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https://www.readbyqxmd.com/read/29684941/opioid-deaths-in-milwaukee-county-wisconsin-2013-2017-the-primacy-of-heroin-and-fentanyl
#1
Brian L Peterson, Sara Schreiber, Nicole Fumo, E Brooke Lerner
Heroin and fentanyl are the overwhelming and increasing cause of opioid deaths in Milwaukee County, Wisconsin. We reviewed all drug and opioid deaths from 2013 to 2017 to delineate the specific opioid drugs involved and changes in their incidence. From 2013 to 2017, 980 deaths were due to opioids, rising from 184 in 2013 to 337 in 2017. In 2017, opioid deaths exceeded combined non-natural deaths from homicide and suicide. Illicit heroin and fentanyl/analogs caused 84% of opioid deaths and 80% of drug deaths, with no increase in deaths due to oral prescription drugs such as oxycodone and hydrocodone...
April 23, 2018: Journal of Forensic Sciences
https://www.readbyqxmd.com/read/29684931/-multiresistant-bacteria-antibiotic-prescription-and-antibiotics-of-last-resort
#2
Winfried V Kern
Ascertaining critical indications for antibiotics and rational prescribing can delay and minimize the spread of antibiotic resistance. Room for improvement lies in particular in a stricter indication, in shortening antibiotic treatment and in initiating more targeted therapies with narrow-spectrum drugs. Not all infections due to multidrug-resistant organisms require treatment with reserve drugs. Detailed susceptibility testing together with enhanced knowledge of pharmacokinetics and -dynamics are needed for adequate treatment decisions...
May 2018: Deutsche Medizinische Wochenschrift
https://www.readbyqxmd.com/read/29684851/mitochondrial-dna-content-reduction-induces-aerobic-glycolysis-and-reversible-resistance-to-drug-induced-apoptosis-in-sw480-colorectal-cancer-cells
#3
Jing-Jing Mou, Jin Peng, Ying-Ying Shi, Na Li, You Wang, Yuan Ke, Yun-Feng Zhou, Fu-Xiang Zhou
Mutations and reductions in mitochondrial DNA (mtDNA), which are frequent in human tumors, may contribute to enhancing their malignant phenotypes. However, the effects of mtDNA abnormalities in colorectal cancer remain largely unknown. In this study, mtDNA-reduced cell model was established by partial depletion of mtDNA in SW480 cells and the effects of mtDNA reduction in colorectal cancer cells were investigated. We found that mtDNA-reduced cells had enhanced glucose uptake and generated markedly higher level of lactate...
April 20, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29684709/the-role-of-natural-selection-in-shaping-genetic-variation-in-a-promising-chagas-disease-drug-target-trypanosoma-cruzi-trans-sialidase
#4
Joseph P Gallant, Raquel Asunción Lima-Cordón, Silvia Justi, Maria Carlota Monroy, Toni Viola, Lori Stevens
Rational drug design creates innovative therapeutics based on knowledge of the biological target to provide more effective and responsible therapeutics. Chagas disease, endemic throughout Latin America, is caused by Trypanosoma cruzi, a protozoan parasite. Current therapeutics are problematic with widespread calls for new approaches. Researchers are using rational drug design for Chagas disease and one target receiving considerable attention is the T. cruzi trans-sialidase protein (TcTS). In T. cruzi, trans-sialidase catalyzes the transfer of sialic acid from a mammalian host to coat the parasite surface membrane and avoid immuno-detection...
April 20, 2018: Infection, Genetics and Evolution
https://www.readbyqxmd.com/read/29684705/dual-tail-arylsulfone-based-benzenesulfonamides-differently-match-the-hydrophobic-and-hydrophilic-halves-of-human-carbonic-anhydrases-active-sites-selective-inhibitors-for-the-tumor-associated-hca-ix-isoform
#5
Hany S Ibrahim, Heba Abdelrasheed Allam, Walaa R Mahmoud, Alessandro Bonardi, Alessio Nocentini, Paola Gratteri, Eslam S Ibrahim, Hatem A Abdel-Aziz, Claudiu T Supuran
The synthesis and characterization of two new sets of arylsulfonehydrazone benzenesulfonamides (4a-4i with phenyl tail and 4j-4q with tolyl tail) are reported. The compounds were designed according to a dual-tails approach to modulate the interactions of the ligands portions at the outer rim of both hydrophobic and hydrophilic active site halves of human isoforms of carbonic anhydrase (CA, EC 4.2.1.1). The synthesized sulfonamides were evaluated in vitro for their inhibitory activity against the following human (h) isoforms, hCA I, II, IV and IX...
