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https://www.readbyqxmd.com/read/28528302/nanomolar-anti-sickling-compounds-identified-by-ligand-based-pharmacophore-approach
#1
Odailson Santos Paz, Milena de Jesus Pinheiro, Renan Fernandes do Espirito Santo, Cristiane Flora Villarreal, Marcelo Santos Castilho
Adenosine receptors are considered as potential targets for drug development against several diseases. The discovery of subtype 2B adenosine receptors role in erythrocyte sickling process proved its importance to neglected diseases such as sickle cell anemia, which affects approximately 29.000 people around the world, but whose treatment is restricted to just one FDA approved drug (hydroxyurea). In order to widen the therapeutic arsenal available to treat sickle cell anemia patients, it is imperative to identify new lead compounds that modify the sickling course and not just its symptoms...
May 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28528115/alcohol-and-other-substance-use-after-bariatric-surgery-prospective-evidence-from-a-u-s-multicenter-cohort-study
#2
Wendy C King, Jia-Yuh Chen, Anita P Courcoulas, Gregory F Dakin, Scott G Engel, David R Flum, Marcelo W Hinojosa, Melissa A Kalarchian, Samer G Mattar, James E Mitchell, Alfons Pomp, Walter J Pories, Kristine J Steffen, Gretchen E White, Bruce M Wolfe, Susan Z Yanovski
BACKGROUND: Empirical evidence suggests Roux-en-Y gastric bypass (RYGB) increases risk of developing alcohol use disorder (AUD). However, prospective assessment of substance use disorders (SUD) after bariatric surgery is limited. OBJECTIVE: To report SUD-related outcomes after RYGB and laparoscopic adjustable gastric banding (LAGB). To identify factors associated with incident SUD-related outcomes. SETTING: 10 U.S. hospitals METHODS: The Longitudinal Assessment of Bariatric Surgery-2 is a prospective cohort study...
March 31, 2017: Surgery for Obesity and related Diseases: Official Journal of the American Society for Bariatric Surgery
https://www.readbyqxmd.com/read/28527817/lymphatic-filariasis-elimination-efforts-in-rufiji-south-eastern-tanzania-decline-in-circulating-filarial-antigen-prevalence-in-young-school-children-after-twelve-rounds-of-mass-drug-administration-and-utilization-of-long-lasting-insecticide-treated-nets
#3
Clarer Jones, Billy Ngasalla, Yahya A Derua, Donath Tarimo, Mwelecele N Malecela
BACKGROUND: Lymphatic filariasis (LF) is a parasitic infection transmitted by mosquito vectors and in sub Saharan Africa it is caused by nematode Wuchereria bancrofti. The disease has been targeted for global elimination by using annual mass drug administration (MDA) strategy. On the other hand, vector control is known to play important complementary role to the MDAs in reducing LF transmission. We report the findings of the effect of MDA and ITNs intervention implemented in endemic area of south-eastern Tanzania METHODS: A cross-sectional study for W...
May 17, 2017: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/28527783/identification-of-novel-selective-p2y6-receptor-antagonists-by-high-throughput-screening-assay
#4
Masaaki Ito, Shin-Ichiro Egashira, Kazuki Yoshida, Tomoko Mineno, Kazuo Kumagai, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Michio Ui, Isao Matsuoka
AIMS: The P2Y6 nucleotide receptor is widely involved in inflammatory responses, and is a promising molecular target for the treatment of inflammatory diseases. Although several P2Y6 receptor antagonists have been developed and evaluated thus far, none has successfully been developed into a therapeutic drug. In this study, we explored new promising compounds that inhibit the human P2Y6 receptor. MAIN METHODS: High-throughput screening (HTS) was used to study the effects of various compounds on human P2Y6 receptors expressed in 1321N1 human astrocytoma cells by monitoring intracellular Ca(2+) concentration ([Ca(2+)]i) levels using an FDSS7000 real-time fluorescence detector...
