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https://www.readbyqxmd.com/read/28741098/regulation-of-paclitaxel-activity-by-microtubule-associated-proteins-in-cancer-chemotherapy
#1
REVIEW
Xingjuan Shi, Xiaoou Sun
Microtubules, highly dynamic components of the cytoskeleton, participate in diverse cellular activities such as mitosis, cell migration, and intracellular trafficking. Dysregulation of microtubule dynamics contributes to the development of serious diseases, including cancer. The dynamic properties and functions of microtubule network are regulated by microtubule-associated proteins. Paclitaxel, an anti-microtubule agent of the taxane family, has shown a success in clinical treatment of many cancer patients...
July 24, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28740519/low-dose-diclofenac-in-patients-with-fragility-fractures
#2
Letizia Vannucci, Caterina Fossi, Giorgio Gronchi, Maria Luisa Brandi
Most osteoporotic patients complain of back pain one year after a fragility vertebral fracture and the frequency of chronic back pain increases with increasing age. The use of the lowest effective dose of an analgesic which is able to control symptoms seems to be a possible solution in order to limit potential side effects in multi-treated elderly patients. Non-steroidal anti-inflammatory drugs (NSAIDs) have a proven efficacy in the treatment of back pain associated with fragility vertebral fractures and diclofenac is available at low-dose subcutaneous injective formulation...
January 2017: Clinical Cases in Mineral and Bone Metabolism
https://www.readbyqxmd.com/read/28734001/control-of-reversible-activation-dynamics-of-ru-%C3%AE-%C3%A2-%C3%AE%C2%BA%C3%A2-c%C3%A2-h%C3%A2-c%C3%A2-h%C3%A2-nh%C3%A2-xy-n-and-the-effect-of-chelate-ligand-variation
#3
Francisco Martínez-Peña, Ana M Pizarro
The potential use of organometallic ruthenium complexes as anticancer drugs is well known. Here we show a family of activatable tethered ruthenium(II) arene complexes of general formula [Ru(η⁶:κ¹-C₆H₅(C₆H₄)NH₂)(XY)]n+ (closed tether-ring) bearing different chelating XY ligands (XY = aliphatic diamine, phenylenediamine, oxalato, bis(phosphino)ethane). The activation of these complexes (closed-to-open tether conversion) occurs in methanol and dimethylsulfoxide at different rates, and to different reaction extents at equilibrium...
July 22, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28733192/pharmacological-evaluation-of-phytochemicals-from-south-indian-black-turmeric-curcuma-caesia-roxb-to-target-cancer-apoptosis
#4
K S Mukunthan, R S Satyan, T N Patel
Curcuma caesia Roxb. (Black turmeric), a perennial herb of the family Zingiberaceae is indigenous to India. C. caesia is used as a spice, food preservative and coloring agent commonly in the Indian subcontinent. Functional parametric pharmacological evaluations like drug ability and toxicity profile of this endangered species is poorly documented. In our present study, among all the extracts of dried C. caesia rhizome viz- hexane, ethyl acetate, methanol and water tested for free radical scavenging capacity by total antioxidant activity (TAO) method, Hexane Rhizome Extract (HRE) wzs found to possess remarkable activity (1200mg ascorbic acid equivalent/100g)...
July 18, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28731962/polymorphisms-in-cytochrome-p450-oxidoreductase-and-its-effect-on-drug-metabolism-and-efficacy
#5
Liang Gong, Cong-Min Zhang, Jin-Feng Lv, Hong-Hao Zhou, Lan Fan
Cytochrome P450 oxidoreductase (POR) has played a potential role in the metabolism of drugs and steroids by supplying electrons to microsomal cytochrome P450 (CYP) enzymes. More than 200 different POR mutations and polymorphisms causing more than 130 amino acid changes in the POR protein have been reported since 2004. A503V is a common amino acid sequence variant encoded by POR*28, whereas A287P and R457H are the most common disease-causing mutations in Europeans and Asians, respectively. Polymorphisms in the POR gene can affect POR activity, CYP-mediated drug metabolism activities, and the efficacy of several clinically used drugs...
July 20, 2017: Pharmacogenetics and Genomics
https://www.readbyqxmd.com/read/28731321/conjugation-dependent-interaction-of-folic-acid-with-folate-binding-protein
#6
Rachel Leah Merzel, Carolina Frey, Junjie Chen, Rachel Garn, Mallory A van Dongen, Casey A Dougherty, Ananda Kandaluru, Philip S Low, E Neil G Marsh, Mark M Banaszak Holl
Serum proteins play a critical role in the transport, uptake, and efficacy of targeted drug therapies, and here we investigate the interactions between folic acid-polymer conjugates and serum folate binding protein (FBP), the soluble form of the cellular membrane-bound folate receptor. We demonstrate that both choice of polymer and method of ligand conjugation affect the interactions between folic acid-polymer conjugates and serum FBP, resulting in changes in the folic acid-induced protein aggregation process...
