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https://www.readbyqxmd.com/read/29454281/probing-the-%C3%AE-pocket-of-the-active-site-of-human-liver-glycogen-phosphorylase-with-3-c-%C3%AE-d-glucopyranosyl-5-4-substituted-phenyl-1-2-4-triazole-inhibitors
#1
Efthimios Kyriakis, Theodora G A Solovou, Sándor Kun, Katalin Czifrák, Béla Szőcs, László Juhász, Éva Bokor, George A Stravodimos, Anastassia L Kantsadi, Demetra S M Chatzileontiadou, Vassiliki T Skamnaki, László Somsák, Demetres D Leonidas
Human liver glycogen phosphorylase (hlGP), a key enzyme in glycogen metabolism, is a valid pharmaceutical target for the development of new anti-hyperglycaemic agents for type 2 diabetes. Inhibitor discovery studies have focused on the active site and in particular on glucopyranose based compounds with a β-1 substituent long enough to exploit interactions with a cavity adjacent to the active site, termed the β-pocket. Recently, C-β-d-glucopyranosyl imidazoles and 1, 2, 4-triazoles proved to be the best known glucose derived inhibitors of hlGP...
February 12, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29454264/development-and-validation-of-uplc-ms-ms-assay-for-quantification-of-cladrin-absolute-bioavailability-and-dose-proportionality-study-in-rats
#2
Mamunur Rashid, Sandeep K Singh, Mohd Yaseen Malik, Sadaf Jahan, Swati Chaturvedi, Isha Taneja, Kanumuri Sivarama Raju, Zaiba Naseem, J R Gayen, Muhammad Wahajuddin
Cladrin, an isoflavone is a major bioactive constituent found in stem bark of Butea monosperma with remarkable osteogenic activity. A speedy and sensitive UPLC coupled tandem mass spectrometry (UPLC-MS/MS) method was developed, validated and successfully applied to bioavailability, blood partitioning, plasma protein binding, intravenous and multiple-dose oral pharmacokinetics of cladrin in rats. Separation was done on C18 column (5.0 μm, 4.6 × 50 mm) using mobile phase containing acetonitrile and 0.10% formic acid in the ratio of 65:35 (v/v) with 0...
January 31, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29454257/infants-agent-individuation-it-s-what-s-on-the-insides-that-counts
#3
Hernando Taborda-Osorio, Erik W Cheries
Adults and preschool-aged children believe that internal properties are more important than external properties when determining an agent's identity over time. The current study examined the developmental origins of this understanding using a manual-search individuation task with 13-month-old infants. Subjects observed semi-transparent objects that looked and behaved like animate agents placed into box that they could reach but not see into. Across trials infants observed objects with either the same- or different-colored insides placed into the box...
February 14, 2018: Cognition
https://www.readbyqxmd.com/read/29454225/low-power-lasers-on-genomic-stability
#4
Larissa Alexsandra da Silva Neto Trajano, Luiz Philippe da Silva Sergio, Ana Carolina Stumbo, Andre Luiz Mencalha, Adenilson de Souza da Fonseca
Exposure of cells to genotoxic agents causes modifications in DNA, resulting to alterations in the genome. To reduce genomic instability, cells have DNA damage responses in which DNA repair proteins remove these lesions. Excessive free radicals cause DNA damages, repaired by base excision repair and nucleotide excision repair pathways. When non-oxidative lesions occur, genomic stability is maintained through checkpoints in which the cell cycle stops and DNA repair occurs. Telomere shortening is related to the development of various diseases, such as cancer...
February 10, 2018: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/29454188/modified-two-step-emulsion-solvent-evaporation-technique-for-fabricating-biodegradable-rod-shaped-particles-in-the-submicron-size-range
#5
Hanieh Safari, Reheman Adili, Michael Holinstat, Omolola Eniola-Adefeso
HYPOTHESIS: Though the emulsion solvent evaporation (ESE) technique has been previously modified to produce rod-shaped particles, it cannot generate small-sized rods for drug delivery applications due to the inherent coupling and contradicting requirements for the formation versus stretching of droplets. The separation of the droplet formation from the stretching step should enable the creation of submicron droplets that are then stretched in the second stage by manipulation of the system viscosity along with the surface-active molecule and oil-phase solvent...
