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Uptake transporters

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https://www.readbyqxmd.com/read/28812834/cost-effectiveness-of-rural-incentive-packages-for-graduating-medical-students-in-lao-pdr
#1
Eric Keuffell, Wanda Jaskiewicz, Khampasong Theppanya, Kate Tulenko
BACKGROUND: The dearth of health workers in rural settings in Lao People's Democratic Republic (PDR) and other developing countries limits healthcare access and outcomes. In evaluating non-wage financial incentive packages as a potential policy option to attract health workers to rural settings, understanding the expected costs and effects of the various programs ex ante can assist policy-makers in selecting the optimal incentive package. METHODS: We use discrete choice experiments (DCEs), costing analyses and recent empirical results linking health worker density and health outcomes to estimate the future location decisions of physicians and determine the cost-effectiveness of 15 voluntary incentives packages for new physicians in Lao PDR...
October 29, 2016: International Journal of Health Policy and Management
https://www.readbyqxmd.com/read/28812276/arundic-acid-increases-expression-and-function-of-astrocytic-glutamate-transporter-eaat1-via-the-erk-akt-and-nf-%C3%AE%C2%BAb-pathways
#2
Pratap Karki, Peter Hong, James Johnson, Edward Pajarillo, Deok-Soo Son, Michael Aschner, Eunsook Y Lee
Glutamate is the major excitatory neurotransmitter in the brain, but excessive synaptic glutamate must be removed to prevent excitotoxic injury and death. Two astrocytic glutamate transporters, excitatory amino acid transporter (EAAT) 1 and 2, play a major role in eliminating excess glutamate from the synapse. Dysregulation of EAAT1 contributes to the pathogenesis of multiple neurological disorders, such as Alzheimer's disease (AD), ataxia, traumatic brain injuries, and glaucoma. In the present study, we investigated the effect of arundic acid on EAAT1 to determine its efficacy in enhancing the expression and function of EAAT1, and its possible mechanisms of action...
August 15, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28812027/l-theanine-administration-modulates-the-absorption-of-dietary-nutrients-and-expression-of-transporters-and-receptors-in-the-intestinal-mucosa-of-rats
#3
Qiongxian Yan, Haiou Tong, Shaoxun Tang, Zhiliang Tan, Xuefeng Han, Chuanshe Zhou
L-theanine has various advantageous functions for human health; whether or not it could mediate the nutrients absorption is unknown yet. The effects of L-theanine on intestinal nutrients absorption were investigated using rats ingesting L-theanine solution (0, 50, 200, and 400 mg/kg body weight) per day for two weeks. The decline of insulin secretion and glucose concentration in the serum was observed by L-theanine. Urea and high-density lipoprotein were also reduced by 50 mg/kg L-theanine. Jejunal and ileac basic amino acids transporters SLC7a1 and SLC7a9, neutral SLC1a5 and SLC16a10, and acidic SLC1a1 expression were upregulated...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28811499/the-role-of-dermcidin-isoform-2-in-the-occurrence-and-severity-of-diabetes
#4
Suman Bhattacharya, Md Mobidullah Khan, Chandradipa Ghosh, Sarbashri Bank, Smarajit Maiti
Diabetes is now epidemic worldwide. Several hundred-million peoples are presently suffering from this disease with other secondary-disorders. Stress, hypertension, sedentary life-style, carbohydrate/lipid metabolic-disorders due to genetic or environmental factors attributes to type-1 and/or type-2 diabetes. Present investigation demonstrates that stress-induced protein dermcidin isoform-2 (DCN-2) which appears in the serum of diabetic-patients play a key-role in this disease pathogenesis/severity. DCN-2 suppresses insulin production-release from liver/pancreas...
August 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28811203/bpn-a-marine-derived-ptp1b-inhibitor-activates-insulin-signaling-and-improves-insulin-resistance-in-c2c12-myotubes
#5
Qi Xu, Jiao Luo, Ning Wu, Renshuai Zhang, Dayong Shi
Insulin resistance is a key feature of type 2 diabetes mellitus (T2DM) and is characterized by defects in insulin signaling. Protein tyrosine phosphatase 1B (PTP1B) is a major negative regulator of insulin signaling cascade and has attracted intensive investigation in recent T2DM therapy study. BPN, a marine-derived bromophenol compound, was isolated from the red alga Rhodomela confervoides. This study investigated the effects of BPN on the insulin signaling pathway in insulin-resistant C2C12 myotubes by inhibiting PTP1B...