July 21, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28723805/acute-pancreatitis-induced-by-etoposide-lobaplatin-combination-chemotherapy-used-for-the-treatment-of-lung-cancer-a-case-report-and-literature-review
#7
Cheng-Liang Cao, Peng-Yu Duan, Wang-Jun Zhang, Le Li, Feng-Zhi Qu, Bei Sun, Gang Wang
RATIONALE: Drug-induced pancreatitis (DIP) is a rare type of pancreatitis that is not usually observed in the clinical practice. It is generally difficult to distinguish from acute pancreatitis (AP) induced by other causes. PATIENT CONCERNS: Here, we report a 62-year-old Chinese female patient with "small cell lung cancer" as the initial presentation. Because the patient could not bear the surgical treatment, the chemotherapy composed of lobaplatin and etoposide was performed...
July 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28721209/recent-advances-in-preventing-stroke-recurrence
#8
REVIEW
J David Spence
Recent advances in secondary stroke prevention include new evidence in hypertension, nutrition, anticoagulation, antiplatelet therapy, intracranial stenosis, percutaneous closure of patent foramen ovale, and lipid-lowering therapy. Individualized therapy for hypertension based on phenotyping with plasma renin and aldosterone markedly improves blood pressure control in patients with resistant hypertension. A Mediterranean diet can reduce the risk of stroke by nearly half. The diagnosis and treatment of metabolic vitamin B12 deficiency, and B vitamins to lower homocysteine, can reduce the risk of stroke by approximately 30%...
2017: F1000Research
https://www.readbyqxmd.com/read/28718624/covalent-enzyme-inhibition-through-fluorosulfate-modification-of-a-non-catalytic-serine-residue
#9
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/28715605/how-to-select-a-nanosimilar
#10
Alain Astier, Amy Barton Pai, Marco Bissig, Daan J A Crommelin, Beat Flühmann, Jean-Daniel Hecq, Josefien Knoeff, Hans-Peter Lipp, Alberto Morell-Baladrón, Stefan Mühlebach
Nanomedicines in the class of nonbiological complex drugs (NBCDs) are becoming increasingly available. Up to 23 nanomedicines have been approved, and approximately 50 are in clinical development. Meanwhile, the first nanosimilars have entered the market through the generic approval pathway, but clinical differences have been observed. Many healthcare professionals may be unaware of this issue and must be informed of these clinically relevant variances. This article provides a tool for rational decision making for the inclusion of nanomedicines into the hospital formulary, including defined criteria for evaluation of substitutability or interchangeability...
July 17, 2017: Annals of the New York Academy of Sciences
https://www.readbyqxmd.com/read/28713851/building-an-experimental-model-of-the-human-body-with-non-physiological-parameters
#11
Joseph M Labuz, Christopher Moraes, David R Mertz, Brendan M Leung, Shuichi Takayama
New advances in engineering and biomedical technology have enabled recent efforts to capture essential aspects of human physiology in microscale, in-vitro systems. The application of these advances to experimentally model complex processes in an integrated platform - commonly called a 'human-on-a-chip (HOC)' - requires that relevant compartments and parameters be sized correctly relative to each other and to the system as a whole. Empirical observation, theoretical treatments of resource distribution systems and natural experiments can all be used to inform rational design of such a system, but technical and fundamental challenges (e...
March 2017: Technology
https://www.readbyqxmd.com/read/28712182/trend-of-irrational-medication-among-the-students-of-department-of-pharmacy-abbottabad-university-of-science-and-technology-in-common-cold-and-flu
#12
Mujeeb Ur Rehman, Saif Ullah Mehsud, Sartaj Ali, Muhammad Ishaq, Mumtaz Ali Khan
BACKGROUND: Common cold and flu are mostly of viral pathogenesis with symptoms in upper respiratory tract. It is highly contagious and close inter-individual contact in winter season increase the spread spectrum. Mis-interpretation with bacterial cause leads to irrationality in its medication. METHODS: A cross-sectional study was conducted among pharmacy department students in February-March 2016. Data were collected through self-administered questionnaire and expressed as percentage frequency...
January 2017: Journal of Ayub Medical College, Abbottabad: JAMC
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
#13
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/28711350/synthesis-and-biological-evaluation-of-pyrrole-based-chalcones-as-cyp1-enzyme-inhibitors-for-possible-prevention-of-cancer-and-overcoming-cisplatin-resistance
#14
Ibidapo S Williams, Prashant Joshi, Linda Gatchie, Mohit Sharma, Naresh K Satti, Ram A Vishwakarma, Bhabatosh Chaudhuri, Sandip B Bharate
Inhibitors of CYP1 enzymes may play vital roles in the prevention of cancer and overcoming chemo-resistance to anticancer drugs. In this letter, we report synthesis of twenty-three pyrrole based heterocyclic chalcones which were screened for inhibition of CYP1 isoforms. Compound 3n potently inhibited CYP1B1 with an IC50 of ∼0.2μM in Sacchrosomes™ and CYP1B1-expressing live human cells. However, compound 3j which inhibited both CYP1A1 and CYP1B1 with an IC50 of ∼0.9µM, using the same systems, also potently antagonized B[a]P-mediated induction of AhR signaling in yeast (IC50, 1...