February 9, 2018: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/29454156/the-glun2b-subunit-represents-a-major-functional-determinant-of-nmda-receptors-in-human-induced-pluripotent-stem-cell-derived-cortical-neurons
#6
Ioana Neagoe, Chang Liu, Alexander Stumpf, Yanmei Lu, Dongping He, Ross Francis, Jun Chen, Paul Reynen, Moulay Hicham Alaoui-Ismaili, Hirokazu Fukui
Abnormal signaling pathways mediated by N-methyl-d-aspartate receptors (NMDARs) have been implicated in the pathogenesis of various CNS disorders and have been long considered as promising points of therapeutic intervention. However, few efforts have been previously described concerning evaluation of therapeutic modulators of NMDARs and their downstream pathways in human neurons with endogenous expression of NMDARs. In the present study, we assessed expression, functionality, and subunit composition of endogenous NMDARs in human induced pluripotent stem cell (hiPSC)-derived cortical neurons (iCell Neurons and iCell GlutaNeurons)...
February 8, 2018: Stem Cell Research
https://www.readbyqxmd.com/read/29454155/immune-checkpoint-inhibitors-in-non-small-cell-lung-cancer-nsclc-approaches-on-special-subgroups-and-unresolved-burning-questions
#7
REVIEW
J Remon, N Vilariño, N Reguart
Immune checkpoint inhibitors (ICIs) have been incorporated in the treatment strategy of advanced non-small cell lung cancer (NSCLC). Beyond the already approved indications in first- and second-line setting of advanced NSCLC, new data has recently emerged demonstrating its efficacy in locally advanced disease as maintenance after chemo-radiotherapy and currently several trials are also exploring its efficacy in earlier stages of the disease to evaluate whether these results could be extrapolated to the adjuvant setting...
February 8, 2018: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/29454148/-68-ga-galmydar-biodistribution-and-radiation-dosimetry-studies-in-rodents
#8
Jothilingam Sivapackiam, Richard Laforest, Vijay Sharma
INTRODUCTION: 68 Ga-Galmydar is an avid transport substrate of ABCB1 (P-Glycoprotein; 170kDa plasma membrane protein), breast cancer resistance protein (BCRP; ABCG2; 72kDa), penetrates human epidermal carcinoma (KB3-1), breast cancer (MCF7), embryonic kidney (HEK 293) tumor cells and rat cardiomyoblasts, and localizes within the mitochondria of tumor and myocardium cells. 68 Ga-Galmydar excretes from blood pool quickly, and shows stable retention within rat myocardium in vivo for extended periods, therefore, the agent shows potential to enable myocardial perfusion imaging...
December 1, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29454114/mitochondria-targeting-mitochondrial-reactive-oxygen-species-with-mitochondriotropic-polyphenolic-based-antioxidants
#9
José Teixeira, Cláudia M Deus, Fernanda Borges, Paulo J Oliveira
Mitochondrial function and regulation of redox balance is fundamental in controlling cellular life and death pathways. Antioxidants have been used to counteract disruption of redox networks, normally associated with progressive loss of cell homeostasis and disease pathophysiology, although therapeutic success is limited mainly due to pharmacokinetic drawbacks. Attempts to improve mitochondrial function in a range of diseases spurred active drug discovery efforts. Currently, the most effective strategy to deliver drugs to mitochondria is the covalent link of lipophilic cations to the bioactive compound...
February 14, 2018: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/29454096/jak-stat-inhibitors-and-other-small-molecule-cytokine-antagonists-for-the-treatment-of-allergic-disease
#10
REVIEW
Michael D Howell, Carolyn Fitzsimons, Paul Smith
OBJECTIVE: To provide an overview of janus kinase (JAK), chemoattractant receptor-homologous molecule expressed on T-helper 2 cells (CRTH2), and phosphodiesterase 4 (PDE4) inhibitors in allergic disorders. DATA SOURCES: PubMed literature review. STUDY SELECTIONS: Articles included in this review discuss the emerging mechanism of action of small molecule inhibitors and their utilization in atopic dermatitis (AD), asthma, and allergic rhinitis (AR)...
