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https://www.readbyqxmd.com/read/28811184/experimental-cocrystal-screening-and-solution-based-scale-up-cocrystallization-methods
#1
REVIEW
Maria Malamatari, Steven A Ross, Dennis Douroumis, Sitaram P Velaga
Cocrystals are crystalline single phase materials composed of two or more different molecular and/or ionic compounds generally in a stoichiometric ratio which are neither solvates nor simple salts. If one of the components is an active pharmaceutical ingredient (API), the term pharmaceutical cocrystal is often used. There is a growing interest among drug development scientists in exploring cocrystals, as means to address physicochemical, biopharmaceutical and mechanical properties and expand solid form diversity of the API...
August 12, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28803938/organoids-as-preclinical-models-to-improve-intraperitoneal-chemotherapy-effectiveness-for-colorectal-cancer-patients-with-peritoneal-metastases-preclinical-models-to-improve-hipec
#2
P Roy, C Canet-Jourdan, M Annereau, O Zajac, M Gelli, S Broutin, L Mercier, A Paci, F Lemare, M Ducreux, D Elias, D Malka, V Boige, D Goéré, F Jaulin
BACKGROUND: Peritoneal metastases (PM), corresponding to tumor implants into the peritoneal cavity, are associated with impaired prognosis and low responsiveness to systemic chemotherapy. A new therapeutic approach has dramatically changed the prognosis of patients with PM from colorectal cancer (CRC), consisting in the association of a complete cytoreductive surgery followed by intraperitoneal chemotherapy associated to hyperthermia (HIPEC). Many drugs have been administered intraperitoneally, but no clear consensus has been approved...
August 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28799226/educational-intervention-on-medication-reviews-aiming-to-reduce-acute-healthcare-consumption-in-elderly-patients-with-potentially-inappropriate-medicines-a-pragmatic-open-label-cluster-randomized-controlled-trial-in-primary-care
#3
K Schmidt-Mende, M Andersen, B Wettermark, J Hasselström
PURPOSE: Potentially inappropriate medicines (PIMs) may cause 10% of unplanned admissions in elderly people. We performed an educational intervention in primary care to reduce acute health care consumption and PIMs through the promotion of medication reviews (MRs) in elderly patients. METHODS: This cluster-randomized controlled trial was conducted in the context of an official campaign promoting rational drug use in elderly people. Sixty-nine primary health care practices with 119,910 patients aged older than or equal to 65 were randomized, with 1 dropout in the intervention group...
August 11, 2017: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/28793831/deciphering-the-crucial-molecular-properties-of-a-series-of-benzothiazole-hydrazone-inhibitors-that-targets-anti-apoptotic-bcl-xl-protein
#4
Parthiban Marimuthu, Pavithra K Balasubramanian, Kalaimathy Singaravelu
The Bcl-2 family proteins are the central regulators of apoptosis. Due to its predominant role in cancer progression, the Bcl-2 family proteins act as attractive therapeutic targets. Recently,molecular series of BenzothiazoleHydrazone(BH) inhibitorsthat exhibits drug-likenesscharacteristics,whichselectivelytargets Bcl-xLhave been reported.In the present study,dockingwas used toexplore the plausible binding mode of the highly active BH inhibitorwith Bcl-xL;and Molecular Dynamics(MD) simulation wasapplied toinvestigate the stability of predicted conformationover time...
August 10, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28793077/prevalence-of-medicine-use-among-brazilian-adults-a-systematic-review
#5
Vanessa Pereira Gomes, Marcus Tolentino Silva, Taís Freire Galvão
The use of medicine in adults has been assessed by some population-based studies in Brazil, but to date there has been no overall estimate of the prevalence of drug consumption. We therefore aimed to estimate the prevalence of medicine use as measured in previously reported cross-sectional studies among Brazilian adults. We conducted a systematic review of the literature, searching in MEDLINE, Embase among others to a date ending January 2017. Two researchers selected the studies, extracted data and assessed methodological quality of those chosen for inclusion...
