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https://www.readbyqxmd.com/read/29031071/discovery-of-thienopyrrolotriazine-derivatives-to-protect-mitochondrial-function-against-a%C3%AE-induced-neurotoxicity
#1
TaeHun Kim, Woo Seung Son, Mohammad Neaz Morshed, Ashwini M Londhe, Seo Yun Jung, Jong-Hyun Park, Woo-Kyu Park, Sang Min Lim, Ki Duk Park, Sung Jin Cho, Kyu-Sung Jeong, Jiyoun Lee, Ae Nim Pae
Recovery of mitochondrial dysfunction has gained increasing attention as an alternative therapeutic strategy for Alzheimer's disease (AD). Recent studies suggested that the 18 kDa mitochondrial translocator protein (TSPO) has the potential to serve as a drug target for the treatment of AD. In this study, we generated a structure-based pharmacophore model and virtually screened a commercial library, identifying SVH07 as a virtual hit, which contained a tricyclic core structure, thieno[2',3':4,5]pyrrolo[1,2-d][1,2,4]triazine group...
September 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29031064/fragment-based-approach-to-identify-ido1-inhibitor-building-blocks
#2
Alice Coletti, Francesca Camponeschi, Elisa Albini, Francesco Antonio Greco, Vincenzo Maione, Chiara Custodi, Federica Ianni, Ursula Grohmann, Ciriana Orabona, Francesca Cantini, Antonio Macchiarulo
Indoleamine 2,3-dioxygenase 1 (IDO1) is attracting a great deal of interest as drug target in immune-oncology being highly expressed in cancer cells and participating to the tumor immune-editing process. Although several classes of IDO1 inhibitors have been reported in literature and patent applications, only few compounds have proved optimal pharmacological profile in preclinical studies to be advanced in clinical trials. Accordingly, the quest for novel structural classes of IDO1 inhibitors is still open...
October 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29029351/development-and-application-of-a-dual-rat-and-human-ahr-activation-assay
#3
Martin R Brown, Helen Garside, Emma Thompson, Saseela Atwal, Chloe Bean, Tony Goodall, Michael Sullivan, Mark J Graham
Significant prolonged AHR activation, classically exhibited following exposure to TCDD (dioxin), can cause a variety of undesirable toxicological effects. Novel pharmaceutical chemistries also have the potential to cause activation of AHR and consequent toxicities in pre-clinical species and man. Previous methods either employed relatively expensive and low throughput primary hepatocyte dosing with PCR endpoint, or low resolution overexpressing reporter gene assays. We have developed, validated and applied an in vitro microtitre plate imaging-based medium throughput screening assay for the assessment of endogenous species-specific AHR activation potential via detection of induction of the surrogate transcriptional target Cytochrome P450 CYP1A1...
September 18, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/29028966/high-rates-of-subsequent-asymptomatic-stis-and-risky-sexual-behavior-in-patients-initially-presenting-with-primary-hiv-1-infection
#4
Dominique L Braun, Alex Marzel, Daniela Steffens, Peter W Schreiber, Christina Grube, Alexandra U Scherrer, Roger D Kouyos, Huldrych F Günthard
Introduction: Knowledge of the characteristics and risk factors of individuals with an asymptomatic sexually transmitted infection (STI) is essential for implementation of targeted STI screening strategies. Methods: Between June 2015 and January 2017 an STI screening was offered to all participants in the Zurich Primary HIV-1 Infection Study. Patients were tested for gonorrhea, chlamydia, syphilis, and hepatitis C virus. Determinants of STI prevalence and incidence were assessed using mixed-model logistic regression and survival analysis...
October 5, 2017: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/29028806/a-novel-immunotoxin-reveals-a-new-role-for-cd321-in-endothelial-cells
#5
Takeshi Fukuhara, Jia Kim, Shintaro Hokaiwado, Makiko Nawa, Hayato Okamoto, Tomohiko Kogiso, Tetsuro Watabe, Nobutaka Hattori
There are currently several antibody therapies that directly target tumors, and antibody-drug conjugates represent a novel moiety as next generation therapeutics. Here, we used a unique screening probe, DT3C, to identify functional antibodies that recognized surface molecules and functional epitopes, and which provided toxin delivery capability. Accordingly, we generated the 90G4 antibody, which induced DT3C-dependent cytotoxicity in endothelial cells. Molecular analysis revealed that 90G4 recognized CD321, a protein localized at tight junctions...
