• SLC6A19 is a system B(0) transporter that mediates epithelial resorption of neutral amino acids across the apical membrane in the kidney and intestine. (wikipedia.org)
  • Throughout, the focus is on epithelial cells and how polarity mechanisms facilitate the development of their apical and basolateral surfaces, tube formation (e.g., in blood vessel development), exchange of waste and nutrients, and the generation and maintenance of specialized structures at the cell surface (e.g., cilia). (cshlpress.com)
  • Since the mid-1960s, it has been known that there are energy-dependent, sodium-coupled glucose transporter (SGLT) and energy-independent, facilitative glucose transporter (GLUT) pathways for glucose uptake in the lung [ 1 ], and that glucose can permeate the alveolar epithelial barrier [ 2 ]. (ersjournals.com)
  • Unlike the other NHE isoforms, NHE3 is recycled between apical membranes and the endosomal compartment of epithelial cells where it has a significant involvement in renal and intestinal Na + absorption. (tocris.com)
  • Antisera directed against OCT1 or OCT2 specifically detected OCT1 in the basolateral membrane of human hepatocytes, OCT2 in tubular epithelial cells of human kidney, and the respective recombinant transporter in the basolateral membrane of MDCKII transfectants. (nih.gov)
  • In third mechanism of drug transport where drug is permeated transcellularly due to its lipophilicity straightaway crosswise at epithelial cell's apical and basolateral membranes. (omicsonline.org)
  • Here we investigated whether polarized monolayers of intestinal epithelial cells might regulate inflammatory responses by secreting IL-8 in a vectorial fashion (i.e. apical versus basolateral) depending on the location of the TLR stimulus. (biomedcentral.com)
  • The CXCR1 receptor for IL-8 was expressed only on the apical membrane of Caco-2 BBE cells and differentiated epithelial cells in the human small intestine and colon. (biomedcentral.com)
  • These results show that IL-8 induces autocrine signalling via an apical CXCR1 in Caco-2 BBE intestinal epithelial cells and that this receptor is also expressed on the apical surface of differentiated human intestinal epithelial cells in vivo , suggesting an autocrine function for IL-8 secreted in the lumen. (biomedcentral.com)
  • Consumed fructose enters enterocytes of the intestinal epithelial apical membrane mediated by glucose transporter 5 (GLUT5). (openveterinaryjournal.com)
  • In the mammalian epithelial cell sheet, TJs regulate molecular transport within the intercellular space and independent compartments of proteins and lipids localized to apical and basolateral membranes [4,5]. (synanet2020.com)
  • The present research was designed to characterize L-Citrulline transport throughout the apical filters involving kidney epithelial tubular cells, utilizing primary-cultured rat renal proximal tubular tissue, as well as the individual renal system proximal tubular mobile line HK-2. (bms-387032inhibitor.com)
  • An ATP-BINDING CASSETTE TRANSPORTERS subfamily protein that is localized on the canalicular membrane of HEPATOCYTES, as well as on the apical membrane of EPITHELIAL CELLS of the DUODENUM, JEJUNUM and PROXIMAL RENAL TUBULE. (bvsalud.org)
  • Methods: Primary mouse enteric neurons (EN) were exposed to a conditioned medium from ACE2-expressing Caco-2 colonic epithelial cells infected with SARS-CoV-2 or treated with tunicamycin (ER stress inducer). (emory.edu)
  • The common polymorphisms of the gene ABCG2 coding the efflux transporter BCRP and the gene SLCO1B1 coding the influx transporter OATP1B1 are associated with the interindividual variation in the effectiveness and tolerability of the cholesterol-lowering statins. (helsinki.fi)
  • In conclusion, the efflux transporter BCRP seems to have a greater significance on regulating the concentration of rosuvastatin in the liver than the influx transporter OATP1B1. (helsinki.fi)
  • The transporters mediate the simultaneous efflux of a hydrogen ion and the influx of a sodium ion across the plasma membrane, the driving force being the inwardly directed electrochemical Na + gradient. (tocris.com)