August 12, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28811192/relative-reinforcing-effects-of-second-generation-synthetic-cathinones-acquisition-of-self-administration-and-fixed-ratio-dose-response-curves-in-rats
#6
REVIEW
Brenda M Gannon, Kayla I Galindo, Melson P Mesmin, Agnieszka Sulima, Kenner C Rice, Gregory T Collins
"Bath salts" preparations contain synthetic cathinones which interact with monoamine transporters and function as either monoamine uptake inhibitors or releasers. 3,4-Methylenedioxypyrovalerone (MDPV), 3,4-methylenedioxymethcathinone (methylone), and 4-methylmethcathinone (mephedrone) were three of the most common cathinones (i.e., "first-generation" cathinones); however, after the US Drug Enforcement Administration placed them under Schedule I regulations, they were replaced with structurally related cathinones that were not subject to regulations (i...
August 12, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28811134/a-new-chemotype-inhibitor-for-the-human-organic-cation-transporter-3-hoct3
#7
Xiaolei Pan, Kavita A Iyer, Hebing Liu, Douglas H Sweet, Małgorzata Dukat
Human organic cation transporters (OCTs) represent an understudied neurotransmitter uptake mechanism for which no selective agents have yet been identified. Several neurotransmitters (e.g. serotonin, norepinephrine) are low-affinity substrates for these transporters, but possess higher affinity for other transporters (e.g. the serotonin or norepinephrine transporters; SERT and NET, respectively). We have identified a new class of OCT inhibitors with a phenylguanidine structural scaffold. Here, we examine the actions of a series of such compounds and report preliminary structure-activity relationships (SARs) - the first dedicated SAR study of OCT3 action...
August 5, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28810701/yeast-genes-involved-in-regulating-cysteine-uptake-affect-production-of-hydrogen-sulfide-from-cysteine-during-fermentation
#8
Chien-Wei Huang, Michelle E Walker, Bruno Fedrizzi, Richard C Gardner, Vladimir Jiranek
An early burst of hydrogen sulfide (H2S) produced by Saccharomyces cerevisiae during fermentation could increase varietal thiols and therefore enhance desirable tropical aromas in varieties such as Sauvignon Blanc. Here we attempted to identify genes affecting H2S formation from cysteine by screening yeast deletion libraries via a colony colour assay on media resembling grape juice. Both Δlst4 and Δlst7 formed lighter coloured colonies and produced significantly less H2S than the wild type on high concentrations of cysteine, likely because they are unable to take up cysteine efficiently...
August 1, 2017: FEMS Yeast Research
https://www.readbyqxmd.com/read/28809844/the-4-vessel-sampling-approach-to-integrative-studies-of-human-placental-physiology-in-vivo
#9
Ane M Holme, Maia B Holm, Marie C P Roland, Hildegunn Horne, Trond M Michelsen, Guttorm Haugen, Tore Henriksen
The human placenta is highly inaccessible for research while still in utero. The current understanding of human placental physiology in vivo is therefore largely based on animal studies, despite the high diversity among species in placental anatomy, hemodynamics and duration of the pregnancy. The vast majority of human placenta studies are ex vivo perfusion studies or in vitro trophoblast studies. Although in vitro studies and animal models are essential, extrapolation of the results from such studies to the human placenta in vivo is uncertain...
August 2, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28809437/the-conditional-stimulation-of-rat-organic-cation-transporter-2-but-not-its-human-ortholog-by-mesoridazine-the-possibility-of-the-involvement-of-the-high-affinity-binding-site-of-the-transporter-in-the-stimulation
#10
Sungwoo Hyung, Wonji Pyeon, Ji Eun Park, Yoo-Kyung Song, Suk-Jae Chung
OBJECTIVES: To study the functional consequences of the human and rat forms of OCT2 in the presence of phenothiazines. METHODS: MDCK cells expressing human or rat OCT2 were established, and MPP+ transport was determined by uptake assays. Concentration dependency was studied for the stimulatory/inhibitory effects of phenothiazines on MPP+ transport. KEY FINDINGS: Among the 11 phenothiazines examined, the majority were found to have comparable effects on transporter function between the orthologous forms, while three phenothiazines, particularly mesoridazine, had complex impacts on transporter function...
