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https://www.readbyqxmd.com/read/28550801/the-nk-1-receptor-antagonist-l-732-138-induces-apoptosis-in-human-gastrointestinal-cancer-cell-lines
#1
Miguel Muñoz, Marisa Rosso, Rafael Coveñas
BACKGROUND: Gastric and colon cancer cells express the neurokinin-1 receptor (NK-1R) and the peptide substance P (SP), after binding to this receptor, elicits the proliferation of gastrointestinal cancer cells and an antiapoptotic effect. In these cells, NK-1R antagonists (L-733,060: a piperidine derivative; aprepitant: a morpholine derivative) block, after binding to the NK-1R, the action of SP and exert an antiproliferative action, both antagonists promote apoptosis and the death of cancer cells...
February 12, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28550249/avn-492-a-novel-highly-selective-5-ht6r-antagonist-preclinical-evaluation
#2
Alexandre V Ivachtchenko, Ilya Okun, Vladimir Aladinskiy, Yan Ivanenkov, Angela Koryakova, Ruben Karapetyan, Oleg Mitkin, Ramiz Salimov, Andrey Ivashchenko
Discovery of 5-HT6 receptor subtype and its exclusive localization within the central nervous system led to extensive investigations of its role in Alzheimer's disease, schizophrenia, and obesity. In the present study, we present preclinical evaluation of a novel highly-potent and highly-selective 5-HT6R antagonist, AVN-492. The affinity of AVN-492 to bind to 5-HT6R (Ki = 91 pM) was more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (Ki = 170 nM). Thus, the compound displayed great 5-HT6R selectivity against all other serotonin receptor subtypes, and is extremely specific against any other receptors such as adrenergic, GABAergic, dopaminergic, histaminergic, etc...
May 25, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28550055/potential-drug-interactions-mediated-by-renal-organic-anion-transporter-oatp4c1
#3
Toshihiro Sato, Eikan Mishima, Nariyasu Mano, Takaaki Abe, Hiroaki Yamaguchi
OATP4C1 is an organic anion transporter expressed in the basolateral membrane of the renal proximal tubules. It plays a major role in the urinary excretion of both exogenous drugs and endogenous compounds. Our previous studies have indicated the importance of OATP4C1 in pathological and physiological conditions; however, the majority of its pharmacological characteristics remained unclear. Therefore, to provide essential information for clinical drug therapy decisions and drug development, we, in this study, attempted to clarify drug interactions mediated by OATP4C1...
May 26, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28549889/synthesis-and-evaluation-of-novel-dual-brd4-hdac-inhibitors
#4
Seika Amemiya, Takao Yamaguchi, Yuichi Hashimoto, Tomomi Noguchi-Yachide
Epigenetic regulation of gene expression via histone acetylation modulates many cellular processes, including apoptosis, the cell cycle, cell growth and differentiation, and inhibitors are promising drug candidates. We have previously developed inhibitors of BRD4, which recognizes acetylated lysine residue on histones and recruits transcription elongation factor to the transcription start site, while inhibitors of histone deacetylase (HDAC), which catalyzes the removal of acetyl groups on histones, are already in clinical use for cancer treatment...
May 17, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28549802/design-synthesis-and-biological-evaluation-of-novel-androst-3-5-diene-3-carboxylic-acid-derivatives-as-inhibitors-of-5%C3%AE-reductase-type-1-and-2
#5
Kejing Lao, Jie Sun, Chong Wang, Weiting Lyu, Boshen Zhou, Ruheng Zhao, Qian Xu, Qidong You, Hua Xiang
5α-Reductase is a key enzyme responsible for dihydrotestosterone biosynthesis and has been recognized as an important target for discovering new drugs against benign prostatic hyperplasia (BPH). In this study, a series of novel steroidal androst-3,5-diene-3-carboxylic acids have been designed and synthesized. Biological evaluations were performed on their 5α-reductase inhibitory activities by both in vitro enzyme inhibition assay and in vivo by prostate weighing method. Results showed that most of them displayed excellent 5α-reductase inhibitory potency...
May 23, 2017: Steroids
https://www.readbyqxmd.com/read/28549433/js-k-a-nitric-oxide-pro-drug-regulates-growth-and-apoptosis-through-the-ubiquitin-proteasome-pathway-in-prostate-cancer-cells
#6
Guobin Tan, Mingning Qiu, Lieqian Chen, Sai Zhang, Longzhi Ke, Jianjun Liu
BACKGROUND: In view of the fact that JS-K might regulate ubiquitin E3 ligase and that ubiquitin E3 ligase plays an important role in the mechanism of CRPC formation, the goal was to investigate the probable mechanism by which JS-K regulates prostate cancer cells. METHODS: Proliferation inhibition by JS-K on prostate cancer cells was examined usingCCK-8 assays. Caspase 3/7 activity assays and flow cytometry were performed to examine whether JS-K induced apoptosis in prostate cancer cells...
