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https://www.readbyqxmd.com/read/29227643/structure-activity-relationship-studies-on-a-series-of-3%C3%AE-bis-4-fluorophenyl-methoxy-tropanes-and-3%C3%AE-bis-4-fluorophenyl-methylamino-tropanes-as-novel-atypical-dopamine-transporter-dat-inhibitors-for-the-treatment-of-cocaine-use-disorders
#1
Mu-Fa Zou, Jianjing Cao, Ara M Abramyan, Theresa Kopajtic, Claudio Zanettini, Daryl A Guthrie, Rana Rais, Barbara S Slusher, Lei Shi, Claus J Loland, Amy Hauck Newman
The development of medications to treat cocaine use disorders has thus far defied success, leaving this patient population without pharmacotherapeutic options. As the dopamine transporter (DAT) plays a prominent role in the reinforcing effects of cocaine that can lead to addiction, atypical DAT inhibitors have been developed that prevent cocaine from binding to DAT, but they themselves are not cocaine-like. Herein, a series of novel DAT inhibitors were synthesized, and based on its pharmacological profile, the lead compound 10a was evaluated in phase I metabolic stability studies in mouse liver microsomes and compared to cocaine in locomotor activity and drug discrimination paradigms in mice...
December 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29227471/inhibiting-mitochondrial-phosphate-transport-as-an-unexploited-antifungal-strategy
#2
Catherine A McLellan, Benjamin M Vincent, Norma V Solis, Alex K Lancaster, Lucas B Sullivan, Cathy L Hartland, Willmen Youngsaye, Scott G Filler, Luke Whitesell, Susan Lindquist
The development of effective antifungal therapeutics remains a formidable challenge because of the close evolutionary relationship between humans and fungi. Mitochondrial function may present an exploitable vulnerability because of its differential utilization in fungi and its pivotal roles in fungal morphogenesis, virulence, and drug resistance already demonstrated by others. We now report mechanistic characterization of ML316, a thiohydantoin that kills drug-resistant Candida species at nanomolar concentrations through fungal-selective inhibition of the mitochondrial phosphate carrier Mir1...
December 11, 2017: Nature Chemical Biology
https://www.readbyqxmd.com/read/29227019/metal-organic-framework-derived-materials-for-sodium-energy-storage
#3
REVIEW
Guoqiang Zou, Hongshuai Hou, Peng Ge, Zhaodong Huang, Ganggang Zhao, Dulin Yin, Xiaobo Ji
Recently, sodium-ion batteries (SIBs) are extensively explored and are regarded as one of the most promising alternatives to lithium-ion batteries for electrochemical energy conversion and storage, owing to the abundant raw material resources, low cost, and similar electrochemical behavior of elemental sodium compared to lithium. Metal-organic frameworks (MOFs) have attracted enormous attention due to their high surface areas, tunable structures, and diverse applications in drug delivery, gas storage, and catalysis...
December 11, 2017: Small
https://www.readbyqxmd.com/read/29226149/role-of-p-glycoprotein-inhibitors-in-the-bioavailability-enhancement-of-solid-dispersion-of-darunavir
#4
Saleha Rehman, Bushra Nabi, Mohammad Fazil, Saba Khan, Naimat Kalim Bari, Romi Singh, Shavej Ahmad, Varinder Kumar, Sanjula Baboota, Javed Ali
Objective: The aim of the present study was to improve bioavailability of an important antiretroviral drug, Darunavir (DRV), which has low water solubility and poor intestinal absorption through solid dispersion (SD) approach incorporating polymer with P-glycoprotein inhibitory potential. Methods: A statistical approach where design of experiment (DoE) was used to prepare SD of DRV with incorporation of P-glycoprotein inhibitors. Using DoE, different methods of preparation, like melt, solvent evaporation, and spray drying method, utilizing carriers like Kolliphor TPGS and Soluplus were evaluated...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29226041/dapagliflozin-cardiovascular-safety-and-benefits-in-type-2-diabetes-mellitus
#5
REVIEW
Fatima Saleem
Sodium-glucose co-transporter 2 inhibitors (SGLT2is) such as dapagliflozin, canagliflozin, and empagliflozin, are a promising new therapy in the treatment of type 2 diabetes mellitus (T2DM). SGLT2is can effectively reduce hyperglycemia thus improving glycemic control and they offer some beneficial effects on the cardiovascular (CV) system which can benefit patients with heart failure in addition toT2DM. The United States Food and Drug Administration requires new diabetes mellitus therapies to show a CV safety profile...