April 10, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29684685/the-identification-of-discontinuous-epitope-in-the-human-cystatin-c-monoclonal-antibody-hcc3-complex
#6
M Rafalik, M Spodzieja, A S Kołodziejczyk, S Rodziewicz-Motowidło, A Szymańska, A Grubb, P Czaplewska
Human cystatin C (hCC) is a cysteine proteinase inhibitor involved in pathophysiological processes of dimerization and amyloid formation. These processes are directly associated with a number of neurodegenerative disorders such as Alzheimer disease or hereditary cystatin C amyloid angiopathy (HCCAA). One of the ideas on how to prevent amyloid formation is to use immunotherapy. HCC3 is one of a group of antibodies binding to hCC and reducing the in vitro formation of cystatin C dimers. Therefore, identification of the binding sites in the hCC-HCC3 complex may facilitate a search of effective drugs against HCCAA as well as understanding the mechanisms of neurodegenerative disorders...
April 20, 2018: Journal of Proteomics
https://www.readbyqxmd.com/read/29684575/draft-genome-sequence-of-field-isolate-brucella-melitensis-strain-2007bm-1-from-india
#7
D K Singh, Bablu Kumar, Garima Shrinet, R P Singh, Aparajita Das, B G Mantur, Abhishek, Aruna Pandey, Piyali Mondal, B K Sajjanar, Soni Doimari, Vijayata Singh, Reena Kumari, A K Tiwari, Gandham Ravikumar
OBJECTIVES: Brucellosis, is among one of the most widespread important global zoonotic diseases which is endemic in many parts of India. Brucella melitensis is supposed to be the most pathogenic species for humans. Here, we report draft genome sequence of B. melitensis strain 2007BM/1 isolated from human in India. METHODS: Genomic DNA was extracted from Brucella culture and was sequenced using an Illumina MiSeq platform. The generated reads were assembled using three de novo assemblers and the draft genome was annotated...
April 20, 2018: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/29684553/fission-yeast-cells-overproducing-hset-kifc1-provides-a-useful-tool-for-identification-and-evaluation-of-human-kinesin-14-inhibitors
#8
Masashi Yukawa, Tomoaki Yamauchi, Naoaki Kurisawa, Shakil Ahmed, Ken-Ichi Kimura, Takashi Toda
Many human cancer cells contain more than two centrosomes, yet these cancer cells can form pseudo-bipolar spindles through the mechanism, called centrosome clustering, and survive, instead of committing lethal multipolar mitoses. Kinesin-14/HSET, a minus end-directed motor, plays a crucial role in centrosome clustering. Accordingly, HSET is deemed to be a promising chemotherapeutic target to selectively kill cancer cells. Recently, three HSET inhibitors (AZ82, CW069 and SR31527) have been reported, but their specificity and efficacy have not been evaluated rigorously...
April 20, 2018: Fungal Genetics and Biology: FG & B
https://www.readbyqxmd.com/read/29684498/multi-modal-characterization-of-vasculature-and-nanoparticle-accumulation-in-five-tumor-xenograft-models
#9
Einar Sulheim, Jana Kim, Annemieke van Wamel, Eugene Kim, Sofie Snipstad, Igor Vidic, Ingeborg Hovde Grimstad, Marius Widerøe, Sverre H Torp, Steinar Lundgren, David J Waxman, Catharina de Lange Davies
Preclinical research has demonstrated that nanoparticles and macromolecules can accumulate in solid tumors due to the enhanced permeability and retention effect. However, drug loaded nanoparticles often fail to show increased efficacy in clinical trials. A better understanding of how tumor heterogeneity affects nanoparticle accumulation could help elucidate this discrepancy and help in patient selection for nanomedicine therapy. Here we studied five human tumor models with varying morphology and evaluated the accumulation of 100 nm polystyrene nanoparticles...
April 20, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29684469/imaging-techniques-to-study-drug-transporter-function-in-vivo
#10
REVIEW
Nicolas Tournier, Bruno Stieger, Oliver Langer
Transporter systems involved in the permeation of drugs and solutes across biological membranes are recognized as key determinants of pharmacokinetics. Typically, the action of membrane transporters on drug exposure to tissues in living organisms is inferred from invasive procedures, which cannot be applied in humans. In recent years, imaging methods have greatly progressed in terms of instruments, synthesis of novel imaging probes as well as tools for data analysis. Imaging allows pharmacokinetic parameters in different tissues and organs to be obtained in a non-invasive or minimally invasive way...
