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https://www.readbyqxmd.com/read/29346833/phase-1b-trial-of-ficlatuzumab-a-humanized-hepatocyte-growth-factor-inhibitory-monoclonal-antibody-in-combination-with-gefitinib-in-asian-patients-with-nsclc
#1
Eng-Huat Tan, Wan-Teck Lim, Myung-Ju Ahn, Quan-Sing Ng, Jin Seok Ahn, Daniel Shao-Weng Tan, Jong-Mu Sun, May Han, Francis C Payumo, Krista McKee, Wei Yin, Marc Credi, Shefali Agarwal, Jaroslaw Jac, Keunchil Park
Hepatocyte growth factor (HGF)/c-Met pathway dysregulation is a mechanism for epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs). Ficlatuzumab (AV-299; SCH 900105), a humanized IgG1 κ HGF inhibitory monoclonal antibody, prevents HGF/c-Met pathway ligand-mediated activation. This phase 1b study assessed the safety/tolerability, pharmacokinetics/pharmacodynamics, and antitumor activity of ficlatuzumab plus gefitinib in Asian patients with previously treated advanced non-small cell lung cancer (NSCLC)...
January 18, 2018: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/29342106/adrenergic-agonists-bind-to-adrenergic-receptor-like-regions-of-the-mu-opioid-receptor-enhancing-morphine-and-methionine-enkephalin-binding-a-new-approach-to-biased-opioids
#2
Robert Root-Bernstein, Miah Turke, Udaya K Tiruttani Subhramanyam, Beth Churchill, Joerg Labahn
Extensive evidence demonstrates functional interactions between the adrenergic and opioid systems in a diversity of tissues and organs. While some effects are due to receptor and second messenger cross-talk, recent research has revealed an extracellular, allosteric opioid binding site on adrenergic receptors that enhances adrenergic activity and its duration. The present research addresses whether opioid receptors may have an equivalent extracellular, allosteric adrenergic binding site that has similar enhancing effects on opioid binding...
January 17, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29341826/mu-opioid-receptors-inhibit-the-exercise-pressor-reflex-by-closing-n-type-calcium-channels-but-not-by-opening-girk-channels-in-rats
#3
Juan A Estrada, Marc P Kaufman
Mu opioid G-protein coupled receptors (MOR) interact with ion channels to decrease neuronal excitability. In humans, intrathecal administration of the MOR agonist, fentanyl, inhibits the exercise pressor reflex, an effect that can be attributed to either the opening of inward rectifying potassium channels (GIRK) or the closing of N-type calcium channels. The purpose of this study was to determine if the highly selective MOR agonist DAMGO attenuates the exercise pressor reflex, and which of these two channels are responsible for this effect...
January 17, 2018: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/29339517/infected-erythrocytes-expressing-dc13-pfemp1-differ-from-recombinant-proteins-in-epcr-binding-function
#4
Yvonne Azasi, Gabriella Lindergard, Ashfaq Ghumra, Jianbing Mu, Louis H Miller, J Alexandra Rowe
Recent advances have identified a new paradigm for cerebral malaria pathogenesis in which endothelial protein C receptor (EPCR) is a major host receptor for sequestration of Plasmodium falciparum-infected erythrocytes (IEs) in the brain and other vital organs. The parasite adhesins that bind EPCR are members of the IE variant surface antigen family Plasmodium falciparum erythrocyte membrane protein 1 (PfEMP1) containing specific adhesion domains called domain cassette (DC) 8 and DC13. The binding interaction site between PfEMP1 and EPCR has been mapped by biophysical and crystallography studies using recombinant proteins...
January 16, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29335066/up-and-down-regulated-leukemia-related-protein-16-affects-er%C3%AE-expression-and-prolactin-secretion-by-gh3-cells
#5
Xing Su, Zhi Qiang Wu, Xiao Jiang Yang, An Ping Wang, Kun Zhao, Tao Guang Wu, Yi Sun, Jie Sun, Zheng Yao Chang, Xiao Yong Guo, Qing Hua Guo, Yi Ming Mu
Prolactinoma is an estrogen-related tumor and leukemia-related protein 16 (LRP16) is correlated with the progression of estrogen-related tumors, but the regulatory mechanism between LRP16 and prolactinoma remain unclear. This study demonstrates a variation in LRP16 with estrogen receptor α (ERα) in prolactinoma models and the up and downregulation effects of LRP16 on prolactin secretion of pituitary adenomas cells (GH3 cells). In our study, 50 male SD rats (30-day-old) were randomly divided into five groups of 10 rats each...
