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Organic Anion Transporters, Sodium-IndependentOrganic Anion TransportersOrganic Anion Transport Protein 1p-Aminohippuric AcidAnion Transport ProteinsAnionsProbenecidUricosuric AgentsOrganic Anion Transport Polypeptide CEstroneBiological TransportSulfobromophthaleinOrganic Cation Transport ProteinsOrganic Anion Transporters, Sodium-DependentOchratoxinsMultidrug Resistance-Associated ProteinsOrganic Anion Transporters, ATP-DependentCarrier ProteinsATP-Binding Cassette TransportersGlutaratesKidneyTaurocholic AcidKidney Tubules, ProximalMembrane Transport ProteinsDicarboxylic AcidsXenopus laevisDicarboxylic Acid TransportersRNA, ComplementaryUnithiolBile CanaliculiPhenolsulfonphthaleinSodium-Phosphate Cotransporter Proteins, Type IOocytesChoroid PlexusRenal AgentsOrganic Cation Transporter 1Leukotriene C4SymportersHyperbilirubinemia, HereditaryBiological Transport, ActiveLLC-PK1 CellsIndicanPenicillin GHyperbilirubinemia2,4-Dichlorophenoxyacetic AcidSulfinpyrazoneIodopyracetCatecholamine Plasma Membrane Transport ProteinsCefotiamFlounderKineticsMolecular Sequence DataJaundice, Chronic IdiopathicIon TransportMethotrexateLiverMercury IsotopesCimetidineRats, Mutant StrainsDehydroepiandrosterone SulfateRats, Sprague-DawleyCell MembraneCell LineRats, Inbred LECP-GlycoproteinRNA, MessengerTissue DistributionAmino Acid SequenceBileCephaloridineDNA, ComplementarySulfuric Acid EstersPharmaceutical PreparationsAminopterinPravastatinTransfectionSteviaGlutathioneBiotinylationDrug InteractionsPhysiological ProcessesUric AcidP-GlycoproteinsLiddle SyndromeAntiportersXanthurenatesCloning, MolecularHepatocytesSalicylatesKetoglutaric AcidsPropionatesDose-Response Relationship, DrugBlood-Brain BarrierSubstrate SpecificityDrug Resistance, MultipleCOS CellsBile Acids and SaltsCyclic P-OxidesXenobioticsFurosemideBiliary TractCells, CulturedXenopusAnion Exchange Protein 1, ErythrocyteRats, WistarBlotting, NorthernKidney CortexPharmacokineticsKidney TubulesMembrane ProteinsAdenosine TriphosphateDogsGlucuronidesChloridesTritiumToxins, BiologicalSequence Homology, Amino AcidReverse Transcriptase Polymerase Chain ReactionBase SequenceMonocarboxylic Acid TransportersBlotting, WesternGlucose Transporter Type 1CHO CellsCholestasisOrganophosphonatesSodiumHEK293 CellsFolic Acid AntagonistsBilirubinChloride-Bicarbonate AntiportersImmunohistochemistryMonosaccharide Transport ProteinsSerotonin Plasma Membrane Transport ProteinsHepatocyte Nuclear Factor 1-alpha4,4'-Diisothiocyanostilbene-2,2'-Disulfonic AcidGene Expression RegulationMice, KnockoutMetabolic Clearance RateDopamine Plasma Membrane Transport ProteinsCercopithecus aethiopsHistamine H2 AntagonistsAdenineImmunoblottingMercuryCricetulusGene ExpressionRecombinant ProteinsExcitatory Amino Acid Transporter 2Protein BindingCarbon RadioisotopesSulfatesCricetinaeMutagenesis, Site-DirectedDiureticsQuinolinesExcitatory Amino Acid Transporter 3BicarbonatesKillifishesAmino Acid Transport System X-AGModels, BiologicalDNA PrimersBinding SitesHydrogen-Ion ConcentrationMicroinjectionsExcitatory Amino Acid Transporter 1IsoquinolinesBenzbromaroneMolecular StructureNorepinephrine Plasma Membrane Transport ProteinsBrainAmino Acid SubstitutionTime FactorsCarboxylic AcidsFluorescent DyesCation Transport ProteinsGlycocholic AcidStructure-Activity RelationshipCationsAmino Acid Transport SystemsFluoresceinGlucose Transporter Type 3GABA Plasma Membrane Transport ProteinsSex CharacteristicsAmino Acid Transport Systems, NeutralEpithelial CellsAnti-Inflammatory Agents, Non-SteroidalMicrovilliRabbitsGlucose Transporter Type 4FluoresceinsCaco-2 CellsAntiviral AgentsMembrane Transport ModulatorsChromatography, High Pressure LiquidGlycosylationSwineMice, Inbred C57BLMalpighian TubulesEstradiolGlucose Transporter Type 2Digoxin
Organic Anion Transporters, Sodium-Independent: A subclass of ORGANIC ANION TRANSPORTERS that do not rely directly or indirectly upon sodium ion gradients for the transport of organic ions.Organic Anion Transporters: Proteins involved in the transport of organic anions. They play an important role in the elimination of a variety of endogenous substances, xenobiotics and their metabolites from the body.Organic Anion Transport Protein 1: A polyspecific transporter for organic cations found primarily in the kidney. It mediates the coupled exchange of alpha-ketoglutarate with organic ions such as P-AMINOHIPPURIC ACID.p-Aminohippuric Acid: The glycine amide of 4-aminobenzoic acid. Its sodium salt is used as a diagnostic aid to measure effective renal plasma flow (ERPF) and excretory capacity.Anion Transport Proteins: Membrane proteins whose primary function is to facilitate the transport of negatively charged molecules (anions) across a biological membrane.Anions: Negatively charged atoms, radicals or groups of atoms which travel to the anode or positive pole during electrolysis.Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.Uricosuric Agents: Gout suppressants that act directly on the renal tubule to increase the excretion of uric acid, thus reducing its concentrations in plasma.Organic Anion Transport Polypeptide C: An organic anion transporter found in human liver. It is capable of transporting a variety organic anions and mediates sodium-independent uptake of bile in the liver.Estrone: An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women.Biological Transport: The movement of materials (including biochemical substances and drugs) through a biological system at the cellular level. The transport can be across cell membranes and epithelial layers. It also can occur within intracellular compartments and extracellular compartments.Sulfobromophthalein: A phenolphthalein that is used as a diagnostic aid in hepatic function determination.Organic Cation Transport Proteins: A family of proteins involved in the transport of organic cations. They play an important role in the elimination of a variety of endogenous substances, xenobiotics, and their metabolites from the body.Organic Anion Transporters, Sodium-Dependent: A subclass of ORGANIC ANION TRANSPORTERS whose transport of organic anions is driven either directly or indirectly by a gradient of sodium ions.Ochratoxins: Isocoumarins found in ASPERGILLUS OCHRACEUS and other FUNGI. Ochratoxin contaminated FOOD has been responsible for cases of FOODBORNE DISEASES.Multidrug Resistance-Associated Proteins: A sequence-related subfamily of ATP-BINDING CASSETTE TRANSPORTERS that actively transport organic substrates. Although considered organic anion transporters, a subset of proteins in this family have also been shown to convey drug resistance to neutral organic drugs. Their cellular function may have clinical significance for CHEMOTHERAPY in that they transport a variety of ANTINEOPLASTIC AGENTS. Overexpression of proteins in this class by NEOPLASMS is considered a possible mechanism in the development of multidrug resistance (DRUG RESISTANCE, MULTIPLE). Although similar in function to P-GLYCOPROTEINS, the proteins in this class share little sequence homology to the p-glycoprotein family of proteins.Organic Anion Transporters, ATP-Dependent: A subclass of ORGANIC ANION TRANSPORTERS whose transport of organic anions is linked directly to the hydrolysis of ATP. The subclass includes those ATP-BINDING CASSETTE TRANSPORTERS that transport organic ions.Carrier Proteins: Transport proteins that carry specific substances in the blood or across cell membranes.ATP-Binding Cassette Transporters: A family of MEMBRANE TRANSPORT PROTEINS that require ATP hydrolysis for the transport of substrates across membranes. The protein family derives its name from the ATP-binding domain found on the protein.GlutaratesKidney: Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.Taurocholic Acid: The product of conjugation of cholic acid with taurine. Its sodium salt is the chief ingredient of the bile of carnivorous animals. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as a cholagogue and cholerectic.Kidney Tubules, Proximal: The renal tubule portion that extends from the BOWMAN CAPSULE in the KIDNEY CORTEX into the KIDNEY MEDULLA. The proximal tubule consists of a convoluted proximal segment in the cortex, and a distal straight segment descending into the medulla where it forms the U-shaped LOOP OF HENLE.Membrane Transport Proteins: Membrane proteins whose primary function is to facilitate the transport of molecules across a biological membrane. Included in this broad category are proteins involved in active transport (BIOLOGICAL TRANSPORT, ACTIVE), facilitated transport and ION CHANNELS.Dicarboxylic AcidsXenopus laevis: The commonest and widest ranging species of the clawed "frog" (Xenopus) in Africa. This species is used extensively in research. There is now a significant population in California derived from escaped laboratory animals.Dicarboxylic Acid Transporters: A family of organic anion transporters that specifically transport DICARBOXYLIC ACIDS such as alpha-ketoglutaric acid across cellular membranes.RNA, Complementary: Synthetic transcripts of a specific DNA molecule or fragment, made by an in vitro transcription system. This cRNA can be labeled with radioactive uracil and then used as a probe. (King & Stansfield, A Dictionary of Genetics, 4th ed)Unithiol: A chelating agent used as an antidote to heavy metal poisoning.Bile Canaliculi: Minute intercellular channels that occur between liver cells and carry bile towards interlobar bile ducts. Also called bile capillaries.Phenolsulfonphthalein: Red dye, pH indicator, and diagnostic aid for determination of renal function. It is used also for studies of the gastrointestinal and other systems.Sodium-Phosphate Cotransporter Proteins, Type