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https://www.readbyqxmd.com/read/29779181/tailoring-acyclovir-prodrugs-with-enhanced-antiviral-activity-rational-design-synthesis-human-plasma-stability-and-in-vitro-evaluation
#1
Radoslav L Chayrov, Evgenios K Stylos, Maria V Chatziathanasiadou, Kiril N Chuchkov, Aleksandra I Tencheva, Androniki D Kostagianni, Tsenka S Milkova, Assia L Angelova, Angel S Galabov, Stoyan A Shishkov, Daniel G Todorov, Andreas G Tzakos, Ivanka G Stankova
Bile acid prodrugs have served as a viable strategy for refining the pharmaceutical profile of parent drugs through utilizing bile acid transporters. A series of three ester prodrugs of the antiherpetic drug acyclovir (ACV) with the bile acids cholic, chenodeoxycholic and deoxycholic were synthesized and evaluated along with valacyclovir for their in vitro antiviral activity against herpes simplex viruses type 1 and type 2 (HSV-1, HSV-2). The in vitro antiviral activity of the three bile acid prodrugs was also evaluated against Epstein-Barr virus (EBV)...
May 19, 2018: Amino Acids
https://www.readbyqxmd.com/read/29779159/an-etiological-approach-to-sexual-offender-assessment-case-formulation-incorporating-risk-assessment-cafira
#2
REVIEW
Leam A Craig, Martin Rettenberger
PURPOSE OF REVIEW: Case formulations (CF) have been the cornerstone of effective practice in clinical psychology since the 1950s and now form one of the core competencies in clinical and forensic assessment. The use of CFs within forensic settings is becoming more relevant when working with offenders who have experienced significant trauma, suffered from personality disorder, and have displayed sexually abusive behavior. Furthermore, most North American and European jurisdictions insist that expert witnesses adopt an idiosyncratic approach to risk assessment and consider the characteristics of the individual as part of a wider formulation of the problem behavior...
May 19, 2018: Current Psychiatry Reports
https://www.readbyqxmd.com/read/29779156/adolescent-isolation-rearing-produces-a-prepulse-inhibition-deficit-correlated-with-expression-of-the-nmda-glun1-subunit-in-the-nucleus-accumbens
#3
Megan L Fitzgerald, Virginia M Pickel
Adolescence is a transition period during which social interaction is necessary for normal brain and behavior development. Severely abnormal social interactions during adolescence can increase the incidence of lifelong psychiatric disease. Decreased prepulse inhibition (PPI) is a quantifiable hallmark of some psychiatric illnesses in humans and can be elicited in rodents by isolation rearing throughout the adolescent transition period. PPI is a measure of sensorimotor gating in which the nucleus accumbens (Acb) is crucially involved...
May 19, 2018: Brain Structure & Function
https://www.readbyqxmd.com/read/29779150/disorienting-dilemmas-the-significance-of-resistance-and-disturbance-in-an-intercultural-program-within-kindergarten-teacher-education
#4
Åsta Birkeland, Siv Ødemotland
As the Norwegian society, and thereby the kindergartens, have become more multicultural, the need for cultivating teachers capable of operating in an ever diversified and global world is highlighted as an important educational strategy within teacher education. The purpose of the specific intercultural program in kindergarten teacher education discussed in this article refers to competences needed as a professional teacher in a multicultural kindergarten. Teachers often have various assumptions and beliefs taken for granted...
May 19, 2018: Integrative Psychological & Behavioral Science
https://www.readbyqxmd.com/read/29779098/stability-of-chromatin-remodeling-complex-subunits-is-determined-by-their-phosphorylation-status
#5
A M Azieva, A A Sheinov, F A Galkin, S G Georgieva, N V Soshnikova
It was found that, in the differentiated cells of mouse brain, the level of core (Brg1 and BAF155) and specific (BRD7, BAF180, and PHF10) subunits of the chromatin-remodeling complex PBAF is reduced compared to the undifferentiated proliferating cells. Phosphorylation of PBAF complex subunits is required for maintaining their stability in differentiated brain cells.
March 2018: Doklady. Biochemistry and Biophysics
https://www.readbyqxmd.com/read/29778963/ph-dependent-silica-nanoparticle-dissolution-and-cargo-release
#6
Giorgia Giovaninni, Colin J Moore, Andrew J Hall, Hugh J Byrne, Vladimir Gubala
The dissolution of microporous silica nanoparticles (NP) in aqueous environments of different biologically relevant pH was studied in order to assess their potential as drug delivery vehicles. Silica NPs, loaded with fluorescein, were prepared using different organosilane precursors (tetraethoxysilane, ethyl triethoxysilane or a 1:1 molar ratio of both) and NP dissolution was evaluated in aqueous conditions at pH 4, pH 6 and pH 7.4. These conditions correspond to the acidity of the intracellular environment (late endosome, early endosome, cytosol respectively) and gastrointestinal tract ('fed' stomach, duodenum and jejunum respectively)...
