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https://www.readbyqxmd.com/read/29667177/adverse-placental-effects-of-valproic-acid-studies-in-perfused-human-placentas
#1
Miriam Rubinchik-Stern, Miriam Shmuel, Jacob Bar, Michal Kovo, Sara Eyal
OBJECTIVE: In utero exposure to valproic acid (VPA) has been associated with worse pregnancy outcomes compared to all other antiepileptic drugs. We have previously shown that VPA alters the expression of placental transporters for hormones and nutrients in vitro and in pregnant mice. Here, our aim was to characterize the effects of short exposure to VPA on the expression of carriers for compounds essential for fetal development in human placentas ex vivo, under controlled conditions...
April 17, 2018: Epilepsia
https://www.readbyqxmd.com/read/29665654/hypericin-affects-cancer-side-populations-via-competitive-inhibition-of-bcrp
#2
Jana Vargová, Jaromír Mikeš, Rastislav Jendželovský, Lucia Mikešová, Barbora Kuchárová, Ľubomír Čulka, Radek Fedr, Ján Remšík, Karel Souček, Alois Kozubík, Peter Fedoročko
OBJECTIVE: Cancer stem-like cells (CSLCs) are considered a root of tumorigenicity and resistance. However, their identification remains challenging. The use of the side population (SP) assay as a credible marker of CSLCs remains controversial. The SP assay relies on the elevated activity of ABC transporters that, in turn, can be modulated by hypericin (HYP), a photosensitizer and bioactive compound of St. John's Wort (Hypericum perforatum), a popular over-the-counter antidepressant. Here we aimed to comprehensively characterize the SP phenotype of cancer cells and to determine the impact of HYP on these cells...
March 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29665383/impact-of-aging-alzheimer-s-disease-and-parkinson-s-disease-on-the-blood-brain-barrier-transport-of-therapeutics
#3
Yijun Pan, Joseph A Nicolazzo
Older people are at greater risk of medicine-induced toxicities resulting from either increased drug sensitivity or age-related pharmacokinetic changes. The scenario is further complicated with the two most prevalent age-related neurodegenerative diseases, Alzheimer's disease (AD) and Parkinson's disease (PD). With aging, AD and PD, there is growing evidence of altered structure and function of the blood-brain barrier (BBB), including modifications to tight junctions and efflux transporters, such as P-glycoprotein...
April 14, 2018: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/29665382/post-production-handling-and-administration-of-protein-pharmaceuticals-and-potential-instability-issues
#4
M Reza Nejadnik, Theodore W Randolph, David B Volkin, Christian Schöneich, John F Carpenter, Daan J A Crommelin, Wim Jiskoot
The safety and efficacy of protein pharmaceuticals depend not only on biological activity, but also on purity levels. Impurities may be process related due to limitations in manufacturing, or product related caused by protein degradation occurring throughout the life history of a product. Although the pharmaceutical biotechnology industry has made great progress in improving bulk and drug product manufacturing as well as company-controlled storage and transportation conditions to minimize the level of degradation, there is less control over the many factors that may subsequently affect product quality after the protein pharmaceuticals are released and shipped by the manufacturer...
April 14, 2018: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29665130/optimization-of-a-drug-transporter-probe-cocktail-potential-screening-tool-for-transporter-mediated-drug-drug-interactions
#5
Peter Stopfer, Thomas Giessmann, Kathrin Hohl, Sabine Hutzel, Sven Schmidt, Dietmar Gansser, Naoki Ishiguro, Mitchell E Taub, Ashish Sharma, Thomas Ebner, Fabian Müller
AIMS: Previous pharmacokinetic characterization of a transporter probe cocktail containing digoxin (P-gp), furosemide (OAT1, OAT3), metformin (OCT2, MATE1, MATE2-K) and rosuvastatin (OATP1B1, OATP1B3, BCRP) in healthy subjects showed increases in rosuvastatin systemic exposure compared to rosuvastatin alone. In this trial, the doses of metformin and furosemide as putative perpetrators were reduced to eliminate their drug-drug interaction (DDI) with rosuvastatin. METHODS: In a randomized, open label, single center, five-treatment, five-period crossover trial, 30 healthy male subjects received as reference treatments separately 0...
