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https://www.readbyqxmd.com/read/28340282/carfilzomib-induces-leukaemia-cell-apoptosis-via-inhibiting-elk1-kiaa1524-elk-1-cip2a-and-activating-pp2a-not-related-to-proteasome-inhibition
#1
Chun-Yu Liu, Feng-Shu Hsieh, Pei-Yi Chu, Wen-Chun Tsai, Chun-Teng Huang, Yuan-Bin Yu, Tzu-Ting Huang, Po-Shen Ko, Man-Hsin Hung, Wan-Lun Wang, Chung-Wai Shiau, Kuen-Feng Chen
Enhancing the tumour suppressive activity of protein phosphatase 2A (PP2A) has been suggested to be an anti-leukaemic strategy. KIAA1524 (also termed CIP2A), an oncoprotein inhibiting PP2A, is associated with disease progression in chronic myeloid leukaemia and may be prognostic in cytogenetically normal acute myeloid leukaemia. Here we demonstrated that the selective proteasome inhibitor, carfilzomib, induced apoptosis in sensitive primary leukaemia cells and in sensitive leukaemia cell lines, associated with KIAA1524 protein downregulation, increased PP2A activity and decreased p-Akt, but not with the proteasome inhibition effect of carfilzomib...
March 24, 2017: British Journal of Haematology
https://www.readbyqxmd.com/read/28340145/human-abuse-potential-of-the-new-opioid-analgesic-molecule-nktr-181-compared-with-oxycodone
#2
Lynn Webster, Jack Henningfield, August R Buchhalter, Suresh Siddhanti, Lin Lu, Aleksandrs Odinecs, Carlo J Di Fonzo, Michael A Eldon
Objective.:  Evaluate the human abuse potential, pharmacokinetics, pharmacodynamics, and safety of NKTR-181, a novel mu-opioid agonist molecule, relative to oxycodone. Design.:  This randomized, single-center, double-blind, active- and placebo-controlled five-period crossover study enrolled healthy, adult, non-physically dependent recreational opioid users. Setting.:  Inpatient clinical research site. Subjects. : Forty-two randomized subjects (73...
March 10, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/28340056/neutrophil-derived-mitochondrial-dna-promotes-receptor-activator-of-nuclear-factor-%C3%AE%C2%BAb-and-its-ligand-signalling-in-rheumatoid-arthritis
#3
Anne Contis, Stéphane Mitrovic, Julie Lavie, Isabelle Douchet, Estibaliz Lazaro, Marie-Elise Truchetet, Cyril Goizet, Cécile Contin-Bordes, Thierry Schaeverbeke, Patrick Blanco, Rodrigue Rossignol, Benjamin Faustin, Christophe Richez, Pierre Duffau
Objectives.: Mitochondrial DNA (mtDNA) contains sequestered damage-associated molecular patterns that might be involved in osteoimmunological pathogenesis of RA. Here, we aimed to investigate the cellular source of mtDNA and its role in RANK ligand (RANKL) expression by RA SF neutrophils. Methods.: The gene expression signature of SF neutrophils was examined by proteomic quantitative analysis. Levels of mtDNA in circulating and SF neutrophils from RA patients and OA control subjects were assessed by real-time PCR...
March 13, 2017: Rheumatology
https://www.readbyqxmd.com/read/28340044/oral-ghrelin-receptor-agonist-mk-0677-increases-serum-insulin-like-growth-factor-1-in-hemodialysis-patients-a-randomized-blinded-study
#4
Garland A Campbell, James T Patrie, Bruce D Gaylinn, Michael O Thorner, Warren K Bolton
Background: . Protein-energy wasting (PEW) in end-stage renal disease (ESRD) patients is associated with increased morbidity and mortality, but options for treatment are limited. Growth hormone (GH) increases insulin-like growth factor 1 (IGF-1), with improved nutritional parameters, but must be given subcutaneously and does not provide normal GH secretion patterns. MK-0677, an oral ghrelin receptor agonist (GRA), maintains normal GH secretion and increases lean body mass in normal subjects; it has not been studied in dialysis patients, an essential step in assessing efficacy and safety prior to clinical trials...
March 3, 2017: Nephrology, Dialysis, Transplantation
https://www.readbyqxmd.com/read/28339898/the-impact-of-the-psychoactive-substances-act-2016-on-the-online-availability-of-mdmb-chmica
#5
M Haden, D M Wood, P I Dargan
Background: In May 2016, the UK Government enacted the Psychoactive Substances Act which made it an offense to produce or supply many drugs including new psychoactive substances (NPS). Aim: We aimed to assess the impact of the Act on the availability of the synthetic cannabinoid receptor agonist methyl 2-[[1-(cyclohexylmethyl)indole-3-carbonyl]amino]-3,3-dimethylbutanoate (MDMB-CHMICA) from internet-based suppliers. Design: Internet snapshot availability study...