May 16, 2018: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29778960/rapid-colorimetric-detection-of-p53-protein-function-using-dna-gold-nanoconjugates-with-applications-for-drug-discovery-and-cancer-diagnostics
#7
Enock Assah, Walter Goh, Xin Ting Zheng, Ting Xiang Lim, Jun Li, David Lane, Farid Ghadessy, Yen Nee Tan
The tumor suppressor protein p53 plays a central role in preventing cancer through interaction with DNA response elements (REs) to regulate target gene expression in cells. Due to its significance in cancer biology, relentless efforts have been directed toward understanding p53-DNA interactions for the development of cancer therapeutics and diagnostics. In this paper, we report a rapid, label-free and versatile colorimetric assay to detect wildtype p53 DNA-binding function in complex solutions. The assay design is based on a concept that alters interparticle-distances between RE-AuNPs from a crosslinking effect induced through tetramerization of wildtype p53 protein (p53-WT) upon binding to canonical DNA motifs modified on gold nanoparticles (RE-AuNPs)...
May 5, 2018: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29778947/dissociable-contributions-of-dorsal-and-ventral-striatal-regions-on-a-rodent-cost-benefit-decision-making-task-requiring-cognitive-effort
#8
Mason M Silveira, Melanie Tremblay, Catharine A Winstanley
Cognitive effort is a ubiquitous process, yet surprisingly little is known about the brain mechanisms responsible for evaluating it. Here, we utilize the rat Cognitive Effort Task (rCET) to probe the striatum's role in deciding between options that vary in the amount of cognitive effort required for success. In the rCET, animals choose to perform either an easy trial, in which the attentional demand is low but the potential reward is small, or a difficult trial which is more attentionally demanding but can yield twice the sugar pellets...
April 24, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29778924/cerbera-odollam-toxicity-a-review
#9
REVIEW
Ritesh G Menezes, Muhammad Shariq Usman, Syed Ather Hussain, Mohammed Madadin, Tariq Jamal Siddiqi, Huda Fatima, Pradhum Ram, Syed Bilal Pasha, S Senthilkumaran, Tooba Qadir Fatima, Sushil Allen Luis
Cerbera odollam is a plant species of the Apocynaceae family. It is often dubbed the 'suicide tree' due to its strong cardiotoxic effects, which make it a suitable means to attempt suicide. The plant grows in wet areas in South India, Madagascar, and Southeast Asia; and its common names include Pong-Pong and Othalanga. The poison rich part of the plant is the kernel which is present at the core of its fruit. The bioactive toxin in the plant is cerberin, which is a cardiac glycoside of the cardenolide class...
May 9, 2018: Journal of Forensic and Legal Medicine
https://www.readbyqxmd.com/read/29778899/dopamine-loss-alters-the-hippocampus-nucleus-accumbens-synaptic-transmission-in-the-tg2576-mouse-model-of-alzheimer-s-disease
#10
Alberto Cordella, Paraskevi Krashia, Annalisa Nobili, Annabella Pignataro, Livia La Barbera, Maria Teresa Viscomi, Alessandro Valzania, Flavio Keller, Martine Ammassari-Teule, Nicola Biagio Mercuri, Nicola Berretta, Marcello D'Amelio
The functional loop involving the ventral tegmental area (VTA), dorsal hippocampus and nucleus accumbens (NAc) plays a pivotal role in the formation of spatial memory and persistent memory traces. In particular, the dopaminergic innervation from the VTA to the hippocampus is critical for hippocampal-related memory function and alterations in the midbrain dopaminergic system are frequently reported in Alzheimer's disease (AD), contributing to age-related decline in memory and non-cognitive functions. However, much less is known about the hippocampus-NAc connectivity in AD...
May 17, 2018: Neurobiology of Disease
https://www.readbyqxmd.com/read/29778875/purification-of-recombinant-trichodysplasia-spinulosa-associated-polyomavirus-vp1-derived-virus-like-particles-using-chromatographic-techniques
#11
Mindaugas Zaveckas, Karolis Goda, Danguole Ziogiene, Alma Gedvilaite
Trichodysplasia spinulosa-associated polyomavirus (TSPyV) has been linked to a rare and recently characterized skin disease occurring in immunocompromised patients. In analogy with other polyomaviruses, the major capsid protein VP1 of TSPyV can self-assemble into virus-like particles (VLPs). VLPs are increasingly applied for the vaccination and diagnostics. Mostly, non-scalable and labor intensive ultracentrifugation-based techniques are used for the purification of VLPs. In this work, we developed a purification procedure for TSPyV VP1 VLPs based on two chromatographic steps, ion-exchange monolith and core bead chromatography...