December 2017: Biomedical and Environmental Sciences: BES
https://www.readbyqxmd.com/read/29331800/nucleus-accumbens-mu-opioid-receptors-regulate-context-specific-social-preferences-in-the-juvenile-rat
#6
Caroline J W Smith, Kevin B Wilkins, Sara Li, Maxwell T Tulimieri, Alexa H Veenema
The μ opioid receptor (MOR) in the nucleus accumbens (NAc) is involved in assigning pleasurable, or hedonic value to rewarding stimuli. Importantly, the hedonic value of a given rewarding stimulus likely depends on an individual's current motivational state. Here, we examined the involvement of MORs in the motivation to interact with a novel or a familiar (cage mate) conspecific in juvenile rats. First, we demonstrated that the selective MOR antagonist CTAP administered into the NAc reduces social novelty preference of juvenile males, by decreasing the interaction time with the novel conspecific and increasing the interaction time with the cage mate...
December 30, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/29330156/application-of-receptor-theory-to-the-design-and-use-of-fixed-proportion-mu-opioid-agonist-and-antagonist-mixtures-in-rhesus-monkeys
#7
Jeremy C Cornelissen, Samuel Obeng, Kenner C Rice, Yan Zhang, S Stevens Negus, Matthew Banks
Receptor theory predicts that fixed-proportion mixtures of a competitive, reversible agonist (e.g. fentanyl) and antagonist (e.g. naltrexone) at a common receptor (e.g. mu opioid receptors; MOR) will result in antagonist proportion-dependent decreases in apparent efficacy of the mixtures and downward shifts in mixture dose-effect functions. The present study tested this hypothesis by evaluating behavioral effects of fixed-proportion fentanyl/naltrexone mixtures in a warm-water tail-withdrawal procedure in rhesus monkeys (n=4)...
January 12, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29323153/skeletal-characterization-of-the-fgfr3-mouse-model-of-achondroplasia-using-micro-ct-and-mri-volumetric-imaging
#8
Mohammed Salman Shazeeb, Megan K Cox, Anurag Gupta, Wen Tang, Kuldeep Singh, Cynthia T Pryce, Robert Fogle, Ying Mu, William D Weber, Dinesh S Bangari, Xiaoyou Ying, Yves Sabbagh
Achondroplasia, the most common form of dwarfism, affects more than a quarter million people worldwide and remains an unmet medical need. Achondroplasia is caused by mutations in the fibroblast growth factor receptor 3 (FGFR3) gene which results in over-activation of the receptor, interfering with normal skeletal development leading to disproportional short stature. Multiple mouse models have been generated to study achondroplasia. The characterization of these preclinical models has been primarily done with 2D measurements...
January 11, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29321379/a-glucose-responsive-insulin-therapy-protects-animals-against-hypoglycemia
#9
Ruojing Yang, Margaret Wu, Songnian Lin, Ravi P Nargund, Xinghai Li, Theresa Kelly, Lin Yan, Ge Dai, Ying Qian, Qing Dallas-Yang, Paul A Fischer, Yan Cui, Xiaolan Shen, Pei Huo, Danqing Dennis Feng, Mark D Erion, David E Kelley, James Mu
Hypoglycemia is commonly associated with insulin therapy, limiting both its safety and efficacy. The concept of modifying insulin to render its glucose-responsive release from an injection depot (of an insulin complexed exogenously with a recombinant lectin) was proposed approximately 4 decades ago but has been challenging to achieve. Data presented here demonstrate that mannosylated insulin analogs can undergo an additional route of clearance as result of their interaction with endogenous mannose receptor (MR), and this can occur in a glucose-dependent fashion, with increased binding to MR at low glucose...
January 11, 2018: JCI Insight
https://www.readbyqxmd.com/read/29301275/generation-and-characterization-of-antibodies-against-opioid-receptors-from-zebrafish
#10
Juan C Arévalo, Enrique Hernández-Jiménez, Ada Jiménez-González, María Torres-Valle, Roman S Iwasaki, Roger López-Bellido, Cristina Vicente-García, Raquel E Rodríguez
The opioid system is well conserved among species and plays a critical role in pain and addiction systems. The use of zebrafish as an experimental model to study development and genetics is extraordinary and has been proven to be relevant for the study of different diseases. The main drawback to its use for the analysis of different pathologies is the lack of protein tools. Antibodies that work in other models are not suitable for zebrafish due to the low degree of homology that exists among the opioid receptor protein sequences in different species...
