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https://www.readbyqxmd.com/read/28721686/rationale-for-initiation-and-titration-of-the-basal-insulin-glp-1ra-fixed-ratio-combination-products-ideglira-and-iglarlixi-for-the-management-of-type-2-diabetes
#1
REVIEW
Virginia Valentine, Jennifer Goldman, Jay H Shubrook
Type 2 diabetes (T2D) is a progressive disease affecting glucose regulation and a major cause of morbidity and mortality globally. Many patients are not escalated up the treatment ladder appropriately despite failing to achieve glycemic control, with barriers such as fear of hypoglycemia, weight gain, and treatment burden recognized as factors. Exogenous basal insulin is titrated to address control of fasting plasma glucose and may preserve residual β-cell function, thus promoting a greater endogenous prandial insulin response...
July 18, 2017: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/28721281/safety-and-efficacy-of-tamsulosin-alfuzosin-or-silodosin-as-monotherapy-for-luts-in-bph-a-double-blind-randomized-trial
#2
Chikka Moga Siddaiah Manohar, Mahadevappa Nagabhushana, Vilvapathy Senguttuvan Karthikeyan, Ramachandra Pudakalkatti Sanjay, Ananth Janardhan Kamath, Ramaiah Keshavamurthy
INTRODUCTION: Currently alpha1-adrenoceptor blockers (AB) are widely used as first-line therapy to improve lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH). We compared the efficacy and safety profile of tamsulosin, alfuzosin and silodosin in LUTS due to BPH. MATERIAL AND METHODS: Consecutive consenting male patients (N = 269) undergoing medical management of BPH with AB from February 2012 to October 2015 were enrolled. Patients were randomized to a 0...
June 30, 2017: Central European Journal of Urology
https://www.readbyqxmd.com/read/28720838/the-efficacy-and-safety-of-sugammadex-for-reversing-postoperative-residual-neuromuscular-blockade-in-pediatric-patients-a-systematic-review
#3
Guangyu Liu, Rui Wang, Yanhong Yan, Long Fan, Jixiu Xue, Tianlong Wang
The aim of this study is to evaluate the efficacy and safety of sugammadex for reversing neuromuscular blockade in pediatric patients. MEDLINE and other three Databases were searched. Randomized clinical trials were included if they compared sugammadex with neostigmine or placebo in pediatric patients undergoing surgery involving the use of rocuronium or vecuronium. The primary outcome was the time interval from administration of reversal agents to train-of-four ratio (TOFr, T4/T1) > 0.9. Incidences of any drug-related adverse events were secondary outcomes...
July 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28720734/lack-of-acrb-efflux-function-confers-loss-of-virulence-on-salmonella-enterica-serovar-typhimurium
#4
Xuan Wang-Kan, Jessica M A Blair, Barbara Chirullo, Jonathan Betts, Roberto M La Ragione, Alasdair Ivens, Vito Ricci, Timothy J Opperman, Laura J V Piddock
AcrAB-TolC is the paradigm resistance-nodulation-division (RND) multidrug resistance efflux system in Gram-negative bacteria, with AcrB being the pump protein in this complex. We constructed a nonfunctional AcrB mutant by replacing D408, a highly conserved residue essential for proton translocation. Western blotting confirmed that the AcrB D408A mutant had the same native level of expression of AcrB as the parental strain. The mutant had no growth deficiencies in rich or minimal medium. However, compared with wild-type SL1344, the mutant had increased accumulation of Hoechst 33342 dye and decreased efflux of ethidium bromide and was multidrug hypersusceptible...
July 18, 2017: MBio
https://www.readbyqxmd.com/read/28720134/in-vitro-antioxidant-and-antimalarial-activities-of-leaves-pods-and-bark-extracts-of-acacia-nilotica-l-del
#5
Muhammad Bilal Sadiq, Pattamon Tharaphan, Kesinee Chotivanich, Joel Tarning, Anil Kumar Anal
BACKGROUND: The emergence of drug resistant malaria is threatening our ability to treat and control malaria in the Southeast Asian region. There is an urgent need to develop novel and chemically diverse antimalarial drugs. This study aimed at evaluating the antimalarial and antioxidant potentials of Acacia nilotica plant extracts. METHODS: The antioxidant activities of leaves, pods and bark extracts were determined by standard antioxidant assays; reducing power capacity, % lipid peroxidation inhibition and ferric reducing antioxidant power assay...