May 9, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29778856/single-versus-standard-multiview-assessment-of-global-longitudinal-strain-for-the-diagnosis-of-cardiotoxicity-during-cancer-therapy
#12
Paaladinesh Thavendiranathan, Tomoko Negishi, Marc-Andre Coté, Martin Penicka, Richard Massey, Goo-Yeong Cho, Krassimira Hristova, Dragos Vinereanu, Bogdan A Popescu, Masaki Izumo, Kazuaki Negishi, Thomas H Marwick
OBJECTIVES: The goal of this study was to compare echocardiographic measurements of global longitudinal strain (GLS) (using 3 apical views) with single-view longitudinal strain (LS, 4- or 2-chamber [4CV_LS and 2CV_LS, respectively]) for detection of cancer-therapy related cardiotoxicity. BACKGROUND: GLS is useful for the detection of cardiotoxicity, but the need for repeated measurements poses a significant burden on busy echocardiography laboratories. A single-view LS measurement, possibly at point of care, could improve efficiency...
May 11, 2018: JACC. Cardiovascular Imaging
https://www.readbyqxmd.com/read/29778853/natural-history-of-diabetic-coronary-atherosclerosis-by-quantitative-measurement-of-serial-coronary-computed-tomographic-angiography-results-of-the-paradigm-study-progression-of-atherosclerotic-plaque-determined-by-computed-tomographic-angiography-imaging
#13
Ung Kim, Jonathon A Leipsic, Stephanie L Sellers, Michael Shao, Philipp Blanke, Martin Hadamitzky, Yong-Jin Kim, Edoardo Conte, Daniele Andreini, Gianluca Pontone, Matthew J Budoff, Ilan Gottlieb, Byoung Kwon Lee, Eun Ju Chun, Filippo Cademartiri, Erica Maffei, Hugo Marques, Sanghoon Shin, Jung Hyun Choi, Renu Virmani, Habib Samady, Peter H Stone, Daniel S Berman, Jagat Narula, Leslee J Shaw, Jeroen J Bax, James K Min, Hyuk-Jae Chang
OBJECTIVES: This study aimed to determine the rate and extent of plaque progression (PP), changes in plaque features, and clinical predictors of PP in patients with diabetes mellitus (DM). BACKGROUND: The natural history of coronary PP in patients with DM is not well established. METHODS: A total of 1,602 patients (age 61.3 ± 9.0 years; 60.3% men; median scan interval 3.8 years) who underwent serial coronary computed tomography angiography over a period of at least 24 months were enrolled and analyzed from the PARADIGM (Progression of Atherosclerotic Plaque Determined by Computed Tomographic Angiography Imaging) trial...
May 11, 2018: JACC. Cardiovascular Imaging
https://www.readbyqxmd.com/read/29778824/-gel-in-core-carbosomes-as-novel-ophthalmic-vehicles-with-enhanced-corneal-permeation-and-residence
#14
Mona A Moustafa, Wessam M El-Refaie, Yosra S R Elnaggar, Ossama Y Abdallah
Carbopol is a good bio-adhesive polymer that increases the residence time in the eye. However, the effect of blinking and lacrimation still reduce the amount of polymer and the incorporated drug available for bioadhesion. Gel-core liposomes are advanced systems offering benefits making it a good tool for improved ocular drug delivery and residence time. Incorporation of carbopol in gel-core liposomes and their potential in ocular delivery have not so far been investigated. Fluconazole (FLZ) was selected as a challenging important ocular antifungal suffering from poor corneal permeation and short residence time...
May 17, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29778702/theoretical-studies-on-electroluminescent-mechanism-of-a-series-of-thermally-activated-delayed-fluorescence-emitters-possessing-asymmetric-triazine-cored-triads
#15
Jinglai Zhang, Huijuan Yuan, Songyan Feng, Keke Wen, Xugeng Guo
A series of thermally activated delayed fluorescence (TADF) emitters using asymmetric-triazine-cored triad as the electron-accepting unit have been investigated theoretically. Based on two experimentally reported TADF molecules (TPXZ-as-TAZ and oDPXZ-as-TAZ), two new molecules (mDPXZ-as-TAZ and pDPXZ-as-TAZ) have been designed to explore the isomeric effect on their TADF properties. The present results reveal that the absorption and emission spectra calculated by the time-dependent density functional theory (TD-DFT) method at the M06-2X level are match well the available experimental findings, and mDPXZ-as-TAZ and pDPXZ-as-TAZ are found to exhibit the same yellow emission as their analogue oDPXZ-as-TAZ...