April 17, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29664675/knockout-of-glucose-transporter-glut6-has-minimal-effects-on-whole-body-metabolic-physiology-in-mice
#6
Frances L Byrne, Ellen M Olzomer, Robert Brink, Kyle L Hoehn
Glucose transporter 6 (GLUT6) is a member of the facilitative glucose transporter family. GLUT6 is up-regulated in several cancers, but is not widely expressed in normal tissues. Previous studies have shown that GLUT6 knockdown kills endometrial cancer cells that express elevated levels of the protein. However, whether GLUT6 represents a viable anti-cancer drug target is unclear because the role of GLUT6 in normal metabolic physiology is unknown. Herein we generated GLUT6 knockout mice to determine how loss of GLUT6 affected whole body glucose homeostasis and metabolic physiology...
April 17, 2018: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29664658/downregulation-of-glut3-promotes-apoptosis-and-chemosensitivity-of-acute-myeloid-leukemia-cells-via-egfr-signaling
#7
Yan Zhuang, Jing Zhao, Xi Xu, Laixi Bi
BACKGROUND: Glucose transporter 3 (GLUT3) plays an important role in tumor progression and drug resistance in numerous malignancies, including acute myeloid leukemia (AML). However, the effect of GLUT3 silencing on treatment of AML remains poorly understood. The purpose of this study was to investigate role of GLUT3 in proliferation and chemosensitivity of AML and its underlying mechanisms. METHODS: The siRNA transfection was conducted using LipofectamineTM 2000...
February 1, 2018: Archives of Iranian Medicine
https://www.readbyqxmd.com/read/29664641/simulations-study-of-single-component-and-mixed-n-alkyl-peg-micelles
#8
Maisa Vuorte, Jukka Määttä, Maria Sammalkorpi
Here, we study one component and mixed n-alkyl-poly(ethylene oxide) (Cm En ) micelles with varying poly(ethylene oxide) (PEG) chain lengths n using coarse-grained molecular simulations. These non-ionic alkyl-PEG surfactants and their aggregates are widely used in bio and chemical technology. As expected, the simulations show that increasing the PEG chain length decreases the alkyl-PEG micelle core diameter and aggregation number but also enhances PEG chain penetration to the core region and spreads the micelle corona...
April 17, 2018: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/29664632/ph-and-amylase-responsive-carboxymethyl-starch-poly-2-isobutyl-acrylic-acid-hybrid-microgels-as-effective-enteric-carriers-for-oral-insulin-delivery
#9
Liang Liu, Ying Zhang, Shuangjiang Yu, Zhen Zhang, Chaoliang He, Xuesi Chen
Oral delivery of insulin has the potential to revolutionize diabetes care since it is regarded as a non-invasive therapeutic approach without the side effects caused by frequent subcutaneous injection. However, the insulin delivery efficiency through oral route was still limited, likely due to the chemical, enzymatic and absorption barriers. In this study, a novel type of pH- and amylase-responsive microgels as an insulin drug carrier for oral administration was developed to improve the drug delivery efficiency...
April 17, 2018: Biomacromolecules
https://www.readbyqxmd.com/read/29664004/-advances-in-the-application-of-exosomes-in-sepsis
#10
Dan Wang, Mengna Zhang, Honghong Pei
Exosomes are of great importance in cell communication and information transmission, which have become a hotspot in recent years. Most studies have focused on the transport of microRNA (miRNA) and proteins, that mediated by exosomes, as well as exosomes as a drug delivery carrier of the feasibility. Therefore, exosomes can be an important method of treatment for systemic inflammatory diseases. This article reviews the relevant literature, mainly on the related characteristics of exosomes, its association with clinical disease, and its application in sepsis...
