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https://www.readbyqxmd.com/read/28345742/a-qualitative-exploration-of-chronic-pain-and-opioid-treatment-among-hiv-patients-with-drug-use-disorders
#1
Sarina R Isenberg, Allysha C Maragh-Bass, Kathleen Ridgeway, Mary C Beach, Amy R Knowlton
OBJECTIVE: The study explored high-risk participants' experiences with pain management regarding clinical access to and use of prescription opioids. DESIGN: Qualitative semistructured interviews and focus groups. SETTING: Data were collected August 2014 to May 2015 at an urban community-based research facility in Baltimore City, MD. PARTICIPANTS: HIV participants with chronic pain and a history of illicit drug use. METHODS: Qualitative coding and analysis used an iterative, inductive, and thematic approach and coders achieved inter-coder consistency...
January 2017: Journal of Opioid Management
https://www.readbyqxmd.com/read/28344555/drug-repurposing-of-the-anthelmintic-niclosamide-to-treat-multidrug-resistant-leukemia
#2
Sami Hamdoun, Philipp Jung, Thomas Efferth
Multidrug resistance, a major problem that leads to failure of anticancer chemotherapy, requires the development of new drugs. Repurposing of established drugs is a promising approach for overcoming this problem. An example of such drugs is niclosamide, a known anthelmintic that is now known to be cytotoxic and cytostatic against cancer cells. In this study, niclosamide showed varying activity against different cancer cell lines. It revealed better activity against hematological cancer cell lines CCRF-CEM, CEM/ADR5000, and RPMI-8226 compared to the solid tumor cell lines MDA-MB-231, A549, and HT-29...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28344466/an-overview-of-pharmacodynamic-modelling-ligand-binding-approach-and-its-application-in-clinical-practice
#3
REVIEW
Mohammed Saji Salahudeen, Prasad S Nishtala
The study of the magnitude and variation of drug response is defined as pharmacodynamics (PDs). PD models examine plasma concentration and effect relationship. It can predict the archetypal effect ([Formula: see text]) of a drug as a function of the drug concentration ([Formula: see text]) and estimate an unknown PD parameter ([Formula: see text]). The PD models have been described as fixed, linear, log-linear, [Formula: see text], sigmoid [Formula: see text], and indirect PD response. Ligand binding model is an example of a PD model that works on the underpinning PD principle of a drug, eliciting its pharmacological effect at the receptor site...
February 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28344126/regulation-of-the-nitric-oxide-oxidase-activity-of-myeloperoxidase-by-pharmacological-agents
#4
Sophie L Maiocchi, Jonathan C Morris, Martin D Rees, Shane R Thomas
The leukocyte-derived heme enzyme myeloperoxidase (MPO) is released extracellularly during inflammation and impairs nitric oxide (NO) bioavailability by directly oxidizing NO or producing NO-consuming substrate radicals. Here, structurally diverse pharmacological agents with activities as MPO substrates/inhibitors or antioxidants were screened for their effects on MPO NO oxidase activity in human plasma and physiological model systems containing endogenous MPO substrates/antioxidants (tyrosine, urate, ascorbate)...
March 23, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28344021/pharmaceutical-cocrystals-salts-and-multicomponent-systems-intermolecular-interactions-and-property-based-design
#5
REVIEW
David J Berry, Jonathan W Steed
As small molecule drugs become harder to develop and less cost effective for patient use, efficient strategies for their property improvement become increasingly important to global health initiatives. Improvements in the physical properties of Active Pharmaceutical Ingredients (APIs), without changes in the covalent chemistry, have long been possible through the application of binary component solids. This was first achieved through the use of pharmaceutical salts, within the last 10-15years with cocrystals and more recently coamorphous systems have also been consciously applied to this problem...
March 23, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28340955/a-practical-framework-toward-prediction-of-breaking-force-and-disintegration-of-tablet-formulations-using-machine-learning-tools
#6
Ilgaz Akseli, Jingjin Xie, Leon Schultz, Nadia Ladyzhynsky, Tommasina Bramante, Xiaorong He, Rich Deanne, Keith R Horspool, Robert Schwabe
Enabling the paradigm of quality by design requires the ability to quantitatively correlate material properties and process variables to measureable product performance attributes. Conventional, quality-by-test methods for determining tablet breaking force and disintegration time usually involve destructive tests, which consume significant amount of time and labor and provide limited information. Recent advances in material characterization, statistical analysis, and machine learning have provided multiple tools that have the potential to develop nondestructive, fast, and accurate approaches in drug product development...