I: A family of sodium-phosphate cotransporter proteins that also transport organic ANIONS. They are low affinity phosphate transporters.Oocytes: Female germ cells derived from OOGONIA and termed OOCYTES when they enter MEIOSIS. The primary oocytes begin meiosis but are arrested at the diplotene state until OVULATION at PUBERTY to give rise to haploid secondary oocytes or ova (OVUM).Choroid Plexus: A villous structure of tangled masses of BLOOD VESSELS contained within the third, lateral, and fourth ventricles of the BRAIN. It regulates part of the production and composition of CEREBROSPINAL FLUID.Renal Agents: Drugs used for their effects on the kidneys' regulation of body fluid composition and volume. The most commonly used are the diuretics. Also included are drugs used for their antidiuretic and uricosuric actions, for their effects on the kidneys' clearance of other drugs, and for diagnosis of renal function.Organic Cation Transporter 1: An organic cation transporter found in kidney. It is localized to the basal lateral membrane and is likely to be involved in the renal secretion of organic cations.Leukotriene C4: The conjugation product of LEUKOTRIENE A4 and glutathione. It is the major arachidonic acid metabolite in macrophages and human mast cells as well as in antigen-sensitized lung tissue. It stimulates mucus secretion in the lung, and produces contractions of nonvascular and some VASCULAR SMOOTH MUSCLE. (From Dictionary of Prostaglandins and Related Compounds, 1990)Symporters: Membrane transporters that co-transport two or more dissimilar molecules in the same direction across a membrane. Usually the transport of one ion or molecule is against its electrochemical gradient and is "powered" by the movement of another ion or molecule with its electrochemical gradient.Hyperbilirubinemia, Hereditary: Inborn errors of bilirubin metabolism resulting in excessive amounts of bilirubin in the circulating blood, either because of increased bilirubin production or because of delayed clearance of bilirubin from the blood.Biological Transport, Active: The movement of materials across cell membranes and epithelial layers against an electrochemical gradient, requiring the expenditure of metabolic energy.LLC-PK1 Cells: Epithelial cell line originally derived from porcine kidneys. It is used for pharmacologic and metabolic studies.Indican: A substance occurring in the urine of mammals and also in blood plasma as the normal metabolite of tryptophan. An increased urinary excretion of indican is seen in Hartnup disease from the bacterial degradation of unabsorbed tryptophan.Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.Hyperbilirubinemia: A condition characterized by an abnormal increase of BILIRUBIN in the blood, which may result in JAUNDICE. Bilirubin, a breakdown product of HEME, is normally excreted in the BILE or further catabolized before excretion in the urine.2,4-Dichlorophenoxyacetic Acid: An herbicide with irritant effects on the eye and the gastrointestinal system.Sulfinpyrazone: A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties.Iodopyracet: An ionic monomeric contrast medium that was formerly used for a variety of diagnostic procedures. (From Martindale, The Extra Pharmacopoeia, 30th ed, p706)Catecholamine Plasma Membrane Transport Proteins: A group of membrane transport proteins that transport biogenic amine derivatives of catechol across the PLASMA MEMBRANE. Catecholamine plasma membrane transporter proteins regulate neural transmission as well as catecholamine metabolism and recycling.Cefotiam: One of the CEPHALOSPORINS that has a broad spectrum of activity against both gram-positive and gram-negative microorganisms.Flounder: Common name for two families of FLATFISHES belonging to the order Pleuronectiformes: left-eye flounders (Bothidae) and right-eye flounders (Pleuronectidae). The latter is more commonly used in research.Kinetics: The rate dynamics in chemical or physical systems.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Jaundice, Chronic Idiopathic: A benign, autosomally recessive inherited hyperbilirubinemia characterized by the presence of a dark pigment in the centrilobular region of the liver cells. There is a functional defect in biliary excretion of bilirubin, cholephilic dyes, and porphyrins. Affected persons may be asymptomatic or have vague constitutional or gastrointestinal symptoms. The liver may be slightly enlarged, and oral and intravenous cholangiography fails to visualize the biliary tract.Ion Transport: The movement of ions across energy-transducing cell membranes. Transport can be active, passive or facilitated. Ions may travel by themselves (uniport), or as a group of two or more ions in the same (symport) or opposite (antiport) directions.Methotrexate: An antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of TETRAHYDROFOLATE DEHYDROGENASE and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA.Liver: A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.Mercury Isotopes: Stable mercury atoms that have the same atomic number as the element mercury, but differ in atomic weight. Hg-196, 198-201, and 204 are stable mercury isotopes.Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.Rats, Mutant Strains: Rats bearing mutant genes which are phenotypically expressed in the animals.Dehydroepiandrosterone Sulfate: The circulating form of a major C19 steroid produced primarily by the ADRENAL CORTEX. DHEA sulfate serves as a precursor for TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE.Rats, Sprague-Dawley: A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.Cell Membrane: The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Rats, Inbred LEC: A cinnamon-colored strain of Long-Evans rats which carries a mutation causing fulminant hepatitis and jaundice, with an associated gross accumulation of copper in the liver. This strain is a model for Wilson's Disease (see HEPATOLENTICULAR DEGENERATION).P-Glycoprotein: A 170-kDa transmembrane glycoprotein from the superfamily of ATP-BINDING CASSETTE TRANSPORTERS. It serves as an ATP-dependent efflux pump for a variety of chemicals, including many ANTINEOPLASTIC AGENTS. Overexpression of this glycoprotein is associated with multidrug resistance (see DRUG RESISTANCE, MULTIPLE).RNA, Messenger: RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.Tissue Distribution: Accumulation of a drug or chemical substance in various organs (including those not relevant to its pharmacologic or therapeutic action). This distribution depends on the blood flow or perfusion rate of the organ, the ability of the drug to penetrate organ membranes, tissue specificity, protein binding. The distribution is usually expressed as tissue to plasma ratios.Amino Acid Sequence: The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.Bile: An emulsifying agent produced in the LIVER and secreted into the DUODENUM. Its composition includes BILE ACIDS AND SALTS; CHOLESTEROL; and ELECTROLYTES. It aids DIGESTION of fats in the duodenum.Cephaloridine: A cephalosporin antibiotic.DNA, Complementary: Single-stranded complementary DNA synthesized from an RNA template by the action of RNA-dependent DNA polymerase. cDNA (i.e., complementary DNA, not circular DNA, not C-DNA) is used in a variety of molecular cloning experiments as well as serving as a specific hybridization probe.Sulfuric Acid Esters: Organic esters of sulfuric acid.Pharmaceutical Preparations: Drugs intended for human or veterinary use, presented in their finished dosage form. Included here are materials used in the preparation and/or formulation of the finished dosage form.Aminopterin: A folic acid derivative used as a rodenticide that has been shown to be teratogenic.Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).Transfection: The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.Stevia: A plant genus of the family ASTERACEAE. Members contain stevioside and other sweet diterpene glycosides. The leaf is used for sweetening (SWEETENING AGENTS).Glutathione: A tripeptide with many roles in cells. It conjugates to drugs to make them more soluble for excretion, is a cofactor for some enzymes, is involved in protein disulfide bond rearrangement and reduces peroxides.Biotinylation: Incorporation of biotinyl groups into molecules.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Physiological Processes: The functions and activities of living organisms that support life in single- or multi-cellular organisms from their origin through the progression of life.Uric Acid: An oxidation product, via XANTHINE OXIDASE, of oxypurines such as XANTHINE and HYPOXANTHINE. It is the final oxidation product of purine catabolism in humans and primates, whereas in most other mammals URATE OXIDASE further oxidizes it to ALLANTOIN.P-Glycoproteins: A subfamily of transmembrane proteins from the superfamily of ATP-BINDING CASSETTE TRANSPORTERS that are closely related in sequence to P-GLYCOPROTEIN. When overexpressed, they function as ATP-dependent efflux pumps able to extrude lipophilic drugs, especially ANTINEOPLASTIC AGENTS, from cells causing multidrug resistance (DRUG RESISTANCE, MULTIPLE). Although P-Glycoproteins share functional similarities to MULTIDRUG RESISTANCE-ASSOCIATED PROTEINS they are two distinct subclasses of ATP-BINDING CASSETTE TRANSPORTERS, and have little sequence homology.Liddle Syndrome: Familial pseudoaldosteronism characterized by autosomal dominant inheritance of hypertension with HYPOKALEMIA; ALKALOSIS; RENIN and ALDOSTERONE level decreases. It is caused by mutations in EPITHELIAL SODIUM CHANNELS beta and gamma subunits. Different mutations in the same EPITHELIAL SODIUM CHANNELS subunits can cause PSEUDOHYPOALDOSTERONISM, TYPE I, AUTOSOMAL DOMINANT.Antiporters: Membrane transporters that co-transport two or more dissimilar molecules in the opposite direction across a membrane. Usually the transport of one ion or molecule is against its electrochemical gradient and is "powered" by the movement of another ion or molecule with its electrochemical gradient.XanthurenatesCloning, Molecular: The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.Hepatocytes: The main structural component of the LIVER. They are specialized EPITHELIAL CELLS that are organized into interconnected plates called lobules.Salicylates: The salts or esters of salicylic acids, or salicylate esters of an organic acid. Some of these have analgesic, antipyretic, and anti-inflammatory activities by inhibiting prostaglandin synthesis.Ketoglutaric Acids: A family of compounds containing an oxo group with the general structure of 1,5-pentanedioic acid. (From Lehninger, Principles of Biochemistry, 1982, p442)Propionates: Derivatives of propionic acid. