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https://www.readbyqxmd.com/read/28102582/beliefs-about-the-causes-of-depression-and-recovery-and-their-impact-on-adherence-dosage-and-successful-tapering-of-antidepressants
#1
Nicola S Klein, Gerard D van Rijsbergen, Mascha C Ten Doesschate, Steven D Hollon, Huibert Burger, Claudi L H Bockting
BACKGROUND: Continuation of antidepressant medication (ADM) after remission is widely used to prevent depressive relapse/recurrence. Little is known about predictors of ADM use in terms of adherence, dosage, and successful tapering. The current study aimed to explore beliefs about the causes of depression and recovery (i.e., causal beliefs) and to examine whether they predict ADM use. METHODS: The data were drawn from a controlled trial and an extension of this trial with additional experience sampling...
January 19, 2017: Depression and Anxiety
https://www.readbyqxmd.com/read/28101163/expression-of-adrenomedullin-in-rats-after-spinal-cord-injury-and-intervention-effect-of-recombinant-human-erythropoietin
#2
Liang Zhao, Yu Jing, Lin Qu, Xiangwei Meng, Yang Cao, Huibing Tan
The expression of adrenomedullin (ADM) in injured tissue of rat spinal cord was observed and the effect of recombinant human erythropoietin was analyzed. A total of 45 Sprague-Dawley rats were selected and divided into 3 equal groups including, a sham-operation group in which rats received an excision of vertebral plate; a spinal cord injury model group and a recombinant human erythropoietin group in which rats with spinal cord injury received a caudal vein injection of 300 units recombinant human erythropoietin after injury...
December 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28098907/synergistic-combination-of-ys-1-and-adriamycin-inhibits-human-renal-cancer-through-erk1-2-signaling-pathway-in%C3%A2-vitro-and-in%C3%A2-vivo
#3
Xiaowen Yu, Qingqing Yang, Sensen Lin, Shengtao Yuan, Li Sun
Adriamycin (ADM) is a principal drug for the treatment of renal cell cancer (RCC). Due to its limited response and high renal and cardiac toxicity, synergistic effects of ADM in combination with other drugs have been widely researched. In this study, we found the combination between YS-1 and ADM, performed higher anticancer activity on 786-O human RCC cells in vitro and in vivo, than that reported on its anti-angiogenesis effect compared with monotherapy of ADM. Our data showed that when combined with ADM, YS-1 promoted the sensitivity of 786-O cells to ADM...
January 16, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28098863/effect-and-mechanism-of-resveratrol-on-drug-resistance-in-human-bladder-cancer-cells
#4
Shanshan Wang, Qian Meng, Qing Xie, Man Zhang
Multidrug resistance (MDR) is a significant barrier to the effective treatment of bladder cancer. In order to improve the management of bladder cancer, it is crucial to identify strategies that may reverse MDR. The effects of three herbal medicines, ginsenoside Rh2, (‑)‑epigallocatechin gallate (EGCG) and resveratrol (RES) on bladder cancer were determined. The effect of these three herbal medicines against the drug resistance in adriamycin (ADM)‑resistant pumc‑91 cells (pumc‑91/ADM) was assessed using the Cell Counting Kit‑8 cell proliferation assay system...
January 12, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28097740/in%C3%A2-vivo-dearomatization-of-the-potent-antituberculosis-agent-btz043-via-meisenheimer-complex-formation
#5
Florian Kloss, Viktor Krchnak, Anna Krchnakova, Sebastian Schieferdecker, Julia Dreisbach, Volker Krone, Ute Möllmann, Michael Hoelscher, Marvin J Miller
Nitrobenzothiazinones are among the most potent antituberculosis agents. Herein, we disclose an unprecedented in vivo reduction process that affords Meisenheimer complexes of the clinical candidates BTZ043 and PBTZ169. The reduction is reversible, occurs in all mammalian species investigated, has a profound influence on the in vivo ADME characteristics, and has considerable implications for the design and implementation of clinical studies. The reduction was confirmed by chemical studies that enabled the complete characterization of the Meisenheimer complex and its subsequent chemistry...
January 18, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28094550/pharmacophore-modelling-atom-based-3d-qsar-generation-and-virtual-screening-of-molecules-projected-for-mpges-1-inhibitory-activity
#6
S Misra, M Saini, H Ojha, D Sharma, K Sharma
COX-2 inhibitors exhibit anticancer effects in various cancer models but due to the adverse side effects associated with these inhibitors, targeting molecules downstream of COX-2 (such as mPGES-1) has been suggested. Even after calls for mPGES-1 inhibitor design, to date there are only a few published inhibitors targeting the enzyme and displaying anticancer activity. In the present study, we have deployed both ligand and structure-based drug design approaches to hunt novel drug-like candidates as mPGES-1 inhibitors...