  • To study this vectorial transport of organic cations, we constructed a double-transfected Madin-Darby canine kidney strain II (MDCKII) cell line permanently expressing the human organic cation transporter 1 (OCT1, SLC22A1) in the basolateral membrane and MDR1 P-glycoprotein (MDR1 P-gp, ABCB1), an adenosine triphosphate (ATP)-dependent efflux pump for organic cations, in the apical membrane. (nih.gov)
  • The specific MDR1 P-gp inhibitor, zosuquidar trihydrochloride (LY335979), strongly inhibited berberine efflux into the apical compartment. (nih.gov)
  • Two types of transporters are identified in intestine i.e. uptake and efflux transporters. (omicsonline.org)
  • The effects of hepatic uptake and efflux transporters on metabolism of digoxin were examined in isolated rat hepatocytes versus microsomes. (aspetjournals.org)
  • Rifampin (an organic anion-transporting peptide 2 inhibitor) or GG918 [GF120918 ( N -(4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]-phenyl)-9,10-dihydro-5-methoxy-9-oxo-4-acridine carboxamide)] (a potent P-glycoprotein inhibitor) were used to estimate effects of uptake or efflux transporters on digoxin metabolism. (aspetjournals.org)
  • These results strongly suggest that the hepatic uptake and efflux transporters that are found in hepatocytes, but not in microsomes, modulate intracellular concentration of digoxin and thus affect metabolism. (aspetjournals.org)
  • Hepatic transporters are roughly categorized into two groups: efflux transporters that are localized on the canalicular (apical) membrane and the more recently discovered uptake transporters that are found on the sinusoidal (basolateral) membrane. (aspetjournals.org)
  • Many of the well studied efflux transporters, such as P-glycoprotein (P-gp), MRP2, and BCRP are members of the ATP-binding cassette transporter superfamily. (aspetjournals.org)
  • Increased drug efflux, via these transporters, lowers intracellular drug concentration, allowing cancer cells to escape the toxic effects of the drugs. (savedelicious.com)
  • MRP4 is an ATP-dependent, unidirectional efflux transporter belonging to the C subfamily of the ABC protein superfamily. (solvobiotech.com)
  • Recently, two new members of the ABC transporter family (ABCG5 and ABCG8 heterodimers) have been discovered in the apical pole of the enterocyte and in the canalicular membrane of hepatocytes. (nih.gov)
  • The primary defect in Dubin-Johnson syndrome is a mutation in an apical canalicular membrane protein responsible for the excretion of bilirubin and other nonbile salt organic anions. (medscape.com)
  • Various authors have studied amino acid transport in cell membranes obtained from the proximal renal tubule of humans, rats, and rabbits. (medscape.com)
  • Therefore, these results advise that amino transporters N(Zero)AT1 along with b(Zero,+)With get excited about your reabsorption of L-Citrulline in the renal system, at the very least in part, by mediating the actual apical membrane layer transportation regarding L-citrulline throughout renal tubule cellular material. (bms-387032inhibitor.com)
  • Transporters on the plasma membrane of tumor cells are promising molecular "Trojan horses" to deliver drugs and imaging agents into cancer cells. (aspetjournals.org)
  • High-confidence identification of ~2,000 proteins, including cytoplasmic, nuclear, plasma membrane, extracellular and unknown/unclassified proteins, was obtained by separating tryptic peptides of renal cortical proteins into 60 fractions by SCX prior to LC-MS/MS. The identified proteins represented the renal cortical proteome with no discernible bias due to protein physicochemical properties, subcellular distribution, biological processes, or molecular function. (biomedcentral.com)
  • Comparison of this renal cortical proteome with published human urinary proteomes demonstrated enrichment of renal extracellular, plasma membrane, and lysosomal proteins in the urine, with a lack of intracellular proteins. (biomedcentral.com)