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the carboxyethane structure.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Blood-Brain Barrier: Specialized non-fenestrated tightly-joined ENDOTHELIAL CELLS with TIGHT JUNCTIONS that form a transport barrier for certain substances between the cerebral capillaries and the BRAIN tissue.Substrate Specificity: A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.Drug Resistance, Multiple: Simultaneous resistance to several structurally and functionally distinct drugs.COS Cells: CELL LINES derived from the CV-1 cell line by transformation with a replication origin defective mutant of SV40 VIRUS, which codes for wild type large T antigen (ANTIGENS, POLYOMAVIRUS TRANSFORMING). They are used for transfection and cloning. (The CV-1 cell line was derived from the kidney of an adult male African green monkey (CERCOPITHECUS AETHIOPS).)Bile Acids and Salts: Steroid acids and salts. The primary bile acids are derived from cholesterol in the liver and usually conjugated with glycine or taurine. The secondary bile acids are further modified by bacteria in the intestine. They play an important role in the digestion and absorption of fat. They have also been used pharmacologically, especially in the treatment of gallstones.Cyclic P-OxidesXenobiotics: Chemical substances that are foreign to the biological system. They include naturally occurring compounds, drugs, environmental agents, carcinogens, insecticides, etc.Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.Biliary Tract: The BILE DUCTS and the GALLBLADDER.Cells, Cultured: Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.Xenopus: An aquatic genus of the family, Pipidae, occurring in Africa and distinguished by having black horny claws on three inner hind toes.Anion Exchange Protein 1, Erythrocyte: A major integral transmembrane protein of the ERYTHROCYTE MEMBRANE. It is the anion exchanger responsible for electroneutral transporting in CHLORIDE IONS in exchange of BICARBONATE IONS allowing CO2 uptake and transport from tissues to lungs by the red blood cells. Genetic mutations that result in a loss of the protein function have been associated with type 4 HEREDITARY SPHEROCYTOSIS.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Blotting, Northern: Detection of RNA that has been electrophoretically separated and immobilized by blotting on nitrocellulose or other type of paper or nylon membrane followed by hybridization with labeled NUCLEIC ACID PROBES.Kidney Cortex: The outer zone of the KIDNEY, beneath the capsule, consisting of KIDNEY GLOMERULUS; KIDNEY TUBULES, DISTAL; and KIDNEY TUBULES, PROXIMAL.Pharmacokinetics: Dynamic and kinetic mechanisms of exogenous chemical and DRUG LIBERATION; ABSORPTION; BIOLOGICAL TRANSPORT; TISSUE DISTRIBUTION; BIOTRANSFORMATION; elimination; and DRUG TOXICITY as a function of dosage, and rate of METABOLISM. LADMER, ADME and ADMET are abbreviations for liberation, absorption, distribution, metabolism, elimination, and toxicology.Kidney Tubules: Long convoluted tubules in the nephrons. They collect filtrate from blood passing through the KIDNEY GLOMERULUS and process this filtrate into URINE. Each renal tubule consists of a BOWMAN CAPSULE; PROXIMAL KIDNEY TUBULE; LOOP OF HENLE; DISTAL KIDNEY TUBULE; and KIDNEY COLLECTING DUCT leading to the central cavity of the kidney (KIDNEY PELVIS) that connects to the URETER.Membrane Proteins: Proteins which are found in membranes including cellular and intracellular membranes. They consist of two types, peripheral and integral proteins. They include most membrane-associated enzymes, antigenic proteins, transport proteins, and drug, hormone, and lectin receptors.Adenosine Triphosphate: An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter.Dogs: The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)Glucuronides: Glycosides of GLUCURONIC ACID formed by the reaction of URIDINE DIPHOSPHATE GLUCURONIC ACID with certain endogenous and exogenous substances. Their formation is important for the detoxification of drugs, steroid excretion and BILIRUBIN metabolism to a more water-soluble compound that can be eliminated in the URINE and BILE.Chlorides: Inorganic compounds derived from hydrochloric acid that contain the Cl- ion.TritiumToxins, Biological: Specific, characterizable, poisonous chemicals, often PROTEINS, with specific biological properties, including immunogenicity, produced by microbes, higher plants (PLANTS, TOXIC), or ANIMALS.Sequence Homology, Amino Acid: The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.Reverse Transcriptase Polymerase Chain Reaction: A variation of the PCR technique in which cDNA is made from RNA via reverse transcription. The resultant cDNA is then amplified using standard PCR protocols.Base Sequence: The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.Monocarboxylic Acid Transporters: A family of proteins involved in the transport of monocarboxylic acids such as LACTIC ACID and PYRUVIC ACID across cellular membranes.Blotting, Western: Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.Glucose Transporter Type 1: A ubiquitously expressed glucose transporter that is important for constitutive, basal GLUCOSE transport. It is predominately expressed in ENDOTHELIAL CELLS and ERYTHROCYTES at the BLOOD-BRAIN BARRIER and is responsible for GLUCOSE entry into the BRAIN.CHO Cells: CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.Cholestasis: Impairment of bile flow due to obstruction in small bile ducts (INTRAHEPATIC CHOLESTASIS) or obstruction in large bile ducts (EXTRAHEPATIC CHOLESTASIS).Organophosphonates: Carbon-containing phosphonic acid compounds. Included under this heading are compounds that have carbon bound to either OXYGEN atom or the PHOSPHOROUS atom of the (P=O)O2 structure.Sodium: A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23.HEK293 Cells: A cell line generated from human embryonic kidney cells that were transformed with human adenovirus type 5.Folic Acid Antagonists: Inhibitors of the enzyme, dihydrofolate reductase (TETRAHYDROFOLATE DEHYDROGENASE), which converts dihydrofolate (FH2) to tetrahydrofolate (FH4). They are frequently used in cancer chemotherapy. (From AMA, Drug Evaluations Annual, 1994, p2033)Bilirubin: A bile pigment that is a degradation product of HEME.Chloride-Bicarbonate Antiporters: Electroneutral chloride bicarbonate exchangers that allow the exchange of BICARBONATE IONS exchange for CHLORIDE IONS across the cellular membrane. The action of specific antiporters in this class serve important functions such as allowing the efficient exchange of bicarbonate across red blood cell membranes as they passage through capillaries and the reabsorption of bicarbonate ions by the kidney.Immunohistochemistry: Histochemical localization of immunoreactive substances using labeled antibodies as reagents.Monosaccharide Transport Proteins: A large group of membrane transport proteins that shuttle MONOSACCHARIDES across CELL MEMBRANES.Serotonin Plasma Membrane Transport Proteins: Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of serotonergic neurons. They are different than SEROTONIN RECEPTORS, which signal cellular responses to SEROTONIN. They remove SEROTONIN from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS. Regulates signal amplitude and duration at serotonergic synapses and is the site of action of the SEROTONIN UPTAKE INHIBITORS.Hepatocyte Nuclear Factor 1-alpha: Hepatocyte nuclear factor 1-alpha is a transcription factor found in the LIVER; PANCREAS; and KIDNEY that regulates HOMEOSTASIS of GLUCOSE.4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid: An inhibitor of anion conductance including band 3-mediated anion transport.Gene Expression Regulation: Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.Mice, Knockout: Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.Metabolic Clearance Rate: Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site.Dopamine Plasma Membrane Transport Proteins: Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of dopaminergic neurons. They remove DOPAMINE from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS and are the target of DOPAMINE UPTAKE INHIBITORS.Cercopithecus aethiops: A species of CERCOPITHECUS containing three subspecies: C. tantalus, C. pygerythrus, and C. sabeus. They are found in the forests and savannah of Africa. The African green monkey (C. pygerythrus) is the natural host of SIMIAN IMMUNODEFICIENCY VIRUS and is used in AIDS research.Histamine H2 Antagonists: Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.Adenine: A purine base and a fundamental unit of ADENINE NUCLEOTIDES.Immunoblotting: Immunologic method used for detecting or quantifying immunoreactive substances. The substance is identified by first immobilizing it by blotting onto a membrane and then tagging it with labeled antibodies.Mercury: A silver metallic element that exists as a liquid at room temperature. It has the atomic symbol Hg (from hydrargyrum, liquid silver), atomic number 80, and atomic weight 200.59. Mercury is used in many industrial applications and its salts have been employed therapeutically as purgatives, antisyphilitics, disinfectants, and astringents. It can be absorbed through the skin and mucous membranes which leads to MERCURY POISONING. Because of its toxicity, the clinical use of mercury and mercurials is diminishing.Cricetulus: A genus of the family Muridae consisting of eleven species. C. migratorius, the grey or Armenian hamster, and C. griseus, the Chinese hamster, are the two species used in biomedical research.Gene Expression: The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.Recombinant Proteins: Proteins prepared by recombinant DNA technology.Excitatory Amino Acid Transporter 2: A glutamate plasma membrane transporter protein found in ASTROCYTES and in the LIVER.Protein Binding: The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.Carbon Radioisotopes: Unstable isotopes of carbon that decay or disintegrate emitting radiation. C atoms with atomic weights 10, 11, and 14-16 are radioactive carbon isotopes.Sulfates: Inorganic salts of sulfuric acid.