August 15, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28808314/cellular-toxicity-pathways-of-inorganic-and-methyl-mercury-in-the-green-microalga-chlamydomonas-reinhardtii
#11
Rebecca Beauvais-Flück, Vera I Slaveykova, Claudia Cosio
Contamination by mercury (Hg) is a worldwide concern because of Hg toxicity and biomagnification in aquatic food webs. Nevertheless, bioavailability and cellular toxicity pathways of inorganic (IHg) and methyl-Hg (MeHg) remain poorly understood. We analyzed the uptake, transcriptomic, and physiological responses in the microalga Chlamydomonas reinhardtii exposed to IHg or MeHg. Bioavailability of MeHg was up to 27× higher than for IHg. Genes involved in cell processes, energy metabolism and transport were dysregulated by both Hg species...
August 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28808258/hexahydroquinolines-are-antimalarial-candidates-with-potent-blood-stage-and-transmission-blocking-activity
#12
Manu Vanaerschot, Leonardo Lucantoni, Tao Li, Jill M Combrinck, Andrea Ruecker, T R Santha Kumar, Kelly Rubiano, Pedro E Ferreira, Giulia Siciliano, Sonia Gulati, Philipp P Henrich, Caroline L Ng, James M Murithi, Victoria C Corey, Sandra Duffy, Ori J Lieberman, M Isabel Veiga, Robert E Sinden, Pietro Alano, Michael J Delves, Kim Lee Sim, Elizabeth A Winzeler, Timothy J Egan, Stephen L Hoffman, Vicky M Avery, David A Fidock
Antimalarial compounds with dual therapeutic and transmission-blocking activity are desired as high-value partners for combination therapies. Here, we report the identification and characterization of hexahydroquinolines (HHQs) that show low nanomolar potency against both pathogenic and transmissible intra-erythrocytic forms of the malaria parasite Plasmodium falciparum. This activity translates into potent transmission-blocking potential, as shown by in vitro male gamete formation assays and reduced oocyst infection and prevalence in Anopheles mosquitoes...
August 14, 2017: Nature Microbiology
https://www.readbyqxmd.com/read/28808127/the-components-of-the-unique-zur-regulon-of-cupriavidus-metallidurans-mediate-cytoplasmic-zinc-handling
#13
Lucy Bütof, Christopher Schmidt-Vogler, Martin Herzberg, Cornelia Große, Dietrich H Nies
Zinc is an essential trace element and at the same time it is toxic at high concentrations. In the beta-proteobacterium Cupriavidus metallidurans the highly efficient removal of surplus zinc from the periplasm is responsible for its outstanding metal resistance. Rather than having a typical Zur-dependent, high-affinity ATP-binding cassette transporter of the ABC protein superfamily for zinc uptake at low concentrations, C. metallidurans instead has the secondary zinc importer ZupT of the ZRT/IRT (ZIP) family...
August 14, 2017: Journal of Bacteriology
https://www.readbyqxmd.com/read/28808062/ablating-tbc1d1-impairs-contraction-induced-sarcolemmal-glucose-transporter-type-4-redistribution-but-not-insulin-mediated-responses-in-rats
#14
Jamie Whitfield, Sabina Paglialunga, Brennan K Smith, Paula M Miotto, Genevieve Simnett, Holly L Robson, Swati S Jain, Eric A F Herbst, Eric M Desjardins, David J Dyck, Lawrence L Spriet, Gregory R Steinberg, Graham P Holloway
TBC1 domain family member 1 (TBC1D1), a Rab GTPase-activating protein and paralogue of Akt substrate of 160 kDa (AS160), has been implicated in both insulin- and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohydrolase (AICAR)-mediated glucose transporter type (GLUT4) translocation. However, the role of TBC1D1 in contracting muscle remains ambiguous. We therefore explored the metabolic consequence of ablating TBC1D1 in both resting and contracting skeletal muscles, utilizing a rat TBC1D1-KO model...
August 14, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28808055/dynamin-dependent-amino-acid-endocytosis-activates-mechanistic-target-of-rapamycin-complex-1-mtorc1
#15
Shusaku Shibutani, Hana Okazaki, Hiroyuki Iwata
The mechanistic target of rapamycin complex 1 (mTORC1) is a master regulator of protein synthesis and potential target for modifying cellular metabolism in various conditions, including cancer and aging. mTORC1 activity is tightly regulated by the availability of extracellular amino acids, and previous studies have revealed that amino acids in the extracellular fluid are transported to the lysosomal lumen. There, amino acids induce recruitment of cytoplasmic mTORC1 to the lysosome by the Rag GTPases, followed by mTORC1 activation by the small GTPase Ras homolog enriched in brain (Rheb)...