  • The very steep gradient is maintained by an energy-driven calcium pump, known as the plasma membrane Ca 2+ ATPase (PMCA). (abdominalkey.com)
  • Renal NHE3 and NaPi2 partition into distinct membrane domains. (ukrocharity.org)
  • Exposure to an acid load increases apical membrane Na + /H + antiporter (NHE3) activity, a process that involves exocytic trafficking of the transporter to the apical membrane. (elsevierpure.com)
  • The Rho kinase inhibitor Y27632 completely blocks acid-induced stress fiber formation and the increases in apical membrane NHE3 abundance and activity, but it has no effect on acid-induced tyrosine phosphorylation of p125 FAK or paxillin. (elsevierpure.com)
  • Membrane expression of NHE3 was determined by surface biotinylation. (emory.edu)
  • In particular, human organic cation transporter 2 (hOCT2) and multidrug and toxin extrusion proteins 1 and 2-K (hMATE1/2-K) likely mediate renal secretion of mIBG, whereas hOCT1 and hOCT3 may contribute to mIBG uptake into normal tissues such as the liver, salivary glands, and heart. (aspetjournals.org)
  • Additionally, MDCKII single transfectants stably expressing OCT1, MDR1 P-gp, or human organic cation transporter 2 (OCT2, SLC22A2) were generated. (nih.gov)
  • We hypothesize that hepatic transporters present in hepatocytes, but not in microsomes, are often the missing link explaining such discrepancies between microsome data and in vivo profiles. (aspetjournals.org)
  • Computer modelling is worth exploiting as a supportive method of other study methods in the pharmacogenetic research, for example when the relative significance of separate transporter proteins is evaluated. (helsinki.fi)
  • Investigating the role of cell membrane proteins has increased over the last decade, as drugdrug interactions and genetic polymorphisms have been found to cause changes in drug pharmacokinetics and dynamics. (helsinki.fi)
  • Norepinephrine transporter, organic cation transporters, and multidrug and toxin extrusion proteins play differential roles in tumor targeting, systemic elimination, and accumulation in normal tissues. (aspetjournals.org)
  • Many of these proteins, such as low-abundance proteins, membrane proteins and proteins with extreme values in pI or MW are traditionally under-represented in 2-DE-based proteomic analysis. (biomedcentral.com)
  • The gene that codes for the cystine transporter, initially termed rBAT, is now known as SLC3A1 (SLC for solute carrier) in the international Genome Database. (medscape.com)
  • It has been reported that solute carrier (SLC) and the ATP-binding cassette (ABC) transporter super families are the major class of membrane transporters [ 14 , 17 ]. (omicsonline.org)
  • The reduced folate carrier (RFC, SLC19A1), thiamine transporter-1 (ThTr1, SLC19A2) and thiamine transporter-2 (ThTr2, SLC19A3) evolved from the same family of solute carriers. (elsevierpure.com)
  • It enters the gastrointestinal tract and is absorbed across the brush border of the small intestine into the enterocytes of the apical membrane of the intestinal epithelium, mediated by glucose transporter 5 (GLUT5) or Solute carrier family 2 A5 (SLC2A5). (openveterinaryjournal.com)
  • Osteoblasts express high levels of the membranous Na+-dependent citrate transporter solute carrier family 13 member 5 (Slc13a5) gene. (biomed.news)
  • The system is having donar and receiver compartment for studying permeation of drug across the membrane. (omicsonline.org)
  • Stimulation of polarized Caco-2 BBE cells with Pam2CSK4 and Pam3CSK4, agonists for TLR2/6 and TLR2/1 from the apical or basolateral sides induced secretion of IL-8 predominantly into the apical compartment regardless of the location of the stimulus, although basolateral stimulation induced smaller amounts of IL-8 compared to apical stimulation. (biomedcentral.com)
  • The cystic fibrosis transmembrane conductance regulator (CFTR) is a member of the ATP binding cassette (ABC) transporter superfamily. (ucl.ac.uk)
  • it is a member of the ABC transporter superfamily. (medscape.com)
  • Iron is absorbed as ferrous ( 2 ) iron via a divalent metal transporter 1 located on the apical membrane of the enterocyte. (fujiorganics.com)
