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https://www.readbyqxmd.com/read/28325370/targeting-the-parasite-to-suppress-malaria-transmission
#1
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
#2
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
#3
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
#4
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
#5
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
https://www.readbyqxmd.com/read/28303493/the-effect-of-molecular-diagnostics-on-the-treatment-of-glioma
#6
REVIEW
Nancy Ann Oberheim Bush, Nicholas Butowski
PURPOSE OF REVIEW: This review summarizes the use of molecular diagnostics in glioma and its effect on the development of novel therapeutics and management decisions. RECENT FINDINGS: Genomic and proteomic profiling of brain tumors has provided significant expansion of our understanding of oncogenesis, characterization, and prognostication of brain tumors. Molecular markers such as MGMT, EGFR, IDH, 1p19q, ATRX, TERT, FGFR-TACC, and BRAF are now being used to classify brain tumors as well as influence management decisions...
April 2017: Current Oncology Reports
https://www.readbyqxmd.com/read/28302416/plant-parts-substitution-based-approach-as-a-viable-conservation-strategy-for-medicinal-plants-a-case-study-of-premna-latifolia-roxb
#7
Ashish Kumar Jena, Maninder Karan, Karan Vasisht
BACKGROUND: Rapid population growth and catastrophic harvesting methods of wild medicinal plants especially trees, result in the exploitation of natural sources and its management is the need of the hour. Dashamoolarishta is an amalgam of roots of ten plants of a popular Ayurvedic FDC formulation consisting of the root of Premna latifolia Roxb. as one of its ingredients. Presently, their populations like many other trees are under threat due to extensive use of the roots by the herbal drug industry...
March 14, 2017: Journal of Ayurveda and Integrative Medicine
https://www.readbyqxmd.com/read/28302016/validation-of-tzd-scaffold-as-potential-aris-pharmacophore-modelling-atom-based-3d-qsar-and-docking-studies
#8
Lalita Dahiya, Manoj Kumar Mahapatra, Ramandeep Kaur, Vipin Kumar, Manoj Kumar
Metabolic disorders associated with diabetic patients are a serious concern. Aldose reductase (ALR2) has been identified as first rate-limiting enzyme in the polyol pathway which catalyzes the reduction of glucose to sorbitol. It represents one of the validated targets to develop potential new chemical entities for the prevention and subsequent progression of microvascular diabetic complications. In order to further understand the intricate structural prerequisites of molecules to act as ALR2 inhibitors, ligand-based pharmacophore model, atom-based 3D-QSAR and structure based drug design studies have been performed on a series of 2,4-thiazolidinedione derivatives with ALR2 inhibitory activity...
March 15, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28302013/multicyclic-peptides-as-scaffolds-for-the-development-of-tumor-targeting-agents
#9
Anastasia Loktev, Uwe Haberkorn, Walter Mier
The lack of specificity of traditional cytotoxic drugs triggers the development of anticancer agents with high selectivity to tumor-specific proteins. The unveiling of target structures such as EGFR or Her2 allows the focused development of novel therapies and has strongly advanced tumor treatment. Tumor-specific high-affinity ligands can be identified by using display techniques such as phage, yeast surface, ribosome and mRNA display. These techniques enable the screening of huge libraries, consequently providing a valuable alternative to rational drug development...
March 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28301004/-the-essentiality-and-rationality-of-the-brazilian-national-listing-of-essential-medicines
#10
Sueli Miyuki Yamauti, José Ruben de Alcântara Bonfim, Silvio Barberato-Filho, Luciane Cruz Lopes
One strategy to implement the rational use of medicines is the adoption of an 'essential medicines list'. The objective of this study was to analyze the list of medicines contained in the Brazilian National Relation of Essential Medicines (Rename, 2013) in terms of essentiality and rationality. Essentiality was determined by comparing this list to the 18th Essential Medicines List (EML) published by the World Health Organization (WHO). Drugs which were part of the Brazilian National Relation of Essential Medicines but not included in the EML were assessed using the classification described in La revue Prescrire to detect medications without added therapeutic value...
March 2017: Ciência & Saúde Coletiva
https://www.readbyqxmd.com/read/28299937/non-covalent-protein-and-peptide-functionalization-of-single-walled-carbon-nanotubes-for-bio-delivery-and-optical-sensing-applications
#11
Alessandra Antonucci, Justyna Kupis-Rozmyslowicz, Ardemis Boghossian
The exquisite structural and optical characteristics of single-walled carbon nanotubes (SWCNTs), combined with the tunable specificities of proteins and peptides, can be exploited to strongly benefit technologies with applications in fields ranging from biomedicine to industrial biocatalysis. The key to exploiting the synergism of these materials is designing protein/peptide-SWCNT conjugation schemes that preserve biomolecule activity while keeping the near-infrared optical and electronic properties of SWCNTs intact...
