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https://www.readbyqxmd.com/read/28097916/exploring-the-first-rimonabant-analog-opioid-peptide-hybrid-compound-as-bivalent-ligand-for-cb1-and-opioid-receptors
#1
Adriano Mollica, Sveva Pelliccia, Valeria Famiglini, Azzurra Stefanucci, Giorgia Macedonio, Annalisa Chiavaroli, Giustino Orlando, Luigi Brunetti, Claudio Ferrante, Stefano Pieretti, Ettore Novellino, Sandor Benyhe, Ferenc Zador, Anna Erdei, Edina Szucs, Reza Samavati, Szalbolch Dvrorasko, Csaba Tomboly, Rino Ragno, Alexandros Patsilinakos, Romano Silvestri
Cannabinoid (CB) and opioid systems are both involved in analgesia, food intake, mood and behavior. Due to the co-localization of µ-opioid (MOR) and CB1 receptors in various regions of the central nervous system (CNS) and their ability to form heterodimers, bivalent ligands targeting to both these systems may be good candidates to investigate the existence of possible cross-talking or synergistic effects, also at sub-effective doses. In this work, we selected from a small series of new Rimonabant analogs one CB1R reverse agonist to be conjugated to the opioid fragment Tyr-D-Ala-Gly-Phe-NH2...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097485/sorption-of-organic-phosphates-and-its-effects-on-aggregation-of-hematite-nanoparticles-in-monovalent-and-bivalent-solutions
#2
Chen-Yang Xu, Jiu-Yu Li, Ren-Kou Xu, Zhi-Neng Hong
Sorption of organic phosphates-myo-inositol hexakisphosphate (IHP) and glycerol phosphate (GP) and its effects on the early stage of hematite aggregation kinetics were investigated at different pH and electrolyte composition. KH2PO4 (KP) was taken as an inorganic P source for comparison. Results indicated that for all types of P, the sorption amounts decreased with increasing solution pH. Sorption amount of IHP was almost two times that of KP, while those of GP and KP were close. Both organic P and inorganic P interacted with hematite via ligand exchange through their phosphate groups, which conveyed negative charges to mineral surface and significantly decreased the zeta potential of hematite...
January 18, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28096107/the-polio-endgame-rationale-behind-the-change-in-immunisation
#3
Julie Garon, Manish Patel
The decades long effort to eradicate polio is nearing the final stages and oral polio vaccine (OPV) is much to thank for this success. As cases of wild poliovirus continue to dwindle, cases of paralysis associated with OPV itself have become a concern. As type-2 poliovirus (one of three) has been certified eradicated and a large proportion of OPV-related paralysis is caused by the type-2 component of OPV, the World Health Assembly endorsed the phased withdrawal of OPV and the introduction of inactivated polio vaccine (IPV) into routine immunisation schedules as a crucial step in the polio endgame plan...
January 17, 2017: Archives of Disease in Childhood
https://www.readbyqxmd.com/read/28094370/probing-sub-nano-level-molecular-packing-and-correlated-positron-annihilation-characteristics-of-ionic-cross-linked-chitosan-membranes-using-positron-annihilation-spectroscopy
#4
Rui Xia, Xingzhong Cao, Meizhen Gao, Peng Zhang, Minfeng Zeng, Baoyi Wang, Long Wei
Chitosan, CS, cross-linked with bivalent palladium has shown enhanced mechanical and thermal properties depending on the transformation of the structure at a microscopic scale. In the present study, CS directly cross-linked by palladium cation membranes (CS-cr-PM) was prepared through a solution-casting method. Mobility of chitosan chains were greatly reduced after crosslinking, making a great reduction in the swelling ratio studied by a water-swelling degree measurement, which led to an improvement in molecular chain rigidity...
January 17, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28087890/overview-of-the-benefits-and-potential-issues-of-the-nonavalent-hpv-vaccine
#5
REVIEW
Luciano Mariani, Mario Preti, Paolo Cristoforoni, Carlo M Stigliano, Antonio Perino
HPV-related diseases affect anogenital and oropharyngeal regions, heavily affecting the psychosexual dimension of both male and female individuals. HPV vaccination programs based on a bivalent or quadrivalent vaccine have opened broad perspectives for primary prevention. A nonavalent HPV vaccine (9vHPV), covering nine genotypes (HPV6, HPV11, HPV16, HPV18, HPV31, HPV33, HPV45, HPV52, and HPV58), might provide further improvement in terms of direct protection. In the present report, efficacy and safety data from 9vHPV vaccine development programs are examined...