  • Sodium-dependent neutral amino acid transporter B(0)AT1 is a protein that in humans is encoded by the SLC6A19 gene. (wikipedia.org)
  • In this study the characteristics of the OATP1B1 transporter were reviewed and new in vitro research method to study protein functions was developed. (helsinki.fi)
  • In 1993, Lee et al cloned a human complementary DNA, rBAT (renal basic amino acid transporter) in chromosome 2, encoding a transport protein for cystine and dibasic amino acids. (medscape.com)
  • The PDS gene encodes a transmembrane protein, known as pendrin, which functions as a transporter of iodide and chloride. (umn.edu)
  • Heme iron can also be absorbed by heme-carrier protein 1 on the apical membrane after which iron is released by the action of lysosomal heme oxygenase. (fujiorganics.com)
  • Glucose is removed from ASL in proximal airways via facilitative glucose transporters, down a concentration gradient generated by intracellular glucose metabolism. (ersjournals.com)
  • In the distal lung, glucose transport via sodium-coupled glucose transporters predominates. (ersjournals.com)
  • In immortalised human airway cells (line H441) with 10 mM glucose in the basolateral medium, apical ASL glucose was 0.24±0.07 mM [ 10 ]. (ersjournals.com)
  • Almost all of this is re-absorbed into the circulation via sodium glucose co-transporters (SGLTs). (bjcardio.co.uk)
  • SGLTs transport sodium and glucose into cells using the sodium gradient created by sodium/potassium ATPase pumps at the basolateral cell membranes. (bjcardio.co.uk)
  • SGLT2, a high-capacity, low-affinity transporter of glucose and sodium is found in high concentration at the brush border membrane of the S1 and S2 segment of the proximal convoluted tubule (PCT). (bjcardio.co.uk)
  • SGLT2 binds to sodium and glucose in the filtrate and these compounds are translocated across the apical cell membrane, an active process driven by the electrochemical sodium gradient between tubular filtrate and the cell. (bjcardio.co.uk)
  • The second stage of re-absorption is the transport of glucose through the utilisation of GLUT2 transporters in the basolateral membrane. (bjcardio.co.uk)
  • CFTR controls the flow of anions through the apical membrane of epithelia. (ucl.ac.uk)
  • Very lipophilic drugs enter the cell membrane through passive diffusion, but polar or ionized organic compounds can enter the cell membrane only by transporters. (helsinki.fi)
  • The high-affinity system mediates uptake of 10% of L-cystine and the dibasic amino acids at the apical membrane of the straight third segment (S3) of the proximal tubule. (medscape.com)
  • Emerging evidences suggest that the polyspecific organic cation transporters play important roles in systemic disposition and tissue-specific uptake of mIBG. (aspetjournals.org)
  • Transporter-mediated uptake has been exploited successfully in nuclear medicine to deliver several radiopharmaceuticals for cancer imaging and treatment ( Zhang and Wang, 2020 ). (aspetjournals.org)
  • The process of secreting organic anions through the proximal tubule cells is achieved via unidirectional transcellular transport involving the uptake of organic anions into the cells from the blood across the basolateral membrane, followed by extrusion across the brush-border membrane into the proximal tubule fluid. (aspetjournals.org)
  • Genetic polymorphism occurs in several genes that code drug metabolizing enzymes or drug transporters. (helsinki.fi)
  • Drug removal is not only dependent on metabolic enzymes, but also on transporters. (helsinki.fi)
  • Transporters in the basolateral membrane of the hepatocyte facilitate drug entry and access to drug metabolizing enzymes. (helsinki.fi)
  • We conclude that the interplay of transporters and enzymes must be considered in defining the intrinsic metabolic clearance of the liver and in evaluating potential drug-drug interactions. (aspetjournals.org)
  • In the Caco-2 BBE model of polarized villus-like epithelium, apical stimulation with TLR2 and TLR5 ligands resulted in the apical secretion of IL-8. (biomedcentral.com)
