Abstract:
:Nucleoside transporters play a critical role in the absorption, disposition, and targeting of therapeutically used nucleosides and nucleoside analogs. This review is focused on the Na(+)-dependent, concentrative nucleoside transporters which are found in a variety of cells including renal, intestinal and hepatic epithelia. Five major Na(+)-dependent nucleoside transporter subtypes have been characterized in isolated tissue preparations: N1 is purine selective; N2 is pyrimidine selective and N3-N5 exhibit variable selectively for both purine and pyrimidine nucleosides. The recent cloning of N1 and N2 nucleoside transporters has provided the first information on the molecular function and structure of concentrative nucleoside transporters. In this manuscript we review the characteristics of the various subtypes of nucleoside transporters and the molecular structure, functional properties, and tissue distribution of the cloned Na(+)-dependent nucleoside transporters. In addition, the interactions of nucleosides and nucleoside analogs with the cloned transporters in mammalian and amphibian expression systems are presented. Mammalian expression systems may be particularly useful during drug development in screening potential compounds for improved bioavailability and tissue specific targeting. Finally, we present our view of future ares of study in the field of nucleoside transporters.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Wang J,Schaner ME,Thomassen S,Su SF,Piquette-Miller M,Giacomini KMdoi
10.1023/a:1012113931332subject
Has Abstractpub_date
1997-11-01 00:00:00pages
1524-32issue
11eissn
0724-8741issn
1573-904Xjournal_volume
14pub_type
杂志文章,评审abstract:PURPOSE:To identify High Molecular Weight Products (HMWP) formed in human insulin formulation during storage. METHODS:Commercial formulation of human insulin was stored at 37°C for 1 year and HMWP was isolated using preparative size exclusion chromatography (SEC) and reverse phase (RP) chromatography. The primary stru...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1600-3
更新日期:2015-06-01 00:00:00
abstract::We describe an assay for acrolein in urine, employing derivatization with m-aminophenol in the presence of ferrous sulfate solution in sulfuric acid. The derivative (7-OH quinoline; DER) and the internal standard (quinine-bisulfate; IS) were separated on a 10-micron particle, 8 mm x 10-cm C18 cartridge in conjunction ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018964401677
更新日期:1993-11-01 00:00:00
abstract:PURPOSE:An asymmetric membrane (AM) tablet was developed for a soluble model compound to study the in vitro drug release mechanisms in challenge conditions, including osmotic gradients, concentration gradients, and under potential coating failure modes. Porous, semipermable membrane integrity may be compromised by a hi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9142-y
更新日期:2007-02-01 00:00:00
abstract::High molecular weight drugs in general, and peptides in particular, are usually delivered by parenteral route because they are poorly absorbed or degraded in the gastrointestinal tract. To optimize therapy, it is desirable to search for nonparenteral routes of administration and to deliver the drug in a controlled-rel...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018948924992
更新日期:1993-06-01 00:00:00
abstract:PURPOSE:To examine the inhibitory potential of enalapril [and other angiotensin converting enzyme (ACE) inhibitors] on glycylsarcosine (GlySar) transport by the high-affinity renal peptide transporter. METHODS:Studies were performed in rabbit renal brush border membrane vesicles in which the uptake of radiolabeled Gly...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018847818766
更新日期:1999-05-01 00:00:00
abstract:PURPOSE:The purpose of the present study was to explore the involvement of indoxyl sulfate (IS) in nephrotoxicity and central nervous system (CNS) toxicity in cisplatin (CDDP)-treated rats. MATERIALS AND METHODS:Renal function was evaluated by serum creatinine and BUN levels. The IS levels in the serum, brain and kidn...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9183-2
更新日期:2007-04-01 00:00:00
abstract:PURPOSE:The purpose of this study was to determine the potential effect of probenecid on the pharmacokinetics of zalcitabine in HIV-positive patients. METHODS:Twelve patients received single oral 1.5 mg doses of zalcitabine alone and during probenecid treatment (500 mg at 8 and 2 hours before and 4 hours after zalcita...
journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1023/a:1016009029536
更新日期:1996-03-01 00:00:00
abstract:PURPOSE:To assess the efficacy of the novel clinical formulation of fenretinide (LAU-7b) for the treatment of allergic asthma. To study the association between LAU-7b treatment in allergic asthma and the modulation of very long chain ceramides (VLCC). METHODS:We used two allergens (OVA and HDM) to induce asthma in mou...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2743-z
更新日期:2020-01-08 00:00:00
abstract:PURPOSE:To develop an efficient tumor vasculature-targeted polymeric micelle delivery system for combretastatin A4 (CA4), a novel antivascular agent. METHODS:CA4-loaded micelles were prepared from poly (ethylene glycol)-b-poly (d, l-lactide) copolymers. RGD peptides that target integrins alphavbeta3 and alphavbeta5, m...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0184-9
更新日期:2010-09-01 00:00:00
abstract:PURPOSE:The addition of high amounts of calcium remains a pharmaceutical concern due to its precipitation with phosphate in total parenteral nutrient (TPN) admixtures, compromising also the stability of the lipid emulsion. MATERIALS AND METHODS:Calcium-phosphate solubility was compared when using binary PN solutions v...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9671-7
更新日期:2008-11-01 00:00:00
abstract::The effect of buprenorphine on bremazocine-induced diuresis was tested in the rat to determine the nature of buprenorphine's action at the ϰ opioid receptor. Both morphine-tolerant and naive rats were used to account for possible antidiuretic effects of buprenorphine at the µ site. Separate experiments established tha...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016340106299
更新日期:1985-07-01 00:00:00
abstract:PURPOSE:Recent studies have demonstrated the potential for a triglyceride (TG) mimetic prodrug to promote the delivery of mycophenolic acid (MPA) to the lymphatic system. Here, the metabolic pathways that facilitate the lymphatic transport of the TG prodrug (1,3-dipalmitoyl-2-mycophenoloyl glycerol, 2-MPA-TG) were exam...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1579-9
更新日期:2015-05-01 00:00:00
abstract:PURPOSE:To elucidate the apical and basolateral components of the total unstirred water layer in regular permeability experiment. METHODS:A novel stirring apparatus was constructed to remove the basolateral unstirred water layer. Caco-2 cells were used as the permeability barrier both in Transwell-type and side-by-sid...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9573-8
更新日期:2008-07-01 00:00:00
abstract:PURPOSE:To investigate the effect of atomization conditions on particle size and stability of spray-freeze dried protein. METHODS:Atomization variables were explored for excipient-free (no zinc added) and zinc-complexed bovine serum albumin (BSA). Particle size was measured by laser diffraction light scattering follow...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007570030368
更新日期:2000-11-01 00:00:00
abstract::A reverse-phase HPLC method for the analysis of tryptic digests of recombinant porcine growth hormone (pGH) has been developed and validated. Digestion was performed at 4 degrees C for a 20-hr period with TPCK-treated trypsin at a 1:20 (w/w) trypsin:pGH ratio. Gradient elution HPLC, using an Aquapore RP300 C8 column, ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018927426268
更新日期:1993-10-01 00:00:00
abstract::The stability of a freeze-dried model protein, ribonuclease A (RNase), was investigated under accelerated storage conditions at 45 degrees C for time periods up to 60 days. Because RNase is a fairly stable molecule around pH 7, lyophilization was performed in phosphate buffers at pH 4.0 or 10.0 to accelerate degradati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015959604616
更新日期:1990-10-01 00:00:00
abstract:PURPOSE:To determine the effect of Sodium N-[8-(2-hydroxybenzoyl)amino]caprylate (SNAC) on the permeation of cromolyn across Caco-2 cell monolayers and explore the molecular basis for the enhanced absorption. METHODS:Transport studies of cromolyn across Caco-2 cell monolayers were conducted in the presence of various ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-7671-9
更新日期:2004-12-01 00:00:00
abstract:PURPOSE:The objective of this work was to assess, in vitro, the passage of P-glycoprotein dependent drugs across brain capillary endothelial cells, when these drugs are associated with a reversing agent. METHODS:An in vitro model of the blood-brain barrier consisting of a coculture of brain capillary endothelial cells...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011913723928
更新日期:1998-07-01 00:00:00