December 7, 2016: International Journal of Gynaecology and Obstetrics
https://www.readbyqxmd.com/read/28081056/guidance-for-assessment-of-poliovirus-vaccination-status-and-vaccination-of-children-who-have-received-poliovirus-vaccine-outside-the-united-states
#6
Mona Marin, Manisha Patel, Steve Oberste, Mark A Pallansch
In 1988, the World Health Assembly resolved to eradicate poliomyelitis (polio). Since then, wild poliovirus (WPV) cases have declined by >99.9%, from an estimated 350,000 cases of polio each year to 74 cases in two countries in 2015 (1). This decrease was achieved primarily through the use of trivalent oral poliovirus vaccine (tOPV), which contains types 1, 2, and 3 live, attenuated polioviruses. Since 2000, the United States has exclusively used inactivated polio vaccine (IPV), which contains all three poliovirus types (2,3)...
January 13, 2017: MMWR. Morbidity and Mortality Weekly Report
https://www.readbyqxmd.com/read/28080968/interoception-homeostatic-emotions-and-sympathovagal-balance
#7
Irina A Strigo, Arthur D Bud Craig
We briefly review the evidence for distinct neuroanatomical substrates that underlie interoception in humans, and we explain how they substantialize feelings from the body (in the insular cortex) that are conjoined with homeostatic motivations that guide adaptive behaviours (in the cingulate cortex). This hierarchical sensorimotor architecture coincides with the limbic cortical architecture that underlies emotions, and thus we regard interoceptive feelings and their conjoint motivations as homeostatic emotions We describe how bivalent feelings, emotions and sympathovagal balance can be organized and regulated efficiently in the bicameral forebrain as asymmetric positive/negative, approach/avoidance and parasympathetic/sympathetic components...
November 19, 2016: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/28078743/bivalent-14-mer-peptide-ligands-of-cxcr4-with-polyproline-linkers-with-anti-chemotactic-activity-against-jurkat-cells
#8
Tomohiro Tanaka, Toru Aoki, Wataru Nomura, Hirokazu Tamamura
Interaction of CXCR4 with its endogenous ligand, stromal-cell derived factor-1 (SDF-1)/CXCL12, induces various physiological functions involving chemotaxis. Bivalent ligands with a polyproline helix bearing a cyclic pentapeptide, FC131, were previously shown to have higher binding affinities for CXCR4 than the corresponding monovalent ligands. Bivalent ligands based on a 14-mer peptide T140 derivative with polyproline linkers have been designed and synthesized. The activity of these peptides as well as the effect of bivalency of the ligand on CXCR4 binding has been assessed...
January 12, 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/28073847/identification-of-ccr2-and-cd180-as-robust-pharmacodynamic-tumor-and-blood-biomarkers-for-clinical-use-with-brd4-bet-inhibitors
#9
Tammie C Yeh, Greg O'Connor, Philip Petteruti, Austin Dulak, Maureen Hattersley, J Carl Barrett, Huawei Chen
PURPOSE: AZD5153 is a novel BRD4/BET inhibitor with a distinctive bivalent bromodomain binding mode. To support its clinical development, we identified pharmacodynamic (PD) biomarkers for use in clinical trials to establish target engagement. EXPERIMENTAL DESIGN: CCR2 and CD180 mRNAs, initially identified from whole transcriptome profiling, were further evaluated by quantitative PCR in hematologic cell lines, xenografts, and whole blood from rat, healthy volunteers, and patients with cancer...
January 10, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28069692/genes-involved-in-development-and-differentiation-are-commonly-methylated-in-cancers-derived-from-multiple-organs-a-single-institutional-methylome-analysis-using-1007-tissue-specimens
#10
Kentaro Ohara, Eri Arai, Yoriko Takahashi, Nanako Ito, Ayako Shibuya, Koji Tsuta, Ryoji Kushima, Hitoshi Tsuda, Hidenori Ojima, Hiroyuki Fujimoto, Shun-Ichi Watanabe, Hitoshi Katai, Takayuki Kinoshita, Tatsuhiro Shibata, Takashi Kohno, Yae Kanai
The aim of this study was to clarify the significance of DNA methylation alterations shared by cancers derived from multiple organs. We analyzed single-institutional methylome data by single-CpG-resolution Infinium assay for 1,007 samples of non-cancerous tissue (N) and corresponding cancerous tissue (T) obtained from lung, stomach, kidney, breast and liver. Principal component analysis revealed that N samples of each organ showed distinct DNA methylation profiles, DNA methylation profiles of N samples of each organ being inherited by the corresponding T samples and DNA methylation profiles of T samples being more similar to those of N samples in the same organ than those of T samples in other organs...