April 2018: Zhonghua Wei Zhong Bing Ji Jiu Yi Xue
https://www.readbyqxmd.com/read/29663893/sglt-2-inhibition-novel-therapeutics-for-reno-and-cardioprotection-in-diabetes-mellitus
#11
Angus Gill, Stephen P Gray, Karin A Jandeleit-Dahm, Anna M D Watson
BACKGROUND: The sodium glucose co-transporter 2 (SGLT2) is primarily located within S1 of the renal proximal tubule being responsible for approximately 90% of glucose re-uptake in the kidney. Inhibition of SGLT2 is an exciting new pharmacological approach for the reduction of blood glucose in type 2 diabetic patients via inhibition of tubular glucose reabsorption. In addition to lowering glucose, this group of drugs has shown significant cardiovascular and renal protective effects. CONCLUSION: This review aims to outline the current state of preclinical research and clinical trials for different SGLT2 inhibitors and outline some of the proposed mechanisms of action, including possible effects on sympathetic nerve activity, which may contribute to the unexpected beneficial cardiovascular and reno-protective effects of this class of compounds...
April 17, 2018: Current Diabetes Reviews
https://www.readbyqxmd.com/read/29663807/reversing-multidrug-resistance-by-multiplexed-gene-silencing-for-enhanced-breast-cancer-chemotherapy
#12
Yanli Li, Xiaonan Gao, Zhengze Yu, Bo Liu, Wei Pan, Na Li, Bo Tang
Multidrug resistance (MDR), as one of the main problems in clinical breast cancer chemotherapy, is closely related with the overexpression of drug efflux transporter P-glycoprotein (P-gp). In this study, a novel drug-loaded nanosystem was developed for inhibiting the P-gp expression and reversing multidrug resistance by multiplexed gene silencing, which composes of graphene oxide (GO) modified with two molecular beacons (MBs) and Doxorubicin (Dox). When the nanosystem was uptaken by the MDR breast cancer cells, Dox was released in the acidic endosomes and MBs were hybridized with target sequences...
April 17, 2018: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29663724/recognizing-drug-facilitated-crimes-detection-and-quantification-of-benzodiazepines-in-beverages-using-fast-liquid-liquid-extraction-with-low-temperature-partitioning-and-paper-spray-mass-spectrometry
#13
Camila de Paula, Marina Jurisch, Evandro Piccin, Rodinei Augusti
A novel methodology using liquid-liquid extraction with low temperature partitioning (LLE-LTP) and paper spray mass spectrometry (PS-MS) was developed to identify and quantify benzodiazepines in beverages. Four types of alcoholic beverages usually consumed in parties and bars were spiked with five distinct benzodiazepines (diazepam, alprazolam, bromazepam, clonazepam and cloxazolam) simulating a drug facilitated crime occurrence. The direct PS-MS analysis of the spiked beverages revealed a remarkable matrix effect with an unclear detection of protonated benzodiazepines...
April 16, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29663413/predicting-pharmacokinetics-pharmacodynamics-in-the-individual-patient-separating-reality-from-hype
#14
REVIEW
Leslie Z Benet
Individualization of patient drug dosing to maximize efficacy and minimize toxicity is the goal of clinical pharmacology. Here we review the history of drug dosing individualization from early predictions for renally eliminated drugs based on kidney function through the introduction of clearance concepts for metabolic processes, the differentiation of volume of distribution between pharmacokinetics and chemistry, the role of transporters, the unique pharmacokinetic aspects of oral dosing, and the relevance of protein binding to the emergence of pharmacogenomics...
April 17, 2018: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29663292/the-potential-role-of-sglt2-inhibitors-in-the-treatment-of-type-1-diabetes-mellitus
#15
Hadi Fattah, Volker Vallon
Type 1 diabetes mellitus is a difficult disease to treat due to the relative paucity of therapeutic options other than injectable insulin. The latter, however, can induce hypoglycemia, which has been linked to enhanced cardiovascular risk. Sodium glucose cotransporter 2 (SGLT2) inhibitors are a new class of oral anti-hyperglycemic medications that do not increase the hypoglycemia risk and are US Food and Drug Administration (FDA) approved in type 2 diabetes mellitus. SGLT2 inhibitors may also be of benefit in type 1 diabetic patients, in addition to insulin, although they have not yet been approved for this indication...