October 5, 2017: Curēus
https://www.readbyqxmd.com/read/29225544/novel-targets-for-developing-antiseizure-and-potentially-antiepileptogenic-drugs
#6
Dipan C Patel, Karen S Wilcox, Cameron S Metcalf
Epilepsy is a chronic neurological disorder caused by abnormal changes in the functions of neuronal circuits and manifested by seizures. It affects patients of all age, substantially worsens the quality of life for the patients as well as their families, and imposes a huge economic burden on the healthcare system. Historically, efforts for discovering and developing antiseizure therapies have been focused on modulating the functions of receptors, transporters, and enzymes expressed by neurons. These drug development efforts have paid off, as we have over 25 antiseizure drugs available in the clinic...
September 2017: Epilepsy Currents
https://www.readbyqxmd.com/read/29225200/sumo-proteases-as-potential-targets-for-cancer-therapy
#7
Piotr Bialik, Katarzyna Woźniak
Sumoylation is one of the post-translational modifications of proteins, responsible for the regulation of many cellular processes, such as DNA replication and repair, transcription, signal transduction and nuclear transport. During sumoylation, SUMO proteins are covalently attached to the ε-amino group of lysine in target proteins via an enzymatic cascade that requires the sequential action of E1, E2 and E3 enzymes. An important aspect of sumoylation is its reversibility, which involves SUMO-specific proteases called SENPs...
December 8, 2017: Postȩpy Higieny i Medycyny Doświadczalnej
https://www.readbyqxmd.com/read/29225192/effects-of-the-new-psychoactive-substances-diclofensine-diphenidine-and-methoxphenidine-on-monoaminergic-systems
#8
Dino Luethi, Marius C Hoener, Matthias E Liechti
Diclofensine, diphenidine, and methoxphenidine are new psychoactive substances (NPSs) that recently appeared on the illicit drug market. Pharmacological profiling of such newly emerged drugs is crucial for a better understanding of their psychotropic effects and toxicity. We therefore investigated the potential of these NPSs to inhibit the norepinephrine, dopamine, and serotonin transporters in human embryonic kidney cells stably transfected with the respective transporters. In addition, we determined monoamine transporter and receptor affinities for the substances...
December 7, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29225041/syringaresinol-suppresses-excitatory-synaptic-transmission-and-picrotoxin-induced-epileptic-activity-in-the-hippocampus-through-presynaptic-mechanisms
#9
Young Seon Cho, Woo Seok Song, Sang Ho Yoon, Kyeong-Yeol Park, Myoung-Hwan Kim
Many neuromodulating drugs acting on the nervous system originate from botanical sources. These plant-derived substances modulate the activity of receptors, ion channels, or transporters in neurons. Their properties make the substances useful for medicine and research. Here, we show that the plant lignan (+)-syringaresinol (SYR) suppresses excitatory synaptic transmission via presynaptic modulation. Bath application of SYR rapidly reduced the slopes of the field excitatory postsynaptic potentials (fEPSPs) at the hippocampal Schaffer collateral (SC)-CA1 synapse in a dose-dependent manner...
December 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29224383/abcb1-is-there-a-role-in-the-drug-treatment-of-parkinson-s-disease
#10
Thomas Müller
The ABCB1 (P-gp, MDR1, CD243) transporters system plays an eminent role in brain detoxification. It protects against endogenous and exogenous toxin transport into the brain parenchyma by supporting toxin efflux over the blood brain barrier. Areas covered: This editorial discusses the role and pro's and con's of ABCB1 modulation in the drug treatment of Parkinson's disease patients. Expert commentary: Experimental findings suggest that drug induced impairment of ABCB1 transporters function may improve symptomatic drug effects...
December 11, 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29224352/functional-characterization-of-human-peptide-histidine-transporter-1-in-stably-transfected-mdck-cells
#11
Feifeng Song, Yongjun Hu, Yuqing Wang, David E Smith, Huidi Jiang
The proton-coupled oligopeptide transporter PHT1 (SLC15A4), which facilitates cross-membrane transport of histidine and small peptides from inside the endosomes or lysosomes to cytosol, plays an important role in intracellular peptide homeostasis and innate immune response. However, it remains a challenge to elucidate functional properties of the PHT1 transporter because of its subcellular localization. The purpose of this study was to re-sort hPHT1 protein from the subcellular to outer cell membrane of MDCK cells stably transfected with human PHT1 mutants, and to characterize its functional activity in these cells...