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.Mutagenesis, Site-Directed: Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.Diuretics: Agents that promote the excretion of urine through their effects on kidney function.QuinolinesExcitatory Amino Acid Transporter 3: A neuronal and epithelial type glutamate plasma membrane transporter protein.Bicarbonates: Inorganic salts that contain the -HCO3 radical. They are an important factor in determining the pH of the blood and the concentration of bicarbonate ions is regulated by the kidney. Levels in the blood are an index of the alkali reserve or buffering capacity.Killifishes: Small oviparous fishes in the family Cyprinodontidae, usually striped or barred black. They are much used in mosquito control.Amino Acid Transport System X-AG: A family of POTASSIUM and SODIUM-dependent acidic amino acid transporters that demonstrate a high affinity for GLUTAMIC ACID and ASPARTIC ACID. Several variants of this system are found in neuronal tissue.Models, Biological: Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment.DNA Primers: Short sequences (generally about 10 base pairs) of DNA that are complementary to sequences of messenger RNA and allow reverse transcriptases to start copying the adjacent sequences of mRNA. Primers are used extensively in genetic and molecular biology techniques.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Hydrogen-Ion Concentration: The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH = log 1/2[1/(H+)], where (H+) is the hydrogen ion concentration in gram equivalents per liter of solution. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)Microinjections: The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.Excitatory Amino Acid Transporter 1: A glial type glutamate plasma membrane transporter protein found predominately in ASTROCYTES. It is also expressed in HEART and SKELETAL MUSCLE and in the PLACENTA.Isoquinolines: A group of compounds with the heterocyclic ring structure of benzo(c)pyridine. The ring structure is characteristic of the group of opium alkaloids such as papaverine. (From Stedman, 25th ed)Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.Molecular Structure: The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.Norepinephrine Plasma Membrane Transport Proteins: Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of noradrenergic neurons. They remove NOREPINEPHRINE from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS. It regulates signal amplitude and duration at noradrenergic synapses and is the target of ADRENERGIC UPTAKE INHIBITORS.Brain: The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.Amino Acid Substitution: The naturally occurring or experimentally induced replacement of one or more AMINO ACIDS in a protein with another. If a functionally equivalent amino acid is substituted, the protein may retain wild-type activity. Substitution may also diminish, enhance, or eliminate protein function. Experimentally induced substitution is often used to study enzyme activities and binding site properties.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Carboxylic Acids: Organic compounds containing the carboxy group (-COOH). This group of compounds includes amino acids and fatty acids. Carboxylic acids can be saturated, unsaturated, or aromatic.Fluorescent Dyes: Agents that emit light after excitation by light. The wave length of the emitted light is usually longer than that of the incident light. Fluorochromes are substances that cause fluorescence in other substances, i.e., dyes used to mark or label other compounds with fluorescent tags.Cation Transport Proteins: Membrane proteins whose primary function is to facilitate the transport of positively charged molecules (cations) across a biological membrane.Glycocholic Acid: The glycine conjugate of CHOLIC ACID. It acts as a detergent to solubilize fats for absorption and is itself absorbed.Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Cations: Positively charged atoms, radicals or groups of atoms which travel to the cathode or negative pole during electrolysis.Amino Acid Transport Systems: Cellular proteins and protein complexes that transport amino acids across biological membranes.Fluorescein: A phthalic indicator dye that appears yellow-green in normal tear film and bright green in a more alkaline medium such as the aqueous humor.Glucose Transporter Type 3: A major glucose transporter found in NEURONS.GABA Plasma Membrane Transport Proteins: A family of plasma membrane neurotransmitter transporter proteins that regulates extracellular levels of the inhibitory neurotransmitter GAMMA-AMINOBUTYRIC ACID. They differ from GABA RECEPTORS, which signal cellular responses to GAMMA-AMINOBUTYRIC ACID. They control GABA reuptake into PRESYNAPTIC TERMINALS in the CENTRAL NERVOUS SYSTEM through high-affinity sodium-dependent transport.Sex Characteristics: Those characteristics that distinguish one SEX from the other. The primary sex characteristics are the OVARIES and TESTES and their related hormones. Secondary sex characteristics are those which are masculine or feminine but not directly related to reproduction.Amino Acid Transport Systems, Neutral: Amino acid transporter systems capable of transporting neutral amino acids (AMINO ACIDS, NEUTRAL).Epithelial Cells: Cells that line the inner and outer surfaces of the body by forming cellular layers (EPITHELIUM) or masses. Epithelial cells lining the SKIN; the MOUTH; the NOSE; and the ANAL CANAL derive from ectoderm; those lining the RESPIRATORY SYSTEM and the DIGESTIVE SYSTEM derive from endoderm; others (CARDIOVASCULAR SYSTEM and LYMPHATIC SYSTEM) derive from mesoderm. Epithelial cells can be classified mainly by cell shape and function into squamous, glandular and transitional epithelial cells.Anti-Inflammatory Agents, Non-Steroidal: Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions.They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects.Microvilli: Minute projections of cell membranes which greatly increase the surface area of the cell.Rabbits: The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.Glucose Transporter Type 4: A glucose transport protein found in mature MUSCLE CELLS and ADIPOCYTES. It promotes transport of glucose from the BLOOD into target TISSUES. The inactive form of the protein is localized in CYTOPLASMIC VESICLES. In response to INSULIN, it is translocated to the PLASMA MEMBRANE where it facilitates glucose uptake.Fluoresceins: A family of spiro(isobenzofuran-1(3H),9'-(9H)xanthen)-3-one derivatives. These are used as dyes, as indicators for various metals, and as fluorescent labels in immunoassays.Caco-2 Cells: Human colonic ADENOCARCINOMA cells that are able to express differentiation features characteristic of mature intestinal cells, such as ENTEROCYTES. These cells are valuable in vitro tools for studies related to intestinal cell function and differentiation.Antiviral Agents: Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly.Membrane Transport Modulators: Agents that affect ION PUMPS; ION CHANNELS; ABC TRANSPORTERS; and other MEMBRANE TRANSPORT PROTEINS.Chromatography, High Pressure Liquid: Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.Glycosylation: The chemical or biochemical addition of carbohydrate or glycosyl groups to other chemicals, especially peptides or proteins. Glycosyl transferases are used in this biochemical reaction.Swine: Any of various animals that constitute the family Suidae and comprise stout-bodied, short-legged omnivorous mammals with thick skin, usually covered with coarse bristles, a rather long mobile snout, and small tail. Included are the genera Babyrousa, Phacochoerus (wart hogs), and Sus, the latter containing the domestic pig (see SUS SCROFA).Mice, Inbred C57BLMalpighian Tubules: Slender tubular or hairlike excretory structures found in insects. They emerge from the alimentary canal between the mesenteron (midgut) and the proctodeum (hindgut).Estradiol: The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids.Glucose Transporter Type 2: A glucose transport facilitator that is expressed primarily in PANCREATIC BETA CELLS; LIVER; and KIDNEYS. It may function as a GLUCOSE sensor to regulate INSULIN release and glucose HOMEOSTASIS.Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666)