February 14, 2018: Annals of Allergy, Asthma & Immunology
https://www.readbyqxmd.com/read/29454091/anlotinib-inhibits-angiogenesis-via-suppressing-the-activation-of-vegfr2-pdgfr%C3%AE-and-fgfr1
#11
Binyan Lin, Xiuming Song, Dawei Yang, Dongsheng Bai, Yuyuan Yao, Na Lu
Tumor cells recruit vascular endothelial cells and circulating endothelial progenitor cells to form new vessels to support their own growth and metastasis. VEGF, PDGF-BB and FGF-2 are three major pro-angiogenic factors and applied to promote angiogenesis. In this research, we demonstrated that anlotinib, a potent multi-tyrosine kinases inhibitor (TKI), showed a significant inhibitory effect on VEGF/PDGF-BB/FGF-2-induced angiogenesis in vitro and in vivo. Wound healing assay, chamber directional migration assay and tube formation assay indicated that anlotinib inhibited VEGF/PDGF-BB/FGF-2-induced cell migration and formation of capillary-like tubes in endothelial cells...
February 14, 2018: Gene
https://www.readbyqxmd.com/read/29454074/nutraceuticals-as-therapeutic-agents-for-atherosclerosis
#12
REVIEW
Joe W E Moss, Jessica O Williams, Dipak P Ramji
Atherosclerosis, a chronic inflammatory disorder of medium and large arteries and an underlying cause of cardiovascular disease (CVD), is responsible for a third of all global deaths. Current treatments for CVD, such as optimized statin therapy, are associated with considerable residual risk and several side effects in some patients. The outcome of research on the identification of alternative pharmaceutical agents for the treatment of CVD has been relatively disappointing with many promising leads failing at the clinical level...
February 14, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29454062/laser-assisted-delivery-of-synergistic-combination-chemotherapy-in-in-vivo-skin
#13
Emily Wenande, Joshua Tam, Brijesh Bhayana, Steven Kyle Schlosser, Emily Ishak, William A Farinelli, Agata Chlopik, Mai P Hoang, Omar R Pinkhasov, Peter Caravan, R Rox Anderson, Merete Haedersdal
The effectiveness of topical drugs for treatment of non-melanoma skin cancer is greatly reduced by insufficient penetration to deep skin layers. Ablative fractional lasers (AFLs) are known to enhance topical drug uptake by generating narrow microchannels through the skin, but information on AFL-drug delivery in in vivo conditions is limited. In this study, we examined pharmacokinetics, biodistribution and toxicity of two synergistic chemotherapy agents, cisplatin and 5-fluorouracil (5-FU), following AFL-assisted delivery alone or in combination in in vivo porcine skin...
February 14, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29454056/biophysical-and-immunological-characterization-of-2-drib-modified-hsa-and-its-implications-in-diabetes-mellitus
#14
Ishrat Jahan Saifi, Km Neelofar, M R Ajmal, Sheelu Shafiq Siddiqi
Glycoxidation of protein may lead to develop diabetes. In the present study, different concentrations of 2-deoxy d-ribose (2-dRib) were used to modify human serum albumin (HSA). Nitro Blue Tetrazolium (NBT) assay results showed that yield of the fructosamine content was directly proportional to the concentration of 2-dRib. UV and fluorescence spectroscopy results showed an increment in hyperchromicity and decrease in fluorescence intensity of 2-dRib modified HSA as compared to native HSA. Further secondary structural changes were confirmed by UV-circular dichroism (UV-CD) and Fourier transform infrared spectroscopy (FT-IR)...
February 14, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29454033/cause-or-coincidence-spontaneous-hematometra-in-young-women-on-depomedroxyprogesterone-acetate-a-small-case-series
#15
Julie G Thorne, Elizabeth H Russell, Danielle Rumbolt, Mary Anne Jamieson
BACKGROUND: Abdominal pain, secondary amenorrhea and abnormal uterine bleeding (AUB) are common gynecologic presentations in adolescence. Rarely this can be associated with an acquired hematometra. Hematometra is a condition of retained blood or clot within the uterus. High dose progestogenic agents in this age group have been implicated in the accumulation of a hematometra without other explanation. CASES: We present 4 cases of hematometra following depomedroxyprogesterone acetate (DMPA) therapy in previously menstruating adolescents...
