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https://www.readbyqxmd.com/read/28723866/a-case-of-resistance-to-tyrosine-kinase-inhibitor-therapy-small-cell-carcinoma-transformation-concomitant-with-plasma-genotyped-t790m-positivity
#1
Yanjun Xu, Zhiyu Huang, Lei Gong, Yun Fan
Although non-small-cell lung cancer patients with epidermal growth factor receptor (EGFR) mutations are responsive to EGFR-tyrosine kinase inhibitors, drug resistances are always inevitable. The secondary somatic EGFR threonine-methionine substitution at position 790 (T790M) mutation accounts for ∼50% of acquired resistance mechanisms. Small cell lung cancer (SCLC) transformation is a relatively rare mechanism, but has recently attracted considerable attention. The coexistence of both the mechanisms in one patient is much more scarce in clinic...
July 18, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28723615/nanoformulations-of-curcumin-an-emerging-paradigm-for-improved-remedial-application
#2
REVIEW
Meeta Gera, Neelesh Sharma, Mrinmoy Ghosh, Do Luong Huynh, Sung Jin Lee, Taesun Min, Taeho Kwon, Dong Kee Jeong
Curcumin is a natural polyphenol and essential curcuminoid derived from the rhizome of the medicinal plant Curcuma longa (L.) is universally acknowledged as "Wonder drug of life". It is a vital consumable and restorative herb, commonly keened for several ailments such as cancer, arthritis, pain, bruises, gastrointestinal quandaries, swelling and much more. Despite its enormous curative potential, the poor aqueous solubility and consequently, minimal systemic bioavailability with rapid degradation are some of the major factors which restrict the utilization of curcumin at medical perspective...
July 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28722515/construction-of-a-plga-based-targeted-sirna-delivery-system-for-treatment-of-osteoporosis
#3
Deniz Sezlev Bilecen, Jose Carlos Rodriguez-Cabello, Hasan Uludag, Vasif Hasirci
Osteoporosis is a systemic skeletal disorder which occurs when the bone turnover balance is disrupted. With the identification of the genes involved in the pathogenesis of the disease, studies on development of new osteoporosis treatments has intensified. RNA interference (RNAi) mechanism uses short interfering RNA (siRNA) to knockdown disease related gene expression as a treatment approach. Targeting while protecting siRNA against hydrolysis by nucleases in vivo is, however, challenging. The maintenance of therapeutic plasma level is also hampered by the clearance of siRNA from the body...
July 19, 2017: Journal of Biomaterials Science. Polymer Edition
https://www.readbyqxmd.com/read/28722470/novel-potent-inhibitors-of-the-histone-demethylase-kdm1a-lsd1-orally-active-in-a-murine-promyelocitic-leukemia-model
#4
Paolo Trifirò, Anna Cappa, Silvia Brambillasca, Oronza A Botrugno, Maria Rosaria Cera, Roberto Dal Zuffo, Paola Dessanti, Giuseppe Meroni, Florian Thaler, Manuela Villa, Saverio Minucci, Ciro Mercurio, Mario Varasi, Paola Vianello
BACKGROUND: Histone lysine demethylases (KDMs) are well-recognized targets in oncology drug discovery. They function at the post-translation level controlling chromatin conformation and gene transcription. KDM1A is a flavin adenine dinucleotide-dependent amine oxidase, overexpressed in several tumor types, including acute myeloid leukemia, neuroblastoma and non-small-cell lung cancer. Among the many known monoamine oxidase inhibitors screened for KDM1A inhibition, tranylcypromine emerged as a moderately active hit, which irreversibly binds to the flavin adenine dinucleotide cofactor...
