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https://www.readbyqxmd.com/read/28220701/deconstructed-analogs-of-bupropion-reveal-structural-requirements-for-transporter-inhibition-versus-substrate-induced-neurotransmitter-release
#1
Abdelrahman R Shalabi, Donna Walther, Michael H Baumann, Richard A Glennon
Bupropion (1), an α-aminophenone uptake inhibitor at plasma membrane transporters for dopamine (DAT) and norepinephrine (NET), is a widely prescribed antidepressant and smoking cessation aid. Cathinone (2), a structurally simpler α-aminophenone, is a substrate-type releasing agent at the same transporters and a recognized drug of abuse. Our goal was to identify the structural features of α-aminophenones that govern the mechanistic transition from uptake inhibition to substrate-induced release. Deconstructed analogs of 1 were synthesized and compared for their ability to interact with DAT, NET, and the serotonin transporter (SERT) using in vitro assay methods...
February 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28219789/acetazolamide-lowers-intracranial-pressure-and-modulates-the-cerebrospinal-fluid-secretion-pathway-in-healthy-rats
#2
Maria Uldall, Hannah Botfield, Inger Jansen-Olesen, Alexandra Sinclair, Rigmor Jensen
Acetazolamide is one of the most widely used drugs for lowering intracranial pressure (ICP) and is believed to reduce cerebrospinal fluid (CSF) secretion via its action on the choroid plexus (CP). In the CP the main driving force for CSF secretion is primarily active transport of Na(+) ions facilitated by the Na/K ATPase. Transmembrane water channels, known as aquaporins (AQP), are also present in the CP and play an important role in the movement of water. In the present study, we investigated the effect of a single dose acetazolamide on the activity of the Na/K ATPase and ICP...
February 17, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28219748/improved-antitumor-activity-and-reduced-toxicity-of-doxorubicin-encapsulated-in-poly-%C3%AE%C2%B5-caprolactone-nanoparticles-in-lung-and-breast-cancer-treatment-an-in-vitro-and-in-vivo-study
#3
Laura Cabeza, Raul Ortiz, Jose Prados, Ángel V Delgado, Maria J Martín-Villena, Beatriz Clares, Gloria Perazzoli, Jose M Entrena, Consolación Melguizo, Jose L Arias
Poly(ε-caprolactone) (PCL) nanoparticles (NPs) offer many possibilities for drug transport because of their good physicochemical properties and biocompatibility. Doxorubicin-loaded PCL NPs have been synthesized to try to reduce the toxicity of doxorubicin (DOX) for healthy tissues and enhance its antitumor effect in two tumor models, breast and lung cancer, which have a high incidence in the global population. PCL NPs were synthesized using a modified nanoprecipitation solvent evaporation method. The in vitro toxicity of PCL NPs was evaluated in breast and lung cancer cell lines from both humans and mice, as was the inhibition of cell proliferation and cell uptake of DOX-loaded PCL NPs compared to free DOX...
February 17, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28219421/regulation-of-voltage-gated-potassium-channels-attenuates-resistance-of-side-population-cells-to-gefitinib-in-the-human-lung-cancer-cell-line-nci-h460
#4
Seon Young Choi, Hang-Rae Kim, Pan Dong Ryu, So Yeong Lee
BACKGROUND: Side-population (SP) cells that exclude anti-cancer drugs have been found in various tumor cell lines. Moreover, SP cells have a higher proliferative potential and drug resistance than main population cells (Non-SP cells). Also, several ion channels are responsible for the drug resistance and proliferation of SP cells in cancer. METHODS: To confirm the expression and function of voltage-gated potassium (Kv) channels of SP cells, these cells, as well as highly expressed ATP-binding cassette (ABC) transporters and stemness genes, were isolated from a gefitinib-resistant human lung adenocarcinoma cell line (NCI-H460), using Hoechst 33342 efflux...
February 21, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28218790/differential-expression-of-hent1-and-hent2-in-colon-cancer-cell-lines
#5
Y Liu, T Zuo, X Zhu, N Ahuja, T Fu
Human equilibrative nucleoside transporters (hENT) 1 and 2, encoded by SLC29A1 and SLC29A2, permit the bidirectional passage of nucleoside analogues into cells and may correlate with clinical responses to chemotherapy in patients with colorectal cancer (CRC). The purpose of this study was to evaluate the expression profiles of SLC29A1 and SLC29A2 in human cancer cell lines. Using quantitative real-time polymerase chain reaction, we comprehensively profiled the transcription levels of SLC29A1 and SLC29A2 in 16 colon cancer cell lines...