December 11, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29223574/evaluation-of-the-effects-of-antiepileptic-drugs-on-folic-acid-uptake-by-human-placental-choriocarcinoma-cells
#12
Yuko Kurosawa, Ayako Furugen, Ayako Nishimura, Katsuya Narumi, Masaki Kobayashi, Ken Iseki
Folate status during pregnancy is important for fetal development and health. The placenta plays an important role in supplying the fetus with folate. Most women with epilepsy continue their medication during pregnancy. In the present study, we aimed to evaluate the effects of 16 antiepileptic drugs, clinically used for treatment of epilepsy, on folic acid uptake in two in vitro placental models, BeWo and JEG-3 cells. Short-term exposure to antiepileptic drugs had no effects on [3H]-folic acid uptake by BeWo cells...
December 6, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/29223569/isolated-mangiferin-and-naringenin-exert-antidiabetic-effect-via-ppar%C3%AE-glut4-dual-agonistic-action-with-strong-metabolic-regulation
#13
Ashok K Singh, Vinit Raj, Amit K Keshari, Amit Rai, Pranesh Kumar, Atul Rawat, Biswanath Maity, Dinesh Kumar, Anand Prakash, Arnab De, Amalesh Samanta, Bolay Bhattacharya, Sudipta Saha
In this study, we isolated two compounds from the leaves of Salacia oblonga (SA1, mangiferin and SA2, naringenin), and their structures were confirmed by infrared spectroscopy, nuclear magnetic resonance (NMR) spectroscopy, and mass spectrometry. SA1 and SA2 were orally administered to streptozotocin-induced diabetic rats at 50 and 100 mg/kg daily for 15 days. Blood glucose level, serum lipid profile, oxidative stress parameters, histopathology, docking, molecular parameters, and NMR-based metabolic perturbation studies were performed to investigate the pharmacological activities of SA1 and SA2...
December 6, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29223352/atp-binding-cassette-transporter-2-abca2-as-a-therapeutic-target
#14
REVIEW
Warren Davis, Kenneth D Tew
The ATP binding cassette transporter ABCA2 is primarily an endolysosomal membrane protein that demonstrates pleiotropic functionalities, coalescing around the maintenance of homeostasis of sterols, sphingolipids and cholesterol. It is most highly expressed in brain tissue and ABCA2 knockout mice express neurological defects consistent with aberrant myelination. Increased expression of the transporter has been linked with resistance to cancer drugs, particularly those possessing a steroid backbone and gene expression (in concert with other genes involved in cholesterol metabolism) was found to be regulated by sterols...
December 6, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29223141/molecular-and-functional-characterization-of-choline-transporter-like-proteins-in-esophageal-cancer-cells-and-potential-therapeutic-targets
#15
Fumiaki Nagashima, Ryohta Nishiyama, Beniko Iwao, Yuiko Kawai, Chikanao Ishii, Tsuyoshi Yamanaka, Hiroyuki Uchino, Masato Inazu
In this study, we examined the molecular and functional characterization of choline uptake in the human esophageal cancer cells. In addition, we examined the influence of various drugs on the transport of [3H]choline, and explored the possible correlation between the inhibition of choline uptake and apoptotic cell death. We found that both choline transporter-like protein 1 (CTL1) and CTL2 mRNAs and proteins were highly expressed in esophageal cancer cell lines (KYSE series). CTL1 and CTL2 were located in the plasma membrane and mitochondria, respectively...
December 8, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/29222980/bonding-of-doxorubicin-to-nanosilica-and-human-serum-albumin-in-various-media
#16
V M Gun'ko, T V Krupska, L S Andriyko, N Yu Klymenko, I V Siora, O A Novikova, A I Marynin, A I Ukrainets, B Charmas, S B Shekhunova, V V Turov
Interaction of doxorubicin hydrochloride (DOX) (anti-cancer drug) with hydro-compacted nanosilica A-300 (cA-300) alone or cA-300/human serum albumin (HSA) at a small content of water (h = 0.4 g per gram of dry silica) in different dispersion media (air, chloroform, and chloroform/trifluoroacetic acid) was analyzed using low-temperature 1H NMR spectroscopy, NMR cryoporometry and quantum chemistry to elucidate specific changes in the interfacial layers. Initial (bulk density ρb ≈ 0.046 g/cm3) and hydro-compacted (ρb ≈ 0...