July 19, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28721344/exploring-patient-characteristics-and-barriers-to-hepatitis-c-treatment-in-patients-on-opioid-substitution-treatment-attending-a-community-based-fibro-scanning-clinic
#5
Des Crowley, Walter Cullen, Eamon Laird, John S Lambert, Tina Mc Hugh, Carol Murphy, Marie Claire Van Hout
BACKGROUND AND OBJECTIVES: Hepatitis C virus (HCV) infection is a major public health issue. There is substandard uptake in HCV assessment and treatment among people who inject drugs (PWID). Community fibroscanning is used to assess disease severity and target treatment. METHODS: A survey was administered to a cohort of chronically HCV infected patients attending a community fibroscanning clinic. Questions targeted diagnosis of HCV, suitability, willingness and barriers to engagement in treatment...
June 2017: Journal of Translational Internal Medicine
https://www.readbyqxmd.com/read/28720783/a-simple-robust-and-efficient-computational-method-for-n-octanol-water-partition-coefficients-of-substituted-aromatic-drugs
#6
Asrin Bahmani, Saadi Saaidpour, Amin Rostami
In this paper, multiple linear regression (MLR) was used to build quantitative structure property relationship (QSPR) of n-octanol-water partition coefficient (logPo/w) of 195 substituted aromatic drugs. The molecular descriptors were calculated for each compound by the VLifeMDS. By applying genetic algorithm/multiple linear regressions (GA/MLR) the most relevant descriptors were selected to build a QSPR model. The robustness of the model was characterized by the statistical validation and applicability domain (AD)...
July 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28720478/monoamine-receptor-interaction-profiles-of-4-thio-substituted-phenethylamines-2c-t-drugs
#7
REVIEW
Dino Luethi, Daniel Trachsel, Marius C Hoener, Matthias E Liechti
BACKGROUND: 4-Thio-substituted phenethylamines (2C-T drugs) are potent psychedelics with poorly defined pharmacological properties. Because of their psychedelic effects, 2C-T drugs are sometimes sold as new psychoactive substances (NPSs). The aim of the present study was to characterize the monoamine receptor and transporter interaction profiles of a series of 2C-T drugs. METHODS: We determined the binding affinities of 2C-T drugs at monoamine receptors and transporters in human cells that were transfected with the respective receptors or transporters...
July 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28719060/drug-use-and-phylogenetic-clustering-of-hepatitis-c-virus-infection-among-people-who-use-drugs-in-vancouver-canada-a-latent-class-analysis-approach
#8
Brendan Jacka, Bethany Bray, Tanya L Applegate, Brandon Dl Marshall, Viviane Dias Lima, Kanna Hayashi, Kora DeBeck, Jayna Raghwani, P Richard Harrigan, Mel Krajden, Julio Montaner, Jason Grebely
BACKGROUND: This study estimated latent classes (i.e., unobserved subgroups in a population) of people who use drugs in Vancouver, Canada and examined how these classes relate to phylogenetic clustering of hepatitis C virus (HCV) infection. METHODS: HCV antibody positive people who use drugs from two cohorts in Vancouver, Canada (1996-2012) with a Core-E2 sequence were included. Time-stamped phylogenetic trees were inferred and phylogenetic clustering was determined by time to most common recent ancestor...
July 18, 2017: Journal of Viral Hepatitis
https://www.readbyqxmd.com/read/28717247/characterization-of-hiv-1-integrase-interaction-with-human-ku70-protein-and-initial-implications-for-drug-targeting
#9
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/28716156/generic-atorvastatin-is-as-effective-as-the-brand-name-drug-lipitor-%C3%A2-in-lowering-cholesterol-levels-a-cross-sectional-retrospective-cohort-study
#10
Alexander Loch, Jan Philipp Bewersdorf, Daniel Kofink, Dzafir Ismail, Imran Zainal Abidin, Ramesh Singh Veriah
BACKGROUND: In a world of ever increasing health care costs, generic drugs represent a major opportunity to ensure access to essential medicines for people who otherwise would be unable to afford them. However, some clinicians and patients are still questioning the safety and effectiveness of generic formulations compared to the proprietary drugs necessitating further systematic research analyzing the generic drugs' efficacy. Our objective was to compare the lipid lowering effects of generic and branded atorvastatin...