abstract:PURPOSE:We reported that suramin produced chemosensitization at nontoxic doses. This benefit was lost at the approximately 10-fold higher, maximally tolerated doses (MTD). The aim of the current study was to identify in patients the chemosensitizing suramin dose that delivers 10-50 microM plasma concentrations over 48 ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-0165-1
更新日期:2006-06-01 00:00:00
abstract::Transdermal drug delivery of ionized drugs can be enhanced by iontophoresis. Drug in the ionic form, contained in some reservoir, can be "phoresed" through the skin with a small current across two electrodes, one above the reservoir and one at a distal skin location. Positive ions can be introduced from the positive p...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016327822325
更新日期:1986-12-01 00:00:00
abstract:PURPOSE:SN-38, a potent chemotherapeutic drug, has not been used clinically because of its severe side effects and poor solubility. In this work, we aimed to evaluate the effect of dose and multiple injections of SN-38-loaded polymeric depots on antitumor efficacy and toxicity in vivo. METHODS:Preparation and characte...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2011-4
更新日期:2016-12-01 00:00:00
abstract:PURPOSE:Performance of a transdermal delivery system (TDS) can be affected by exposure to elevated temperature, which can lead to unintended safety issues. This study investigated TDS and skin temperatures and their relationship in vivo, characterized the effective thermal resistance of skin, and identified the in vitr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2171-x
更新日期:2017-07-01 00:00:00
abstract::Assessment of bioavailability/bioequivalence generally relies on the comparison of rate and extent of drug absorption between products. Rate of absorption is commonly expressed by peak concentration (C(max)) and time to peak concentration (T(max)), although these parameters are indirect measures of absorption rate. Re...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-011-0421-x
更新日期:2011-08-01 00:00:00
abstract::The technique of Affinity capillary electrophoresis (ACE) is a useful tool to characterize complexation and partition equilibria. A wide range of applications in pharmaceutics has been presented: the determination of pKA values, of association constants between drugs and cyclodextrins or amphiphilic compounds as well ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:
更新日期:1999-11-01 00:00:00
abstract:PURPOSE:To develop a non-viral gene delivery system in the form of an oil-in-water (o/w) lipid emulsion. METHOD:Cationic lipid emulsions were formulated with soybean oil, 1,2-dioleoyl-sn-glycero-3-trimethylammonium-propane (DOTAP) as a cationic emulsifier and other co-emulsifiers. The physical characteristics of the l...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007553106681
更新日期:2000-03-01 00:00:00
abstract::One of the authors has his name incorrectly indexed in PubMed and SpringerLink as "Laird Forrest M" (last name "Laird Forrest"). His name should index as "Forrest M. Laird" with last name as "Forrest". ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,已发布勘误
doi:10.1007/s11095-018-2463-9
更新日期:2018-07-25 00:00:00
abstract:PURPOSE:To study the expression of P-glycoprotein (P-gp), lung resistance-related protein (LRP), and caveolin-1 (cav-1) in the human bronchial epithelial cell line 16HBE14o-. METHODS:The presence of P-gp, LRP, and cav-1 in 16HBE14o- cell layers was evaluated using immunocytochemical staining and visualization with con...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1023230328687
更新日期:2003-04-01 00:00:00
abstract:PURPOSE:Non-small cell lung cancer is the leading cause of cancer related deaths globally. Considering the side effects and diminishing chemosensitivity to chemotherapy, novel treatment approaches are sought. Hence, we aim to develop a liposomal co-delivery system of pDNA expressing shRNA against PFKFB3 (pshPFKFB3) and...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2244-x
更新日期:2017-11-01 00:00:00
abstract::Microbial metabolism studies of the semisynthetic antimalarial anhydrodihydroartemisinin (1), have shown that it is metabolized by a number of microorganisms. Large scale fermentation with Streptomyces lavendulae L-105 and Rhizopogon species (ATCC 36060) have resulted in the isolation of four microbial metabolites. Th...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018979202933
更新日期:1994-07-01 00:00:00
abstract::Emulsions (o/w) were prepared from solid-state emulsions comprised of various matrix materials and oils and the resultant particle size properties determined. Results suggest that for those matrices that can form solid-state emulsions, the droplet size decreased as a function of time, as previously observed. The final...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018912100826
更新日期:1993-08-01 00:00:00