LeProT1, a transporter for proline, glycine betaine, and gamma-amino butyric acid in tomato pollen. (1/946)

During maturation, pollen undergoes a period of dehydration accompanied by the accumulation of compatible solutes. Solute import across the pollen plasma membrane, which occurs via proteinaceous transporters, is required to support pollen development and also for subsequent germination and pollen tube growth. Analysis of the free amino acid composition of various tissues in tomato revealed that the proline content in flowers was 60 times higher than in any other organ analyzed. Within the floral organs, proline was confined predominantly to pollen, where it represented >70% of total free amino acids. Uptake experiments demonstrated that mature as well as germinated pollen rapidly take up proline. To identify proline transporters in tomato pollen, we isolated genes homologous to Arabidopsis proline transporters. LeProT1 was specifically expressed both in mature and germinating pollen, as demonstrated by RNA in situ hybridization. Expression in a yeast mutant demonstrated that LeProT1 transports proline and gamma-amino butyric acid with low affinity and glycine betaine with high affinity. Direct uptake and competition studies demonstrate that LeProT1 constitutes a general transporter for compatible solutes.  (+info)

Cloning and functional characterization of a new multispecific organic anion transporter, OAT-K2, in rat kidney. (2/946)

We have isolated a cDNA coding a new organic anion transporter, OAT-K2, expressed specifically in rat kidney. The OAT-K2 cDNA had an open reading frame encoding a 498-amino acid protein (calculated molecular mass of 55 kDa) that shows 91% identity with the rat kidney-specific organic anion transporter, OAT-K1. Reverse transcription-coupled polymerase chain reaction analyses revealed that the OAT-K2 mRNA was expressed predominantly in the proximal convoluted tubules, proximal straight tubules, and cortical collecting ducts. When expressed in Xenopus oocytes, OAT-K2 stimulated the uptake of hydrophobic organic anions, such as taurocholate, methotrexate, folate, and prostaglandin E2, although its homolog OAT-K1 transported methotrexate and folate, but not taurocholate and prostaglandin E2. In MDCK cells stably transfected with the OAT-K1 and OAT-K2 cDNAs, each transporter was localized functionally to the apical membranes and showed transport activity similar to that in the oocyte. Moreover, the efflux of preloaded taurocholate was also enhanced across the apical membrane in OAT-K2 transfectant. The taurocholate transport by OAT-K2-expressing cells showed saturability (Km = 10.3 microM). Several organic anions, bile acids, cardiac glycosides, and steroids had potent inhibitory effects on the OAT-K2-mediated taurocholate transport in the transfectant. These findings suggest that the OAT-K2 participates in epithelial transport of hydrophobic anionic compounds in the kidney.  (+info)

