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https://www.readbyqxmd.com/read/29334656/activated-protein-c-suppresses-osteoclast-differentiation-via-endothelial-protein-c-receptor-protease-activated-receptor-1-sphingosine-1-phosphate-receptor-and-apolipoprotein-e-receptor-2
#1
Kakunoshin Yoshida, Nobuyuki Akita, Takayuki Okamoto, Kunihiro Asanuma, Atsumasa Uchida, Akihiro Sudo, Motomu Shimaoka, Koji Suzuki, Tatsuya Hayashi
INTRODUCTION: Bone remodeling relies on a delicate balance between formation and resorption of bone tissues, processes in which bone-forming osteoblasts and bone-resorbing osteoclasts play central roles. Recently, we reported that anticoagulant activated protein C (APC) promotes osteoblast proliferation, but the role of the blood coagulation system in bone remodeling remains unclear. In this study, to further elucidate the relationship between bone remodeling and blood coagulation, we investigated the effect of APC on osteoclast differentiation...
January 3, 2018: Thrombosis Research
https://www.readbyqxmd.com/read/29334372/pharmacological-blockade-of-asct2-dependent-glutamine-transport-leads-to-antitumor-efficacy-in-preclinical-models
#2
Michael L Schulte, Allie Fu, Ping Zhao, Jun Li, Ling Geng, Shannon T Smith, Jumpei Kondo, Robert J Coffey, Marc O Johnson, Jeffrey C Rathmell, Joe T Sharick, Melissa C Skala, Jarrod A Smith, Jordan Berlin, M Kay Washington, Michael L Nickels, H Charles Manning
The unique metabolic demands of cancer cells underscore potentially fruitful opportunities for drug discovery in the era of precision medicine. However, therapeutic targeting of cancer metabolism has led to surprisingly few new drugs to date. The neutral amino acid glutamine serves as a key intermediate in numerous metabolic processes leveraged by cancer cells, including biosynthesis, cell signaling, and oxidative protection. Herein we report the preclinical development of V-9302, a competitive small molecule antagonist of transmembrane glutamine flux that selectively and potently targets the amino acid transporter ASCT2...
January 15, 2018: Nature Medicine
https://www.readbyqxmd.com/read/29334275/laparoscopic-ovarian-drilling-versus-gnrh-antagonist-combined-with-cabergoline-as-a-prophylaxis-against-the-re-development-of-ovarian-hyperstimulation-syndrome
#3
Emaduldin Seyam, Enas Hefzy
OBJECTIVE: The aim of this work was to investigate the value of laparoscopic ovarian drilling (LOD) compared with GnRH antagonist flexible protocol combined with cabergoline (Cb), as a prophylaxis against the re-development of ovarian hyperstimulation syndrome (OHSS) in women with clomiphene citrate-resistant polycystic ovary disease (CCR-PCOD) who had severe OHSS before in a previous ICSI cycle. STUDY DESIGN: It is a prospective controlled study, where 250 CCR-PCOD women (n = 250) with a history of severe OHSS before, had been recruited for the study...
January 15, 2018: Gynecological Endocrinology
https://www.readbyqxmd.com/read/29333938/structure-based-engineering-to-restore-high-affinity-binding-of-an-isoform-selective-anti-tgf%C3%AE-1-antibody
#4
Dana M Lord, Julie J Bird, Denise M Honey, Annie Best, Anna Park, Ronnie R Wei, Huawei Qiu
Metelimumab (CAT192) is a human IgG4 monoclonal antibody developed as a TGFβ1-specific antagonist. It was tested in clinical trials for the treatment of scleroderma but later terminated due to lack of efficacy. Subsequent characterization of CAT192 indicated that its TGFβ1 binding affinity was reduced by ∼50-fold upon conversion from the parental single-chain variable fragment (scFv) to IgG4. We hypothesized this result was due to decreased conformational flexibility of the IgG that could be altered via engineering...
January 15, 2018: MAbs
https://www.readbyqxmd.com/read/29333669/blood-pressure-and-goal-titration-of-neurohormonal-antagonists-the-tortoise-wins-again
#5
EDITORIAL
Hector O Ventura, Mandeep R Mehra
No abstract text is available yet for this article.