August 2017: Ciência & Saúde Coletiva
https://www.readbyqxmd.com/read/28792760/structural-basis-of-wee-kinases-functionality-and-inactivation-by-diverse-small-molecule-inhibitors
#6
Jin-Yi Zhu, Rebecca Ann Duenes Cuellar, Norbert Berndt, Hee Eun Lee, Sanne H Olesen, Mathew P Martin, Jeffrey T Jensen, Gunda I Georg, Ernst Schönbrunn
Members of the Wee family of kinases negatively regulate the cell cycle via phosphorylation of CDK1 and are considered potential drug targets. Herein, we investigated the structure-function relationship of human Wee1, Wee2 and Myt1 (PKMYT1). Purified recombinant full-length proteins and kinase domain constructs differed substantially in phosphorylation states and catalytic competency suggesting complex mechanisms of activation. A series of crystal structures revealed unique features that distinguish Wee1 and Wee2 from Myt1 and establish the structural basis of differential inhibition by the widely used Wee1 inhibitor MK-1775...
August 9, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28791593/key-pharmacokinetic-essentials-of-fixed-dosed-combination-products-case-studies-and-perspectives
#7
Ranjeet Prasad Dash, Rana Rais, Nuggehally R Srinivas
Fixed-dose combinations are gaining popularity because they provide convenience while enhancing patient compliance. Literature examples suggest that many fixed-dose combinations are being rationalized and investigated for their potential utility in therapy. This article provides an introspection into the pharmacokinetic essentials that need to be considered prior to implementing a fixed-dose combination strategy. While the drug-drug interaction potential is an important question for the two drugs in a fixed-dose combination, the occurrence of a drug-drug interaction in itself is not a negative outcome for the proposed fixed-dose combination...
August 8, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28789605/analysis-of-distribution-and-antibiotic-resistance-of-pathogens-isolated-from-the-paediatric-population-in-shenmu-hospital-from-2011-2015
#8
Yang Hui-Min, Wang Yan-Ping, Yong Lin Liu, Bilal Haider Shamsi, He Bo, Meng Xu-Chun
Objective This study aimed to investigate the epidemiology and changes in antibacterial susceptibility of children in Shenmu City, northern Shaanxi, and provide a basis for rational drug use. Methods The distribution and drug resistance pattern of pathogenic bacteria isolated from children were retrospectively analysed. Results A total of 573 strains of pathogens were cultivated. A total of 201 (35.07%) strains of Gram-positive cocci and 183 (31.93%) strains of Gram-negative cocci were detected. A total of 189 (32...
January 1, 2017: Journal of International Medical Research
https://www.readbyqxmd.com/read/28789564/a-sar-based-mechanistic-study-on-the-combined-toxicities-of-sulfonamides-and-quorum-sensing-inhibitors-on-escherichia-coli
#9
C Chen, D Wang, H Wang, Z Lin, Z Fang
Quorum sensing inhibitors (QSIs) are promising alternatives to antibiotics, but they are discharged into the environment after their use cycle. This poses joint effects on the organisms in the environment. Therefore, it is of great importance to study the combined toxicities of QSIs and antibiotics. In this study, we investigated the single and combined toxicities of four potential QSIs and 11 sulfonamides (SAs) on Escherichia coli. The results revealed that the single toxicities of SAs were greater than those of QSIs, and the toxicities were found positively related to the binding energies (Ebind) with their target proteins, for both antibiotics and QSIs...
July 2017: SAR and QSAR in Environmental Research
https://www.readbyqxmd.com/read/28780179/cyp106a2-a-versatile-biocatalyst-with-high-potential-for-biotechnological-production-of-selectively-hydroxylated-steroid-and-terpenoid-compounds
#10
REVIEW
Daniela Schmitz, Simon Janocha, Flora Marta Kiss, Rita Bernhardt
CYP106A2 from Bacillus megaterium ATCC13368, was identified in the 1970s as one of the first bacterial steroid hydroxylases responsible for the conversion of progesterone to 15β-hydroxyprogesterone. Later on it has been proven to be a potent hydroxylase of numerous 3-oxo-Δ(4) as well as 3-hydroxy-Δ(5)-steroids and has recently also been characterized as a regioselective allylic bacterial diterpene hydroxylase. The main hydroxylation position of CYP106A2 is thought to be influenced by the functional groups at C3 position in the steroid core leading to a favored 15β-hydroxylation of 3-oxo-Δ(4)-steroids and 7β-hydroxylation of 3-hydroxy-Δ(5)-steroids...