January 2, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29296674/dynamic-strategic-bond-analysis-yields-a-ten-step-synthesis-of-20-nor-salvinorin-a-a-potent-%C3%AE%C2%BA-or-agonist
#11
Jeremy J Roach, Yusuke Sasano, Cullen L Schmid, Saheem Zaidi, Vsevolod Katritch, Raymond C Stevens, Laura M Bohn, Ryan A Shenvi
Salvinorin A (SalA) is a plant metabolite that agonizes the human kappa-opioid receptor (κ-OR) with high affinity and high selectivity over mu- and delta-opioid receptors. Its therapeutic potential has stimulated extensive semisynthetic studies and total synthesis campaigns. However, structural modification of SalA has been complicated by its instability, and efficient total synthesis has been frustrated by its dense, complex architecture. Treatment of strategic bonds in SalA as dynamic and dependent on structural perturbation enabled the identification of an efficient retrosynthetic pathway...
December 27, 2017: ACS Central Science
https://www.readbyqxmd.com/read/29295973/protein-inspired-antibiotics-active-against-vancomycin-and-daptomycin-resistant-bacteria
#12
Mark A T Blaskovich, Karl A Hansford, Yujing Gong, Mark S Butler, Craig Muldoon, Johnny X Huang, Soumya Ramu, Alberto B Silva, Mu Cheng, Angela M Kavanagh, Zyta Ziora, Rajaratnam Premraj, Fredrik Lindahl, Tanya A Bradford, June C Lee, Tomislav Karoli, Ruby Pelingon, David J Edwards, Maite Amado, Alysha G Elliott, Wanida Phetsang, Noor Huda Daud, Johan E Deecke, Hanna E Sidjabat, Sefetogi Ramaologa, Johannes Zuegg, Jason R Betley, Andrew P G Beevers, Richard A G Smith, Jason A Roberts, David L Paterson, Matthew A Cooper
The public health threat posed by a looming 'post-antibiotic' era necessitates new approaches to antibiotic discovery. Drug development has typically avoided exploitation of membrane-binding properties, in contrast to nature's control of biological pathways via modulation of membrane-associated proteins and membrane lipid composition. Here, we describe the rejuvenation of the glycopeptide antibiotic vancomycin via selective targeting of bacterial membranes. Peptide libraries based on positively charged electrostatic effector sequences are ligated to N-terminal lipophilic membrane-insertive elements and then conjugated to vancomycin...
January 2, 2018: Nature Communications
https://www.readbyqxmd.com/read/29289718/a-high-fat-high-sugar-western-diet-alters-dorsal-striatal-glutamate-opioid-and-dopamine-transmission-in-mice
#13
Brandon M Fritz, Braulio Muñoz, Fuqin Yin, Casey Bauchle, Brady K Atwood
Understanding neuroadaptations involved in obesity is critical for developing new approaches to treatment. Diet-induced neuroadaptations within the dorsal striatum have the capacity to drive excessive food seeking and consumption. Five week old C57BL/6J mice consumed a high-fat, high-sugar 'western diet' (WD) or a control 'standard diet' (SD) for 16 weeks. Weight gain, glucose tolerance, and insulin tolerance were measured to confirm an obese-like state. Following these 16 weeks, electrophysiological recordings were made from medium spiny neurons (MSNs) in the medial (DMS) and lateral (DLS) portions of dorsal striatum to evaluate diet effects on neuronal excitability and synaptic plasticity...
December 28, 2017: Neuroscience
https://www.readbyqxmd.com/read/29286104/treatment-with-shuyu-capsule-increases-5-ht1ar-level-and-activation-of-camp-pka-creb-pathway-in-hippocampal-neurons-treated-with-serum-from-a-rat-model-of-depression
#14
Xiao-Long Wang, Jie Gao, Xiao-Yu Wang, Xiao-Fei Mu, Sheng Wei, Ling Xue, Ming-Qi Qiao
Depressive disorder (DD) is one of the typical affective disorders with a high morbidity, high suicide rate and high recurrence rate. Dysfunction of the 5‑hydroxytryptamine 1A receptor (5‑HT1AR) in the brain may serve an important role in the pathogenesis of DD. Currently, selective serotonin reuptake inhibitors are the first line antidepressants with 60‑70% efficacy and severe adverse effects. Previous studies have demonstrated that Chinese herbal medicines, including the Shuyu capsule (SYC), are effective antidepressants with few side effects...
December 22, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29277141/in-silico-studies-of-conformational-dynamics-of-mu-opioid-receptor-performed-using-gaussian-accelerated-molecular-dynamics
#15
Jun-Min Liao, Yeng-Tseng Wang
G-protein-coupled receptors play a crucial role in various signaling pathways and function as targets for treating a wide spectrum of diseases. Since the 20th century, extensive research has been conducted on the Mu opioid receptor (MOR) as a drug target. We examined the MOR inactivation and activation processes by using an enhanced sampling method (Gaussian accelerated molecular dynamics), the binding pocket site area method, the root-mean-square deviation method, and the free energy (potential of mean force) method...