January 15, 2018: European Journal of Heart Failure
https://www.readbyqxmd.com/read/29333613/pharmacokinetics-pharmacodynamics-and-clinical-use-of-trazodone-and-its-active-metabolite-m-chlorophenylpiperazine-in-the-horse
#6
J L Davis, J Schirmer, E Medlin
Trazodone is a serotonin receptor antagonist and reuptake inhibitor used extensively as an anxiolytic in human and small animal veterinary medicine. The aims of this study were to determine the pharmacokinetics of oral trazodone in experimental horses and to evaluate the effect of oral trazodone in clinical horses. Six experimental horses were administered trazodone at 7.5 or 10 mg/kg. Plasma concentrations of trazodone and its metabolite (m-CPP) were determined via UPLC-MS/MS. Noncompartmental pharmacokinetic analysis, sedation and ataxia scores were determined...
January 14, 2018: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29333402/interleukin-1b-il-1b-31-and-il-1b-511-and-interleukin-1-receptor-antagonist-il-1ra-gene-polymorphisms-in-primary-immune-thrombocytopenia
#7
Deependra Kumar Yadav, Anil Kumar Tripathi, Divya Gupta, Saurabh Shukla, Aloukick Kumar Singh, Ashutosh Kumar, Jyotsna Agarwal, K N Prasad
Background: Immune thrombocytopenia (ITP) is an immune-mediated disease caused by autoantibodies against platelets membrane glycoproteins GPIIb/IIIa and GPIb/IX. The etiology of ITP remains unclear. This study evaluated the association of polymorphisms in interleukin (IL)-1B-31, IL-1B-511, and IL-1Ra with ITP. Methods: Genotyping of IL-1B-31, IL-1B-511, and IL-1Ra was performed in 118 ITP patients and 100 controls by polymerase chain reaction restriction fragment length polymorphism and detection of variable number tandem repeats...
December 2017: Blood Research
https://www.readbyqxmd.com/read/29333091/in-vitro-and-in-vivo-effects-of-mirna-19b-20a-92a-on-gastric-cancer-stem-cells-and-the-related-mechanism
#8
Qianwen Shao, Jing Xu, Xin Guan, Bing Zhou, Wei Wei, Rong Deng, Dongzhen Li, Xinyu Xu, Haitao Zhu
We aimed to analyze the in vitro and in vivo effects of miRNA-19b/20a/92a on gastric cancer stem cells (GCSCs) and the related mechanism. GCSCs were cultured until adherence and differentiation, and subjected to miRNA microarray analysis to find and to verify miRNA deletion. Cells stably expressing lentivirus carrying miRNA-19b/20a/92a were constructed by transfection. The relationship between miRNA-19b/20a/92a and renewal of GCSCs was studied by the tumor sphere assay, and that between miRNA-19b/20a/92a and their proliferation was explored with MTT and colony formation assays...
2018: International Journal of Medical Sciences
https://www.readbyqxmd.com/read/29332977/the-role-of-wnt-signalling-in-angiogenesis
#9
REVIEW
Jun Jun Olsen, Sebastian Öther-Gee Pohl, Abhijeet Deshmukh, Malini Visweswaran, Natalie C Ward, Frank Arfuso, Mark Agostino, Arun Dharmarajan
Angiogenesis is a normal biological process wherein new blood vessels form from the growth of pre-existing blood vessels. Preventing angiogenesis in solid tumours by targeting pro-angiogenic factors including vascular endothelial growth factor (VEGF), angiopoietin-1 (Ang-1), basic fibroblast growth factor (bFGF), hepatocyte growth factor, and platelet-derived growth factor (PDGF) is currently under investigation for cancer treatment. Concurrently targeting the cell signalling pathways involved in the transcriptional and post-translational regulation of these factors may provide positive therapeutic results...