May 26, 2017: BMC Cancer
https://www.readbyqxmd.com/read/28549369/safety-analysis-of-occupational-exposure-of-healthcare-workers-to-residual-contaminations-of-cytotoxic-drugs-using-fmeca-security-approach
#7
Laetitia Minh Mai Le, Delphine Reitter, Sophie He, Franck Té Bonle, Amélie Launois, Diane Martinez, Patrice Prognon, Eric Caudron
Handling cytotoxic drugs is associated with chemical contamination of workplace surfaces. The potential mutagenic, teratogenic and oncogenic properties of those drugs create a risk of occupational exposure for healthcare workers, from reception of starting materials to the preparation and administration of cytotoxic therapies. The Security Failure Mode Effects and Criticality Analysis (FMECA) was used as a proactive method to assess the risks involved in the chemotherapy compounding process. FMECA was carried out by a multidisciplinary team from 2011 to 2016...
May 22, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28549321/studies-on-free-radical-scavenging-cancer-cell-antiproliferation-and-calf-thymus-dna-interaction-of-schiff-bases
#8
Cleiton M da Silva, Marina M Silva, Fabiano S Reis, Ana Lúcia T G Ruiz, João E de Carvalho, Josué C C Santos, Isis M Figueiredo, Rosemeire B Alves, Luzia V Modolo, Ângelo de Fátima
Thirty-nine Schiff bases were synthesized by performing microwave-assisted condensation of the corresponding aldehydes and aromatic amines. Their reactive nitrogen species (RNS) scavenging activity and inhibitory effects against cancer cell growth were then subsequently investigated. Additionally, the interaction between the calf thymus DNA (ctDNA) and selected Schiff bases was evaluated using fluorescence spectroscopy, and their binding parameters were determined. The yields of the various compounds ranged from moderate to excellent (43-99%) after only a 2-min reaction...
May 17, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28549311/reaction-of-diazepam-and-related-benzodiazepines-with-chlorine-kinetics-transformation-products-and-in-silico-toxicological-assessment
#9
Inmaculada Carpinteiro, Rosario Rodil, José Benito Quintana, Rafael Cela
In this work, the reaction of four benzodiazepines (diazepam, oxazepam, nordazepam and temazepam) during water chlorination was studied by means of liquid chromatography-quadrupole-time of flight-mass spectrometry (LC-QTOF-MS). For those compounds that showed a significant degradation, i.e. diazepam, oxazepam and nordazepam, parameters affecting to the reaction kinetics (pH, chlorine and bromide level) were studied in detail and transformation products were tentatively identified. The oxidation reactions followed pseudofirst-order kinetics with rate constants in the range of 1...
May 3, 2017: Water Research
https://www.readbyqxmd.com/read/28549262/passive-sampling-of-wastewater-as-a-tool-for-the-long-term-monitoring-of-community-exposure-illicit-and-prescription-drug-trends-as-a-proof-of-concept
#10
J A Baz-Lomba, Christopher Harman, Malcolm Reid, Kevin V Thomas
A passive sampling device, the Polar Organic Chemical Integrative Sampler (POCIS), was calibrated in-situ over a 4-week period in Oslo (Norway) for 10 illicit drugs and pharmaceuticals with the goal of developing an approach for monitoring long-term wastewater drug loads. The calibrations were performed in triplicate using three different overlapping calibration sets under changing environmental conditions that allowed the uncertainty of the sampling rates to be evaluated. All 10 compounds exhibited linear uptake kinetics and provided sampling rates of between 0...
May 20, 2017: Water Research
https://www.readbyqxmd.com/read/28548834/subtly-modulating-glycogen-synthase-kinase-3-%C3%AE-allosteric-inhibitors-development-and-their-potential-for-the-treatment-of-chronic-diseases
#11
Valle Palomo, Daniel I Pérez, Carlos Roca, Cara Anderson, Natalia Rodriguez-Muela, Concepción Pérez, Jose A Morales-Garcia, Julio A Reyes, Nuria E Campillo, Ana M Pérez-Castillo, Lee L Rubin, Lubov T Timchenko, Carmen Gil, Ana Martínez
Glycogen synthase kinase 3 β (GSK-3β) is a central target in several unmet diseases. To increase the specificity of GSK-3β inhibitors in chronic treatments we are developing small molecules allowing subtle modulation of GSK-3β activity. Design synthesis, structure-activity relationships and binding mode of quinoline-3-carbohydrazide derivatives as allosteric modulators of GSK-3β are here presented. Furthermore, we show how allosteric binders may overcome the β-catenin side effects associated to strong GSK-3β inhibition...
