Neurociencias , Centro de Investigación y de Estudios Avanzados del IPN , Ciudad de México , México.

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 H receptor (hHR and hHR) on [S]-GTPγS binding, forskolin-induced cAMP formation, depolarization-induced increase in the intracellular concentration of Ca ions ([Ca]i) and depolarization-evoked [H]-dopamine release. Maximal specific binding (B) of [H]-N-methyl-histamine to cell membranes was 953 ± 204 and 555 ± 140 fmol/mg protein for SH-SY5Y-hHR and SH-SY5Y-hHR cells, respectively, with similar dissociation constants (K, 0.86 nM and 0. Read More

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http://dx.doi.org/10.1080/10799893.2018.1448995DOI Listing
April 2018
8 Reads

Deciphering PPARγ activation in cardiometabolic syndrome: studies by in silico and in vivo experimental assessment.

J Recept Signal Transduct Res 2018 Apr 27;38(2):122-132. Epub 2018 Feb 27.

a Department of Pharmacy, School of Chemical Sciences and Pharmacy , Central University of Rajasthan , Ajmer , India.

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). Read More

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http://dx.doi.org/10.1080/10799893.2018.1436560DOI Listing
April 2018
2 Reads

JTC-801 exerts anti-proliferative effects in human osteosarcoma cells by inducing apoptosis.

J Recept Signal Transduct Res 2018 Apr 15;38(2):133-140. Epub 2018 Feb 15.

a Department of Orthopaedics , The 2nd Hospital of Jilin University , Changchun , PR China.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1436561DOI Listing
April 2018
32 Reads

The effects of all-trans retinoic acid on estrogen receptor signaling in the estrogen-sensitive MCF/BUS subline.

J Recept Signal Transduct Res 2018 Apr 15;38(2):112-121. Epub 2018 Feb 15.

a Division of Toxicology , Wageningen University , Wageningen , The Netherlands.

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 (E) 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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1436559DOI Listing
April 2018
5 Reads

Cell signal transduction: hormones, neurotransmitters and therapeutic drugs relate to purine nucleotide structure.

Authors:
W R Williams

J Recept Signal Transduct Res 2018 Apr 6;38(2):101-111. Epub 2018 Feb 6.

a Faculty of Life Sciences & Education , University of South Wales , Cardiff , UK.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1431279DOI Listing
April 2018
2 Reads

Leptin and chronic kidney diseases.

J Recept Signal Transduct Res 2018 Apr 1;38(2):89-94. Epub 2018 Feb 1.

b Department of Pediatrics, Xinhua Hospital , Shanghai Jiao Tong University School of Medicine , Shanghai , China.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1431278DOI Listing
April 2018
6 Reads

Structural insights of Staphylococcus aureus FtsZ inhibitors through molecular docking, 3D-QSAR and molecular dynamics simulations.

J Recept Signal Transduct Res 2018 Feb;38(1):61-70

a Department of Chemistry , University College of Science, Osmania University , Hyderabad , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1426607DOI Listing
February 2018
2 Reads

Effects of LPA and LPA on the regulation of colony formation activity in colon cancer cells treated with anticancer drugs.

J Recept Signal Transduct Res 2018 Feb;38(1):71-75

a Division of Molecular Oncology , Kindai University , Higashiosaka, Osaka , Japan.

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 (LPA) to LPA). 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). Read More

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http://dx.doi.org/10.1080/10799893.2018.1426608DOI Listing
February 2018
2 Reads

Characterization of free fatty acid receptors expression in an obesity rat model with high sucrose diet.

J Recept Signal Transduct Res 2018 Feb;38(1):76-82

a Pharmacobiology Department , Cinvestav-IPN Unidad Coapa , Mexico City , Mexico.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1426609DOI Listing
February 2018
13 Reads

Computational screening, ensemble docking and pharmacophore analysis of potential gefitinib analogues against epidermal growth factor receptor.

J Recept Signal Transduct Res 2018 Feb;38(1):48-60

a Department of Zoology , Sri Venkateswara University , Tirupati , India.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1426603DOI Listing
February 2018
12 Reads

Combination therapy Eve and Pac to induce apoptosis in cervical cancer cells by targeting PI3K/AKT/mTOR pathways.

J Recept Signal Transduct Res 2018 Feb;38(1):83-88

b Department of Gynaecology and Obstetrics , Qingdao 3rd People's Hospital , Qingdao , China.

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. Read More

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http://dx.doi.org/10.1080/10799893.2018.1426610DOI Listing
February 2018
4 Reads

Identification of new potential HIV-1 reverse transcriptase inhibitors by QSAR modeling and structure-based virtual screening.