January 9, 2017: Carcinogenesis
https://www.readbyqxmd.com/read/28067257/enhanced-tumor-targeting-selectivity-by-modulating-bispecific-antibody-binding-affinity-and-format-valence
#11
Yariv Mazor, Kris F Sachsenmeier, Chunning Yang, Anna Hansen, Jessica Filderman, Kathy Mulgrew, Herren Wu, William F Dall'Acqua
Bispecific antibodies are considered attractive bio-therapeutic agents owing to their ability to target two distinct disease mediators. Cross-arm avidity targeting of antigen double-positive cancer cells over single-positive normal tissue is believed to enhance the therapeutic efficacy, restrict major escape mechanisms and increase tumor-targeting selectivity, leading to reduced systemic toxicity and improved therapeutic index. However, the interplay of factors regulating target selectivity is not well understood and often overlooked when developing clinically relevant bispecific therapeutics...
January 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28065582/bivalent-flagellin-immunotherapy-protects-mice-against-pseudomonas-aeruginosa-infections-in-both-acute-pneumonia-and-burn-wound-models
#12
Hosein Ahmadi, Bahador Behrouz, Gholamreza Irajian, Nour Amirmozafari, Sara Naghavi
Pseudomonas aeruginosa infections are a serious challenge to therapy because of the complex pathogenesis and paucity of new effective antibiotics, thus renewing interest in antibody-based therapeutic strategies. Immunotherapy strategies typically target selected virulence factors that are expressed by the majority of clinical strains of P. aeruginosa, particularly because virulence factors mediate infection. Type a and b flagellins (flagellin a+b) of P. aeruginosa are acute virulence factors that play a major role in the establishment of infection...
January 5, 2017: Biologicals: Journal of the International Association of Biological Standardization
https://www.readbyqxmd.com/read/28056824/the-emerging-landscape-of-dynamic-dna-methylation-in-early-childhood
#13
Cheng-Jian Xu, Marc Jan Bonder, Cilla Söderhäll, Mariona Bustamante, Nour Baïz, Ulrike Gehring, Soesma A Jankipersadsing, Pieter van der Vlies, Cleo C van Diemen, Bianca van Rijkom, Jocelyne Just, Inger Kull, Juha Kere, Josep Maria Antó, Jean Bousquet, Alexandra Zhernakova, Cisca Wijmenga, Isabella Annesi-Maesano, Jordi Sunyer, Erik Melén, Yang Li, Dirkje S Postma, Gerard H Koppelman
BACKGROUND: DNA methylation has been found to associate with disease, aging and environmental exposure, but it is unknown how genome, environment and disease influence DNA methylation dynamics in childhood. RESULTS: By analysing 538 paired DNA blood samples from children at birth and at 4-5 years old and 726 paired samples from children at 4 and 8 years old from four European birth cohorts using the Illumina Infinium Human Methylation 450 k chip, we have identified 14,150 consistent age-differential methylation sites (a-DMSs) at epigenome-wide significance of p < 1...
January 5, 2017: BMC Genomics
https://www.readbyqxmd.com/read/28053902/human-papilloma-virus-in-oral-cancer
#14
REVIEW
Soung Min Kim
Cervical cancer is the second most prevalent cancer among women, and it arises from cells that originate in the cervix uteri. Among several causes of cervical malignancies, infection with some types of human papilloma virus (HPV) is well known to be the greatest cervical cancer risk factor. Over 150 subtypes of HPV have been identified; more than 40 types of HPVs are typically transmitted through sexual contact and infect the anogenital region and oral cavity. The recently introduced vaccine for HPV infection is effective against certain subtypes of HPV that are associated with cervical cancer, genital warts, and some less common cancers, including oropharyngeal cancer...