July 17, 2017: BMC Research Notes
https://www.readbyqxmd.com/read/28715605/how-to-select-a-nanosimilar
#11
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/28713018/effect-of-increased-surface-hydrophobicity-via-drug-conjugation-on-the-clearance-of-inhaled-pegylated-polylysine-dendrimers
#12
Shadabul Haque, Victoria M McLeod, Seth Jones, Sandy Fung, Michael Whittaker, Michelle McIntosh, Colin Pouton, David J Owen, Christopher J H Porter, Lisa M Kaminskas
PEGylated polylysine dendrimers are attractive and well tolerated inhalable drug delivery platforms that have the potential to control the release, absorption kinetics and lung retention time of conjugated drugs. The clinical application of these systems though, would likely require partial substitution of surface PEG groups with drug molecules that are anticipated to alter their lung clearance kinetics and clearance pathways. In the current study, we therefore evaluated the impact of increased surface hydrophobicity via substitution of 50% surface PEG groups with a model hydrophobic drug (α-carboxyl OtButylated methotrexate) on the lung clearance of a Generation 5 PEGylated polylysine dendrimer in rats...
July 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28712749/nicotine-and-cocaine-triggered-methamphetamine-reinstatement-in-female-and-male-sprague-dawley-rats
#13
Steven T Pittenger, Shinnyi Chou, Scott T Barrett, Isabella Catalano, Maxwell Lydiatt, Rick A Bevins
Preclinical studies have demonstrated a return to methamphetamine (meth)-seeking behavior (reinstatement) induced by injections of meth administered by the experimenter (drug-prime). Notably, females tend to be more sensitive to drug-prime; often displaying more reinstatement behavior when compared to males. While meth-primed reinstatement of meth-seeking behavior has been established, little is known about the ability of other drugs of abuse to substitute for meth during drug-primed reinstatement; nicotine and cocaine were the focus of the present work...
July 13, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28712298/the-fragment-network-a-chemistry-recommendation-engine-built-using-a-graph-database
#14
Richard J Hall, Christopher W Murray, Marcel L Verdonk
The hit validation stage of a fragment-based drug discovery campaign involves probing the SAR around one or more fragment hits. This often requires a search for similar compounds in a corporate collection or from commercial suppliers. The Fragment Network is a graph database that allows a user to efficiently search chemical space around a compound of interest. The result set is chemically intuitive, naturally grouped by substitution pattern and meaningfully sorted according to the number of observations of each transformation in medicinal chemistry databases...
July 15, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28711857/methotrexate-f127-conjugated-mesoporous-zinc-hydroxyapatite-as-an-efficient-drug-delivery-system-for-overcoming-chemotherapy-resistance-in-osteosarcoma-cells
#15
Azadeh Meshkini, Hamid Oveisi
The resistance of cancer cells to chemotherapeutic agents and the poor selectivity of drugs toward tumor cells are regarded as the main impediments in successful cancer therapy. Currently, the design and fabrication of stimulus-responsive drug delivery systems with high specificity toward cancer cells are gaining increasing attention and they show a promising potential for clinical applications. In this study, mesoporous zinc-substituted hydroxyapatite has been synthesized and served as a drug delivery vehicle owing to its biocompatibility and high drug loading capacity...
July 4, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28710963/2-substituted-3-7-8-trimethylnaphtho-1-2-b-furan-4-5-diones-as-specific-l-shaped-nqo1-mediated-redox-modulators-for-the-treatment-of-non-small-cell-lung-cancer
#16
Xiaojin Zhang, Jinlei Bian, Xiang Li, Xingsen Wu, Yanan Dong, Qidong You
Based on the scaffold of 3,7,8-trimethylnaphtho[1,2-b]furan-4,5-dione, a series of L-shaped derivatives with substituted side chains at the position of C2 were designed by analyzing the binding mode with NQO1. The drug-like compound 6q (named as DDO-7178) emerged as the most specific substrate of the two-electron oxidoreductase NQO1 and could hardly be reduced by one-electron oxidoreductases CPR (NQO1/CPR = 20.8). In addition, compound 6q showed much improved physicochemical properties such as water solubility than the control β-lap...