  • However, it is not known if CXCR1 is expressed on the apical or basolateral poles in polarized Caco-2 BBE cells or human intestinal tissue or whether the direction of TLR signalling influences the direction of IL-8 secretion. (biomedcentral.com)
  • We investigated whether the location (i.e. apical or basolateral) of TLR agonists influenced the production and direction of IL-8 secretion. (biomedcentral.com)
  • However, this transporter may be important where active renal secretion is suspected, or where changes in circulating levels of bile salts are observed. (solvobiotech.com)
  • Vasoactive intestinal peptides (VIP) expression and secretion by EN were assessed by RT-PCR and ELISA, respectively. (emory.edu)
  • Contributors discuss how cells coordinate signaling pathways, membrane trafficking, and cytoskeletal remodeling to ensure proper spatial arrangement of cellular components. (cshlpress.com)
  • These cells are equipped on their apical and basal membrane with copper transporters CTR1 and ATP7A. (researchgate.net)
  • Human Embryonic Kidney cells (HEK) is a human derived mammalian cell-line that is widely used in the study of OATP1B1 transporter. (helsinki.fi)
  • The expression of OATP1B1 transporter in HEK293 cells was successful. (helsinki.fi)
  • HEK293 cells expressing OATP1B1 transporter are well suited for the study of the SLCO1B1-gene. (helsinki.fi)
  • mIBG enters cancer cells through the norepinephrine transporter (NET) where the radioactive decay of 131 I causes DNA damage, cell death, and tumor necrosis. (aspetjournals.org)
  • To elucidate the molecular mechanisms for the tubular excretion of diuretics, we have elucidated the interactions of human organic anion transporters (hOATs) with diuretics using cells stably expressing hOATs. (aspetjournals.org)
  • When transfected cells were grown polarized on permeable filter supports, berberine was transferred from the basolateral to the apical compartments many times faster by MDCK-OCT1/MDR1 P-gp double transfectants than by MDCK-OCT1 or MDCK-MDR1 P-gp single transfectants. (nih.gov)
  • Magadi tilapia gill pavement cells exhibited a trafficking of dense-cored vesicles between the well-developed Golgi cisternae and the apical membrane. (mcmaster.ca)
  • MRP4 localizes to different membranes in different polarized cells. (solvobiotech.com)
  • In the liver, choroid plexus, prostatic acinar cells, and the GIT, MRP4 is expressed at the basolateral membrane, while in the brain capillary endothelium and renal proximal tubule cells it is expressed at the apical membrane [2-6]. (solvobiotech.com)
  • The proton-coupled folate transporter (PCFT, SLC46A1) is the mechanism by which folates are absorbed across the apical-brush-border membrane of the proximal small intestine. (elsevierpure.com)
  • Organic Anion Transporting Polypeptide 2B1 (OATP2B1) is an influx transporter expressed widely throughout the body in tissues such as intestine, liver, brain, placenta and skeletal muscle. (helsinki.fi)
  • Emerging evidences suggest that the polyspecific organic cation transporters are the major transporters driving the systemic elimination and tissue-specific disposition of mIBG in normal organs. (aspetjournals.org)
  • Sodium-hydrogen exchangers (Na + /H + exchangers, NHE) are ATP-independent membrane glycoprotein transporters that are involved in the regulation of intracellular pH, cell volume and the cellular response to hormones and mitogens. (tocris.com)
  • During her graduate training, Dr. Riquier-Brison received an NIH-sponsored pre-doctoral training fellowship to study the regulation of sodium transporters in the renal proximal tubule during hypertension. (ukrocharity.org)
  • The calcium ion is essential to any physiologic phenomena, including preservation of the integrity of cellular membranes, neuromuscular activity, regulation of endocrine and exocrine secretory activities, blood coagulation, activation of the complement system, and bone metabolism. (abdominalkey.com)