July 18, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28719813/comparative-stability-indicating-chromatographic-methods-for-determination-of-4-hexylresorcinol-in-pharmaceutical-formulation-and-shrimps
#6
Rafeek F Shokry, Lories I Bebawy, Mohamed R Elghobashy, Samah S Abbas
Three chromatographic stability-indicating methods were developed for determination of 4-hexylresorcinol in pure form and in a pharmaceutical formulation. Method A was based on a gradient elution liquid chromatographic HPLC determination of 4-hexylresorcinol, its related impurities and in presence of its degradation products. UPLC-MS/MS (Method B) was described for determination of the cited drug in presence of its degradation products. Method C was a thin- layer chromatography (TLC)-densitometry method for the separation and determination of the active ingredient, one of its related impurities and in presence of its degradation products...
July 8, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28719378/chemical-stability-of-morphine-ropivacaine-and-ziconotide-in-combination-for-intrathecal-analgesia
#7
Julien Robert, Jérémy Sorrieul, Elsa Rossignol, Hélène Beaussart, Hélène Kieffer, Caroline Folliard, Denis Dupoiron, Catherine Devys
Pain is the most feared symptom amongst individuals living with cancer. In 15% to 20% of patients, conventional analgesic therapy either fails to relieve pain or induces adverse effects. Intrathecal drug delivery systems may present an effective alternative for pain management. The Cancerology Center Paul Papin protocol includes an admixture of morphine, ropivacaine, and ziconotide in intrathecal preparations. These drugs are administered by a fully implantable or an external pump. Syringes or polyolefin infusion bags are prepared for refill just before use...
July 2017: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28719180/heterologous-expression-purification-and-functional-analysis-of-plasmodium-falciparum-phosphatidylinositol-3-kinase
#8
Matthew Hassett, Anna Sternberg, Bryce Riegel, Craig J Thomas, Paul David Roepe
The Plasmodium falciparum malarial parasite genome appears to encode one and only one phosphatidylinositol 3'-kinase (PI3K) and sequence analysis suggests that the enzyme is a "class III" or "Vps34" type PI3K. The PfVps34 has generated excitement as a possible druggable target and potentially a key target of artemisinin-based antimalarials. In this study, we optimize the PfVps34 gene for heterologous expression in yeast, purify the protein to homogeneity, use a recently validated quantitative assay for phosphatidylinositol 3'-phosphate (PI3P) production from phosphatidylinositol (PI) (Hassett et al...
July 18, 2017: Biochemistry
https://www.readbyqxmd.com/read/28718812/therapeutic-efficacy-of-the-novel-stimuli-sensitive-nano-ferritins-containing-doxorubicin-in-a-head-and-neck-cancer-model
#9
Verena Damiani, Elisabetta Falvo, Giulio Fracasso, Luca Federici, Martina Pitea, Vincenzo De Laurenzi, Gianluca Sala, Pierpaolo Ceci
Doxorubicin is employed alone or in combination for the treatment of several hematological and solid malignancies; despite its efficacy, there are associated cardiotoxicity limits both in its application in patients with heart disease risk factors and also in its long-term use. HFt-MP-PAS40 is a genetically engineered human ferritin heavy chain (HFt)-based construct able to efficiently entrap and deliver doxorubicin to cancer cells. HF-MP-PAS contains a short motif sequence (defined as MP) responsive to proteolytic cleavage by tumor matrix metalloproteases (MMPs), located between each HFt subunit and a masking polypeptide sequence rich in proline (P), alanine (A), and serine (S) residues (PAS)...
July 18, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28718624/covalent-enzyme-inhibition-through-fluorosulfate-modification-of-a-non-catalytic-serine-residue
#10
Olugbeminiyi O Fadeyi, Lise R Hoth, Chulho Choi, Xidong Feng, Ariamala Gopalsamy, Erik C Hett, Robert E Kyne, Ralph P Robinson, Lyn H Jones
Irreversible enzyme inhibitors often utilize the reaction of a protein cysteine residue with an appropriately positioned electrophile (an acrylamide for example) in the ligand template. Cysteine residues are not always available for site-specific protein labeling and therefore new approaches are needed to expand the toolkit of appropriate electrophiles that target alternative amino acids. We have previously described the rational targeting of tyrosine residues in the active site of a protein (the mRNA decapping scavenger enzyme, DcpS) using inhibitors armed with sulfonyl fluoride electrophiles that additionally enabled the subsequent development of clickable probe technology to measure drug-target occupancy in live cells...