2017: PloS One
https://www.readbyqxmd.com/read/29027787/detection-of-t4-polynucleotide-kinase-via-allosteric-aptamer-probe-platform
#6
Mingxuan Gao, Jingjing Guo, Yanling Song, Zhi Zhu, Chaoyong James Yang
As a vital enzyme in DNA phosphorylation and restoration, T4 polynuceotide kinase (T4 PNK) has aroused great interest in recent years. Numerous strategies have been established for highly sensitive detection of T4 PNK based on diverse signal amplification techniques. However, they often need sophisticated design, a variety of auxiliary reagents and enzymes, or cumbersome manipulations. Herein, we have designed a new kind of allosteric aptamer probe consisting of streptavidin aptamer (SA aptamer) and the complementary DNA (cDNA) for simple detection of T4 PNK without signal amplification and with minimized interference in complex biological samples...
October 13, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29027495/monitoring-and-managing-antibiotic-resistance-in-refugee-children
#7
Helena C Maltezou, Dana Elhadad, Daniel Glikman
The past decade the Middle East and Southeastern Europe have witnessed an enormous movement of refugees due to the Syrian war and conflicts in Asia and Africa. Although carriage of and infections with multi-drug resistant (MDR) pathogens in refugees have been reported, pediatric data are scarce. Areas covered: MDR bacterial carriage and infections, and MDR-tuberculosis (TB) in refugee children from 2010. Expert commentary: High MDR carriage rates in refugee children are attributed to high pre-civil war MDR rates, war-damaged infrastructure and healthcare systems, and poor hygiene conditions...
October 13, 2017: Expert Review of Anti-infective Therapy
https://www.readbyqxmd.com/read/29027455/-construction-and-verification-of-nf-%C3%AE%C2%BAb-luciferase-reporter-gene-system
#8
Zhilan Guo, Luyang Che, Jingzhe Li, Zhenxiao Sun, Changzhen Liu
To quantify the transcriptional activity of NF-κB and to screen drugs related to the regulation of NF-κB activation, we constructed a recombinant plasmid through deleting the original CMV promoter of retrovirus vector pQCXIP and inserting the NF-κB enhancer and NanoLuc luciferase sequence into the vector. Then, using the recombinant plasmid we constructed a cell line in which the expression of NanoLuc luciferase (NLuc) was regulated by NF-κB. The inserted sequences were verified by restriction endonuclease digestion and sequencing...
October 25, 2016: Sheng Wu Gong Cheng Xue Bao, Chinese Journal of Biotechnology
https://www.readbyqxmd.com/read/29027446/-interactions-of-aminoglycosides-with-rnas-and-proteins-via-carbohydrate-microarray
#9
Xueyu Wang, Xiaoli Wang, Beilei Zhang, Jing Hu, Jian Yin
Aminoglycosides are broad-spectrum antibacterials to treat bacterial infections, especially gram-negative bacteria infections. However, aminoglycosides are losing efficacy because of the increase in antibiotic resistance and their inherent toxicity, attracting more interests in developing new aminoglycosides. Several clinically used aminoglycosides are mainly exerted by inhibition of protein synthesis through binding to bacterial rRNA. The bacterial ribosome RNA is the most currently exploited RNA drug target...
October 25, 2016: Sheng Wu Gong Cheng Xue Bao, Chinese Journal of Biotechnology
https://www.readbyqxmd.com/read/29027430/-virtual-screening-of-anti-angiogenesis-flavonoids-from-sophora-flavescens
#10
Xi-Xin Chen, Yi Liu, Rong Huang, Lin-Lin Zhao, Lei Chen, Shu-Mei Wang
Angiogenesis is a dynamic, multi-step process. It is known that about 70 diseases are related to angiogenesis. Both the experimental and the literature reports showed that Sophora flavescens inhibit angiogenesis significantly, but the material basis and the mechanism of action have not been clear. In this study, molecular docking was used for screening of anti-angiogenesis flavonoids from the roots of S. flavescens. One handred and twenty-six flavonoids selected from S. flavescens were screened in the docking ligand database with six targets(VEGF-a,TEK,KDR,Flt1,FGFR1 and FGFR2) as the receptors...