January 17, 2017: SAR and QSAR in Environmental Research
https://www.readbyqxmd.com/read/28091613/adrenomedullin-promotes-angiogenesis-in-epithelial-ovarian-cancer-through-upregulating-hypoxia-inducible-factor-1%C3%AE-and-vascular-endothelial-growth-factor
#7
Yi Zhang, Yang Xu, Jian Ma, Xiaoyan Pang, Mei Dong
Adrenomedullin (ADM) is a multi-functional peptide related to many kinds of tumors. This study was aimed to investigate the role of ADM on angiogenesis in epithelial ovarian cancer (EOC) and its possible mechanism. The expressions of ADM, vascular endothelial growth factor (VEGF), hypoxia-inducible factor-1α (HIF-1α) and CD34 were examined by immunohistochemistry staining. The relationship among ADM, HIF-1α, VEGF and micro-vessel density (MVD) was assessed in 56 EOC tissues. CAOV3 cells were stably transfected with pcDNA-ADM (plasmid overexpressing ADM gene) or pRNA-shADM (small interfering RNA for ADM gene)...
January 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28089234/oncogenic-kras-induced-increase-in-fluid-phase-endocytosis-is-dependent-on-n-wasp-and-is-required-for-the-formation-of-pancreatic-preneoplastic-lesions
#8
Clara Lubeseder-Martellato, Katharina Alexandrow, Ana Hidalgo-Sastre, Irina Heid, Sophie Luise Boos, Thomas Briel, Roland M Schmid, Jens T Siveke
Fluid-phase endocytosis is a homeostatic process with an unknown role in tumor initiation. The driver mutation in pancreatic ductal adenocarcinoma (PDAC) is constitutively active KRas(G12D), which induces neoplastic transformation of acinar cells through acinar-to-ductal metaplasia (ADM). We have previously shown that KRas(G12D)-induced ADM is dependent on RAC1 and EGF receptor (EGFR) by a not fully clarified mechanism. Using three-dimensional mouse and human acinar tissue cultures and genetically engineered mouse models, we provide evidence that (i) KRas(G12D) leads to EGFR-dependent sustained fluid-phase endocytosis (FPE) during acinar metaplasia; (ii) variations in plasma membrane tension increase FPE and lead to ADM in vitro independently of EGFR; and (iii) that RAC1 regulates ADM formation partially through actin-dependent regulation of FPE...
December 24, 2016: EBioMedicine
https://www.readbyqxmd.com/read/28088085/new-pyridazinone-4-carboxamides-as-new-cannabinoid-receptor-type-2-inverse-agonists-synthesis-pharmacological-data-and-molecular-docking
#9
Giulio Ragusa, María Gómez-Cañas, Paula Morales, Carmen Rodríguez-Cueto, María R Pazos, Battistina Asproni, Elena Cichero, Paola Fossa, Gerard A Pinna, Nadine Jagerovic, Javier Fernández-Ruiz, Gabriele Murineddu
In the last few years, cannabinoid type-2 receptor (CB2R) selective ligands have shown a great potential as novel therapeutic drugs in several diseases. With the aim of discovering new selective cannabinoid ligands, a series of pyridazinone-4-carboxamides was designed and synthesized, and the new derivatives tested for their affinity toward the hCB1R and hCB2R. The 6-(4-chloro-3-methylphenyl)-2-(4-fluorobenzyl)-N-(cis-4-methylcyclohexyl)-3-oxo-2,3-dihydropyridazine-4-carboxamide (9) displayed high CB2-affinity (KiCB2 = 2...
January 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28081581/differences-in-gene-expression-and-gene-associations-in-epicardial-fat-compared-to-subcutaneous-fat
#10
J Yim, S W Rabkin
Epicardial adipose tissue (EAT) plays a role in cardiac physiology and may contribute to the development of coronary artery disease. Our objective was to determine whether there was a significant difference in gene expression in EAT compared to subcutaneous adipose tissue (SAT) and to identify potential relationships. MEDLINE and EMBASE were searched using the key terms "Epicardial Adipose Tissue" or "Epicardial Fat" in combination with "RNA", "mRNA", or "gene". The entry criteria were studies that presented primary data including expression levels of mRNA in human EAT compared with SAT and an expression of variance (SD)...
January 12, 2017: Hormone and Metabolic Research, Hormon- und Stoffwechselforschung, Hormones et Métabolisme
https://www.readbyqxmd.com/read/28078629/effect-of-microneedle-type-on-transdermal-permeation-of-rizatriptan
#11
Chandrateja Uppuluri, Ashraf Sultana Shaik, Tao Han, Atul Nayak, Karthik J Nair, Benjamin R Whiteside, Buchi N Nalluri, Diganta B Das
The present study was aimed to investigate the effect of salient microneedle (MN) geometry parameters like length, density, shape and type on transdermal permeation of rizatriptan (RIZ). Studies were carried out using two types of MN devices viz. AdminPatch® arrays (ADM) (0.6, 0.9, 1.2 and 1.5 mm lengths) and laboratory-fabricated polymeric MNs (PMs) of 0.6 mm length. In the case of the PMs, arrays were applied three times at different places within a 1.77-cm(2) skin area (PM-3) to maintain the MN density closer to 0...