January 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28340702/selective-solid-phase-extraction-of-jwh-synthetic-cannabinoids-by-using-computationally-designed-peptides
#7
Marcello Mascini, Camilla Montesano, German Perez, Joseph Wang, Dario Compagnone, Manuel Sergi
The objective of the present work is to demonstrate a rational way to prepare selective sorbents able to extract simultaneously several structural analogs. For this purpose the binding specificity of two hexapeptides computationally designed (VYWLVW and YYIGGF) versus four synthetic cannabinoids Naphthalen-1-yl-(1-pentylindol-3-yl)methanone (JWH 018), naphthalen-1-yl-(1-butylindol-3-yl)methanone (JWH 073), (R)-(1-((1-methylpiperidin-2-yl)methyl)-1H-indol-3-yl)(naphthalen-1-yl)methanone (AM 1220) and (R)-(+)-[2,3-Dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-napthalenylmethanone (WIN 55) was computationally studied and then experimentally tested by solid-phase extraction (SPE) clean-up and ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) analysis...
May 15, 2017: Talanta
https://www.readbyqxmd.com/read/28340357/ruthenium-complexes-with-phenylterpyridine-derivatives-target-cell-membrane-and-trigger-death-receptors-mediated-apoptosis-in-cancer-cells
#8
Zhiqin Deng, Pan Gao, Lianling Yu, Bin Ma, Yuanyuan You, Leung Chan, Chaoming Mei, Tianfeng Chen
Elucidation of the communication between metal complexes and cell membrane may provide useful information for rational design of metal-based anticancer drugs. Herein we synthesized a novel class of ruthenium (Ru) complexes containing phtpy derivatives (phtpy = phenylterpyridine), analyzed their structure-activity relationship and revealed their action mechanisms. The result showed that, the increase in the planarity of hydrophobic Ru complexes significantly enhanced their lipophilicity and cellular uptake...
March 18, 2017: Biomaterials
https://www.readbyqxmd.com/read/28338292/rational-drug-design-of-indazole-based-diarylurea-derivatives-as-anticancer-agents
#9
Yan-Yan Chu, He-Juan Cheng, Zhenhua Tian, Jian-Chun Zhao, Gang Li, Yang-Yang Chu, Chang-Jun Sun, Wen-Bao Li
A series of novel indazole-based diarylurea derivatives targeting c-kit were designed by structure-based drug design. The derivatives were prepared and their antiproliferative activities were evaluated against human colon cancer HCT-116 cell line and hepatocellular carcinoma PLC/PRF/5 cell line. The antiproliferative activities demonstrated that six out of nine compounds exhibited comparable activities with Sorafenib against HCT-116. The structure-activity relationship (SAR) analysis indicated that the indazole ring part tolerated different kinds of substituents, the N position of the central pyridine ring played key roles in antiproliferative activity...
March 24, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28337524/quantitative-analysis-of-efficacy-and-associated-factors-of-calcium-intake-on-bone-mineral-density-in-postmenopausal-women
#10
J Wu, L Xu, Y Lv, L Dong, Q Zheng, L Li
A model-based meta-analysis method was performed to quantitatively analyze the efficacy characteristics of calcium intake in BMD increase among postmenopausal women. We found that age and calcium intake dose were key factors affecting the efficiency and onset of BMD change, and daily 1200 mg calcium was suggested to be a beneficial dosage. INTRODUCTION: This paper aims to quantify the efficacy of calcium intake in preventing bone mineral density (BMD) decrease among postmenopausal women and to investigate the factors that may affect the efficacy...