February 28, 2017: QJM: Monthly Journal of the Association of Physicians
https://www.readbyqxmd.com/read/28339772/heterologous-desensitization-of-cardiac-%C3%AE-adrenergic-signal-via-hormone-induced-%C3%AE-ar-arrestin-pde4-complexes
#6
Qian Shi, Minghui Li, Delphine Mika, Qin Fu, Sungjin Kim, Jason Phan, Ao Shen, Gregoire Vandecasteele, Yang K Xiang
Aims: Cardiac β-adrenergic receptor (βAR) signaling is susceptible to heterologous desensitization by different neurohormonal stimuli in clinical conditions associated with heart failure. We aim to examine the underlying mechanism of cross talk between βARs and a set of G-protein coupled receptors (GPCRs) activated by hormones/agonists. Methods and results: Rat ventricular cardiomyocytes were used to determine heterologous phosphorylation of βARs under a series of GPCR agonists...
February 21, 2017: Cardiovascular Research
https://www.readbyqxmd.com/read/28339742/topiramate-modulates-post-infarction-inflammation-primarily-by-targeting-monocytes-or-macrophages
#7
Zhaohui Wang, Shiyuan Huang, Yuling Sheng, Xu Peng, Hui Liu, Nan Jin, Jun Cai, Yanwen Shu, Ting Li, Ping Li, Cheng Fan, Xiaofan Hu, Wenyong Zhang, Rui Long, Ya You, Caihong Huang, Yi Song, Chunhua Xiang, Jue Wang, Yong Yang, Kun Liu
Aims: Monocytes/macrophages response plays a key role in post-infarction inflammation that contributes greatly to post-infarction ventricular remodeling and cardiac rupture. Therapeutic targeting of the GABAA receptor, which is enriched in monocytes/macrophages but not expressed in the myocardium, may be possible after myocardial infarction. Methods and results: After MI was induced by ligation of the coronary artery, C57BL/6 mice were intraperitoneally administered with one specific agonist or antagonist of the GABAA receptor (topiramate or bicuculline), in the setting of presence or depletion of monocytes/macrophages...
February 17, 2017: Cardiovascular Research
https://www.readbyqxmd.com/read/28339619/relationship-of-neuropeptide-ff-receptors-with-pubertal-maturation-of-gilts%C3%A2
#8
Jennifer F Thorson, Neely L Heidorn, Vitaly Ryu, Krzysztof Czaja, Danny J Nonneman, C Richard Barb, Gary J Hausman, Gary A Rohrer, Ligia D Prezotto, Richard B McCosh, Elane C Wright, Brett R White, Bradley A Freking, William T Oliver, Stanley M Hileman, Clay A Lents
Mechanisms governing the timing of puberty in pigs are poorly understood. A genome-wide association study for age at first estrus in pigs identified candidate genes including neuropeptide FF receptor 2 (NPFFR2), which is a putative receptor for RFamide-related peptides (RFRP). RFRP has been shown to negatively regulate secretion of reproductive hormones from hypothalamic and pituitary tissue of pigs in culture. Here, the porcine NPFFR2 gene was further screened and four potentially functional variants were identified to be associated with age at first estrus in pigs (1,288 gilts)...
January 28, 2017: Biology of Reproduction
https://www.readbyqxmd.com/read/28339456/in-errata-kratom-the-new-legal-high-on-the-block-the-case-of-an-emerging-opioid-receptor-agonist-with-substance-abuse-potential
#9
(no author information available yet)
No abstract text is available yet for this article.
March 2017: Pain Physician
https://www.readbyqxmd.com/read/28339390/stability-of-fentanyl-citrate-in-polyolefin-bags
#10
Ronald F Donnelly
Fentanyl is used to manage pain because it is a potent lipophilic opiate agonist. The stability of fentanyl in polyolefin bags when diluted to either 10 µg/mL or 50 µg/mL with sodium chloride 0.9% has not been studied. The chemical stability of fentanyl 50 µg/mL packaged in polyvinyl chloride bags has been studied, however, the stability in polyolefin bags is lacking. Polyolefin bags were aseptically filled with either 10-µg/mL or 50-µg/mL fentanyl solution. Containers were then stored at either 5°C and protected from light or 22°C and exposed to light for 93 days...