March 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29027279/long-non-coding-rna-pvt1-emerging-biomarker-in-digestive-system-cancer
#11
REVIEW
Dan-Dan Zhou, Xiu-Fen Liu, Cheng-Wei Lu, Om Prakash Pant, Xiao-Dong Liu
The digestive system cancers are leading cause of cancer-related death worldwide, and have high risks of morbidity and mortality. More and more long non-coding RNAs (lncRNAs) have been studied to be abnormally expressed in cancers and play a key role in the process of digestive system tumour progression. Plasmacytoma variant translocation 1 (PVT1) seems fairly novel. Since 1984, PVT1 was identified to be an activator of MYC in mice. Its role in human tumour initiation and progression has long been a subject of interest...
October 12, 2017: Cell Proliferation
https://www.readbyqxmd.com/read/29026754/medication-discrepancies-and-potentially-inadequate-prescriptions-in-elderly-adults-with-polypharmacy-in-ambulatory-care
#12
Juan Víctor Ariel Franco, Sergio Adrián Terrasa, Karin Silvana Kopitowski
OBJECTIVES: The objective of this study is to describe the frequency and type of medication discrepancies (MD) through medication reconciliation and to describe the frequency of potentially inadequate prescription (PIP) medications using screening tool of older persons' prescriptions criteria. DESIGN: Cross-sectional comparison of electronic medical record (EMR) medication lists and patient's self-report of their comprehensive medication histories obtained through telephone interviews...
January 2017: Journal of Family Medicine and Primary Care
https://www.readbyqxmd.com/read/29026500/effectiveness-of-resilience-training-on-ego-control-and-hardiness-of-illicit-drug-users
#13
Amin Roustaei, Babollah Bakhshipoor, Younes Doostian, Ali Akbar Goodiny, Mansoureh Koohikar, Omid Massah
BACKGROUND: The aim of this research was to determine the effectiveness of resilience training upon ego-control and hardiness of the addicted persons. METHODS: This was a semi-experimental study with pretest and posttest control groups which was conducted in Sari, Iran, during 2014-2015. Thirty persons were selected among 240 illicit drug users who underwent screening. Resilience training was performed in ten sessions for the experimental group. The Kobasa hardiness questionnaire and self-restraint scale (SRS) were used for data collection and multivariate covariance test was performed for data analysis...
January 2017: Addiction & Health
https://www.readbyqxmd.com/read/29026363/highly-accelerated-onset-of-hydroxychloroquine-macular-retinopathy
#14
Ethan M Stern, Jordan S Johnson, Donald A Mazzulla
BACKGROUND: Hydroxychloroquine (HCQ, Plaquenil) is often prescribed in lieu of other sulfate antimalarials to treat rheumatologic diseases because of its pharmacologic efficacy and few reported side effects. However, a known potential side effect of HCQ is retinal toxicity. CASE REPORT: A 61-year-old black female presented for screening of ophthalmic disease 2 months after initiation of HCQ for the treatment of polyarthralgia with a positive rheumatoid factor. At the time of the examination, she had taken a cumulative total of 19...
2017: Ochsner Journal
https://www.readbyqxmd.com/read/29026164/production-and-evaluation-of-parathyroid-hormone-receptor1-ligands-with-intrinsic-or-assembled-peroxidase-domains
#15
Xavier Charest-Morin, Patrice E Poubelle, François Marceau
Parathyroid hormone (PTH) can be C-terminally extended without significant affinity loss for the PTH1 receptor (PTHR1). We developed fusion protein ligands with enzymatic activity to probe PTHR1s at the cell surface. Two fusion proteins were generated by linking PTH to the N-terminus of either horseradish peroxidase (PTH-HRP) or the genetically modified soybean peroxidase APEX2 (PTH-APEX2). Alternatively, myc-tagged PTH (PTH-myc) was combined with antibodies, some of which HRP-conjugated, in the extracellular fluid...