J Recept Signal Transduct Res 2018 Feb 19;38(1):37-47. Epub 2017 Dec 19.

a Department of Chemistry , University of Zabol , Zabol , Iran.

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 EC values were collected. Then, different types of molecular descriptors were calculated. Read More

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http://dx.doi.org/10.1080/10799893.2017.1414844DOI Listing
February 2018
5 Reads

An optimized protocol for the in vitro generation and functional analysis of human PD1/PD-L1 signal.

J Recept Signal Transduct Res 2018 Feb 18;38(1):31-36. Epub 2017 Dec 18.

d Pharmaceutical Technology Institute , Mashhad University of Medical Sciences , Mashhad , Iran.

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. Read More

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http://dx.doi.org/10.1080/10799893.2017.1414843DOI Listing
February 2018
5 Reads

The role of ERK and Smad2 signal pathways in the alternatively activated macrophages induced by TGF-β1 and high-ambient glucose.

J Recept Signal Transduct Res 2018 Feb 4;38(1):27-30. Epub 2017 Dec 4.

a Department of Nephrology , the Six Affiliated Hospital of Sun Yat-sen University , Guangzhou , China.

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. Read More

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http://dx.doi.org/10.1080/10799893.2017.1407340DOI Listing
February 2018
10 Reads

TRH receptor mobility in the plasma membrane is strongly affected by agonist binding and by interaction with some cognate signaling proteins.

J Recept Signal Transduct Res 2018 Feb 14;38(1):20-26. Epub 2017 Nov 14.

a Department of Physiology, Faculty of Science , Charles University , Prague , Czech Republic.

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 G proteins. Read More

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http://dx.doi.org/10.1080/10799893.2017.1398756DOI Listing
February 2018
3 Reads

Identifying novel small molecule antagonists for mLST8 protein using computational approaches.

J Recept Signal Transduct Res 2018 Feb 17;38(1):1-11. Epub 2017 Oct 17.

a Centre for Bioinformatics, School of Life Sciences , Pondicherry University , Puducherry , India.

Mammalian lethal with SEC13 protein 8 (mLST8), is an indispensable protein subunit of mammalian target of rapamycin (mTOR) signaling pathway that interacts with the kinase domain of mTOR protein, thereby stabilizing its active site. Experimental studies reported the over expression of mLST8 in human colon and prostate cancers by activation of both mTORC1/2 complexes and subsequent downstream substrates leading to tumor progression. Considering its role, targeting mLST8 protein would be a therapeutic approach against tumor progression in colon and prostate cancers. Read More

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http://dx.doi.org/10.1080/10799893.2017.1387920DOI Listing
February 2018
8 Reads

Identification of novel scaffolds to inhibit human mitotic kinesin Eg5 targeting the second allosteric binding site using in silico methods.

J Recept Signal Transduct Res 2018 Feb 17;38(1):12-19. Epub 2017 Oct 17.

a Department of Biotechnology , School of Chemical and Biotechnology, SASTRA University , Thanjavur , India.

Human mitotic kinesins are potential anticancer drug targets because of their essential role in mitotic cell division. The kinesin Eg5 (Kinesin-5, kif11) has gained much attention in this regard and has many inhibitors in different phases of clinical trials. All drug candidates considered for Eg5 so far binds to the binding site (Site 1) formed by the loop L5, helices α2 and α3 and are uncompetitive to ATP/ADP. Read More

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http://dx.doi.org/10.1080/10799893.2017.1387922DOI Listing
February 2018
2 Reads

Ligand-based virtual screening, molecular docking, QSAR and pharmacophore analysis of quercetin-associated potential novel analogs against epidermal growth factor receptor.

J Recept Signal Transduct Res 2017 Dec;37(6):600-610

a Department of Zoology, Division of Cancer Informatics , Sri Venkateswara University , Tirupati , India.

The present study was to explore expectation and examination of therapeutic potential quercetin analogs as efficient anticancer agents against human epidermal growth factor receptor (EGFR), which is a consistent hallmark for moderating the non-small-cell lung carcinoma (NSCLC). Here, ligand-based virtual screening, pharmacophore approach and molecular docking were established as rational strategies for recognition of small analogs against the ligand binding domain of EGFR (PDB code: 1XKK). Adverse effects, toxicogenomics and pharmacokinetics reported that 10 candidates showed reliable consequences with less side effects and more efficient for target receptor. Read More

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http://dx.doi.org/10.1080/10799893.2017.1377237DOI Listing
December 2017
11 Reads

Probing voltage sensing domain of KCNQ2 channel as a potential target to combat epilepsy: a comparative study.