August 14, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28806519/pluronic-p85-f68-micelles-of-baicalein-could-interfere-with-mitochondria-to-overcome-mrp2-mediated-efflux-and-offer-improved-anti-parkinsonian-activity
#16
Tongkai Chen, Ye Li, Chuwen Li, Xiang Yi, Ruibing Wang, Simon Ming Yuen Lee, Ying Zheng
Overexpression of the drug efflux transporter multidrug resistance-associated protein 2 (MRP2) in the gastrointestinal tract and blood-brain barrier compromises the oral delivery of drugs to the circulation system and brain in the treatment of Parkinson's disease (PD). In this study, we aim to develop small-sized Pluronic P85/F68 micelles loaded with baicalein (B-MCs) to overcome MRP2-mediated efflux and to investigate related mechanism, as well as the anti-Parkinsonian efficacy. Spherical and sustained-release B-MCs have a mean particle size of 40...
August 14, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28806296/the-risk-of-necrotizing-enterocolitis-differs-among-preterm-pigs-fed-formulas-with-either-lactose-or-maltodextrin
#17
Randal K Buddington, Samantha L Davis, Karyl K Buddington
OBJECTIVES: When breast milk is unavailable for preterm infants, formulas are needed that won't increase the risk of necrotizing enterocolitis (NEC). Adding novel ingredients to formula to reduce NEC has not been effective clinically. Instead, we tested the prediction that NEC can be reduced by removing the maltodextrin now included in preterm formulas. METHODS: The preterm pig model of spontaneous NEC was used to evaluate growth, health, and intestinal responses to 6-7 days of feeding formulas that were identical except for the source of carbohydrate; either 100% lactose or maltodextrin; colostrum was used as the control...
August 11, 2017: Journal of Pediatric Gastroenterology and Nutrition
https://www.readbyqxmd.com/read/28806072/modeling-of-the-passive-permeation-of-mercury-and-methylmercury-complexes-through-a-bacterial-cytoplasmic-membrane
#18
Jing Zhou, Micholas Dean Smith, Sarah J Cooper, Xiaolin Cheng, Jeremy C Smith, Jerry M Parks
Cellular uptake and export are important steps in the biotransformation of mercury (Hg) by microorganisms. However, the mechanisms of transport across biological membranes remain unclear. Membrane-bound transporters are known to be relevant, but passive permeation may also be involved. Inorganic Hg(II) and methylmercury ([CH3Hg]+) are commonly complexed with thiolate ligands. Here, we have performed extensive molecular dynamics simulations of the passive permeation of Hg(II) and [CH3Hg]+ complexes with thiolate ligands through a model bacterial cytoplasmic membrane...
August 14, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28805727/leaf-physiological-and-proteomic-analysis-to-elucidate-silicon-induced-adaptive-response-under-salt-stress-in-rosa-hybrida-rock-fire
#19
Prabhakaran Soundararajan, Abinaya Manivannan, Chung Ho Ko, Sowbiya Muneer, Byoung Ryong Jeong
Beneficial effects of silicon (Si) on growth and development have been witnessed in several plants. Nevertheless, studies on roses are merely reported. Therefore, the present investigation was carried out to illustrate the impact of Si on photosynthesis, antioxidant defense and leaf proteome of rose under salinity stress. In vitro-grown, acclimatized Rosa hybrida 'Rock Fire' were hydroponically treated with four treatments, such as control, Si (1.8 mM), NaCl (50 mM), and Si+NaCl. After 15 days, the consequences of salinity stress and the response of Si addition were analyzed...
August 14, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28804697/evaluation-of-satellite-and-reanalysis-based-global-net-surface-energy-flux-and-uncertainty-estimates
#20
Chunlei Liu, Richard P Allan, Michael Mayer, Patrick Hyder, Norman G Loeb, Chris D Roberts, Maria Valdivieso, John M Edwards, Pier-Luigi Vidale
The net surface energy flux is central to the climate system yet observational limitations lead to substantial uncertainty. A combination of satellite-derived radiative fluxes at the top of atmosphere adjusted using the latest estimation of the net heat uptake of the Earth system, and the atmospheric energy tendencies and transports from the ERA-Interim reanalysis are used to estimate surface energy flux globally. To consider snowmelt and improve regional realism, land surface fluxes are adjusted through a simple energy balance approach at each grid point...
June 27, 2017: Journal of Geophysical Research. Atmospheres: JGR
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