July 18, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28717873/orchestration-of-h3k27-methylation-mechanisms-and-therapeutic-implication
#11
REVIEW
Mei-Ren Pan, Ming-Chuan Hsu, Li-Tzong Chen, Wen-Chun Hung
Histone proteins constitute the core component of the nucleosome, the basic unit of chromatin. Chemical modifications of histone proteins affect their interaction with genomic DNA, the accessibility of recognized proteins, and the recruitment of enzymatic complexes to activate or diminish specific transcriptional programs to modulate cellular response to extracellular stimuli or insults. Methylation of histone proteins was demonstrated 50 years ago; however, the biological significance of each methylated residue and the integration between these histone markers are still under intensive investigation...
July 17, 2017: Cellular and Molecular Life Sciences: CMLS
https://www.readbyqxmd.com/read/28717654/fusion-to-flaviviral-leader-peptide-targets-hiv-1-reverse-transcriptase-for-secretion-and-reduces-its-enzymatic-activity-and-ability-to-induce-oxidative-stress-but-has-no-major-effects-on-its-immunogenic-performance-in-dna-immunized-mice
#12
Anastasia Latanova, Stefan Petkov, Yulia Kuzmenko, Athina Kilpeläinen, Alexander Ivanov, Olga Smirnova, Olga Krotova, Sergey Korolev, Jorma Hinkula, Vadim Karpov, Maria Isaguliants, Elizaveta Starodubova
Reverse transcriptase (RT) is a key enzyme in viral replication and susceptibility to ART and a crucial target of immunotherapy against drug-resistant HIV-1. RT induces oxidative stress which undermines the attempts to make it immunogenic. We hypothesized that artificial secretion may reduce the stress and make RT more immunogenic. Inactivated multidrug-resistant RT (RT1.14opt-in) was N-terminally fused to the signal providing secretion of NS1 protein of TBEV (Ld) generating optimized inactivated Ld-carrying enzyme RT1...
2017: Journal of Immunology Research
https://www.readbyqxmd.com/read/28717247/characterization-of-hiv-1-integrase-interaction-with-human-ku70-protein-and-initial-implications-for-drug-targeting
#13
Andrey N Anisenko, Ekaterina S Knyazhanskaya, Artur O Zalevsky, Julia Yu Agapkina, Aleksander I Sizov, Timofey S Zatsepin, Marina B Gottikh
Human Ku70/Ku80 protein is known to influence HIV-1 replication. One of the possible reasons may be the protection of integrase from proteasomal degradation by Ku70 subunit. We demonstrated that recombinant HIV-1 integrase and Ku70 form a stable complex, while no interaction of Ku70 with integrase from prototype foamy virus was observed. By analyzing protein subdomains we determined two binding sites in the structure of both Ku70 and integrase: the 51-160 a.a. region of integrase interacts with residues 251-438 of Ku70, whereas Ku70 N-terminal domain (1-250 a...
July 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28716729/study-of-new-interactions-of-glitazone-s-stereoisomers-and-the-endogenous-ligand-15d-pgj2-on-six-different-ppar-gamma-proteins
#14
Samuel Álvarez-Almazán, Martiniano Bello, Feliciano Tamay-Cach, Marlet Martínez-Archundia, Diana Alemán-González-Duhart, José Correa-Basurto, Jessica Elena Mendieta-Wejebe
Diabetes mellitus is a chronic disease characterized by hyperglycemia, insulin resistance and hyperlipidemia. Glitazones or thiazolidinediones (TZD) are drugs that act as insulin-sensitizing agents whose molecular target is the peroxisome proliferator-activated receptor gamma (PPARγ). The euglycemic action of TZD has been linked with the induction of type 4 glucose transporter. However, it has been shown that the effect of TZD depends on the specific stereoisomer that interacts with PPARγ. Therefore, this work is focused on exploring the interactions and geometry adopted by glitazone's stereoisomers and one endogenous ligand on different conformations of the six crystals of the PPARγ protein using molecular docking and molecular dynamics (MD) simulations accompanied by the MMGBSA approach...
July 14, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28715674/the-presence-of-licit-and-illicit-drugs-in-police-stations-and-their-implications-for-workplace-drug-testing
#15
Gregory S Doran, Ralph Deans, Carlo De Filippis, Chris Kostakis, Julia A Howitt
The presence of licit and illicit drug residues on surfaces was studied in 10 police stations and a central drug evidence store in New South Wales, Australia, with the results compared to similar surfaces in four public buildings (to establish a community baseline). The results of almost 850 workplace surface swabs were also compared to the outcome of drug analysis in urine and hair samples volunteered by police officers. Surfaces were swabbed with alcohol and the swabs were extracted and analysed by LC-MS/MS...