February 16, 2017: Genetics and Molecular Research: GMR
https://www.readbyqxmd.com/read/28218523/transepithelial-transport-of-ywdhnnpqir-and-its-metabolic-fate%C3%AF-with-cytoprotection-against-oxidative-stress%C3%AF-in-human-intestinal-caco-2-cells
#6
Feiran Xu, Lifeng Wang, Xingrong Ju, Jing Zhang, Shi Yin, Jiayi Shi, Rong He, Qiang Yuan
Studies on the antioxidant peptides extracted from foodstuff sources have included not only experiments to elucidate the chemical characteristics of them but have also investigated their bioavailability and intracellular mechanisms. This study was designed to clarify the absorption and antioxidative activity of YWDHNNPQIR (named RAP) which derived from rapeseed protein using Caco-2 cells transwell model. Results showed that 0.8% RAP (C0=0.2mM, t=90min) could maintain the original structure to across the Caco-2 cell monolayers via the intracellular transcytosis pathway, and the Papp (drug apparent absorption rate) was (6...
February 20, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28217823/novel-insight-from-computational-virtual-screening-depict-the-binding-potential-of-selected-phytotherapeutics-against-probable-drug-targets-of-clostridium-difficile
#7
Suman Kamath, Sinosh Skariyachan
This study explores computational screening and molecular docking approaches to screen novel herbal therapeutics against probable drug targets of Clostridium difficile. The essential genes were predicted by comparative genome analysis of C. difficile and best homologous organisms using BLAST search at database of essential genes (DEG). The functions of these genes in various metabolic pathways were predicted and some of these genes were considered as potential targets. Three major proteins were selected as putative targets, namely permease IIC component, ABC transporter and histidine kinase...
February 20, 2017: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/28217741/transcriptome-level-signatures-in-gene-expression-and-gene-expression-variability-during-bacterial-adaptive-evolution
#8
Keesha E Erickson, Peter B Otoupal, Anushree Chatterjee
Antibiotic-resistant bacteria are an increasingly serious public health concern, as strains emerge that demonstrate resistance to almost all available treatments. One factor that contributes to the crisis is the adaptive ability of bacteria, which exhibit remarkable phenotypic and gene expression heterogeneity in order to gain a survival advantage in damaging environments. This high degree of variability in gene expression across biological populations makes it a challenging task to identify key regulators of bacterial adaptation...
January 2017: MSphere
https://www.readbyqxmd.com/read/28217095/endogenous-protein-interactome-of-human-udp-glucuronosyltransferases-exposed-by-untargeted-proteomics
#9
Michèle Rouleau, Yannick Audet-Delage, Sylvie Desjardins, Mélanie Rouleau, Camille Girard-Bock, Chantal Guillemette
The conjugative metabolism mediated by UDP-glucuronosyltransferase enzymes (UGTs) significantly influences the bioavailability and biological responses of endogenous molecule substrates and xenobiotics including drugs. UGTs participate in the regulation of cellular homeostasis by limiting stress induced by toxic molecules, and by controlling hormonal signaling networks. Glucuronidation is highly regulated at genomic, transcriptional, post-transcriptional and post-translational levels. However, the UGT protein interaction network, which is likely to influence glucuronidation, has received little attention...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28216505/-effect-of-hypoxia-on-expression-of-multidrug-resistance-protein-2-and-its-regulation-mechanism
#10
Bingfeng Luo, Wenbin Li, Rong Wang, Hui Lu, Tao Yang, Zhengping Jia
Drug efflux transporters plays a key role in pharmacokinetics parameters changes. In recent years, in addition to P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), MRP2 has become an advanced research hotspot. Several signaling pathways andtranscription factors have been reported to be involved in regulation of MRP2 expression in hypoxic microenvironment of tumor, such as peroxisome proliferators-activated receptors (PPARα), nuclear factor κB (NF-κB), pregnane X receptor (PXR), farnesoid X receptor (FXR), constitutive androstane receptor (CAR) and microRNA...