February 14, 2018: Journal of Pediatric and Adolescent Gynecology
https://www.readbyqxmd.com/read/29454018/co-circulation-of-classic-and-novel-astrovirus-strains-in-patients-with-acute-gastroenteritis-in-germany
#16
Sonja Jacobsen, Marina Höhne, Andreas Mas Marques, Klara Beslmüller, C-Thomas Bock, Sandra Niendorf
OBJECTIVES: In order to analyze the molecular epidemiology of human astroviruses (HAstV) in Germany, a retrospective long term study was performed to characterize circulating human astrovirus in patients with acute gastroenteritis in Germany. METHODS: A total of 2877 stool samples, collected between January 2010 and December 2015 from sporadic cases and outbreaks of acute gastroenteritis were retrospectively analyzed for astrovirus. A two step PCR algorithm was developed and used to identify and characterize human astrovirus infections...
February 14, 2018: Journal of Infection
https://www.readbyqxmd.com/read/29454008/temozolomide-affects-extracellular-vesicles-released-by-glioblastoma-cells
#17
Gwennan André-Grégoire, Nicolas Bidère, Julie Gavard
Glioblastoma multiforme (GBM) is the most aggressive primary tumour within the brain as well as the most common and lethal cerebral cancer, mainly because of treatment failure. Indeed, tumour recurrence is inevitable and fatal in a short period of time. Glioblastoma stem-like cells (GSCs) are thought to participate in tumour initiation, expansion, resistance to treatments, including to the alkylating chemotherapeutic agent temozolomide, and relapse. Here, we assessed whether extracellular vesicles (EVs) released by GSCs could disseminate factors involved in resistance mechanisms...
February 14, 2018: Biochimie
https://www.readbyqxmd.com/read/29453966/gamma-irradiation-inactivates-honey-bee-fungal-microsporidian-and-viral-pathogens-and-parasites
#18
Michael Simone-Finstrom, Kate Aronstein, Michael Goblirsch, Frank Rinkevich, Lilia de Guzman
Managed honey bee (Apis mellifera) populations are currently facing unsustainable losses due to a variety of factors. Colonies are challenged with brood pathogens, such as the fungal agent of chalkbrood disease, the microsporidian gut parasite Nosema sp., and several viruses. These pathogens may be transmitted horizontally from worker to worker, vertically from queen to egg and via vectors like the parasitic mite, Varroa destructor. Despite the fact that these pathogens are widespread and often harbored in wax comb that is reused from year to year and transferred across beekeeping operations, few, if any, universal treatments exist for their control...
February 14, 2018: Journal of Invertebrate Pathology
https://www.readbyqxmd.com/read/29453947/evaluation-of-the-effects-of-rp5063-a-novel-multimodal-serotonin-receptor-modulator-as-single-agent-therapy-and-co-administrated-with-sildenafil-bosentan-and-treprostinil-in-a-monocrotaline-induced-pulmonary-arterial-hypertension-rat-model
#19
Laxminarayan Bhat, Jon Hawkinson, Marc Cantillon, Dasharatha G Reddy, Seema R Bhat, Charles-E Laurent, Annie Bouchard, Marzena Biernat, Dany Salvail
Pulmonary arterial hypertension (PAH), a condition that is defined by pulmonary vasculature constriction and remodeling, involves dysfunctional signaling of the serotonin (5-HT) receptors, 5-HT 2/2B/7 . In a rat model of monocrotaline (MCT)-induced PAH, the effectiveness of RP5063 (RP), a dopamine and 5-HT receptor modulator, was evaluated as monotherapy and as an adjunct to standard PAH treatments. After a single 60mg/kg dose of MCT, rats received vehicle (MCT+Veh; gavage twice-daily [b.i.d.]), RP (10mg/kg; gavage b...
February 14, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29453908/effective-anti-adhesives-of-uropathogenic-escherichia-coli
#20
Rosana Ribić, Tomislav Meštrović, Marijana Neuberg, Goran Kozina
Urinary tract infections (UTIs) caused by uropathogenic Escherichia coli (UPEC) are among the most common infectious diseases in humans. Due to their frequent occurrence in the community and nosocomial settings, as well as the development of resistance to the commonly prescribed antimicrobial agents, an enormous financial burden is placed on healthcare systems around the world. Therefore, novel approaches to the prevention and treatment of UTIs are needed. Although UPEC may harbour a plethora of virulence factors, type I fimbriae and P pili are two of the most studied adhesive organelles, since the attachment to host cells in the urinary tract is a crucial step towards infection...
March 1, 2018: Acta Pharmaceutica
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