April 16, 2018: Drugs
https://www.readbyqxmd.com/read/29663259/clinical-investigation-of-coproporphyrins-as-sensitive-biomarkers-to-predict-mild-to-strong-oatp1b-mediated-drug-drug-interactions
#16
Annett Kunze, Emmanuel Njumbe Ediage, Lieve Dillen, Mario Monshouwer, Jan Snoeys
INTRODUCTION: Coproporphyrin (CP) I and III have recently been proposed as endogenous clinical biomarkers to predict organic anion-transporting polypeptide 1B (OATP1B)-mediated drug-drug interactions (DDIs). In the present study, we first investigated the in vitro selectivity of CPI and CPIII towards drug uptake and efflux transporters. We then assessed the in vivo biomarker sensitivity towards OATP1B inhibition. METHODS: To assess transporter selectivity, incubations with CPI and CPIII were performed in vitro, using single transporter-expressing and control systems...
April 16, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29662344/manipulating-nanoparticle-transport-within-blood-flow-through-external-forces-an-exemplar-of-mechanics-in-nanomedicine
#17
REVIEW
Huilin Ye, Zhiqiang Shen, Le Yu, Mei Wei, Ying Li
A large number of nanoparticles (NPs) have been raised for diverse biomedical applications and some of them have shown great potential in treatment and imaging of diseases. Design of NPs is essential for delivery efficacy due to a number of biophysical barriers, which prevents the circulation of NPs in vascular flow and their accumulation at tumour sites. The physiochemical properties of NPs, so-called '4S' parameters, such as size, shape, stiffness and surface functionalization, play crucial roles in their life journey to be delivered to tumour sites...
March 2018: Proceedings. Mathematical, Physical, and Engineering Sciences
https://www.readbyqxmd.com/read/29661915/residues-contributing-to-drug-transport-by-abcg2-are-localised-to-multiple-drug-binding-pockets
#18
Megan H Cox, Parth Kapoor, Deborah A Briggs, Ian D Kerr
Multidrug binding and transport by the ATP binding cassette transporter ABCG2 is a factor in the clinical resistance to chemotherapy in leukaemia, and a contributory factor to the pharmacokinetic profiles of many other prescribed drugs. Despite its importance, the structural basis of multidrug transport, i.e. the ability to transport multiple distinct chemicals, has remained elusive. Previous research has shown that at least two residues positioned towards the cytoplasmic end of transmembrane helix 3 (TM3) of the transporter play a role in drug transport...
April 16, 2018: Biochemical Journal
https://www.readbyqxmd.com/read/29661875/hc2091-kills-mycobacterium-tuberculosis-by-targeting-the-mmpl3-mycolic-acid-transporter
#19
Huiqing Zheng, John T Williams, Garry B Coulson, Elizabeth R Haiderer, Robert B Abramovitch
Tuberculosis, caused by the intracellular pathogen Mycobacterium tuberculosis (Mtb), is a deadly disease that requires a long course of treatment. The emergence of drug resistant strains has driven efforts to discover new small molecules that can kill the bacterium. Here we report characterizations of the compound HC2091 that kills Mtb in a time- and dose-dependent manner in vitro , as well as inhibiting Mtb growth in macrophages. Whole genome sequencing of spontaneous resistant mutants to HC2091 identified single nucleotide variants in the mmpL3 mycolic acid transporter gene...
April 16, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29661614/a-fluorescence-based-imaging-approach-to-pharmacokinetic-analysis-of-intracochlear-drug-delivery
#20
Andrew M Ayoob, Marcello Peppi, Vishal Tandon, Robert Langer, Jeffrey T Borenstein
Advances in microelectromechanical systems (MEMS) technologies are enhancing the development of intracochlear delivery devices for the treatment of hearing loss with emerging pharmacological therapies. Direct intracochlear delivery addresses the limitations of systemic and intratympanic delivery. However, optimization of delivery parameters for these devices requires pharmacokinetic assessment of the spatiotemporal drug distribution inside the cochlea. Robust methods of measuring drug concentration in the perilymph have been developed, but lack spatial resolution along the tonotopic axis or require complex physiological measurements...
April 5, 2018: Hearing Research
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