J Recept Signal Transduct Res 2017 Dec 31;37(6):578-589. Epub 2017 Aug 31.

a Department of Pharmacy, School of Chemical Sciences and Pharmacy , Central University of Rajasthan , Kishangarh, Ajmer , Rajasthan , India.

Multidrug resistance along with side-effects of available anti-epileptic drugs and unavailability of potent and effective agents in submicromolar quantities presents the biggest therapeutic challenges in anti-epileptic drug discovery. The molecular modeling techniques allow us to identify agents with novel structures to match the continuous urge for its discovery. KCNQ2 channel represents one of the validated targets for its therapy. Read More

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http://dx.doi.org/10.1080/10799893.2017.1369122DOI Listing
December 2017
3 Reads

A bioluminescence resonance energy transfer 2 (BRET2) assay for monitoring seven transmembrane receptor and insulin receptor crosstalk.

J Recept Signal Transduct Res 2017 Dec 30;37(6):590-599. Epub 2017 Aug 30.

c Department of Diabetes and Cardiovascular Disease , Novo Nordisk A/S , Maalov , Denmark.

The angiotensin AT receptor is a seven transmembrane (7TM) receptor, which mediates the regulation of blood pressure. Activation of angiotensin AT receptor may lead to impaired insulin signaling indicating crosstalk between angiotensin AT receptor and insulin receptor signaling pathways. To elucidate the molecular mechanisms behind this crosstalk, we applied the BRET technique to monitor the effect of angiotensin II on the interaction between Rluc tagged insulin receptor and GFP tagged insulin receptor substrates 1, 4, 5 (IRS1, IRS4, IRS5) and Src homology 2 domain-containing protein (Shc). Read More

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http://dx.doi.org/10.1080/10799893.2017.1369123DOI Listing
December 2017
6 Reads

Insulin suppresses MPP-induced neurotoxicity by targeting integrins and syndecans in C6 astrocytes.

J Recept Signal Transduct Res 2017 Dec 30;37(6):550-559. Epub 2017 Aug 30.

a Department of Pharmacology and Toxicology, Metabolic Diseases Research Laboratory, School of Dentistry , Kyung Hee University , Seoul , South Korea.

Parkinson's disease (PD) is the second most common neurodegenerative disease in the elderly. In central nervous system, astrocytes regulates 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, C6 astroglial cells have been used to study the in vitro PD model induced by 1-methyl-4-phenyl pyridinium (MPP). Read More

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http://dx.doi.org/10.1080/10799893.2017.1369119DOI Listing
December 2017
8 Reads

Synergic prooxidant, apoptotic and TRPV1 channel activator effects of alpha-lipoic acid and cisplatin in MCF-7 breast cancer cells.

J Recept Signal Transduct Res 2017 Dec 29;37(6):569-577. Epub 2017 Aug 29.

a Vocational High School of Islahiye , Gaziantep University , Gaziantep , Turkey.

Background: Resistance to cisplatin (Cisp) in the treatment of breast cancer is a major obstacle. Alpha-lipoic acid (ALA) has both antioxidant and oxidant properties. ALA has been used on stimulation mechanisms of apoptosis and oxidative stress in the treatment of cancer with a combination of chemotherapeutic agents, although its role on molecular mechanisms in the cancer cells has not been clarified yet. Read More

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http://dx.doi.org/10.1080/10799893.2017.1369121DOI Listing
December 2017
10 Reads

Prorenin receptor (PRR)-mediated NADPH oxidase (Nox) signaling regulates VEGF synthesis under hyperglycemic condition in ARPE-19 cells.

J Recept Signal Transduct Res 2017 Dec 25;37(6):560-568. Epub 2017 Aug 25.

a Department of Ophthalmology , Emory University School of Medicine , Atlanta , GA , USA.

The stimulation of angiotensin II (Ang II), the effector peptide of renin-angiotensin system, has been reported to increase the expression of vascular endothelial growth factor (VEGF) through the activation of the Ang II type 1 receptor (AT1R). In this study, we investigated whether hyperglycemia (HG, 33 mM glucose) in ARPE-19 cells could promote the expression of VEGF independently of Ang II through prorenin receptor (PRR), via an NADPH oxidase (Nox)-dependent mechanism. ARPE-19 cells were treated with the angiotensin converting enzyme (ACE) inhibitor perindopril to block the synthesis of Ang II. Read More

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http://dx.doi.org/10.1080/10799893.2017.1369120DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5994760PMC
December 2017
38 Reads