March 23, 2017: Osteoporosis International
https://www.readbyqxmd.com/read/28336347/solution-conformations-of-a-linked-construct-of-the-zika-virus-ns2b-ns3-protease
#11
Mithun C Mahawaththa, Benjamin J G Pearce, Bim Graham, Christian D Klein, Christoph Nitsche, Gottfried Otting
The Zika virus presents a serious risk for global health. Crystal structures of different constructs of the Zika virus NS2B-NS3 protease (NS2B-NS3pro) have been determined with the aim to provide a basis for rational drug discovery. In these structures, the C-terminal β-hairpin of NS2B, NS2Bc, was observed to be either disordered (open conformation) or bound to NS3pro complementing the substrate binding site (closed conformation). Enzymatically active constructs of flaviviral NS2B-NS3 proteases commonly used for inhibitor testing contain a covalent peptide linker between NS2B and NS3pro...
March 20, 2017: Antiviral Research
https://www.readbyqxmd.com/read/28335614/therapeutic-targeting-of-protein-kinase-ck2-gene-expression-in-feline-oral-squamous-cell-carcinoma-a-naturally-occurring-large-animal-model-of-head-and-neck-cancer
#12
Claire Cannon, Janeen Trembley, Betsy Kren, Gretchen Unger, M Gerard O'Sullivan, Ingrid Cornax, Jaime Modiano, Khalil Ahmed
Protein kinase CK2 (CK2) is a highly promising target for cancer therapy and anti-CK2 gene expression therapy has shown effectiveness in rodent models of human head and neck cancer (HNC). To date, there has been no large animal model of cancer in which to further explore anti-CK2 therapies. Feline oral squamous cell carcinoma (FOSCC) has been proposed as a large animal model for human HNC and we have previously shown that CK2 is a rational target in FOSCC. We hypothesized that a novel tenfibgen coated tumor-specific nanocapsule carrying RNAi oligonucleotides targeting feline CK2α and CK2α' (TBG-RNAi-fCK2αα') would be safe in cats with FOSCC...
March 23, 2017: Human Gene Therapy. Clinical Development
https://www.readbyqxmd.com/read/28333136/targeting-3-phosphoinositide-dependent-protein-kinase-1-associated-with-drug-resistant-renal-cell-carcinoma-using-new-oridonin-analogs
#13
Jiancheng Zhou, Eun-Jin Yun, Wei Chen, Ye Ding, Kaijie Wu, Bin Wang, Chunyong Ding, Elizabeth Hernandez, John Santoyo, Rey-Chen Pong, Haiying Chen, Dalin He, Jia Zhou, Jer-Tsong Hsieh
The current agents used for renal cell carcinoma (RCC) only exhibit the moderate response rate among patients. Development of drug resistance eventually fuels the need of either more potent drugs or new drugs to target the resistant pathways. Oridonin is a diterpenoid isolated from the Chinese medicinal herb Rabdosia rubescens and has been shown to have antitumor activities in many cancers. We previously developed new synthetic methodologies to modify structurally diversified diterpenoids and designed a series of nitrogen-enriched oridonin analogs...
March 23, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28332827/subcellular-chemical-imaging-of-antibiotics-in-single-bacteria-using-c60-secondary-ion-mass-spectrometry
#14
Hua Tian, David A Six, Thomas Krucker, Jennifer A Leeds, Nicholas Winograd
The inherent difficulty of discovering new and effective antibacterials and the rapid development of resistance particularly in Gram-negative bacteria, illustrates the urgent need for new methods that enable rational drug design. Here we report the development of 3D imaging cluster secondary ion mass spectrometry (SIMS) as a label-free approach to chemically map small molecules in aggregated and single Escherichia coli cells, with ~300 nm spatial resolution and high chemical sensitivity. The feasibility of quantitative analysis was explored, and a non-linear relationship between treatment dose and signal for tetracycline and ampicillin, two clinically-used antibacterials, was observed...
March 23, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28331865/growth-hormone-utilization-review-in-a-pediatric-primary-care-setting
#15
Fatemeh Sayarifard, Fereshteh Bakhshi Imcheh, Shirinsadat Badri, Toktam Faghihi, Mostafa Qorbani, Mania Radfar
OBJECTIVE: One of the main problems facing public health providers and administrators in many countries is ensuring the rational use of high-cost drugs. In this regard, on-going process of medication use evaluation can be considered as a useful tool. In this study, we evaluated certain usage aspects of a highly-cost medication, that is, recombinant growth hormone (GH). METHODS: This cross-sectional study conducted from August 2012 to August 2014. Children receiving GH ± gonadotropin releasing hormone (GnRH) analogs were included in the study...