April 20, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29684377/biphasic-modulation-of-camp-levels-by-the-contraceptive-nomegestrol-acetate-impact-on-p-glycoprotein-expression-and-activity-in-hepatic-cells
#11
Guillermo Nicolás Tocchetti, Camila Juliana Domínguez, Felipe Zecchinati, Maite Rocío Arana, María Laura Ruiz, Silvina Stella Maris Villanueva, Johanna Weiss, Aldo Domingo Mottino, Juan Pablo Rigalli
ABC transporters are key players in drug excretion with alterations in their expression and activity by therapeutic agents potentially leading to drug-drug interactions. The interaction potential of nomegestrol acetate (NMGA), a synthetic progestogen increasingly used as oral contraceptive, had never been explored. In this work we evaluated (1) the effect of NMGA on ABC transporters in the human hepatic cell line HepG2 and (2) the underlying molecular mechanism. NMGA (5, 50 and 500 nM) increased P-glycoprotein (P-gp) expression at both protein and mRNA levels and reduced intracellular calcein accumulation, indicating an increase also in transporter activity...
April 20, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29684118/spontaneous-endometriosis-in-cynomolgus-monkeys-as-a-clinically-relevant-experimental-model
#12
A Nishimoto-Kakiuchi, S Netsu, S Okabayashi, K Taniguchi, H Tanimura, A Kato, M Suzuki, T Sankai, R Konno
STUDY QUESTION: Does spontaneous endometriosis in cynomolgus monkeys have the characteristics required of a good experimental model? SUMMARY ANSWER: Spontaneous endometriosis in cynomolgus monkeys exhibited similar clinicopathological characteristics to the human disease and was useful as an experimental model. WHAT IS KNOWN ALREADY: The prevalence of endometriosis in autopsied cynomolgus monkeys (Macaca fascicularis) in a breeding colony was reported to be 28...
April 19, 2018: Human Reproduction
https://www.readbyqxmd.com/read/29684076/differences-in-labour-participation-between-people-living-with-hiv-and-the-general-population-results-from-spain-along-the-business-cycle
#13
Luz María Peña Longobardo, Juan Oliva-Moreno
BACKGROUND: HIV/AIDS (Human immunodeficiency virus/Acquired immune deficiency syndrome) not only has a strong impact on the health of the worldwide population but also affects the labour status of HIV-positive people. The primary aim of this paper is to compare the labour participation of people living with HIV (PlwHIV) with the labour participation of the general population along the last business cycle in Spain. METHOD: The data used are from the Hospital Survey on HIV-AIDS, with a total sample size of 4,651 PlwHIV and the Labour Force Survey from 2001 to 2010, with a total sample size of 660,674 individuals as general population...
2018: PloS One
https://www.readbyqxmd.com/read/29683800/generation-and-characterization-of-a-paclitaxel-resistant-human-gastric-carcinoma-cell-line
#14
Ling Fu, Fen Yin, Xiao-Rui Li, Bing-Kai Han, Chuang Zhang, Jun-Wei Wang, Yu-Qing Wang, Yue-Feng Bi, Hong-Min Liu
The main aim of this study was to establish a novel paclitaxel (PTX)-resistant human gastric carcinoma cell line and to investigate its biological significance. A cell line, MGC803/PTX, was established by gradually increasing PTX density on the basis of MGC803 over a period of 10 months. In addition, a pair of resistant cell lines (SW620 and SW620/PTX) were added to further explain the resistant mechanism of PTX. The drug resistance index and stability of MGC803/PTX cells were detected using the Cell Counting Kit-8 method...
April 20, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29683659/the-identification-of-potent-selective-and-orally-available-inhibitors-of-ataxia-telangiectasia-mutated-atm-kinase-the-discovery-of-azd0156-8-6-3-dimethylamino-propoxy-pyridin-3-yl-3-methyl-1-tetrahydro-2h-pyran-4-yl-1-3-dihydro-2h-imidazo-4-5-c-quinolin-2
#15
Kurt G Pike, Bernard Barlaam, Elaine Cadogan, Andrew Campbell, Yingxue Chen, Nicola Colclough, Nichola L Davies, Camila DeAlmeida, Sébastien L Degorce, Myriam Didelot, Allan Dishington, Richard Ducray, Stephen T Durant, Lorraine A Hassall, Jane L Holmes, Gareth D Hughes, Philip A MacFaul, Keith R Mulholland, Thomas M McGuire, Gilles Ouvry, Martin Pass, Graeme R Robb, Natalie Stratton, Zhenhua Wang, Joanne Wilson, Baochang Zhai, Kang Zhao, Nidal Al-Huniti
ATM inhibitors, such as 7, have demonstrated the anti-tumor potential of ATM inhibition when combined with DNA double strand break-inducing agents in mouse xenograft models. However, the properties of 7 result in a relatively high predicted clinically efficacious dose. In an attempt to minimize attrition during clinical development we sought to identify ATM inhibitors with a low predicted clinical dose (<50 mg) and focussed on strategies to increase both ATM potency and predicted human pharmacokinetic half-life (predominantly through the increase of volume of distribution)...