May 17, 2017: Life Sciences
https://www.readbyqxmd.com/read/28527704/anti-madcam-antibody-pf-00547659-for-ulcerative-colitis-turandot-a-phase-2-randomised-double-blind-placebo-controlled-trial
#5
Séverine Vermeire, William J Sandborn, Silvio Danese, Xavier Hébuterne, Bruce A Salzberg, Maria Klopocka, Dino Tarabar, Tomas Vanasek, Miloš Greguš, Paul A Hellstern, Joo Sung Kim, Miles P Sparrow, Kenneth J Gorelick, Michelle Hinz, Alaa Ahmad, Vivek Pradhan, Mina Hassan-Zahraee, Robert Clare, Fabio Cataldi, Walter Reinisch
BACKGROUND: PF-00547659 is a fully human monoclonal antibody that binds to human mucosal addressin cell adhesion molecule-1 (MAdCAM-1) to selectively reduce lymphocyte homing to the intestinal tract. We aimed to assess the efficacy and safety of PF-00547659 in patients with moderate to severe ulcerative colitis. METHODS: This phase 2, randomised, double-blind, placebo-controlled clinical trial recruited patients aged 18-65 years from 105 centres in 21 countries, with a history (≥3 months) of active ulcerative colitis extending more than 15 cm beyond the anal verge (with a total Mayo score ≥6 and a Mayo endoscopic subscore ≥2) who had failed or were intolerant to at least one conventional therapy...
May 17, 2017: Lancet
https://www.readbyqxmd.com/read/28526972/patient-experiences-attitudes-and-expectations-towards-receiving-information-about-anti-tnf-medication-a-quantitative-study
#6
Jon Packham, Paul Arkell, Tom Sheeran, Ann Brownfield, Anthony Cadwgan, Sarah Ryan
The objective of the study was to measure patient attitudes and experience of information received during drug counselling for rheumatoid arthritis (RA) medications. This is a cross-sectional UK postal questionnaire study. Three RA patient groups-disease-modifying antirheumatic drugs (DMARDs) only, first anti-tumour necrosis factor (anti-TNF) and failed anti-TNF-were sent postal questionnaires. Data on patient history/demographics, drug counselling experience, knowledge of drug side effects, attitudes to vaccinations, cancer screening and blood borne virus testing was collected; 264/679 (39%) patients responded (median age 65 years, 66% female, median disease duration 15 years)...
May 19, 2017: Clinical Rheumatology
https://www.readbyqxmd.com/read/28526932/inpatient-addiction-consultation-for-hospitalized-patients-increases-post-discharge-abstinence-and-reduces-addiction-severity
#7
Sarah E Wakeman, Joshua P Metlay, Yuchiao Chang, Grace E Herman, Nancy A Rigotti
BACKGROUND: Alcohol and drug use results in substantial morbidity, mortality, and cost. Individuals with alcohol and drug use disorders are overrepresented in general medical settings. Hospital-based interventions offer an opportunity to engage with a vulnerable population that may not otherwise seek treatment. OBJECTIVE: To determine whether inpatient addiction consultation improves substance use outcomes 1 month after discharge. DESIGN: Prospective quasi-experimental evaluation comparing 30-day post-discharge outcomes between participants who were and were not seen by an addiction consult team during hospitalization at an urban academic hospital...
May 19, 2017: Journal of General Internal Medicine
https://www.readbyqxmd.com/read/28526447/toxicity-screening-of-a-novel-poly-methylmethacrylate-eudragit-nanocarrier-on-l929-fibroblasts
#8
Diogo Graça, Henriqueta Louro, Joana Santos, Kamila Dias, Lídia Gonçalves, António Almeida, Maria João Silva, Ana Bettencourt
Toxicity screening of a novel poly(methylmethacrylate)-Eudragit nanocarrier on L929 fibroblasts Translation of innovative drug delivery nanosystems into the market involves an early toxicity screening in the development phase. Previously, we showed that inclusion of the polymer (Eudragit, EUD) into poly(methylmethacrylate) (PMMA) nanoparticles (NP) resulted in a novel nanocarrier (PMMA-EUD) with an improved biomedical performance. The safety of this novel nanoparticulate system (PMMA-EUDNPs) was assessed in this work and compared to that of the original PMMANPs by using an integrated approach, comprising in vitro toxicity assessment and NPs physicochemical characterization in water and cell medium...
May 16, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28526075/testing-times-trends-in-availability-price-and-market-share-of-malaria-diagnostics-in-the-public-and-private-healthcare-sector-across-eight-sub-saharan-african-countries-from-2009-to-2015
#9
Kara Hanson, Catherine Goodman
BACKGROUND: The World Health Organization guidelines have recommended that all cases of suspected malaria should receive a confirmatory test with microscopy or a malaria rapid diagnostic test (RDT), however evidence from sub-Saharan Africa (SSA) illustrates that only one-third of children under five with a recent fever received a test. The aim of this study was to evaluate availability, price and market share of microscopy and RDT from 2009/11 to 2014/15 in 8 SSA countries, to better understand barriers to improving access to malaria confirmatory testing in the public and private health sectors...