July 5, 2017: Forensic Science International
https://www.readbyqxmd.com/read/28715108/ivermectin-activates-girk-channels-in-a-pip2-dependent-g%C3%AE-%C3%AE-independent-manner-and-an-amino-acid-residue-at-the-slide-helix-governs-the-activation
#16
I-Shan Chen, Michihiro Tateyama, Yuko Fukata, Motonari Uesugi, Yoshihiro Kubo
Ivermectin (IVM) is a widely used antiparasitic drug in humans and pets which activates glutamate-gated Cl(-) channel in parasites. It is also known that IVM binds to the transmembrane domains (TMs) of several ligand-gated channels, such as Cys-loop receptors and P2X receptors. In this study, we found that the G-protein-gated inwardly rectifying K(+) (GIRK) channel is activated by IVM directly. By electrophysiological recordings in Xenopus oocytes, we observed that IVM activates GIRK channel in a phosphatidylinositol-4,5-biphosphate (PIP2 )-dependent manner, and that the IVM-mediated GIRK activation is independent of Gβγ ...
July 17, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28713152/metastatic-anaplastic-lymphoma-kinase-1-alk-1-rearranged-inflammatory-myofibroblastic-sarcoma-to-the-brain-with-leptomeningeal-involvement-favorable-response-to-serial-alk-inhibitors-a-case-report
#17
Cai Yuan, Muchou J Ma, John V Parker, Tarek M Mekhail
BACKGROUND ALK gene rearrangements as oncogenic drivers have been described in many cancers, including inflammatory myofibroblastic sarcoma (IMS). The first-generation ALK inhibitor was limited in its ability to cross the blood-brain-barrier to treat brain metastasis. Drug-resistance invariably develops over time in ALK-rearranged tumors, which leads to disease progression. The newer generations of ALK inhibitors are designed to have higher potency in ALK inhibition and improved CNS penetration. CASE REPORT We report a rare case of pulmonary IMS with ALK-1 gene rearrangement and multiple brain metastases as initial presentation...
July 17, 2017: American Journal of Case Reports
https://www.readbyqxmd.com/read/28712038/binding-mode-prediction-and-md-mmpbsa-based-free-energy-ranking-for-agonists-of-rev-erb%C3%AE-ncor
#18
Yvonne Westermaier, Sergio Ruiz-Carmona, Isabelle Theret, Françoise Perron-Sierra, Guillaume Poissonnet, Catherine Dacquet, Jean A Boutin, Pierre Ducrot, Xavier Barril
The knowledge of the free energy of binding of small molecules to a macromolecular target is crucial in drug design as is the ability to predict the functional consequences of binding. We highlight how a molecular dynamics (MD)-based approach can be used to predict the free energy of small molecules, and to provide priorities for the synthesis and the validation via in vitro tests. Here, we study the dynamics and energetics of the nuclear receptor REV-ERBα with its co-repressor NCoR and 35 novel agonists. Our in silico approach combines molecular docking, molecular dynamics (MD), solvent-accessible surface area (SASA) and molecular mechanics poisson boltzmann surface area (MMPBSA) calculations...
July 15, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28711760/investigation-of-the-binding-free-energies-of-fda-approved-drugs-against-subtype-b-and-c-sa-hiv-pr-oniom-approach
#19
Z K Sanusi, T Govender, G E M Maguire, S B Maseko, J Lin, H G Kruger, B Honarparvar
Human immune virus subtype C is the most widely spread HIV subtype in Sub-Sahara Africa and South Africa. A profound structural insight on finding potential lead compounds is therefore necessary for drug discovery. The focus of this study is to rationalize the nine Food and Drugs Administration (FDA) HIV antiviral drugs complexed to subtype B and C-SA PR using ONIOM approach. To achieve this, an integrated two-layered ONIOM model was used to optimize the geometrics of the FDA approved HIV-1 PR inhibitors for subtype B...
June 29, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28711506/sodium-selenate-activated-wnt-%C3%AE-catenin-signaling-and-repressed-amyloid-%C3%AE-formation-in-a-triple-transgenic-mouse-model-of-alzheimer-s-disease
#20
Na Jin, Huazhang Zhu, Xiao Liang, Wei Huang, Qingguo Xie, Peng Xiao, Jiazuan Ni, Qiong Liu
Accumulating evidences show that selenium dietary intake is inversely associated with the mortality of Alzheimer's disease (AD). Sodium selenate has been reported to reduce neurofibrillary tangles (NFT) in the tauopathic mouse models, but its effects on the Wnt/β-catenin signaling pathway and APP processing remain unknown during AD formation. In this paper, triple transgenic AD mice (3×Tg-AD) had been treated with sodium selenate in drinking water for 10month before the detection of hippocampal pathology...
July 12, 2017: Experimental Neurology
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