May 17, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/29778689/network-analysis-of-a-proposed-exit-pathway-for-protons-to-the-p-side-of-cytochrome-c-oxidase
#16
Xiuhong Cai, Kamran Haider, Jianxun Lu, Slaven Radic, Chang Yun Son, Qiang Cui, M R Gunner
Cytochrome c Oxidase (CcO) reduces O2 , the terminal electron acceptor, to water in the aerobic respiration electron transport chain. The energy released by O2 reductions is stored by removing eight protons from the high pH, N-side, of the membrane with four used for chemistry in the active site and four pumped to the low pH, P-side. The proton transfers must occur along controllable proton pathways that prevent energy dissipating movement towards the N-side. The CcO N-side has well established D- and K-channels to deliver protons to the protein interior...
May 17, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29778543/expression-of-a-functional-intrabody-against-hepatitis-c-virus-core-protein-in-escherichia-coli-and-silkworm-pupae
#17
Tatsuya Kato, Moeko Hasegawa, Takeshi Yamamoto, Takatsugu Miyazaki, Ryosuke Suzuki, Takaji Wakita, Tetsuro Suzuki, Enoch Y Park
It has been shown that the single-domain intrabody 2H9-L against the hepatitis C virus (HCV) capsid (core) protein inhibits the viral propagation and NF-κB promoter activity induced by the HCV core. In this study, 2H9-L fused with the FLAG tag sequence was expressed in both Escherichia coli and silkworm pupae and then purified. In addition, the full-length and its C terminal deletions of the HCV core protein, i.e., 1-123 amino acid residues (C123), 1-152 amino acid residues (C152), 1-177 amino acid residues (C177) and 1-191 amino acid residues (C191), were expressed as fusion proteins with a 6 × His tag at their N-terminus in E...
May 17, 2018: Protein Expression and Purification
https://www.readbyqxmd.com/read/29778513/the-immune-response-of-rhesus-macaques-to-novel-vaccines-comprising-hepatitis-b-virus-s-pres1-and-core-antigens
#18
Xia Chuai, Bangxiang Xie, Hong Chen, Xinyi Tan, Wen Wang, Baoying Huang, Yao Deng, Wenhui Li, Wenjie Tan
Therapeutic vaccines represent a unique approach to hepatitis B virus (HBV) treatment and have the potential to induce long-term control of infection. This study explored the immune responses of rhesus macaques to novel vaccines comprising the S, PreS1, and Core antigens of the HBV that showed promise as prophylactic and therapeutic approaches in a mouse model. The tested vaccines included two DNA vaccines (pVRC-SS1, pVRC-CS1), an HBV particle subunit (HBSS1) vaccine and the recombinant vaccinia virus- (RVJ-) based vaccines (RVJSS1 and RVJCS1) in which SS1 containing S (1-223 aa) and PreS1 (21-47 aa), CS1 containing Core (1-144 aa) and PreS1 (1-42 aa)...
May 16, 2018: Vaccine
https://www.readbyqxmd.com/read/29778349/a-contemporary-prostate-biopsy-risk-calculator-based-on-multiple-heterogeneous-cohorts
#19
Donna P Ankerst, Johanna Straubinger, Katharina Selig, Lourdes Guerrios, Amanda De Hoedt, Javier Hernandez, Michael A Liss, Robin J Leach, Stephen J Freedland, Michael W Kattan, Robert Nam, Alexander Haese, Francesco Montorsi, Stephen A Boorjian, Matthew R Cooperberg, Cedric Poyet, Emily Vertosick, Andrew J Vickers
BACKGROUND: Prostate cancer prediction tools provide quantitative guidance for doctor-patient decision-making regarding biopsy. The widely used online Prostate Cancer Prevention Trial Risk Calculator (PCPTRC) utilized data from the 1990s based on six-core biopsies and outdated grading systems. OBJECTIVE: We prospectively gathered data from men undergoing prostate biopsy in multiple diverse North American and European institutions participating in the Prostate Biopsy Collaborative Group (PBCG) in order to build a state-of-the-art risk prediction tool...
May 16, 2018: European Urology
https://www.readbyqxmd.com/read/29778265/a-guide-to-the-economics-of-hepatitis-c-virus-cure-in-2017
#20
REVIEW
Benjamin P Linas, Shayla Nolen
This commentary reviews the core principals of cost-effectiveness and applies them to the rapidly evolving context of hepatitis C virus treatment in the United States. The article provides a foundation of evidence that hepatitis C virus treatment provides good economic value, even though it is expensive, and even when treating people who inject drugs who are at high risk for hepatitis C virus reinfection. The price of medications has decreased, but the high price continues to limit access to care. This wedge between cost effectiveness and affordability stands front and center as one of the leading obstacles to elimination...
June 2018: Infectious Disease Clinics of North America
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