May 19, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28525527/is-it-useful-to-add-acetaminophen-to-high-potency-opioids-in-cancer-related-pain
#10
Oscar Corsi, Pedro E Pérez-Cruz
Pain is one of the most frequent and relevant symptoms in cancer patients. The World Health Organization's analgesic ladder proposes the use of strong opioids associated with adjuvants such as acetaminophen or nonsteroidal anti-inflammatory drugs in step III. However, it is unclear whether adding acetaminophen to an analgesic regimen based on strong opioids has any benefit in cancer patients with moderate to severe pain. To answer this question we searched in Epistemonikos database, which is maintained by screening multiple information sources...
May 4, 2017: Medwave
https://www.readbyqxmd.com/read/28525356/synthesis-biological-activity-and-molecular-modeling-study-of-new-schiff-bases-incorporated-with-indole-moiety
#11
Ahmed H Halawa, Shimaa Mohamed Abd El-Gilil, Ahmed H Bedair, Mohamed Shaaban, Marcel Frese, Norbert Sewald, Essam M Eliwa, Ahmed M El-Agrody
A new series of heterocyclic Schiff bases 2-9 containing indole moiety were synthesized by facile and efficient condensation of indole-3/2/5-carboxaldehyde (1a/1b/1c) with different aromatic and heterocyclic primary amines using conventional and/or microwave irradiation methods. The structures of the obtained compounds were assigned by sophisticated spectroscopic and spectrometric techniques (1D-NMR, 2D-NMR and MS). The synthesized compounds were screened for their cytotoxicity and antibacterial activities...
May 18, 2017: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
https://www.readbyqxmd.com/read/28525328/establishment-of-5-fluorouracil-resistant-canine-mammary-tumor-cell-line
#12
B Zhou, D Zhang, S M Pei, H Zhang, H C Du, Y P Jin, D G Lin
Canine mammary tumors are the most common neoplasms in intact female dogs. The surgery cannot always solve the problem, chemotherapy are recommend to these patients. However, chemotherapy could always fail because of multidrug resistance (MDR). Through stepwise increasing 5-Fluorouracil (5-FU) concentration in the culture medium, a 5-FU-resistant canine mammary tumor cell line CMT7364/5-FU was established to disclose the molecular mechanism of the drug resistance. Cell morphology, cell sensitivity to drugs, growth curves, expression of proteins, and chemo-sensitivity in vivo were compared between the parental cell line and resistant cell line...
March 28, 2017: Polish Journal of Veterinary Sciences
https://www.readbyqxmd.com/read/28525268/rational-design-of-novel-allosteric-dihydrofolate-reductase-inhibitors-showing-antibacterial-effects-on-drug-resistant-e-coli-escape-variants
#13
Bharath Srinivasan, João V Rodrigues, Sam Tonddast-Navaei, Eugene Shakhnovich, Jeffrey Skolnick
In drug-discovery, systematic variations of substituents on a common scaffold and bioisosteric replacements are often used to generate diversity and obtain molecules with better biological effects. However, this could saturate the small-molecule diversity pool resulting in drug-resistance. On the other hand, conventional drug-discovery relies on targeting known pockets on protein surfaces leading to drug resistance by mutations of critical pocket residues. Here, we present a two-pronged strategy of designing novel drugs that target unique pockets on a protein's surface to overcome the above problems...
May 19, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28525267/the-supernatant-from-hepatocyte-cultures-with-drugs-that-cause-idiosyncratic-liver-injury-activates-macrophage-inflammasomes
#14
Ryuji Kato, Jack Uetrecht
There is increasing evidence that most idiosyncratic drug-induced liver injury (IDILI) is immune mediated, and in most cases reactive metabolites appear to be responsible for induction of this immune response. Reactive metabolites can cause cell damage with the release of damage-associated molecular patterns (DAMPs), which is thought to be involved in immune activation. Presumably the reason that the liver is a common target of idiosyncratic drug reactions is because it is the major site of drug metabolism and reactive metabolite formation...