January 28, 2017: Zhong Nan da Xue Xue Bao. Yi Xue Ban, Journal of Central South University. Medical Sciences
https://www.readbyqxmd.com/read/28216464/exosomes-as-novel-bio-carriers-for-gene-and-drug-delivery
#11
REVIEW
Xin-Chi Jiang, Jian-Qing Gao
Clinical treatments have stalled in certain diseases due to a lack of proper therapeutic delivery systems. Recent studies have identified exosomes for their potential use as cell-free therapies, which may provide a novel mechanism for solving this problem. Exosomes are nanoscale extracellular vesicles that can transport rich cargos of proteins, lipids, DNA, and RNA. It is increasingly recognized that exosomes play a complex role in not only the physiological conditions but also pathological ones. Accumulating evidence suggests that exosomes are of paramount importance in distant cell-cell communication because they can enter the circulation when secreted and pass through additional biological barriers...
February 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28216371/atp-binding-cassette-transporters-in-tumor-endothelial-cells-and-resistance-to-metronomic-chemotherapy
#12
Kyoko Hida, Hiroshi Kikuchi, Nako Maishi, Yasuhiro Hida
Drug resistance is a major problem in anticancer therapy. ATP-binding cassette (ABC) transporters have a role in the multidrug resistance. A new regimen of chemotherapy has been proposed, called "metronomic chemotherapy". Metronomic chemotherapy is the frequent, regular administration of drug doses designed to maintain low, but active, concentrations of chemotherapeutic drugs over prolonged periods of time, without causing serious toxicities. Metronomic chemotherapy regimens were developed to optimize the antitumour efficacy of agents that target the tumour vasculature instead of tumour cells, and to reduce toxicity of antineoplastic drugs" [1]...
February 16, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28216264/potential-functional-and-pathological-side-effects-related-to-off-target-pharmacological-activity
#13
James J Lynch, Terry R Van Vleet, Scott W Mittelstadt, Eric A G Blomme
Most pharmaceutical companies test their discovery-stage proprietary molecules in a battery of in vitro pharmacology assays to try to determine off-target interactions.During all phases of drug discovery and development, various questions arise regarding potential side effects associated with such off-target pharmacological activity.Here we present a scientific literature curation effort undertaken to determine and summarize the most likely functional and pathological outcomes associated with interactions at 70 receptors, enzymes, ion channels and transporters with established links to adverse effects...
February 16, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28216144/patient-ipsc-derived-neurons-for-disease-modeling-of-frontotemporal-dementia-with-mutation-in-chmp2b
#14
Yu Zhang, Benjamin Schmid, Nanett K Nikolaisen, Mikkel A Rasmussen, Blanca I Aldana, Mikkel Agger, Kirstine Calloe, Tina C Stummann, Hjalte M Larsen, Troels T Nielsen, Jinrong Huang, Fengping Xu, Xin Liu, Lars Bolund, Morten Meyer, Lasse K Bak, Helle S Waagepetersen, Yonglun Luo, Jørgen E Nielsen, Bjørn Holst, Christian Clausen, Poul Hyttel, Kristine K Freude
The truncated mutant form of the charged multivesicular body protein 2B (CHMP2B) is causative for frontotemporal dementia linked to chromosome 3 (FTD3). CHMP2B is a constituent of the endosomal sorting complex required for transport (ESCRT) and, when mutated, disrupts endosome-to-lysosome trafficking and substrate degradation. To understand the underlying molecular pathology, FTD3 patient induced pluripotent stem cells (iPSCs) were differentiated into forebrain-type cortical neurons. FTD3 neurons exhibited abnormal endosomes, as previously shown in patients...
February 6, 2017: Stem Cell Reports
https://www.readbyqxmd.com/read/28216016/the-n-terminal-region-of-organic-anion-transporting-polypeptide-1b3-oatp1b3-plays-an-essential-role-in-regulating-its-plasma-membrane-trafficking
#15
Se-Eun Chun, Nilay Thakkar, Yunseok Oh, Ji Eun Park, Songhee Han, Gongmi Ryoo, Hyunggu Hahn, Sang Hyun Maeng, Young-Ran Lim, Byung Woo Han, Wooin Lee
Organic anion transporting polypeptide 1B3 (OATP1B3) is a major influx transporter mediating the hepatic uptake of various endogenous substrates as well as clinically important drugs such as statins and anticancer drugs. However, molecular mechanisms controlling the membrane trafficking of OATP1B3 have been largely unknown. Several reports recently indicated the presence of a distinct, cancer-type OATP1B3 variant lacking the N-terminal 28 amino acids compared to OATP1B3 expressed in non-malignant hepatocytes...