January 2017: Journal of Research in Pharmacy Practice
https://www.readbyqxmd.com/read/28325370/targeting-the-parasite-to-suppress-malaria-transmission
#16
R E Sinden
This article attempts to draw together current knowledge on the biology of Plasmodium and experience gained from past control campaigns to interpret and guide current efforts to discover and develop exciting new strategies targeting the parasite with the objective of interrupting transmission. Particular note is made of the advantages of targeting often unappreciated small, yet vital, bottleneck populations to enhance both the impact and the useful lifetime of hard-won interventions. A case is made for the standardization of methods to measure transmission blockade to permit the rational comparison of how diverse interventions (drugs, vaccines, insecticides, Genetically Modified technologies) targeting disparate aspects of parasite biology may impact upon the commonly used parameter of parasite prevalence in the human population...
2017: Advances in Parasitology
https://www.readbyqxmd.com/read/28325214/antibody-based-cancer-therapy-successful-agents-and-novel-approaches
#17
D Hendriks, G Choi, M de Bruyn, V R Wiersma, E Bremer
Since their discovery, antibodies have been viewed as ideal candidates or "magic bullets" for use in targeted therapy in the fields of cancer, autoimmunity, and chronic inflammatory disorders. A wave of antibody-dedicated research followed, which resulted in the clinical approval of a first generation of monoclonal antibodies for cancer therapy such as rituximab (1997) and cetuximab (2004), and infliximab (2002) for the treatment of autoimmune diseases. More recently, the development of antibodies that prevent checkpoint-mediated inhibition of T cell responses invigorated the field of cancer immunotherapy...
2017: International Review of Cell and Molecular Biology
https://www.readbyqxmd.com/read/28322159/towards-predicting-the-cytochrome-p450-modulation-from-qsar-to-proteochemometric-modeling
#18
Watshara Shoombuatong, Philip Prathipati, Veda Prachayasittikul, Nalini Schaduangrat, Aijaz Ahmad Malik, Reny Pratiwi, Sompon Wanwimolruk, Jarl E S Wikberg, Matthew Paul Gleeson, Ola Spjuth, Chanin Nantasenamat
Drug metabolism determines the fate of a drug when it enters the human body and is a critical factor in defining their absorption, distribution, metabolism, excretion and toxicity (ADMET) characteristics. Among the various drug metabolizing enzymes, cytochrome P450s (CYP450) constitute an important protein family that aside from functioning in xenobiotic metabolism is also responsible for a diverse array of other roles encompassing steroid and cholesterol biosynthesis, fatty acid metabolism, calcium homeostasis, neuroendocrine functions and growth regulation...
March 20, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28319781/systematic-study-of-imidazoles-inhibiting-ido1-via-the-integration-of-molecular-mechanics-and-quantum-mechanics-calculations
#19
Yi Zou, Fang Wang, Yan Wang, Wenjie Guo, Yihua Zhang, Qiang Xu, Yisheng Lai
Indoleamine 2,3-dioxygenase 1 (IDO1) is regarded as an attractive target for cancer immunotherapy. To rationalize the detailed interactions between IDO1 and its inhibitors at the atomic level, an integrated computational approach by combining molecular mechanics and quantum mechanics methods was employed in this report. Specifically, the binding modes of 20 inhibitors was initially investigated using the induced fit docking (IFD) protocol, which outperformed other two docking protocols in terms of correctly predicting ligand conformations...
March 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28315070/mechanisms-of-resistance-in-multiple-myeloma
#20
Athanasios Papadas, Fotis Asimakopoulos
Multiple myeloma (MM) is an incurable hematopoietic cancer that is characterized by malignant plasma cell infiltration of the bone marrow and/or extramedullary sites. Multi-modality approaches including "novel agents," traditional chemotherapy, and/or stem cell transplantation are used in MM therapy. Drug resistance, however, ultimately develops and the disease remains incurable for the vast majority of patients. In this chapter, we review both tumor cell-autonomous and non-autonomous (microenvironment-dependent) mechanisms of drug resistance...
March 18, 2017: Handbook of Experimental Pharmacology
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