April 23, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29683402/identification-and-evaluation-of-bioactive-natural-products-as-potential-inhibitors-of-human-microtubule-affinity-regulating-kinase-4-mark4
#16
Taj Mohammad, Faez Iqbal Khan, Kevin A Lobb, Asimul Islam, Faizan Ahmad, Md Imtaiyaz Hassan
Microtubule affinity-regulating kinase 4 (MARK4) has recently been identified as a potential drug target for several complex diseases including cancer, diabetes and neurodegenerative disorders. Inhibition of MARK4 activity is an appealing therapeutic option to treat such diseases. Here, we have performed structure-based virtual high-throughput screening of 100,000 naturally occurring compounds from ZINC database against MARK4 to find its potential inhibitors. The resulted hits were selected based on the binding affinities, docking scores and selectivity...
April 23, 2018: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29683392/synthetic-polymannose-as-a-drug-carrier-synthesis-toxicity-and-anti-fungal-activity-of-polymannose-amphotericin-b-conjugates
#17
Arul Prakash Francis, Sneha Gurudevan, A Jayakrishnan
Polymannose (PM) having a weight-average molar mass (Mw ) of 30-53 kDa was synthesized by the polycondensation of mannose using phosphorous acid as the catalyst and characterized by various techniques such as NMR, IR, GPC and polarimetry. 2D NMR results confirmed the presence of (1→ 6)-linked α-D-mannose residues as backbone with O-3 and O-2 substituted linear or branched chains in PM. Amphotericin B (AmB) was conjugated to periodate-oxidized PM through Schiff's linkages at 20 wt% concentration. The AmB-PM conjugates were highly soluble in phosphate buffered saline (180-250 mg/mL), exhibited negligible hemolytic potential to human erythrocytes even at a concentration of 200 μg /mL (equivalent to ~ 40 μg/mL AmB) and were non-toxic to human embryonic kidney (HEK293T) cells even at a concentration of 250 μg/mL (equivalent to ~ 50 μg/mL AmB)...
April 23, 2018: Journal of Biomaterials Science. Polymer Edition
https://www.readbyqxmd.com/read/29683096/novel-anthraquinone-derivatives-as-dual-inhibitors-of-topoisomerase-2-and-casein-kinase-2-in-silico-studies-synthesis-and-biological-evaluation-on-leukemic-cell-lines
#18
Abbas Kabir, Kalpana Tilekar, Neha Upadhyay, C S Ramaa
Background - Cancer being a complex disease, single targeting agents remains unsuccessful. This calls for "multiple targeting", wherein a single drug is so designed that it will modulate the activity of multiple protein targets. Topoisomerase 2 (Top2) helps in removing DNA tangles and super-coiling during cellular replication, Casein Kinase 2 (CK2) is involved in the phosphorylation of multitude of protein targets. Thus, in the present work, we have tried to develop dual inhibitors of Top2 and CK2...
April 22, 2018: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29682967/in-vivo-two-photon-fluorescence-imaging-of-the-activity-of-the-inflammatory-biomarker-lta4h-in-a-mouse-pneumonia-model
#19
Hui Wang, Ke Xue, Ping Li, Yuyun Yang, Zixu He, Wei Zhang, Wen Zhang, Bo Tang
Severe atmospheric haze caused by industrial pollution has severely affected human health and led to the increasing incidence of cardiopulmonary diseases, including pneumonia. Conventional methods for diagnosis of pneumonia are complicated and tedious, and current clinical imaging techniques might cause organ injuries to some extent. Therefore, an accurate, fast, and intact imaging method must be developed to diagnose pneumonia in the early stages. In this study, we propose a new two-photon fluorescence probe, named as ASPC, for detection of the activity of the inflammatory biomarker LTA4H through specific recognition and cleavage of amides containing the unnatural amino acid L-AspBzl...
April 23, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29682682/molecular-and-clinical-roles-of-incretin-based-drugs-in-patients-with-heart-failure
#20
REVIEW
Bassant Orabi, Rasha Kaddoura, Amr S Omar, Cornelia Carr, Abdulaziz Alkhulaifi
Glucagon-like peptide-1 (GLP-1) agonists and dipeptidyl peptidase-4 (DPP-4) inhibitors produce some beneficial and deleterious effects in diabetic patients not mediated by their glycemic lowering effects, and there is a need for better understanding of the molecular basis of these effects. They possess antioxidant and anti-inflammatory effects with some direct vasodilatory action (animal and human trial data) that may indirectly influence heart failure (HF). Unlike GLP-1R agonists, signaling for HF adverse effects was observed with two DPP-4 inhibitors, saxagliptin and alogliptin...
April 23, 2018: Heart Failure Reviews
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