August 2, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28780123/molecular-insights-into-the-role-of-a-distal-f240a-mutation-that-alters-cyp1a1-activity-towards-persistent-organic-pollutants
#11
Veronika Navrátilová, Markéta Paloncýová, Karel Berka, Shintaro Mise, Yuki Haga, Chisato Matsumura, Toshiyuki Sakaki, Hideyuki Inui, Michal Otyepka
BACKGROUND: Cytochromes P450 are major drug-metabolizing enzymes involved in the biotransformation of diverse xenobiotics and endogenous chemicals. Persistent organic pollutants (POPs) are toxic hydrophobic compounds that cause serious environmental problems because of their poor degradability. This calls for rational design of enzymes capable of catalyzing their biotransformation. Cytochrome P450 1A1 isoforms catalyze the biotransformation of some POPs, and constitute good starting points for the design of biocatalysts with tailored substrate specificity...
August 2, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28775266/in-silico-model-of-the-human-clc-kb-chloride-channel-pore-mapping-biostructural-pathology-and-drug-screening
#12
Maxime Louet, Sara Bitam, Naziha Bakouh, Yohan Bignon, Gabrielle Planelles, David Lagorce, Maria A Miteva, Dominique Eladari, Jacques Teulon, Bruno O Villoutreix
The human ClC-Kb channel plays a key role in exporting chloride ions from the cytosol and is known to be involved in Bartter syndrome type 3 when its permeation capacity is decreased. The ClC-Kb channel has been recently proposed as a potential therapeutic target to treat hypertension. In order to gain new insights into the sequence-structure-function relationships of this channel, to investigate possible impacts of amino-acid substitutions, and to design novel inhibitors, we first built a structural model of the human ClC-Kb channel using comparative modeling strategies...
August 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28774136/role-of-hydrogen-bonding-in-the-formation-of-adenine-chains-on-cu-110-surfaces
#13
Lanxia Cheng
Understanding the adsorption properties of DNA bases on metal surfaces is fundamental for the rational control of surface functionalization leading to the realisation of biocompatible devices for biosensing applications, such as monitoring of particular parameters within bio-organic environments and drug delivery. In this study, the effects of deposition rate and substrate temperature on the adsorption behavior of adenine on Cu(110) surfaces have been investigated using scanning tunneling microscopy (STM) and density functional theory (DFT) modeling, with a focus on the characterization of the morphology of the adsorbed layers...
December 16, 2016: Materials
https://www.readbyqxmd.com/read/28770387/data-to-decisions-creating-a-culture-of-model-driven-drug-discovery
#14
Frank K Brown, Farida Kopti, Charlie Zhenyu Chang, Scott A Johnson, Meir Glick, Chris L Waller
Merck & Co., Inc., Kenilworth, NJ, USA, is undergoing a transformation in the way that it prosecutes R&D programs. Through the adoption of a "model-driven" culture, enhanced R&D productivity is anticipated, both in the form of decreased attrition at each stage of the process and by providing a rational framework for understanding and learning from the data generated along the way. This new approach focuses on the concept of a "Design Cycle" that makes use of all the data possible, internally and externally, to drive decision-making...
August 2, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28767443/antiangiogenic-agents-after-first-line-and-sorafenib-plus-chemoembolization-a-systematic-review
#15
REVIEW
Andrea Casadei Gardini, Daniele Santini, Giuseppe Aprile, Nicola Silvestris, Emanuele Felli, Francesco Giuseppe Foschi, Giorgio Ercolani, Giorgia Marisi, Martina Valgiusti, Alessandro Passardi, Marco Puzzoni, Marianna Silletta, Brunetti Oronzo, Giovanni Gerardo Cardellino, Giovanni Luca Frassineti, Mario Scartozzi
Transarterial chemoembolization (TACE) is the standard treatment for intermediate stage, although the combination of TACE with sorafenib may theoretically benefit HCC patients in intermediate stage. Owing to the significant antiangiogenic effect of sorafenib and the limitation of TACE, it is rational to combine them. Though the strategy of combining TACE and sorafenib has been increasingly used in patients with unresectable HCC but the current evidence is controversial and its clinical role has not been determined yet...