December 5, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/29222397/indoxyl-sulfate-upregulates-liver-p-glycoprotein-expression-and-activity-through-aryl-hydrocarbon-receptor-signaling
#17
Tacy Santana Machado, Stéphane Poitevin, Pascale Paul, Nathalie McKay, Noémie Jourde-Chiche, Tristan Legris, Annick Mouly-Bandini, Françoise Dignat-George, Philippe Brunet, Rosalinde Masereeuw, Stéphane Burtey, Claire Cerini
In patients with CKD, not only renal but also, nonrenal clearance of drugs is altered. Uremic toxins could modify the expression and/or activity of drug transporters in the liver. We tested whether the uremic toxin indoxyl sulfate (IS), an endogenous ligand of the transcription factor aryl hydrocarbon receptor, could change the expression of the following liver transporters involved in drug clearance: SLC10A1, SLC22A1, SLC22A7, SLC47A1, SLCO1B1, SLCO1B3, SLCO2B1, ABCB1, ABCB11, ABCC2, ABCC3, ABCC4, ABCC6, and ABCG2 We showed that IS increases the expression and activity of the efflux transporter P-glycoprotein (P-gp) encoded by ABCB1 in human hepatoma cells (HepG2) without modifying the expression of the other transporters...
December 8, 2017: Journal of the American Society of Nephrology: JASN
https://www.readbyqxmd.com/read/29221992/active-mediated-transport-of-chloramphenicol-and-thiamphenicol-in-a-calu-3-lung-epithelial-cell-model
#18
S N Nurbaeti, J C Olivier, C Adier, S Marchand, W Couet, J Brillault
Pulmonary administration enables high local concentrations along with limited systemic side-effects, but not all ATB could be good candidates. In this perspective, diffusion of the ATB chloramphenicol (CHL) and thiamphenicol (THA) through the lung has been evaluated to re-assess their potential for pulmonary administration. The apparent permeability (Papp) was evaluated with the Calu-3 cell model. Influence of drug transporters was assessed with the PSC-833, MK-571, and KO-143 inhibitors. The influence of CHL and THA on the cell uptake of rhodamin123 and fluorescein was also evaluated...
December 5, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29221858/photochemical-internalization-enhanced-macrophage-delivered-chemotherapy
#19
Diane Shin, Catherine Christie, David Ju, Rohit Kumar Nair, Stephanie Molina, Kristian Berg, Tatiana B Krasieva, Steen J Madsen, Henry Hirschberg
BACKGROUND: Macrophage (Ma) vectorization of chemotherapeutic drugs has the advantage for cancer therapy in that it can actively target and maintain an elevated concentration of drugs at the tumor site, preventing their spread into healthy tissue. A potential drawback is the inability to deliver a sufficient number of drug-loaded Ma into the tumor, thus limiting the amount of active drug delivered. This study examined the ability of photochemical internalization (PCI) to enhance the efficacy of released drug by Ma transport...
December 5, 2017: Photodiagnosis and Photodynamic Therapy
https://www.readbyqxmd.com/read/29221813/neonatal-programming-with-testosterone-propionate-reduces-dopamine-transporter-expression-in-nucleus-accumbens-and-methylphenidate-induced-locomotor-activity-in-adult-female-rats
#20
Tatiana Dib, Jonathan Martínez-Pinto, Miguel Reyes-Parada, Gonzalo E Torres, Ramón Sotomayor-Zárate
Research in programming is focused on the study of stimuli that alters sensitive periods in development, such as prenatal and neonatal stages, that can produce long-term deleterious effects. These effects can occur in various organs or tissues such as the brain, affecting brain circuits and related behaviors. Our laboratory has demonstrated that neonatal programming with sex hormones affects the mesocorticolimbic circuitry, increasing the synthesis and release of dopamine (DA) in striatum and nucleus accumbens (NAcc)...
December 5, 2017: Behavioural Brain Research
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