November 2016: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28339199/structure-based-discovery-of-new-antagonist-and-biased-agonist-chemotypes-for-the-kappa-opioid-receptor
#11
Zhong Zheng, Xi-Ping Huang, Thomas J Mangano, Rodger Zou, Xin Chen, Saheem Zaidi, Bryan L Roth, Raymond C Stevens, Vsevolod Katritch
The ongoing epidemics of opioid overdose raises an urgent need for effective anti-addiction therapies and addiction-free painkillers. The κ-opioid receptor (KOR) has emerged as a promising target for both indications, raising demand for new chemotypes of KOR antagonists, as well as G-protein-biased agonists. We employed the crystal structure of the KOR-JDTic complex and ligand-optimized structural templates to perform virtual screening of available compound libraries for new KOR ligands. The prospective virtual screening campaign yielded a high 32% hit rate, identifying novel fragment-like and lead-like chemotypes of KOR ligands...
March 24, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28335516/marine-diterpenes-molecular-modeling-of-thrombin-inhibitors-with-potential-biotechnological-application-as-an-antithrombotic
#12
Rebeca Cristina Costa Pereira, André Luiz Lourenço, Luciana Terra, Paula Alvarez Abreu, Valéria Laneuville Teixeira, Helena Carla Castro
Thrombosis related diseases are among the main causes of death and incapacity in the world. Despite the existence of antithrombotic agents available for therapy, they still present adverse effects like hemorrhagic risks which justify the search for new options. Recently, pachydictyol A, isopachydictyol A, and dichotomanol, three diterpenes isolated from Brazilian marine brown alga Dictyota menstrualis were identified as potent antithrombotic molecules through inhibition of thrombin, a key enzyme of coagulation cascade and a platelet agonist...
March 20, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28334990/insulin-resistance-and-exendin-4-treatment-for-multiple-system-atrophy
#13
Fares Bassil, Marie-Hélène Canron, Anne Vital, Erwan Bezard, Yazhou Li, Nigel H Greig, Seema Gulyani, Dimitrios Kapogiannis, Pierre-Olivier Fernagut, Wassilios G Meissner
Multiple system atrophy is a fatal sporadic adult-onset neurodegenerative disorder with no symptomatic or disease-modifying treatment available. The cytopathological hallmark of multiple system atrophy is the accumulation of α-synuclein aggregates in oligodendrocytes, forming glial cytoplasmic inclusions. Impaired insulin/insulin-like growth factor-1 signalling (IGF-1) and insulin resistance (i.e. decreased insulin/IGF-1) have been reported in other neurodegenerative disorders such as Alzheimer's disease. Increasing evidence also suggests impaired insulin/IGF-1 signalling in multiple system atrophy, as corroborated by increased insulin and IGF-1 plasma concentrations in multiple system atrophy patients and reduced IGF-1 brain levels in a transgenic mouse model of multiple system atrophy...
March 14, 2017: Brain: a Journal of Neurology
https://www.readbyqxmd.com/read/28334727/discovering-the-relative-efficacy-of-inhaled-medications-for-chronic-obstructive-pulmonary-disease-multiple-treatment-comparisons
#14
Ying Zhu, Tong Zhang, Haiyan Li, Yang Yang, Qiong Chen, Lei Kong, Bo Tai
BACKGROUND: Chronic obstructive pulmonary disease (COPD) is managed by three major classes of inhaled medications: inhaled corticosteroids (ICS), long-acting Beta 2-agonist (LABA), long-acting muscarinic antagonist (LAMA). Single inhaled medication is usually replaced by combined inhaled medications for efficacy enhancement. However, this practice should be supported by clinical evidence for large-scale implementations. METHODS: The relative efficacy of inhaled medications is determined by three endpoints: changes in the trough forced expiratory volume in 1 second (tFEV1), changes in the St George's Respiratory Questionnaire (SGRQ) score and the proportion of SGRQ responders which represents a reduction in SGRQ total score at week 24 of ≥4...
March 27, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28334444/the-partial-dopamine-d2-receptor-agonist-aripiprazole-is-associated-with-weight-gain-in-adolescent-anorexia-nervosa
#15
Guido K W Frank, Megan E Shott, Jennifer O Hagman, Marissa A Schiel, Marisa C DeGuzman, Brogan Rossi
OBJECTIVE: Finding medication to support treatment of anorexia nervosa has been difficult. Neuroscience-based approaches may help in this effort. Recent brain imaging studies in adults and adolescents with anorexia nervosa suggest that dopamine-related reward circuits are hypersensitive and could provide a treatment target. METHODS: Here, we present a retrospective chart review of 106 adolescents with anorexia nervosa some of whom were treated with the dopamine D2 receptor partial agonist aripiprazole during treatment in a specialized eating disorder program...