November 2017: Clinical Biochemist. Reviews
https://www.readbyqxmd.com/read/29332567/nociceptin-orphanin-fq-peptide-nop-receptor-modulators-an-update-in-structure-activity-relationships
#10
Carlo Mustazza, Stefano Pieretti, Francesca Marzoli
Nociceptin /Orphanin FQ Peptide" receptor (NOPr) is a G-protein-coupled receptor with the nociceptin/orphanin FQ peptide (N/OFQ) as endogenous agonist. It is expressed in the nervous system as well as in some non-neural tissues. Its activation has pronociceptive effect at the supraspinal level, whereas at the spinal level it produces nociceptive effects at low doses and antinociceptive effects at higher doses. NOPr is also involved in mood and blood pressure regulation, immunoregulation, airway constriction, feeding, urination, bowel motility, learning and memory...
January 10, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29332354/inhibition-of-telomerase-potentiates-enzalutamide-efficiency-of-androgen-sensitive-human-prostate-cancer-cells
#11
Karaca Kaan Gecgel, Mustafa Muduroglu, Suat Erdogan
PURPOSE: Androgen deprivation therapy (ADT) is one of the main strategies to treat prostate cancer (PCa) at various stages of its development. Androgen receptor (AR) antagonists such as enzalutamide are mainstay treatments for castration-sensitive prostate cancer. Though, a majority of patients initially respond to ADT, most will eventually progress to castrate-resistant, due to the development of different mutations on the AR. PCa cells express high telomerase activity, and there is a correlation between the total activity of telomerase and the Gleason score...
November 2017: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
https://www.readbyqxmd.com/read/29332256/dopamine-dependent-social-information-processing-in-non-human-primates
#12
Young-A Lee, Sarah Lionnet, Akemi Kato, Yukiori Goto
RATIONALE: Dopamine (DA) is a neurotransmitter whose roles have been suggested in various aspects of brain functions. Recent studies in rodents have reported its roles in social function. However, how DA is involved in social information processing in primates has largely remained unclear. OBJECTIVES: We investigated prefrontal cortical (PFC) activities associated with social vs. nonsocial visual stimulus processing. METHODS: Near-infrared spectroscopy (NIRS) was applied to Japanese macaques, along with pharmacological manipulations of DA transmission, while they were gazing at social and nonsocial visual stimuli...
January 14, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29332129/aspergillus-fumigatus-increased-par-2-expression-and-elevated-proinflammatory-cytokines-expression-through-the-pathway-of-par-2-erk1-2-in-cornea
#13
Yawen Niu, Guiqiu Zhao, Cui Li, Jing Lin, Nan Jiang, Chengye Che, Jie Zhang, Qiang Xu
Purpose: To determine the role of protease-activated receptor-2 (PAR-2) in cornea infected by Aspergillus fumigatus. Methods: PAR-2 was tested in normal and infected corneas of C57BL/6 mice. Mice corneas were infected with A. fumigatus with or without pretreatment of PAR-2 antagonist (FSLLRY-NH2). Polymorphonuclear neutrophilic leukocytes (PMNs) were stimulated with 75% ethanol-killed A. fumigatus with or without pretreatment of FSLLRY-NH2. Disease severity was documented by clinical score and photographs with a slit lamp...
January 1, 2018: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/29332054/dementia-and-atrial-fibrillation-a-dangerous-combination-for-ischemic-stroke-and-mortality
#14
Daniele Pastori, Kazuo Miyazawa, Gregory Y H Lip
The risk of developing dementia is increased in patients with atrial fibrillation (AF), with the incidence of both conditions increasing with aging. Patients with dementia frequently do not receiving adequate thrombo-prophylaxis, because of the inability to monitor INR and/or to achieve and maintain good compliance with anticoagulant treatment. Under-treatment is therefore an important contributor to the increased risk of ischemic stroke and mortality in this subgroup of AF patients. In newly-diagnosed patients with AF starting oral anticoagulation, the presence of cognitive impairment should be considered in addition to the calculation of the SAMe-TT2R2 score, as part of an integrated decision management pathway to choose the most appropriate oral anticoagulant [i...