June 15, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28708940/the-street-like-synthesis-of-krokodil-results-in-the-formation-of-an-enlarged-cluster-of-known-and-new-morphinans-with-therapeutic-potential
#17
José Soares, Emanuele Alves, André Silva, Natália Figueiredo, João F Neves, Sara Cravo, Maria Rangel, Annibal Netto, Félix Carvalho, Ricardo Jorge Dinis-Oliveira, Carlos Afonso
"Krokodil" is the street name for a homemade injectable drug that has been used as a cheap substitute for heroin. Codeine is the opioid starting material for krokodil synthesis and desomorphine is the opioid claimed to be the main component of krokodil and the main responsible for its addictive and psychoactive characteristics. However, due to its peculiar manufacture, using cheap raw materials, krokodil is composed by a large and complex mixture of different substances. In order to shed some light upon the chemical complexity of krokodil, its profiling was conducted by reverse phase high performance liquid chromatography coupled to photodiode array detector (RP-HPLC-DAD) and by liquid chromatography coupled to high resolution tandem mass spectrometry (LC-ESI-IT-Orbitrap-MS)...
July 14, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28708938/interactions-between-quinolones-and-bacillus-anthracis-gyrase-and-the-basis-of-drug-resistance
#18
Rachel E Ashley, Robert Hunter Lindsey, Sylvia A McPherson, Charles L Turnbough, Robert J Kerns, Neil Osheroff
Gyrase appears to be the primary cellular target for quinolone antibacterials in multiple pathogenic bacteria, including Bacillus anthracis, the causative agent of anthrax. Given the significance of this type II topoisomerase as a drug target, it is critical to understand how quinolones interact with gyrase and how specific mutations lead to resistance. However, these important issues have yet to be addressed for a canonical gyrase. Therefore, we utilized a mechanistic approach to characterize quinolone interactions with wild-type B...
July 14, 2017: Biochemistry
https://www.readbyqxmd.com/read/28708385/chloroquine-modified-hydroxyethyl-starch-as-a-polymeric-drug-for-cancer-therapy
#19
Richard Sleightholm, Bin Yang, Fei Yu, Ying Xie, David Oupický
Hydroxyethyl starch (HES) is a clinically used polysaccharide colloidal plasma volume expander. The goal of this study was to synthesize HES modified with hydroxychloroquine (HCQ) as a novel polymeric drug with the ability to inhibit the invasive character of pancreatic cancer (PC) cells. HES was conjugated with HCQ using a simple carbonyldiimidazole coupling to prepare Chloroquine-modified HES (CQ-HES). CQ-HES with various degrees of HCQ substitution were synthesized and characterized. Atomic force microscopy was used to demonstrate a pH-dependent assembly of CQ-HES into well-defined nanoparticles...
July 14, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28707284/fixed-dose-versus-off-label-combination-of-isosorbide-dinitrate-plus-hydralazine-hydrochloride-retrospective-propensity-matched-analysis-in-black-medicare-patients-with-heart-failure
#20
Elizabeth Ofili, Inder Anand, Richard Allen Williams, Ola Akinboboye, Liou Xu, Gary Puckrein
INTRODUCTION: Based upon the findings of the African-American Heart Failure Trial, the US Food and Drug Administration approved the fixed-dose combination of isosorbide dinitrate (ISDN) and hydralazine hydrochloride (HYD) (FDC-ISDN/HYD) as a new drug for treatment of heart failure (HF) in self-identified African Americans. According to the FDA, FDC-ISDN/HYD has no therapeutic equivalent. However, off-label combinations of the separate generic drugs ISDN and HYD (OLC-ISDN+HYD) or isosorbide mononitrate (ISMN) and HYD (OLC-ISMN+HYD) are routinely substituted without any supporting outcome data...
July 13, 2017: Advances in Therapy
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