May 26, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28548561/effect-of-honey-and-royal-jelly-against-cisplatin-induced-nephrotoxicity-in-patients-with-cancer
#12
Hasnaa Osama, Aya Abdullah, Bassma Gamal, Dina Emad, Doha Sayed, Eman Hussein, Eman Mahfouz, Joy Tharwat, Sally Sayed, Shrouk Medhat, Treza Bahaa, Mohamed E A Abdelrahim
OBJECTIVES: Cisplatin constitutes one of the most potent antineoplastic drugs; however, nephrotoxicity limited its eligibility for optimal clinical use. This study was designed to evaluate the role of honey and royal jelly with antioxidant properties in the protection of cisplatin-induced acute kidney injury in patients with cancer. METHODS: Patients with cancer assigned for cisplatin chemotherapy were randomly divided into bee honey and royal jelly groups pretreated before the initiation and during cisplatin chemotherapeutic regimen and control group on cisplatin only...
May 26, 2017: Journal of the American College of Nutrition
https://www.readbyqxmd.com/read/28548305/development-and-validation-of-an-lc-ms-ms-method-to-quantify-lysergic-acid-diethylamide-lsd-iso-lsd-2-oxo-3-hydroxy-lsd-and-nor-lsd-and-identify-novel-metabolites-in-plasma-samples-in-a-controlled-clinical-trial
#13
Patrick C Dolder, Matthias E Liechti, Katharina M Rentsch
BACKGROUND: Lysergic acid diethylamide (LSD) is a widely used recreational drug. The aim of this study was to develop and validate a liquid chromatography tandem mass spectrometry (LC-MS/MS) method for the quantification of LSD, iso-LSD, 2-oxo-3-hydroxy LSD (O-H-LSD), and nor-LSD in plasma samples from 24 healthy subjects after controlled administration of 100 μg LSD in a clinical trial. In addition, metabolites that have been recently described in in vitro studies, including lysergic acid monoethylamide (LAE), lysergic acid ethyl-2-hydroxyethylamide (LEO), 2-oxo-LSD, trioxylated-LSD, and 13/14-hydroxy-LSD, should be identified...
May 26, 2017: Journal of Clinical Laboratory Analysis
https://www.readbyqxmd.com/read/28548080/discovery-of-first-in-class-reversible-dual-small-molecule-inhibitors-against-g9a-and-dnmts-in-hematological-malignancies
#14
Edurne San José-Enériz, Xabier Agirre, Obdulia Rabal, Amaia Vilas-Zornoza, Juan A Sanchez-Arias, Estibaliz Miranda, Ana Ugarte, Sergio Roa, Bruno Paiva, Ander Estella-Hermoso de Mendoza, Rosa María Alvarez, Noelia Casares, Victor Segura, José I Martín-Subero, François-Xavier Ogi, Pierre Soule, Clara M Santiveri, Ramón Campos-Olivas, Giancarlo Castellano, Maite Garcia Fernandez de Barrena, Juan Roberto Rodriguez-Madoz, Maria José García-Barchino, Juan Jose Lasarte, Matias A Avila, Jose Angel Martinez-Climent, Julen Oyarzabal, Felipe Prosper
The indisputable role of epigenetics in cancer and the fact that epigenetic alterations can be reversed have favoured development of epigenetic drugs. In this study, we design and synthesize potent novel, selective and reversible chemical probes that simultaneously inhibit the G9a and DNMTs methyltransferase activity. In vitro treatment of haematological neoplasia (acute myeloid leukaemia-AML, acute lymphoblastic leukaemia-ALL and diffuse large B-cell lymphoma-DLBCL) with the lead compound CM-272, inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death...
May 26, 2017: Nature Communications
https://www.readbyqxmd.com/read/28547936/fragment-based-drug-discovery-as-alternative-strategy-to-the-drug-development-for-neglected-diseases
#15
REVIEW
Juliana da Fonseca Rezende E Mello, Renan Augusto Gomes, Drielli Gomes Vital-Fujii, Glaucio Monteiro Ferreira, Gustavo Henrique Goulart Trossini
Neglected diseases (NDs) affect large populations and almost whole continents, representing 12% of the global health burden. In contrast, the treatment available today is limited and sometimes ineffective. Under this scenery, the Fragment-Based Drug Discovery (FBDD) emerged as one of the most promising alternatives to the traditional methods of drug development. This method allows achieving new lead compounds with smaller size of fragment libraries. Even with the wide Fragment-Based Drug Discovery success resulting in new effective therapeutic agents against different diseases, until this moment few studies have been applied this approach for NDs area...