December 25, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29261544/mu-opioid-receptors-in-ganglia-but-not-in-muscle-mediate-peripheral-analgesia-in-rat-muscle-pain
#16
Ana Bagues, María Isabel Martín, Alejandro Higuera-Matas, Jesús Esteban-Hernández, Emilio Ambrosio, Eva María Sánchez-Robles
BACKGROUND: Previous studies have demonstrated the participation of peripheral μ-opioid receptors (MOR) in the antinociceptive effect of systemically administered morphine and loperamide in an orofacial muscle pain model, induced by hypertonic saline, but not in a spinally innervated one, in rats. In this study, we determine whether this peripheral antinociceptive effect is due to the activation of MOR localized in the muscle, ganglia, or both. METHODS: To determine the local antinociceptive effect of morphine and loperamide, 2 models of acute muscle pain (trigeminal and spinal) were used...
December 19, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29259946/genetic-analysis-of-mu-and-kappa-opioid-receptor-and-comt-enzyme-in-cancer-pain-tunisian-patients-under-opioid-treatment
#17
Imen Chatti, Jean-Baptiste Woillard, Amira Mili, Isabelle Creveaux, Ilhem Ben Charfeddine, Jihène Feki, Sarah Langlais, Leila Ben Fatma, Ali Saad, Moez Gribaa, Frédéric Libert
Background: Pain and its opioid treatments are complex measurable traits. Responses to morphine in terms of pain control is likely to be determined by many factors, including the underlying pain sensitivity of the patient, along with nature and extent of the painful process, concomitant medications, genetic and other clinical and environmental factors. This study investigated genetic polymorphisms implicated in the inter-individual pain response variability to opioid treatment in the Tunisian population...
December 2017: Iranian Journal of Public Health
https://www.readbyqxmd.com/read/29259544/dichotomous-effects-of-mu-opioid-receptor-activation-on-striatal-low-threshold-spike-interneurons
#18
Rasha Elghaba, Enrico Bracci
Striatal low-threshold spike interneurons (LTSIs) are tonically active neurons that express GABA and nitric oxide synthase and are involved in information processing as well as neurovascular coupling. While mu opioid receptors (MORs) and their ligand encephalin are prominent in the striatum, their action on LTSIs has not been investigated. We addressed this issue carrying out whole-cell recordings in transgenic mice in which the NPY-expressing neurons are marked with green fluorescent protein (GFP). The MOR agonist (D-Ala(2), N-MePhe(4), Gly-ol)-enkephalin (DAMGO) produced dual effects on subpopulations of LTSIs...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29250179/no-association-between-triple-negative-breast-cancer-and-prognosis-of-patients-receiving-breast-conserving-treatment
#19
Lan Mu, Yuxiang Liu, Meng Xiao, Weise Liu, Miao Liu, Xin Wang
The role of triple-negative breast cancer (TNBC) in breast-conserving treatment is controversial. The present study aimed at evaluating the prognosis of patients with TNBC following breast-conserving treatment (BCT) within 5 years. The present study investigated a cohort of 757 patients with early stage breast cancer, diagnosed and treated with BCT between January 2002 and March 2010 at Tianjin Medical University Cancer Institute and Hospital. The patients were divided into three groups according to receptor expression: Estrogen receptor (ER) or progesterone receptor (PR)-positive; epidermal growth factor receptor 2 (HER2)-enriched: ER and PR negative but HER2-positive; TNBC: ER, PR and HER2 receptor-negative...
December 2017: Oncology Letters
https://www.readbyqxmd.com/read/29249810/schizophrenia-and-depression-two-poles-of-endocannabinoid-system-deregulation
#20
María Rodríguez-Muñoz, Pilar Sánchez-Blázquez, Luis F Callado, J Javier Meana, Javier Garzón-Niño
The activity of certain G protein-coupled receptors (GPCRs) and of glutamate N-Methyl-D-aspartate receptors (NMDARs) is altered in both schizophrenia and depression. Using postmortem prefrontal cortex samples from subjects with schizophrenia or depression, we observed a series of opposite changes in the expression of signaling proteins that have been implicated in the cross-talk between GPCRs and NMDARs. Thus, the levels of HINT1 proteins and NMDAR NR1 subunits carrying the C1 cytosolic segment were increased in depressives and decreased in schizophrenics, respect to matched controls...
December 18, 2017: Translational Psychiatry
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