October 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29026148/exclusive-and-combined-use-of-statins-and-aspirin-and-the-risk-of-pancreatic-cancer-a-case-control-study
#16
Livia Archibugi, Matteo Piciucchi, Serena Stigliano, Roberto Valente, Giulia Zerboni, Viola Barucca, Michele Milella, Patrick Maisonneuve, Gianfranco Delle Fave, Gabriele Capurso
Data on the association between aspirin and statin use and Pancreatic Ductal AdenoCarcinoma (PDAC) risk are conflicting. These drugs are often co-prescribed, but no studies evaluated the potential combined or confounding effect of the two at the same time. We aimed to investigate the association between aspirin and statin exclusive and combined use and PDAC occurrence. Data on environmental factors, family and medical history were screened in a case-control study. PDAC cases were matched to controls for age and gender...
October 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29025977/an-approach-to-discovering-novel-muscarinic-m1-receptor-positive-allosteric-modulators-with-potent-cognitive-improvement-and-minimized-gastrointestinal-dysfunction
#17
Emi Kurimoto, Satoru Matsuda, Yuji Shimizu, Yuu Sako, Takao Mandai, Takahiro Sugimoto, Hiroki Sakamoto, Haruhide Kimura
Activation of muscarinic M1 receptor (M1R) is a promising approach for improving cognitive impairment in Alzheimer's disease. However, an M1 selective positive allosteric modulator (PAM), benzyl quinolone carboxylic acid (BQCA), at 30 mg/kg, induced diarrhea in wild-type mice, but not in M1R knock-out mice. Moreover, BQCA (0.1-1000 nM) augmented electric field stimulation (EFS) -induced ileum contraction in an in vitro Magnus assay. Thus, we decided to establish a drug-screening strategy to discover novel M1 PAMs producing potent cognitive improvement with minimized gastrointestinal (GI) dysfunction...
October 12, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29025875/a-small-molecule-compound-inhibits-a-collagen-specific-molecular-chaperone-and-could-represent-a-potential-remedy-for-fibrosis
#18
Shinya Ito, Koji Ogawa, Koh Takeuchi, Motoki Takagi, Masahito Yoshida, Takatsugu Hirokawa, Shoshiro Hirayama, Kazuo Shin-Ya, Ichio Shimada, Takayuki Doi, Naoki Goshima, Tohru Natsume, Kazuhiro Nagata
Fibrosis can disrupt tissue structure and integrity and impair organ function. Fibrosis is characterized by abnormal collagen accumulation in the extracellular matrix. Pharmacological inhibition of collagen secretion therefore represents a promising strategy for the management of fibrotic disorders, such as liver and lung fibrosis. Hsp47 is an endoplasmic reticulum (ER)-resident collagen-specific molecular chaperone essential for correct folding of procollagen in the ER. Genetic deletion of Hsp47 or inhibition of its interaction with procollagen interferes with procollagen triple helix production, which vastly reduces procollagen secretion from fibroblasts...
October 12, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29024987/development-and-validation-of-an-eight-item-brief-form-of-the-soapp-r-soapp-8
#19
Ryan A Black, Stacey A McCaffrey, Albert J Villapiano, Robert N Jamison, Stephen F Butler
Objective: Although the Screener and Opioid Assessment for Patients with Pain-Revised (SOAPP-R) has become a widely used screener for aberrant opioid-related behavior in adults, the length of the instrument may limit its utility. The purpose of the current study was to develop a short form of the SOAPP-R by retaining as few items as possible while maximizing predictive accuracy. Methods: Participants (N = 555), recruited from pain clinics, completed the 24-item SOAPP-R and participated in a five-month follow-up visit to evaluate aberrant drug-related behaviors...
August 11, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/29024910/leishmanicidal-and-cytotoxic-activity-of-hederagenin-bistriazolyl-derivatives
#20
Diego Rodríguez-Hernández, Luiz C A Barbosa, Antonio J Demuner, Amalyn Nain-Perez, Sebastião R Ferreira, Ricardo T Fujiwara, Raquel M de Almeida, Lucie Heller, René Csuk
Aiming to obtain new potent leishmanicidal and cytotoxic compounds from natural sources, the triterpene hederagenin was converted into several new 1,2,3-triazolyl derivatives tethered at C-23 and C-28. For this work hederagenin was isolated from fruits of Sapindus saponaria and reacted with propargyl bromide to afford as a major product bis-propargylic derivative 1 in 74%. Submitting this compound to Huisgen 1,3-dipolar cycloaddition reactions with several azides afforded the derivatives 2-19 with yields in the range of 40-87%...
September 22, 2017: European Journal of Medicinal Chemistry
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