March 16, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28297583/assessment-of-drug-sensitivity-in-hematopoietic-stem-and-progenitor-cells-from-acute-myelogenous-leukemia-and-myelodysplastic-syndrome-ex-vivo
#12
Katherine L B Knorr, Laura E Finn, B Douglas Smith, Allan D Hess, James M Foran, Judith E Karp, Scott H Kaufmann
Current understanding suggests that malignant stem and progenitor cells must be reduced or eliminated for prolonged remissions in myeloid neoplasms such as acute myelogenous leukemia (AML) or myelodysplastic syndrome (MDS). Multicolor flow cytometry has been widely used to distinguish stem and myeloid progenitor cells from other populations in normal and malignant bone marrow. In this study, we present a method for assessing drug sensitivity in MDS and AML patient hematopoietic stem and myeloid progenitor cell populations ex vivo using the investigational Nedd8-activating enzyme inhibitor MLN4924 and standard-of-care agent cytarabine as examples...
March 2017: Stem Cells Translational Medicine
https://www.readbyqxmd.com/read/28294043/polysaccharide-based-materials-associated-with-or-coordinated-to-gold-nanoparticles-synthesis-and-medical-application
#13
Débora P Facchi, Joziel A da Cruz, Elton G Bonafé, Antonio G B Pereira, André R Fajardo, Sandro A S Venter, Johny P Monteiro, Edvani C Muniz, Alessandro F Martins
BACKGROUND: Gold nanoparticles (AuNPs) have enormous potential for application in imaging, diagnosis, and therapies in the medical field. AuNPs are renowned for their localized surface plasmon resonance (LSPR) properties, large surface area, and biocompatibility with body fluids. Further, AuNPs have featured prominently in new methodologies for cancer treatments, like photothermal and imaging therapies. Although AuNPs present enormous potential for application in the medical field, their instability under physiological conditions prevents further uses...
March 9, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28293883/rational-design-and-applications-of-semisynthetic-modular-biosensors-snifits-and-lucids
#14
Helen Farrants, Julien Hiblot, Rudolf Griss, Kai Johnsson
Biosensors are used in many fields to measure the concentration of analytes, both in a cellular context and in human samples for medical care. Here, we outline the design of two types of modular biosensors: SNAP-tag-based indicators with a Fluorescent Intramolecular Tether (SNIFITs) and LUCiferase-based Indicators of Drugs (LUCIDs). These semisynthetic biosensors quantitatively measure analyte concentrations in vitro and on cell surfaces by an intramolecular competitive mechanism. We provide an overview of how to design and apply SNIFITs and LUCIDs...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28293709/metabolic-perturbation-to-enhance-polyketide-and-nonribosomal-peptide-antibiotic-production-using-triclosan-and-ribosome-targeting-drugs
#15
Yukinori Tanaka, Masumi Izawa, Yoshikazu Hiraga, Yuya Misaki, Tomoko Watanabe, Kozo Ochi
Although transcriptional activation of pathwayspecific positive regulatory genes and/or biosynthetic genes is primarily important for enhancing secondary metabolite production, reinforcement of substrate supply, as represented by primary metabolites, is also effective. For example, partial inhibition of fatty acid synthesis with ARC2 (an analog of triclosan) was found to enhance polyketide antibiotic production. Here, we demonstrate that this approach is effective even for industrial high-producing strains, for example enhancing salinomycin production by 40%, reaching 30...