January 11, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28076885/cross-linking-of-porcine-acellular-dermal-matrices-negatively-affects-induced-neovessel-formation-using-platelet-rich-plasma-in-a-rat-model-of-hernia-repair
#12
Joseph S Fernandez-Moure, Jeffrey L Van Eps, Leif Peterson, Beverly A Shirkey, Zachary K Menn, Fernando Cabrera, Azim Karim, Ennio Tasciotti, Bradley K Weiner, Warren A Ellsworth
The degree of crosslinking within acellular dermal matrices (ADM) seems to correlate to neovascularization when used in ventral hernia repair (VHR). Platelet-rich plasma (PRP) enhances wound healing through several mechanisms including neovascularization, but research regarding its effect on soft tissue healing in VHR is lacking. We sought to study the effect of crosslinking on PRP-induced neovascularization in a rodent model of bridging VHR. We hypothesized that ADM crosslinking would negatively affect PRP-induced neovessel formation...
January 11, 2017: Wound Repair and Regeneration
https://www.readbyqxmd.com/read/28074615/a-database-of-optimized-proteomic-quantitative-methods-for-284-human-drug-disposition-related-proteins-for-applications-in-pbpk-modeling
#13
Marc Vrana, Dale Whittington, Vivek Nautiyal, Bhagwat Prasad
The aim of this study was to create an open access repository of validated LC-MS/MS (MRM) methods for quantifying 284 important proteins associated with drug absorption, distribution, metabolism and excretion (ADME). Various in silico and experimental approaches were used to select surrogate peptides and optimize instrument parameters for LC-MS/MS quantification of the selected proteins. The final methods were uploaded to an online public database (ADME QPrOmics(TM); www.qpromics.uw.edu/qpromics/assay/) which provides essential information for facile method development in triple quadrupole MS instruments...
January 11, 2017: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/28073115/pyridazine-based-scaffolds-as-privileged-structures-in-anti-cancer-therapy
#14
M Jaballah, R Serya, K Abouzid
Pyridazines, their oxo derivatives; pyridazinone as well as fused bi- or tricyclic pyridazine containing scaffolds are key structural features of many biologically active compounds with diverse pharmacological applications, including cancer therapy. Since protein kinases play prominent role in tumor biology, the inhibition of its signaling pathway is considered an effective therapeutic option for the treatment of cancer.Based on the various advantages of pyridazines in drug design including modulation of the physico-chemical properties, improving ADME and toxicity profile as well as easy and diverse synthetic methods of access, makes them an invaluable tool for designing compounds as future drugs for targeted cancer treatment...
January 10, 2017: Drug Research
https://www.readbyqxmd.com/read/28065780/drug-likeness-prediction-of-chemical-constituents-isolated-from-chinese%C3%A2-materia%C3%A2-medica-ciwujia
#15
Shuai-Nan Zhang, Xu-Zhao Li, Xu-Yan Yang
ETHNOPHARMACOLOGICAL RELEVANCE: Ciwujia (CWJ), one of the most commonly used Chinese materia medicas (CMMs), is derived from the roots, rhizomes, and stems of Acanthopanax senticosus harms (AS). CWJ has been used for the treatment of various central nervous system (CNS) and peripheral system diseases. Drug-likeness prediction can help to analyze the absorption, distribution, metabolism, and excretion (ADME) processes of the compounds in CWJ, as well as their potential therapeutic and toxic effects, which is of significance in the confirmation of the active material bases of CWJ...
January 5, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28057438/oncogenic-kras-induced-increase-in-fluid-phase-endocytosis-is-dependent-on-n-wasp-and-is-required-for-the-formation-of-pancreatic-preneoplastic-lesions
#16
Clara Lubeseder-Martellato, Katharina Alexandrow, Ana Hidalgo-Sastre, Irina Heid, Sophie Luise Boos, Thomas Briel, Roland M Schmid, Jens T Siveke
Fluid-phase endocytosis is a homeostatic process with an unknown role in tumor initiation. The driver mutation in pancreatic ductal adenocarcinoma (PDAC) is constitutively active KRas(G12D), which induces neoplastic transformation of acinar cells through acinar-to-ductal metaplasia (ADM). We have previously shown that KRas(G12D)-induced ADM is dependent on RAC1 and EGF receptor (EGFR) by a not fully clarified mechanism. Using three-dimensional mouse and human acinar tissue cultures and genetically engineered mouse models, we provide evidence that (i) KRas(G12D) leads to EGFR-dependent sustained fluid-phase endocytosis (FPE) during acinar metaplasia; (ii) variations in plasma membrane tension increase FPE and lead to ADM in vitro independently of EGFR; and (iii) that RAC1 regulates ADM formation partially through actin-dependent regulation of FPE...