March 23, 2017: International Journal of Eating Disorders
https://www.readbyqxmd.com/read/28334072/the-lateral-habenula-as-a-relay-of-cortical-information-to-process-working-memory
#16
Victor Mathis, Alexandra Barbelivien, Monique Majchrzak, Chantal Mathis, Jean-Christophe Cassel, Lucas Lecourtier
Working memory is a cognitive ability allowing the temporary storage of information to solve problems or adjust behavior. While working memory is known to mainly depend on the medial prefrontal cortex (mPFC), very few is known about how cortical information are relayed subcortically. By its connectivity, the lateral habenula (lHb) might act as a subcortical relay for cortical information. Indeed, the lHb receives inputs from several mPFC subregions, and recent findings suggest a role for the lHb in online processing of spatial information, a fundamental aspect of working memory...
October 13, 2016: Cerebral Cortex
https://www.readbyqxmd.com/read/28333356/the-safety-and-efficacy-of-controlled-ovarian-hyperstimulation-for-fertility-preservation-in-women-with-early-breast-cancer-a-systematic-review
#17
Rachael J Rodgers, Geoffrey D Reid, Juliette Koch, Rebecca Deans, William L Ledger, Michael Friedlander, Robert B Gilchrist, Kirsty A Walters, Jason A Abbott
STUDY QUESTION: Can controlled ovarian hyperstimulation (COH) for fertility preservation be effectively conducted in women with breast cancer without worsening their prognosis? SUMMARY ANSWER: COH with co-administration of letrozole suppresses oestradiol levels without significantly impacting oocyte yield or decreasing disease-free survival rates. WHAT IS KNOWN ALREADY: Oestradiol has the capacity to stimulate the proliferation of breast cancer cells...
February 27, 2017: Human Reproduction
https://www.readbyqxmd.com/read/28333341/systemic-administration-of-sialorphin-attenuates-experimental-colitis-in-mice-via-interaction-with-mu-and-kappa-opioid-receptors
#18
M Salaga, A Mokrowiecka, D Jacenik, A I Cygankiewicz, E Malecka-Panas, R Kordek, W M Krajewska, M K Sobocinska, E Kamysz, J Fichna
Background and Aims: Pharmacological treatment and/or maintenance of remission in inflammatory bowel disease (IBD) is currently one of the biggest challenges in the field of gastroenterology. Here we aimed to assess the anti-inflammatory effect and the mechanism of action of sialorphin, the natural blocker of the endogenous opioid peptide-degrading enzymes neprilysin (NEP) and aminopeptidase N (APN), in the mouse models of IBD and the changes in the expression of these enzymes in IBD patients...
March 18, 2017: Journal of Crohn's & Colitis
https://www.readbyqxmd.com/read/28333316/convergent-balancing-selection-on-the-mu-opioid-receptor-in-primates
#19
Carolyn G Sweeney, Juliette M Rando, Helen N Panas, Gregory M Miller, Donna M Platt, Eric J Vallender
The mu opioid receptor is involved in many natural processes including stress response, pleasure, and pain. Mutations in the gene also have been associated with opiate and alcohol addictions as well as with responsivity to medication targeting these disorders. Two common and mutually exclusive polymorphisms have been identified in humans, A118G (N40D), found commonly in non-African populations, and C17T (V6A), found almost exclusively in African populations. While A118G has been studied extensively for associations and in functional assays, C17T is much less well understood...
March 15, 2017: Molecular Biology and Evolution
https://www.readbyqxmd.com/read/28332884/asthma-control-in-london-secondary-school-children
#20
Katherine Harris, Gioia Mosler, Samson A Williams, Abigail Whitehouse, Rosalind Raine, Jonathan Grigg
OBJECTIVE: The asthma control test (ACT) is a validated tool for assessing control in asthmatic children aged 12 years and older. Using the ACT, we sought to assess asthma control and knowledge in London secondary school children. METHODS: Secondary schools in London, UK, participated in this study. Children with doctor-diagnosed asthma were invited to complete an online questionnaire that included the ACT and questions about asthma. Suboptimal asthma control was defined as an ACT score of ≤ 19 out of a maximum score of 25...
March 23, 2017: Journal of Asthma: Official Journal of the Association for the Care of Asthma
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