Muscle contractile activity increases fatty acid metabolism and transport and FAT/CD36. (3/946)

We have examined whether 1) fatty acid (FA) uptake, 2) FA transporter expression, and 3) FA metabolism are increased when the oxidative capacity of skeletal muscle is increased. The oxidative capacities of red and white tibialis anterior and extensor digitorum longus muscles were increased via chronic stimulation (10 Hz, 24 h/day for 7 days). The contralateral muscles served as controls. After 7 days of increased muscle activity 1) palmitate uptake by giant sarcolemmal vesicles was increased twofold (P < 0.05), 2) the expression of FA translocase (FAT)/CD36 was increased at both the mRNA (3.2- to 10-fold) and protein (3.4-fold) levels, and 3) palmitate oxidation and esterification into triacylglycerols and phospholipids were increased 1.5-, 2.7-, and 1.7-fold, respectively (P < 0.05). These data show that when the oxidative capacity of muscle is increased, there is a parallel increase in the rate of FA transport and FA transporters at the sarcolemmal membrane, which is associated with the enhanced expression of the membrane transporter FAT/CD36.  (+info)

Identification of the amine-polyamine-choline transporter superfamily 'consensus amphipathic region' as the target for inactivation of the Escherichia coli GABA transporter GabP by thiol modification reagents. Role of Cys-300 in restoring thiol sensitivity to Gabp lacking Cys. (4/946)

The Escherichia coli gamma-aminobutyric acid transporter GabP (gab permease) contains a functionally significant cysteine residue (Cys-300) within its consensus amphipathic region (CAR), a putative channel-forming structure that extends out of transmembrane helix 8 and into the adjoining cytoplasmic loop 8-9 of transporters from the amine-polyamine-choline (APC) superfamily. Here we show that of the five cysteine residues (positions 158, 251, 291, 300 and 443) in the E. coli GabP, Cys-300 is the one that renders the transport activity sensitive to inhibition by thiol modification reagents: whereas substituting Ala for Cys-300 mimics the inhibitory effect of thiol modification, substituting Ala at position 158, 251, 291 or 443 preserves robust transport activity and confers no resistance to thiol inactivation; and whereas the robustly active Cys-300 single-Cys mutant is fully sensitive to thiol modification, other single-Cys mutants (Cys at 158, 251, 291 or 443) exhibit kinetically compromised transport activities that resist further chemical inactivation by thiol reagents. The present study reveals additionally that Cys-300 exhibits (1) sensitivity to hydrophobic thiol reagents, (2) general resistance to bulky (fluorescein 5-maleimide) and/or charged {2-sulphonatoethyl methanethiosulphonate or [2-(trimethylammonium)ethyl] methanethiosulphonate} thiol reagents and (3) a peculiar sensitivity to p-chloromercuribenzenesulphonate (PCMBS). The accessibility of PCMBS to Cys-300 (located midway through the lipid bilayer) might be related to the structural similarity that it shares with guvacine (1, 2,3,6-tetrahydro-3-pyridinecarboxylic acid), a transported GabP substrate. These structural requirements for thiol sensitivity provide the first chemical evidence consistent with channel-like access to the polar surface of the CAR, a physical configuration that might provide a basis for understanding how this region impacts the function of APC transporters generally [Closs, Lyons, Kelly and Cunningham (1993) J. Biol. Chem. 268, 20796-20800] and the gab permease particularly [Hu and King (1998) Biochem. J. 300, 771-776].  (+info)

PDZ-mediated interactions retain the epithelial GABA transporter on the basolateral surface of polarized epithelial cells. (5/946)

The PDZ target motifs located in the C-terminal end of many receptors and ion channels mediate protein-protein interactions by binding to specific PDZ-containing proteins. These interactions are involved in the localization of surface proteins on specialized membrane domains of neuronal and epithelial cells. However, the molecular mechanism responsible for this PDZ protein-dependent polarized localization is still unclear. This study first demonstrated that the epithelial gamma-aminobutyric acid (GABA) transporter (BGT-1) contains a PDZ target motif that mediates the interaction with the PDZ protein LIN-7 in Madin-Darby canine kidney (MDCK) cells, and then investigated the role of this interaction in the basolateral localization of the transporter. It was found that although the transporters from which the PDZ target motif was deleted were still targeted to the basolateral surface, they were not retained but internalized in an endosomal recycling compartment. Furthermore, an interfering BGT peptide determined the intracellular relocation of the native transporter. These data indicate that interactions with PDZ proteins determine the polarized surface localization of target proteins by means of retention and not targeting mechanisms. PDZ proteins may, therefore, act as a sort of membrane protein sorting machinery which, by recognizing retention signals (the PDZ target sequences), prevents protein internalization.  (+info)

Multiple G protein-coupled receptors initiate protein kinase C redistribution of GABA transporters in hippocampal neurons. (6/946)

Neurotransmitter transporters function in synaptic signaling in part through the sequestration and removal of neurotransmitter from the synaptic cleft. A recurring theme of transporters is that many can be functionally regulated by protein kinase C (PKC); some of this regulation occurs via a redistribution of the transporter protein between the plasma membrane and the cytoplasm. The endogenous triggers that lead to PKC-mediated transporter redistribution have not been elucidated. G-protein-coupled receptors that activate PKC are likely candidates to initiate transporter redistribution. We tested this hypothesis by examining the rat brain GABA transporter GAT1 endogenously expressed in hippocampal neurons. Specific agonists of G-protein-coupled acetylcholine, glutamate, and serotonin receptors downregulate GAT1 function. This functional inhibition is dose-dependent, mimicked by PKC activators, and prevented by specific receptor antagonists and PKC inhibitors. Surface biotinylation experiments show that the receptor-mediated functional inhibition correlates with a redistribution of GAT1 from the plasma membrane to intracellular locations. These data demonstrate (1) that endogenous GAT1 function can be regulated by PKC via subcellular redistribution, and (2) that signaling via several different G-protein-coupled receptors can mediate this effect. These results raise the possibility that some effects of G-protein-mediated alterations in synaptic signaling might occur through changes in the number of transporters expressed on the plasma membrane and subsequent effects on synaptic neurotransmitter levels.  (+info)

Protein-mediated palmitate uptake and expression of fatty acid transport proteins in heart giant vesicles. (7/946)