December 2016: Journal of the Korean Association of Oral and Maxillofacial Surgeons
https://www.readbyqxmd.com/read/28053505/spotlight-on-the-9-valent-hpv-vaccine
#15
REVIEW
Pier Luigi Lopalco
Starting in 2006, vaccination against human papillomavirus (HPV) has been progressively implemented in most developed countries. Two vaccines have been successfully used, a bivalent vaccine targeting HPV-related cancers (bHPV) and a quadrivalent vaccine (qHPV) targeting both HPV-related cancers and genital warts. Between December 2014 and June 2015, a new nonavalent HPV vaccine (9vHPV) was granted marketing authorization in the USA and Europe. The 9vHPV was developed from the qHPV and includes five additional HPV types that should increase the level of protection toward HPV-related cancers...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28051346/a-conjugate-of-two-tpa-binding-rna-aptamers-efficiently-inhibits-fibrinolysis
#16
Nils Bjerregaard, Daniel M Dupont, Peter A Andreasen
Uncontrolled bleeding is a major cause of mortality. Lysine analogues are routinely used in the management of bleeding, but several studies indicate a risk of serious detrimental effects upon their administration. In this study, we report a bivalent conjugate "3218" of two RNA aptamers selected for binding to the serine protease tissue-type plasminogen activator (tPA), the principal initiator of fibrinolysis in mammals. The constituent monomeric aptamers, K32v2 and K18v2, were previously demonstrated to weakly inhibit fibrinolysis...
January 4, 2017: Nucleic Acid Therapeutics
https://www.readbyqxmd.com/read/28050945/a-novel-poly-ligand-exchanger-cu-%C3%A2-loaded-chelating-resin-for-the-removal-of-ammonia-nitrogen-in-aqueous-solutions
#17
Quanzhou Chen, Kanggen Zhou, Yan Chen, Aihe Wang, Fang Liu
In this paper, A poly ligand exchanger (PLE), Cu(II)-loaded chelating resin bearing the functional group of weak iminodiacetate acid was prepared to efficiently remove ammonia from solutions. Batch adsorption equilibrium experiments were conducted under a range of conditions to determine the optimum adsorption conditions. The effects of contact time, pH, resin dosage and temperature on the removal of ammonia by Cu(II)-loaded resin were determined. The maximum removal efficiency was reached at pH 9.5 at room temperature 25°C in 300min...
January 4, 2017: Environmental Technology
https://www.readbyqxmd.com/read/28043046/mechanisms-of-microbial-community-structure-and-biofouling-shifts-under-multivalent-cations-stress-in-membrane-bioreactors
#18
Yu Miao, Xuechao Guo, Wei Jiang, Xu-Xiang Zhang, Bing Wu
Five lab-scale membrane bioreactors (MBRs) were continuously operated to investigate the mechanisms and linkages of the microbial community and membrane fouling with trivalent metal cations (Fe(III) and Al(III)) and bivalent metal cations (Ca(II) and Mg(II)) shock loads. COD and NH4(+)-N removals showed recovery trends along with treatment process in the presence of metals. Trivalent metal cations reduced trans-membrane pressure (TMP) as well as fouling rate (dTMP/dt) and extended membrane module replacement period by binding activated sludge extracellular polymeric substance (EPS) and effluent soluble microbial product (SMP) productions...
December 19, 2016: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/28042336/bivalent-brain-shuttle-increases-antibody-uptake-by-monovalent-binding-to-the-transferrin-receptor
#19
Greta Hultqvist, Stina Syvänen, Xiaotian T Fang, Lars Lannfelt, Dag Sehlin
The blood-brain barrier (BBB) is an obstacle for antibody passage into the brain, impeding the development of immunotherapy and antibody-based diagnostics for brain disorders. In the present study, we have developed a brain shuttle for active transport of antibodies across the BBB by receptor-mediated transcytosis. We have thus recombinantly fused two single-chain variable fragments (scFv) of the transferrin receptor (TfR) antibody 8D3 to the light chains of mAb158, an antibody selectively binding to Aβ protofibrils, which are involved in the pathogenesis of Alzheimer's disease (AD)...
2017: Theranostics
https://www.readbyqxmd.com/read/28042137/immunogenicity-and-safety-of-human-papillomavirus-hpv-vaccination-in-asian-populations-from-six-countries-a-meta-analysis
#20
Didik Setiawan, Jos Luttjeboer, Koen B Pouwels, Jan C Wilschut, Maarten J Postma
Cervical cancer is a serious public-health problem in Asian countries. Since human papillomavirus (HPV) infection is the main risk factor for cervical cancer, HPV vaccination is considered a promising strategy to prevent cervical cancer. However, comprehensive immunogenicity and safety information for Asian populations is lacking. We searched four electronic databases including PubMed, EMBASE, Cochrane Library, and clinicaltrials.gov. We reviewed selected manuscripts and extracted the pooled relative risk (RR) from immunogenicity and safety information on HPV vaccination among women in Asian countries...
January 1, 2017: Japanese Journal of Clinical Oncology
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