July 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/28767108/bioorganometallic-ferrocene-tripeptide-nanoemulsions
#16
Xuejiao Yang, Yuefei Wang, Wei Qi, Rongxin Su, Zhimin He
We demonstrate an effective strategy to prepare highly stable nanoemulsions using ferrocene-modified tripeptides. Compared with traditional nanoemulsions, bioorganometallic peptide nanoemulsions are appealing for a number of reasons, including long-term and outstanding thermal stability, redox activity and biocompatibility. The formed nanoemulsions could remain stable for more than four months at room temperature, which is the highest stability reported so far for peptide and protein emulsifiers. The phase behaviour and size distribution of the emulsions could be precisely tailored by altering the temperature, solvent ratio and redox state of the ferrocene moiety...
August 2, 2017: Nanoscale
https://www.readbyqxmd.com/read/28766952/inhibition-of-the-%C3%AE-carbonic-anhydrase-from-the-dandruff-producing-fungus-malassezia-globosa-with-monothiocarbamates
#17
Alessio Nocentini, Daniela Vullo, Sonia Del Prete, Sameh M Osman, Fatmah A S Alasmary, Zeid AlOthman, Clemente Capasso, Fabrizio Carta, Paola Gratteri, Claudiu T Supuran
A series of monothiocarbamates (MTCs) was investigated for the inhibition of the β-class carbonic anhydrase (CAs, EC 4.2.1.1) from the fungal parasite Malassezia globosa, MgCA. These MTCs incorporate various scaffolds, among which aliphatic amine with 1-4 carbons atom in their molecule, morpholine, piperazine, as well as phenethylamine and benzylamine derivatives. All the reported MTCs displayed a better efficacy in inhibiting MgCA compared to the clinically used sulphonamide drug acetazolamide (KI of 74 μM), with KIs spanning between 1...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28761757/mechanisms-of-action-and-rationale-for-the-use-of-checkpoint-inhibitors-in-cancer
#18
REVIEW
Clemence Granier, Eleonore De Guillebon, Charlotte Blanc, Helene Roussel, Cecile Badoual, Elia Colin, Antonin Saldmann, Alain Gey, Stephane Oudard, Eric Tartour
The large family of costimulatory molecules plays a crucial role in regulation of the immune response. These molecules modulate TCR signalling via phosphorylation cascades. Some of the coinhibitory members of this family, such as PD-1 and CTLA-4, already constitute approved targets in cancer therapy and, since 2011, have opened a new area of antitumour immunotherapy. Many antibodies targeting other inhibitory receptors (Tim-3, VISTA, Lag-3 and so on) or activating costimulatory molecules (OX40, GITR and so on) are under evaluation...
2017: ESMO Open
https://www.readbyqxmd.com/read/28760489/mdr-in-cancer-addressing-the-underlying-cellular-alterations-with-the-use-of-nanocarriers
#19
REVIEW
Manu S Singh, Salma N Tammam, Maryam A Shetab Boushehri, Alf Lamprecht
Multidrug resistance (MDR) is associated with a wide range of pathological changes at different cellular and intracellular levels. Nanoparticles (NPs) have been extensively exploited as the carriers of MDR reversing payloads to resistant tumor cells. However, when properly formulated in terms of chemical composition and physicochemical properties, NPs can serve as beyond delivery systems and help overcome MDR even without carrying a load of chemosensitizers or MDR reversing molecular cargos. Whether serving as drug carriers or beyond, a wise design of the nanoparticulate systems to overcome the cellular and intracellular alterations underlying the resistance is imperative...
July 28, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28759875/an-overview-of-benzo-b-thiophene-based-medicinal-chemistry
#20
Rangappa S Keri, Karam Chand, Srinivasa Budagumpi, Sasidhar Balappa Somappa, Siddappa A Patil, Bhari Mallanna Nagaraja
Among sulfur containing heterocycles, benzothiophene and its derivatives are at the focus as these candidates have structural similarities with active compounds to develop new potent lead molecules in drug design. Benzo[b]thiophene scaffold is one of the privileged structures in drug discovery as this core exhibits various biological activities allowing them to act as anti-microbial, anti-cancer, anti-inflammatory, anti-oxidant, anti-tubercular, anti-diabetic, anti-convulsant agents and many more. Further, numerous benzothiophene-based compounds as clinical drugs have been extensively used to treat various types of diseases with high therapeutic potency, which has led to their extensive developments...
July 22, 2017: European Journal of Medicinal Chemistry
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