2018: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/29332033/effect-of-dual-tasking-on-anticipatory-and-compensatory-postural-adjustments-in-response-to-external-perturbations-in-individuals-with-nonspecific-chronic-low-back-pain-electromyographic-analysis
#15
Ladan Hemmati, Soraya Piroozi, Zahra Rojhani-Shirazi
BACKGROUND: In patients with chronic low back pain (CLBP), postural control is a demanding task in terms of attention. Although the attentional demands of postural control have been investigated in these patients, the attentional demands of postural recovery during dual task performance have not been evaluated in patients with nonspecific CLBP. OBJECTIVE: To investigate the effect of dual tasking on anticipatory and compensatory postural adjustments in response to an external perturbation in patients with nonspecific CLBP...
December 29, 2017: Journal of Back and Musculoskeletal Rehabilitation
https://www.readbyqxmd.com/read/29331969/temporal-trends-in-antithrombotic-treatment-of-real-world-uk-patients-with-newly-diagnosed-atrial-fibrillation-findings-from-the-garfield-af-registry
#16
Patricia N Apenteng, Haiyan Gao, Fd Richard Hobbs, David A Fitzmaurice
OBJECTIVE: To investigate evolving patterns in antithrombotic treatment in UK patients with newly diagnosed non-valvular atrial fibrillation (AF). DESIGN: Prospective, multicentre, international registry. SETTING: 186 primary care practices in the UK. PARTICIPANTS: 3482 participants prospectively enrolled in four sequential cohorts (cohort 2 (C2) n=830, diagnosed September 2011 to April 2013; cohort 3 (C3) n=902, diagnosed April 2013 to June 2014; cohort 4 (C4) n=850, diagnosed July 2014 to June 2015; cohort 5 (C5) n=900, diagnosed June 2015 to July 2016)...
January 13, 2018: BMJ Open
https://www.readbyqxmd.com/read/29331963/response-to-standard-dose-of-ustekinumab-for-childhood-onset-deficiency-of-interleukin-36-receptor-antagonist-by-cherqaoui-et-al
#17
Nadia Bonekamp, Roberta Caorsi, Joost Frenkel, Marco Gattorno
No abstract text is available yet for this article.
January 13, 2018: Annals of the Rheumatic Diseases
https://www.readbyqxmd.com/read/29331922/minimum-alveolar-concentration-key-concepts-and-a-review-of-its-pharmacological-reduction-in-dogs-part-1
#18
REVIEW
Rachel Reed, Thomas Doherty
OBJECTIVE: To outline the major components of the minimum alveolar concentration (MAC) and review the literature in regard to pharmacological manipulation of the MAC of halothane, isoflurane, sevoflurane, enflurane, and desflurane in dogs. The pharmacologic agents included are alpha-2 agonists, benzodiazepines, propofol, maropitant, opioids, lidocaine, acepromazine, non-steroidal anti-inflammatory agents, and NMDA antagonists. Part 1 will focus on summarizing the relevance, measurement, and mechanisms of MAC and review the effects of alpha-2 agonists, benzodiazepines, and propofol on MAC...
January 9, 2018: Research in Veterinary Science
https://www.readbyqxmd.com/read/29331804/toll-like-receptor-9-antagonist-suppresses-humoral-immunity-in-experimental-autoimmune-myasthenia-gravis
#19
Peng Zhang, Chun-Lin Yang, Ru-Tao Liu, Heng Li, Min Zhang, Na Zhang, Long-Tao Yue, Cong-Cong Wang, Ying-Chun Dou, Rui-Sheng Duan
Recent studies have demonstrated the important role of toll-like receptor 9 (TLR9) signalling in autoimmune diseases, but its role in myasthenia gravis (MG) has not been fully established. We show herein that blocking TLR9 signalling via the suppressive oligodeoxynucleotide (ODN) H154 alleviated the symptoms of experimental autoimmune myasthenia gravis (EAMG). With the downregulation of dendritic cells (DCs), TLR9 interruption reduced follicular helper T cells (Tfh) and germinal centre (GC) B cells, leading to decreased antibody production...
January 11, 2018: Molecular Immunology
https://www.readbyqxmd.com/read/29331800/nucleus-accumbens-mu-opioid-receptors-regulate-context-specific-social-preferences-in-the-juvenile-rat
#20
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
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