March 14, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28293235/distribution-of-cfr-in-staphylococcus-spp-and-escherichia-coli-strains-from-pig-farms-in-china-and-characterization-of-a-novel-cfr-carrying-f43-a-b-plasmid
#16
Xiao-Qin Liu, Jing Wang, Wei Li, Li-Qing Zhao, Yan Lu, Jian-Hua Liu, Zhen-Ling Zeng
The multi-resistance gene cfr is widely distributed among various gram-positive and gram-negative species in livestock in China. To better understand the epidemiology of cfr among Staphylococcus spp. and E. coli isolates, 254 Staphylococcus spp. and 398 E. coli strains collected from six swine farms in China were subjected to prevalence and genetic analysis. Forty (15.7%) Staphylococcus spp. isolates, including 38 Staphylococcus sciuri strains, one Staphylococcus chromogenes strain, and one Staphylococcus lentus strain, and two (0...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28292016/pharmacokinetic-changes-of-norfloxacin-based-on-expression-of-mrp2-after-acute-exposure-to-high-altitude-at-4300m
#17
Bingfeng Luo, Rong Wang, Wenbin Li, Tao Yang, Chang Wang, Hui Lu, Anpeng Zhao, Juanhong Zhang, Zhengping Jia
BACKGROUND: This study was to investigate the influence of physiological changes and the expression of MRP2 efflux transporter on the pharmacokinetics of norfloxacin after acute exposure to high altitude 4300m. METHODS AND RESULTS: The rats were randomly divided into high altitude group and plain group. Blood gas and biochemical analysis showed that the physiological parameters significantly changed at high altitude. The mRNA and protein expression of MRP2 in high altitude group were higher than plain group in rat small intestine and kidney, while was reduced in rat liver...
March 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28291352/understanding-the-molecular-determinant-of-reversible-human-monoamine-oxidase-b-inhibitors-containing-2h-chromen-2-one-core-structure-based-and-ligand-based-derived-3-d-qsar-predictive-models
#18
Milan Mladenovic, Alexandros Patsilinakos, Adele Pirolli, Manuela Sabatino, Rino Ragno
Monoamine oxidase B (MAO B) catalyzes the oxidative deamination of aryalkylamines neurotransmitters with concomitant reduction of oxygen to hydrogen peroxide. Consequently, the enzyme's malfunction can induce oxidative damage to mitochondrial DNA and mediates development of Parkinson's disease. Thus, MAO B emerges as a promising target for developing pharmaceuticals potentially useful to treat this vicious neurodegenerative condition. Aiming to contribute to the development of drugs with the reversible mechanism of MAO B inhibition only, herein, an extended in silico-in vitro procedure for the selection of novel MAO B inhibitors is demonstrated, including: (1) definition of optimized and validated structure-based (SB) 3-D QSAR models derived from available co-crystallized inhibitor-MAO B complexes; (2) elaboration of structure-activity relationships (SAR) features for either irreversible or reversible MAO B inhibitors to characterize and improve coumarin-based inhibitor activity (Protein Data Bank ID: 2V61) as the most potent reversible lead compound; (3) definition of structure-based (SB) and ligand-based (LB) alignment rules assessments by which virtually any untested potential MAO B inhibitor might be evaluated; (4) predictive ability validation of the best 3-D QSAR model through SB/LB modeling of four coumarin-based external test sets (267 compounds); (5) design and SB/LB alignment of novel coumarin-based scaffolds experimentally validated through synthesis and biological evaluation in vitro...
March 14, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28289911/transcriptomics-as-a-tool-to-discover-new-antibacterial-targets
#19
REVIEW
Ángel Domínguez, Elisa Muñoz, M Carmen López, Miguel Cordero, José Pedro Martínez, Miguel Viñas
The emergence of antibiotic-resistant pathogens, multiple drug-resistance, and extremely drug-resistant strains demonstrates the need for improved strategies to discover new drug-based compounds. The development of transcriptomics, proteomics, and metabolomics has provided new tools for global studies of living organisms. However, the compendium of expression profiles produced by these methods has introduced new scientific challenges into antimicrobial research. In this review, we discuss the practical value of transcriptomic techniques as well as their difficulties and pitfalls...
March 13, 2017: Biotechnology Letters
https://www.readbyqxmd.com/read/28289383/the-citrus-flavanone-naringenin-produces-cardioprotective-effects-in-hearts-from-1-year-old-rat-through-activation-of-mitobk-channels
#20
Lara Testai, Eleonora Da Pozzo, Ilaria Piano, Luisa Pistelli, Claudia Gargini, Maria Cristina Breschi, Alessandra Braca, Claudia Martini, Alma Martelli, Vincenzo Calderone
Background and Purpose: Incidence of cardiovascular disorders increases with age, because of a dramatic fall of endogenous self-defense mechanisms and increased vulnerability of myocardium. Conversely, the effectiveness of many cardioprotective drugs is blunted in hearts of 1 year old rat. The Citrus flavanone naringenin (NAR) was reported to promote cardioprotective effects against ischemia/reperfusion (I/R) injury, through the activation of mitochondrial large conductance calcium-activated potassium channel (mitoBK)...
2017: Frontiers in Pharmacology
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