February 2017: EBioMedicine
https://www.readbyqxmd.com/read/28055204/design-synthesis-of-novel-potent-selective-orally-bioavailable-adenosine-a2a-receptor-antagonists-and-their-biological-evaluation
#17
Sujay Basu, Dinesh A Barawkar, Sachin Thorat, Yogesh D Shejul, Meena Patel, Minakshi Naykodi, Vaibhav Jain, Yogesh Salve, Vandna Prasad, Sumit Chaudhary, Indraneel Ghosh, Ganesh Bhat, Azfar Quraishi, Harish Patil, Shariq Ansari, Suraj Menon, Vishal Unadkat, Rhishikesh Thakare, Madhav S Seervi, Ashwinkumar V Meru, Siddhartha De, Ravi K Bhamidipati, Sreekanth R Rouduri, Venkata P Palle, Anita Chug, Kasim A Mookhtiar
Our initial structure-activity relationship studies on 7-methoxy-4-morpholino-benzothiazole derivatives featured by aryloxy-2-methylpropanamide moieties at the 2-position led to identification of compound 25 as a potent and selective A2A adenosine receptor (A2AAdoR) antagonist with reasonable ADME and pharmacokinetic properties. However, poor intrinsic solubility and low to moderate oral bioavailability made this series unsuitable for further development. Further optimization using structure-based drug design approach resulted in discovery of potent and selective adenosine A2A receptor antagonists bearing substituted 1-methylcyclohexyl-carboxamide groups at position 2 of the benzothiazole scaffold and endowed with better solubility and oral bioavailability...
January 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28053999/b-cell-populations-discriminate-between-pediatric-and-adult-onset-multiple-sclerosis
#18
Alexander Schwarz, Bettina Balint, Mirjam Korporal-Kuhnke, Sven Jarius, Kathrin von Engelhardt, Alexandra Fürwentsches, Cornelia Bussmann, Friedrich Ebinger, Brigitte Wildemann, Jürgen Haas
OBJECTIVE: To comparatively assess the B-cell composition in blood and CSF of patients with pediatric-onset multiple sclerosis (pedMS) and adult-onset multiple sclerosis (adMS). METHODS: In this cross-sectional study, we obtained blood and CSF samples from 25 patients with pedMS (8-18 years) and 40 patients with adMS (23-65 years) and blood specimens from 66 controls (1-55 years). By using multicolor flow cytometry, we identified naive, transitional, isotype class-switched memory, nonswitched memory, and double-negative memory B-cell subsets as well as plasmablasts (PB) and terminally differentiated plasma cells (PC)...
January 2017: Neurology® Neuroimmunology & Neuroinflammation
https://www.readbyqxmd.com/read/28051266/one-stage-breast-reconstruction-techniques-in-elderly-patients-to-preserve-quality-of-life
#19
M Maruccia, M Mazzocchi, L A Dessy, M G Onesti
OBJECTIVE: The aim of this study was to review one-stage breast reconstruction techniques performed in elderly patients at our institution to identify the criteria of selection of each in terms of outcomes and quality of life. PATIENTS AND METHODS: Patients older than 65 years who underwent one-stage breast reconstruction between January 2004 and July 2014 at our hospital were included. Patients and procedure-related data were collected from the medical records...
December 2016: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28050899/adrenomedullin-a-marker-of-impaired-hemodynamics-organ-dysfunction-and-poor-prognosis-in-cardiogenic-shock
#20
Heli Tolppanen, Mercedes Rivas-Lasarte, Johan Lassus, Jordi Sans-Roselló, Oliver Hartmann, Matias Lindholm, Mattia Arrigo, Tuukka Tarvasmäki, Lars Köber, Holger Thiele, Kari Pulkki, Jindrich Spinar, John Parissis, Marek Banaszewski, Jose Silva-Cardoso, Valentina Carubelli, Alessandro Sionis, Veli-Pekka Harjola, Alexandre Mebazaa
BACKGROUND: The clinical CardShock risk score, including baseline lactate levels, was recently shown to facilitate risk stratification in patients with cardiogenic shock (CS). As based on baseline parameters, however, it may not reflect the change in mortality risk in response to initial therapies. Adrenomedullin is a prognostic biomarker in several cardiovascular diseases and was recently shown to associate with hemodynamic instability in patients with septic shock. The aim of our study was to evaluate the prognostic value and association with hemodynamic parameters of bioactive adrenomedullin (bio-ADM) in patients with CS...
December 2017: Annals of Intensive Care
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