July 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28708390/softwood-lignin-self-assembly-for-nanomaterial-design
#15
Stefan Salentinig, Mark Schubert
Lignin is a natural, renewable biopolymer synthesized by plants. It is a macromolecule consisting of aromatic structures with high density of functional groups making it an ideal precursor for the design of sustainable biomaterials for applications such as drug delivery. The rational design of these materials requires an in-depth understanding of the underlying lignin self-assembly in solution. Colloidal transformations from nano-sized lignin assemblies to sub-micron sized spherical particles upon solvent exchange were studied using small angle X-ray scattering, dynamic light scattering and electron microscopy...
July 14, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28707592/rational-drug-design-of-antineoplastic-agents-using-3d-qsar-cheminformatic-and-virtual-screening-approaches
#16
Jelica Vucicevic, Katarina Nikolic, John B O Mitchell
BACKGROUND: Computer-Aided Drug Design has strongly accelerated the development of novel antineoplastic agents by helping in the hit identification, optimization, and evaluation. RESULTS: Computational approaches such as cheminformatic search, virtual screening, pharmacophore modeling, molecular docking and dynamics have been developed and applied to explain the activity of bioactive molecules, design novel agents, increase the success rate of drug research, and decrease the total costs of drug discovery...
July 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28705120/qsar-docking-admet-system-pharmacology-studies-on-tormentic-acid-derivatives-for-anticancer-activity
#17
Sarfaraz Alam, Feroz Khan
To explore the anticancer compounds from tormentic acid derivatives, a quantitative structure-activity relationship (QSAR) model was developed by the multiple linear regression methods. The developed QSAR model yielded a high activity-descriptors relationship accuracy of 94% referred by regression coefficient (r(2)= 0.94) and a high activity prediction accuracy of 91%. The QSAR study indicates that chemical descriptors, chiV5, T_T_Cl_7, T_2_T_4, SsCH3count, and Epsilon3 are significantly correlated with anticancer activity...
July 14, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28705017/impact-of-geometry-optimization-methods-on-qsar-modelling-a-case-study-for-predicting-human-serum-albumin-binding-affinity
#18
S Önlü, M Türker Saçan
Quantitative structure-activity relationship (QSAR) modelling is a major tool employed in the prediction of various endpoints. However, current QSAR literature is missing a full understanding of the impact of quantum chemical calculation methods on the estimation of molecular descriptors and model performance. Here, we provide a comprehensive analysis of the quantitative effects of different geometry optimization methods (semi-empirical, ab initio Hartee-Fock and density functional theory) on the molecular descriptors...
July 14, 2017: SAR and QSAR in Environmental Research
https://www.readbyqxmd.com/read/28702309/encouraging-rational-antibiotic-use-in-childhood-pneumonia-a-focus-on-vietnam-and-the-western-pacific-region
#19
REVIEW
Nguyen T K Phuong, Tran T Hoang, Pham H Van, Lolyta Tu, Stephen M Graham, Ben J Marais
Globally, pneumonia is considered to be the biggest killer of infants and young children (aged <5 years) outside the neonatal period, with the greatest disease burden in low- and middle-income countries. Optimal management of childhood pneumonia is challenging in settings where clinicians have limited information regarding the local pathogen and drug resistance profiles. This frequently results in unnecessary and poorly targeted antibiotic use. Restricting antibiotic use is a global priority, particularly in Asia and the Western Pacific Region where excessive use is driving high rates of antimicrobial resistance...
2017: Pneumonia
https://www.readbyqxmd.com/read/28699813/prolylcarboxypeptidase-prcp-inhibitors-and-the-therapeutic-uses-thereof-a-patent-review
#20
Thomas H Graham
Prolylcarboxypeptidase (PrCP) is a serine protease that produces or degrades signaling proteins in several important pathways including the renin-angiotensin system (RAS), kallikrein-kinin system (KKS) and pro-opiomelanocortin (POMC) system. PrCP has the potential to be a therapeutic target for cardiovascular, inflammatory and metabolic diseases. Numerous classes of PrCP inhibitors have been developed by rational drug design and from high-throughput screening hits. These inhibitors have been tested in mouse models to assess their potential as new therapeutics...
July 12, 2017: Expert Opinion on Therapeutic Patents
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