February 16, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28215696/recurrent-venous-thrombosis-under-rivaroxaban-and-carbamazepine-for-symptomatic-epilepsy
#16
Claudia Stöllberger, Josef Finsterer
BACKGROUND: The direct oral anticoagulant (DOAC) rivaroxaban, an oral Factor Xa inhibitor, is increasingly used as an alternative to vitamin-K-antagonists (VKAs). Absorption and elimination of DOACs are dependent on the permeability glycoprotein (P-gp) efflux transporter protein system, and DOACs are substrates of the hepatic cytochrome P 450 3A4 (CYP3A4) enzymes. Therefore, drug-interactions may occur when DOACs are administered with drugs affecting the activity of P-gp or CYP3A4 systems...
February 3, 2017: Neurologia i Neurochirurgia Polska
https://www.readbyqxmd.com/read/28215192/music-genre-as-a-predictor-of-resource-utilization-at-outdoor-music-concerts
#17
Michael S Westrol, Susmith Koneru, Norah McIntyre, Andrew T Caruso, Faizan H Arshad, Mark A Merlin
OBJECTIVES: The aim of this study was to examine the various modern music genres and their effect on the utilization of medical resources with analysis and adjustment for potential confounders. METHODS: A retrospective review of patient logs from an open-air, contemporary amphitheater over a period of 10 years was performed. Variables recorded by the medical personnel for each concert included the attendance, description of the weather, and a patient log in which nature and outcome were recorded...
February 20, 2017: Prehospital and Disaster Medicine
https://www.readbyqxmd.com/read/28215138/amino-acid-ester-prodrugs-of-nucleoside-and-nucleotide-antivirals
#18
Marcela Krečmerová
The review covers basic principles of the prodrug strategy applied to antiviral nucleoside drugs or drug candidates. Specific role of amino acids as promoieties is explained with respect to transport mechanisms, pharmacokinetics and a low toxicity of compounds. Synthetic approaches to the most important representatives (compounds under clinical investigations or available on the market) are described, including valacyclovir, valganciclovir, valomaciclovir stearate, valcyclopropavir, valtorcitabine, valopicitabine and several attempts to amino acid modifications of antiretroviral nucleosides...
February 16, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28214545/potential-of-amphiphilic-graft-copolymer-%C3%AE-tocopherol-succinate-g-carboxymethyl-chitosan-in-modulating-the-permeability-and-anticancer-efficacy-of-tamoxifen
#19
Sunil K Jena, Sanjaya K Samal, Shamandeep Kaur, Mahesh Chand, Abhay T Sangamwar
Recent studies showed an enhanced oral bioavailability of tamoxifen (TMX) by hydrophobically modified α-tocopherol succinate-g-carboxymethyl chitosan (Cmc-TS) micelles. As a continued effort, here we evaluated TMX-loaded polymeric micelles (TMX-PMs) for its enhanced permeability with increased anticancer efficacy and decreased hepatotoxicity. We employed co-solvent evaporation technique to encapsulate TMX into Cmc-TS. Apparent permeability assay of TMX-PMs was performed on Caco-2 cell line. The absorptive transport of TMX increased significantly about 3...
February 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28214542/several-hpept1-transported-drugs-are-substrates-of-the-e-coli-proton-coupled-oligopeptide-transporter-ydgr
#20
Bala K Prabhala, Nanda G Aduri, Mazhar Iqbal, Moazur Rahman, Michael Gajhede, Paul R Hansen, Osman Mirza
Proton-dependent oligopeptide transporters (POTs) are secondary active transporters found in all kingdoms of life. POTs utilize the proton electrochemical gradient for the uptake of nutrient dipeptides and tripeptides. The human POT hPepT1 is known to transport a number of drugs. As part of ongoing studies on substrate specificities of POTs from E. coli, our aim in this study was to investigate whether bacterial POTs could also transport these drugs. For this, we selected the common orally administered drugs sulpiride, bestatin, valacyclovir, ampicillin and oseltamivir, that are all transported by hPepT1...
February 15, 2017: Research in Microbiology
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