May 26, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28547797/vitamin-d-receptor-agonists-regulate-ocular-developmental-angiogenesis-and-modulate-expression-of-dre-mir-21-and-vegf
#16
Stephanie L Merrigan, Breandán N Kennedy
BACKGROUND AND PURPOSE: Pathological growth of ocular vasculature networks can underpin visual impairment in neovascular age-related macular degeneration, proliferative diabetic retinopathy and retinopathy of prematurity. Our aim was to uncover novel pharmacological regulators of ocular angiogenesis by phenotype-based screening in zebrafish. EXPERIMENTAL APPROACH: A bioactive chemical library of 465 drugs was screened to identify small molecule inhibitors of ocular hyaloid vasculature (HV) angiogenesis in zebrafish larvae...
May 26, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28546962/recent-advances-of-curcumin-in-the-prevention-and-treatment-of-renal-fibrosis
#17
REVIEW
Xuejiao Sun, Yi Liu, Cheng Li, Xiting Wang, Ruyuan Zhu, Chenyue Liu, Haixia Liu, Lili Wang, Rufeng Ma, Min Fu, Dongwei Zhang, Yu Li
Curcumin, a polyphenol derived from the turmeric, has received attention as a potential treatment for renal fibrosis primarily because it is a relatively safe and inexpensive compound that contributes to kidney health. Here, we review the literatures on the applications of curcumin in resolving renal fibrosis in animal models and summarize the mechanisms of curcumin and its analogs (C66 and (1E,4E)-1,5-bis(2-bromophenyl) penta-1,4-dien-3-one(B06)) in preventing inflammatory molecules release and reducing the deposition of extracellular matrix at the priming and activation stage of renal fibrosis in animal models by consulting PubMed and Cnki databases over the past 15 years...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28546915/label-free-and-regenerative-electrochemical-microfluidic-biosensors-for-continual-monitoring-of-cell-secretomes
#18
Su Ryon Shin, Tugba Kilic, Yu Shrike Zhang, Huseyin Avci, Ning Hu, Duckjin Kim, Cristina Branco, Julio Aleman, Solange Massa, Antonia Silvestri, Jian Kang, Anna Desalvo, Mohammed Abdullah Hussaini, Su-Kyoung Chae, Alessandro Polini, Nupura Bhise, Mohammad Asif Hussain, HeaYeon Lee, Mehmet R Dokmeci, Ali Khademhosseini
Development of an efficient sensing platform capable of continual monitoring of biomarkers is needed to assess the functionality of the in vitro organoids and to evaluate their biological responses toward pharmaceutical compounds or chemical species over extended periods of time. Here, a novel label-free microfluidic electrochemical (EC) biosensor with a unique built-in on-chip regeneration capability for continual measurement of cell-secreted soluble biomarkers from an organoid culture in a fully automated manner without attenuating the sensor sensitivity is reported...
May 2017: Advanced Science (Weinheim, Baden-Wurttemberg, Germany)
https://www.readbyqxmd.com/read/28546583/hybridizing-feature-selection-and-feature-learning-approaches-in-qsar-modeling-for-drug-discovery
#19
Ignacio Ponzoni, Víctor Sebastián-Pérez, Carlos Requena-Triguero, Carlos Roca, María J Martínez, Fiorella Cravero, Mónica F Díaz, Juan A Páez, Ramón Gómez Arrayás, Javier Adrio, Nuria E Campillo
Quantitative structure-activity relationship modeling using machine learning techniques constitutes a complex computational problem, where the identification of the most informative molecular descriptors for predicting a specific target property plays a critical role. Two main general approaches can be used for this modeling procedure: feature selection and feature learning. In this paper, a performance comparative study of two state-of-art methods related to these two approaches is carried out. In particular, regression and classification models for three different issues are inferred using both methods under different experimental scenarios: two drug-like properties, such as blood-brain-barrier and human intestinal absorption, and enantiomeric excess, as a measurement of purity used for chiral substances...
May 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28546540/a-bioactive-chemical-markers-based-strategy-for-quality-assessment-of-botanical-drugs-xuesaitong-injection-as-a-case-study
#20
Zhenzhong Yang, Qing Shao, Zhiwei Ge, Ni Ai, Xiaoping Zhao, Xiaohui Fan
Current chemical markers based quality assessment methods largely fail to reflect intrinsic chemical complexity and multiple mechanisms of action of botanical drugs (BD). The development of novel quality markers is greatly needed. Here we propose bioactive chemical markers (BCM), defined as a group of chemo-markers that exhibit similar pharmacological activities comparable to the whole BD, which can therefore be used to effectively assess the quality of BD. As a proof-of-concept, a BCM-based strategy was developed and applied to Xuesaitong Injection (XST) for assessing the efficacy and consistency of different batches...
May 25, 2017: Scientific Reports
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