Giant sarcolemmal vesicles were isolated from rat heart and hindlimb muscles for a) characterization of long-chain fatty acid transport in the absence of metabolism and b) comparison of fatty acid transport protein expression with fatty acid transport. Giant vesicles contained cytosolic fatty acid binding protein. Palmitate uptake was completely divorced from its metabolism. All palmitate taken up was recovered in the intravesicular cytosol as unesterified FA. Palmitate uptake by heart vesicles exhibited a K m of 9.7 nm, similar to that of muscle (K m = 9.7 nm). Vmax (2.7 pmol/mg protein/s) in heart was 8-fold higher than in muscle (0.34 pmol/mg protein/s). Palmitate uptake was inhibited in heart (55-80%) and muscle (31-50%) by trypsin, phloretin, sulfo-N-succinimidyloleate (SSO), or a polyclonal antiserum against the 40 kDa plasma membrane fatty acid binding protein (FABPpm). Palmitate uptake by heart and by red and white muscle vesicles correlated well with the expression of fatty acid translocase (FAT/CD36) and fatty acid binding protein FABPpm, which may act in concert. The expression of fatty acid transport protein (FATP), was 10-fold lower in heart vesicles than in white muscle vesicles. It is concluded that long-chain fatty acid uptake by heart and muscle vesicles is largely protein-mediated, involving FAT/CD36 and FABPpm. The role of FATP in muscle and heart remains uncertain.  (+info)

Passive water and ion transport by cotransporters. (8/946)

1. The rabbit Na+-glucose (SGLT1) and the human Na+-Cl--GABA (GAT1) cotransporters were expressed in Xenopus laevis oocytes, and passive Na+ and water transport were studied using electrical and optical techniques. Passive water permeabilities (Lp) of the cotransporters were determined from the changes in oocyte volume in response to osmotic gradients. The specific SGLT1 and GAT1 Lp values were obtained by measuring Lp in the presence and absence of blockers (phlorizin and SKF89976A). In the presence of the blockers, the Lp values of oocytes expressing SGLT1 and GAT1 were indistinguishable from the Lp of control oocytes. Passive Na+ transport (Na+ leak) was obtained from the blocker-sensitive Na+ currents in the absence of substrates (glucose and GABA). 2. Passive Na+ and water transport through SGLT1 were blocked by phlorizin with the same sensitivity (inhibitory constant (Ki), 3-5 microM). When Na+ was replaced with Li+, phlorizin also inhibited Li+ and water transport, but with a lower affinity (Ki, 100 microM). When Na+ was replaced by choline, which is not transported, the SGLT1 Lp was indistinguishable from that in Na+ or Li+, but in this case water transport was less sensitive to phlorizin. 3. The activation energies (Ea) for passive Na+ and water transport through SGLT1 were 21 and 5 kcal mol-1, respectively. The high Ea for Na+ transport is comparable to that of Na+-glucose cotransport and indicates that the process is dependent on conformational changes of the protein, while the low Ea for water transport is similar to that of water channels (aquaporins). 4. GAT1 also behaved as an SKF89976A-sensitive water channel. We did not observe passive Na+ transport through GAT1. 5. We conclude that passive water and Na+ transport through cotransporters depend on different mechanisms: Na+ transport occurs by a saturable uniport mechanism, and water permeation is through a low conductance water channel. In the case of SGLT1, we suggest that both the water channel and water cotransport could contribute to isotonic fluid transport across the intestinal brush border membrane.  (+info)