May 19, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28524801/association-of-ugt2b7-ugt1a9-abcg2-and-il23r-polymorphisms-with-rejection-risk-in-kidney-transplant-patients
#15
Heloísa Lizotti Cilião, Rossana Batista Oliveira Camargo-Godoy, Marilesia Ferreira de Souza, Mariana Bisarro Dos Reis, Lorena Iastrenski, Vinicius Daher Alvares Delfino, Silvia Regina Rogatto, Ilce Mara de Syllos Cólus
Despite advances in testing compatibility between donor and recipient, graft rejection remains a current concern. Single-nucleotide polymorphisms (SNPs) that codify altered enzymes of metabolism, drug transport, and the immune system may contribute to graft rejection in transplant patients. This study examined the association between SNPs present in genes of these processes and occurrence of graft rejection episodes in 246 kidney transplant patients, 35% of which were diagnosed with rejection. Genotype-gene expression associations were also assessed...
May 19, 2017: Journal of Toxicology and Environmental Health. Part A
https://www.readbyqxmd.com/read/28524758/seeking-safety-group-therapy-for-co-occurring-substance-use-disorder-and-ptsd-among-transgender-women-living-with-hiv-a-pilot-study
#16
Susannah Empson, Yvette P Cuca, Jennifer Cocohoba, Carol Dawson-Rose, Katy Davis, Edward L Machtinger
Transgender women living with HIV experience high rates of substance use, violence, and post-traumatic stress disorder (PTSD). Seeking Safety is a manualized, present-focused, cognitive-behavioral therapy program designed to address co-occurring substance use and PTSD. Seeking Safety has evidence of efficacy in a variety of populations but had not been evaluated specifically with people living with HIV or transgender women. We pilot-tested a 12-session Seeking Safety program with a group of transgender women living with HIV who reported substance use and a history of violence...
May 19, 2017: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/28524719/polyester-based-microdisc-systems-for-sustained-release-of-neuroprotective-phosphine-borane-complexes
#17
David A Janus, Christopher J Lieven, Megan E Crowe, Leonard A Levin
Phosphine-borane complexes are recently developed redox-active drugs that are neuroprotective in models of optic nerve injury and radioprotective in endothelial cells. However, a single dose of these compounds is short-lived, necessitating development of sustained-release formulations of these novel molecules. We screened a library of biodegradable co- and non-block polyester polymer systems for release of incorporated phosphine-borane complexes to evaluate them as drug delivery systems for use in chronic disease...
May 19, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28524181/common-pitfalls-in-preclinical-cancer-target-validation
#18
REVIEW
William G Kaelin
An alarming number of papers from laboratories nominating new cancer drug targets contain findings that cannot be reproduced by others or are simply not robust enough to justify drug discovery efforts. This problem probably has many causes, including an underappreciation of the danger of being misled by off-target effects when using pharmacological or genetic perturbants in complex biological assays. This danger is particularly acute when, as is often the case in cancer pharmacology, the biological phenotype being measured is a 'down' readout (such as decreased proliferation, decreased viability or decreased tumour growth) that could simply reflect a nonspecific loss of cellular fitness...
May 19, 2017: Nature Reviews. Cancer
https://www.readbyqxmd.com/read/28524079/assembly-of-hepatocyte-spheroids-using-magnetic-3d-cell-culture-for-cyp450-inhibition-induction
#19
Pujan K Desai, Hubert Tseng, Glauco R Souza
There is a significant need for in vitro methods to study drug-induced liver injury that are rapid, reproducible, and scalable for existing high-throughput systems. However, traditional monolayer and suspension cultures of hepatocytes are difficult to handle and risk the loss of phenotype. Generally, three-dimensional (3D) cell culture platforms help recapitulate native liver tissue phenotype, but suffer from technical limitations for high-throughput screening, including scalability, speed, and handling. Here, we developed a novel assay for cytochrome P450 (CYP450) induction/inhibition using magnetic 3D cell culture that overcomes the limitations of other platforms by aggregating magnetized cells with magnetic forces...
May 18, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28524077/highly-stereoselective-synthesis-of-a-compound-collection-based-on-the-bicyclic-scaffolds-of-natural-products
#20
Murali Annamalai, Stanimira Hristeva, Martyna Bielska, Raquel Ortega, Kamal Kumar
Despite the great contribution of natural products in the history of successful drug discovery, there are significant limitations that persuade the pharmaceutical industry to evade natural products in drug discovery research. The extreme scarcity as well as structural complexity of natural products renders their practical synthetic access and further modifications extremely challenging. Although other alternative technologies, particularly combinatorial chemistry, were embraced by the pharmaceutical industry to get quick access to a large number of small molecules with simple frameworks that often lack three-dimensional complexity, hardly any success was achieved in the discovery of lead molecules...
May 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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