  • Recent studies have shown that transporters can mediate drug-drug interactions, and transporter genes are subject to genetic polymorphism which may affect pharmacokinetic parameters of a drug, such as absorption, distribution, and excretion. (helsinki.fi)
  • 1 - 3 For example, in vivo light/dark transitions trigger RPE physiological changes that homeostatically maintain the chemical composition and volume of the extracellular spaces separating the apical membrane/photoreceptor and basolateral/Bruch membrane interfaces. (arvojournals.org)
  • The in vitro method developed in this study remains in the research team as a tool to investigate the polymorphisms of the SLCO1B1-gene, the inhibition of the transporter and possible drug interactions. (helsinki.fi)
  • Discovery of the hepatic canalicular and intestinal cholesterol transporters. (nih.gov)
  • It is expressed in the kidney, blood-brain barrier (BBB), liver, and other tissues, and its localization to the basolateral or apical membranes is tissue-dependent. (solvobiotech.com)
  • This means that, for instance, in the liver (where its abundance is relatively low) it effluxes its substrates into the bloodstream, whilst in the kidney (where it is one of the dominating ABC transporters [7]) it effluxes into the urine. (solvobiotech.com)
  • The highest ranked molecular functions were characteristic of tubular epithelium, and included binding, catalytic activity, transporter activity, structural molecule activity, and carrier activity. (biomedcentral.com)
  • Zhao, R & Goldman, ID 2013, ' Folate and thiamine transporters mediated by facilitative carriers (SLC19A1-3 and SLC46A1) and folate receptors ', Molecular aspects of medicine , vol. 34, no. 2-3, pp. 373-385. (elsevierpure.com)
  • These pumps have broad drug specificity and belong to a family of ATP-binding cassette (ABC) transporters, of which P-glycoprotein (PGP) is one of the most important members. (savedelicious.com)
  • Since many clinically used drugs are transported by OATP2B1, changes in the function of the transporter due to genetic polymorphism could lead to altered pharmacokinetics or -dynamics of OATP2B1 substrate drugs. (helsinki.fi)
  • The clinical use of mIBG as a radiopharmaceutical in cancer diagnosis and treatment can be further improved by taking a holistic approach considering mIBG transporters in both cancer and normal tissues. (aspetjournals.org)
  • A 1700 base pair cDNA for a putative Magadi tilapia urea transporter (mtUT) was cloned, sequenced and found to display high homology with urea transporters from mammals, amphibians and other fishes. (mcmaster.ca)
  • It comprises 12 putative membrane spanning helices and lacks the additional N-terminal helices found in MRP1, MRP2, MRP3, and MRP6 [8]. (solvobiotech.com)
  • Thiazides and loop diuretics exhibit their diuretic effects from the luminal side by inhibiting the Na + -Cl - cotransporter of the distal tubule and the Na + -K + -2Cl - co-transporter of the loop of Henle, respectively ( Ives, 2001 ). (aspetjournals.org)
  • Acute hypertension provokes acute trafficking of distal tubule NaCl co-transporter (NCC) to subapical cytoplasmic vesicles. (ukrocharity.org)
  • Angiotensin II provokes acute trafficking of distal tubule NaCl co-transporter (NCC) to apical membrane. (ukrocharity.org)
  • The mean transepithelial potential (TEP) was 1.19 ± 0.24 mV (mean ± SEM, n = 31), apical positive, and the mean transepithelial resistance ( R T ) was 178.7 ± 9.9 Ω·cm 2 (mean ± SEM, n = 31). (arvojournals.org)
  • Thus, serum water is forced across the membrane, and the ultrafiltrate is analyzed for calcium concentration and then corrected for total serum solids. (abdominalkey.com)
  • For usual absorption of drug it is soluble then it will reach intestinal wall in dissolved state and later absorbed in gut membranes combining all above transport mechanisms. (omicsonline.org)
  • Furthermore, urea transport was inhibited by classic inhibitors of mammalian and piscine urea transporters in the order thiourea>N-methylurea>acetamide. (mcmaster.ca)
  • Intestinal transporters play important role in drug's absorption and in turn its oral bioavailability . (omicsonline.org)