Solute Carrier Organic Anion Transporter Family Member 1B1 (SLCO1B1) Genotype, Statin, Varies - Mayo Clinic Laboratories |...Solute Carrier Organic Anion Transporter Family Member 1B1 (SLCO1B1) Genotype, Statin, Varies - Mayo Clinic Laboratories |...
The most common adverse drug reaction associated with statins is skeletal muscle toxicity, which can include myalgia (with and without elevated creatine kinase levels), muscle weakness, muscle cramps, myositis, and rhabdomyolysis.(1) Rhabdomyolysis, while rare, is of clinical concern because of the risk for death as a result of cardiac arrhythmia, renal failure, and disseminated intravascular coagulation. While the underlying causes of statin-associated myopathy are not known, several hypotheses have been formulated, including those related to the biochemical pathway of cholesterol synthesis inhibition and statin metabolism.. SLCO1B1 encodes the organic anion-transporting polypeptide 1B1 (OATP1B1) influx transporter located on the basolateral membrane of hepatocytes. OATP1B1 facilitates the hepatic uptake of statins as well as other endogenous compounds (eg, bilirubin). Changes in the activity of this transporter (eg, through genetic variations or drug-drug interactions) can increase the ...
Solute carrier organic anion transporter family member 1B3 - DrugBankSolute carrier organic anion transporter family member 1B3 - DrugBank
This project is supported by the Canadian Institutes of Health Research (award #111062), Alberta Innovates - Health Solutions, and by The Metabolomics Innovation Centre (TMIC), a nationally-funded research and core facility that supports a wide range of cutting-edge metabolomic studies. TMIC is funded by Genome Alberta, Genome British Columbia, and Genome Canada, a not-for-profit organization that is leading Canadas national genomics strategy with funding from the federal government. Maintenance, support, and commercial licensing is provided by OMx Personal Health Analytics, Inc. Designed by Educe Design & Innovation Inc. ...
Solute carrier organic anion transporter family member 1B3 - Molecular Target Profile - BCIQSolute carrier organic anion transporter family member 1B3 - Molecular Target Profile - BCIQ
International biotechnology industry analysis, data and networking focused on translation, research, development, regulation, commercialization, partnering and funding.
SLCO1A2 - wikidocSLCO1A2 - wikidoc
Solute carrier organic anion transporter family member 1A2 is a protein that in humans is encoded by the SLCO1A2 gene.[1][2] This gene encodes a sodium-independent transporter which mediates cellular uptake of organic ions in the liver. Its substrates include bile acids, bromosulphophthalein, and some steroidal compounds. The protein is a member of the SLC21A family of solute carriers. Alternate splicing of this gene results in three transcript variants encoding two different isoforms.[2] ...
SLCO2A1 Gene - GeneCards | SO2A1 Protein | SO2A1 AntibodySLCO2A1 Gene - GeneCards | SO2A1 Protein | SO2A1 Antibody
Complete information for SLCO2A1 gene (Protein Coding), Solute Carrier Organic Anion Transporter Family Member 2A1, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene Compendium
SLCO1B3 Gene - GeneCards | SO1B3 Protein | SO1B3 AntibodySLCO1B3 Gene - GeneCards | SO1B3 Protein | SO1B3 Antibody
Complete information for SLCO1B3 gene (Protein Coding), Solute Carrier Organic Anion Transporter Family Member 1B3, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene Compendium
Slco1a1 (house mouse) | Gene Target - PubChemSlco1a1 (house mouse) | Gene Target - PubChem
Gene target information for Slco1a1 - solute carrier organic anion transporter family, member 1a1 (house mouse). Find diseases associated with this biological target and compounds tested against it in bioassay experiments.
anti-SLCO1A2 antibody | GeneTexanti-SLCO1A2 antibody | GeneTex
SLCO1A2 antibody (solute carrier organic anion transporter family, member 1A2) for ELISA, WB. Anti-SLCO1A2 pAb (GTX87607) is tested in Human samples. 100% Ab-Assurance.
M.D. | Einstein/Montefiore Department of MedicineM.D. | Einstein/Montefiore Department of Medicine
Selected publications:. Kanai,N Lu,R Satriano,J Bao,Y Wolkoff,AW Schuster,VL. Identification and characterization of a prostaglandin transporter. Science 268: 866-869, 1995.. Itoh,S Lu,R Bao,Y Morrow,JD Roberts,LJ Schuster,VL. Structural determinants of substrates for the prostaglandin transporter "PGT". Mol Pharm 50: 736-742, 1996.. Lu,R Kanai,N Bao,Y Schuster,VL. Cloning, in vitro expression, and tissue distribution of a human prostaglandin transporter cDNA "hPGT". J Clin Invest 98: 1142-1149, 1996.. Schuster,VL Lu,R Coca-Prados,M. Identification and characterization of a prostaglandin transporter widely-expressed in ocular and other secretory epithelia. Survey Ophthalmol 41: S41-S45, 1997.. Schuster,VL. Molecular mechanisms of prostaglandin transport. Ann Rev Physiol 60: 221-242, 1998.. Chan,B Satriano,JA Pucci,M Schuster,VL. Mechanism of PGE2 transport across the plasma membrane of HeLa cells and Xenopus oocytes expressing the prostaglandin transporter "PGT". J Biol Chem 273: 6689-6697, ...
Interindividual Variability in Hepatic Organic Anion-Transporting Polypeptides and P-Glycoprotein (ABCB1) Protein Expression:...Interindividual Variability in Hepatic Organic Anion-Transporting Polypeptides and P-Glycoprotein (ABCB1) Protein Expression:...
Interindividual variability in protein expression of organic anion-transporting polypeptides (OATPs) OATP1B1, OATP1B3, OATP2B1, and multidrug resistance-linked P-glycoprotein (P-gp) or ABCB1 was quantified in frozen human livers (n = 64) and cryopreserved human hepatocytes (n = 12) by a validated liquid chromatography tandem mass spectroscopy (LC-MS/MS) method. Membrane isolation, sample workup, and LC-MS/MS analyses were as described before by our laboratory. Briefly, total native membrane proteins, isolated from the liver tissue and cryopreserved hepatocytes, were trypsin digested and quantified by LC-MS/MS using signature peptide(s) unique to each transporter. The mean ± S.D. (maximum/minimum range in parentheses) protein expression (fmol/µg of membrane protein) in human liver tissue was OATP1B1- 2.0 ± 0.9 (7), OATP1B3- 1.1 ± 0.5 (8), OATP2B1- 1 1.7 ± 0.6 (5), and P-gp- 0.4 ± 0.2 (8). Transporter expression in the liver tissue was comparable to that in the cryopreserved hepatocytes. ...
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In the present study, we found that the C-1 carboxylic acid group was essential for optimal substrate binding to the FP receptor. Replacement of the carboxylic acid group by larger moieties with a similar pK a, such as acylsulfonamide and tetrazole, substantially decreased binding affinity. The prostaglandin transporter PGT, on the other hand, recognized a fairly wide range of anionic substrates at C-1. In contrast, insertion of cyclic substituents in the omega chain increased binding to the FP receptor but reduced affinity for PGT, and substitution for the 15-hydroxyl group produced only a modest reduction in FP receptor binding but eliminated binding by PGT.. Prostaglandins and thromboxanes bind to a number of structurally diverse molecules, such as their cell-surface receptors (EP, FP, IP, DP, and TP) (Breyer et al., 1996a), the prostaglandin transporter PGT (Itoh et al., 1996), peroxisome proliferator-activated receptors α and γ (Forman et al., 1995; Kliewer et al., 1995), and ...
The prostaglandin transporter (PGT) as a potential mediator of ovulation | Science Translational MedicineThe prostaglandin transporter (PGT) as a potential mediator of ovulation | Science Translational Medicine
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Multispecific Substrate Recognition of Kidney-Specific Organic Anion Transporters OAT-K1 and OAT-K2 | Journal of Pharmacology...Multispecific Substrate Recognition of Kidney-Specific Organic Anion Transporters OAT-K1 and OAT-K2 | Journal of Pharmacology...
We characterized the interactions of various compounds with OAT-K1 and OAT-K2, kidney-specific organic anion transporters. By using Madin-Darby canine kidney cells stably transfected with OAT-K1 or OAT-K2 cDNA, the antitumor drug methotrexate, the mycotoxin ochratoxin A, endogenous organic anions (thyroid hormones, taurocholic acid, and conjugated steroids), and the antiretroviral drug zidovudine were shown to be substrates for these transporters. Although the apparent Michaelis constant (Km) values of methotrexate for OAT-K1 and OAT-K2 were 2.1 and 1.8 μM, respectively, 2.5 mM methotrexate inhibited only 20% of the 125I-thyroid hormones uptake via these transporters. In addition, 100 μM methotrexate did not have any effect on [3H]zidovudine uptake via OAT-K1 or OAT-K2. Similarly, several substrates caused little or no mutual inhibition at concentrations much higher than theirKm values for these transporters. Moreover, intracellular methotrexate trans-stimulated the OAT-K1- and OAT-K2-mediated ...
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With efforts to reduce cytochrome P450-mediated clearance (CL) during the early stages of drug discovery, transporter-mediated CL mechanisms are becoming more prevalent. However, the prediction of plasma concentration-time profiles for such compounds using physiologically based pharmacokinetic (PBPK) modeling is far less established in comparison with that for compounds with passively mediated pharmacokinetics (PK). In this study, we have assessed the predictability of human PK for seven organic anion-transporting polypeptide (OATP) substrates (pravastatin, cerivastatin, bosentan, fluvastatin, rosuvastatin, valsartan, and repaglinide) for which clinical intravenous data were available. In vitro data generated from the sandwich culture human hepatocyte system were simultaneously fit to estimate parameters describing both uptake and biliary efflux. Use of scaled active uptake, passive distribution, and biliary efflux parameters as inputs into a PBPK model resulted in the overprediction of exposure ...
Anika Dzierlenga, PhD | College of Pharmacy - University of ArizonaAnika Dzierlenga, PhD | College of Pharmacy - University of Arizona
3. Bodeman, C.E.; Dzierlenga, A.L.; Tally, C.M.; Mulligan, R.M.; Lake, A.D.; Cherrington, N.J.; McKarns, S.C. "Differential Regulation of Hepatic Organic cation Transporter 1. Organic Anion-Transporting Polypeptide 1a4, Bile-Salt Export Pump, and Multidrug Resistance-Associated Protein 2.Transporter Expression in Lymphocyte-Deficient Mice Associates with Interleukin-6 Production." J Pharmacol Exp Ther., 2013, 347, 136-144 ...
Membrane & Intracellular Transport | The EMBO JournalMembrane & Intracellular Transport | The EMBO Journal
Beyond their roles in generating nerve impulses, ion channels are important for many facets of cell biology, including swelling and osmotic stress responses. Sabirov and colleagues now report that the prostaglandin transporter SLCO2A1 is a central component of the ubiquitous Maxi‐Cl anion channel. These findings add to a growing number of transporters displaying ion channel activity and not only provide a molecular handle for future Maxi‐Cl physiological and biophysical studies, but also underscore general questions about the principles that underlie such transporter/channel dual‐use behavior.. See also: RZ Sabirov et al (November 2017) ...
Impact of OATP transporters on pharmacokinetics. - PubMed - NCBIImpact of OATP transporters on pharmacokinetics. - PubMed - NCBI
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on...Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on...
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
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In this study, we characterized the transport function and transcriptional regulation of the OATP2B1 1e variant. The SLCO2B1 1e variant encoding OATP2B1-Short was cloned from a human liver cDNA library. Heterologous expression of OATP2B1-Short (1e) in HeLa cells resulted in cell surface expression and functional transport activity. We found no pronounced differences in transport activity between the OATP2B1-FL and OATP2B1-Short proteins for two typical OATP substrates: rosuvastatin and estrone 3-sulfate. However, we did see a significant increase in rosuvastatin uptake by OATP2B1-Short, but not for OATP2B1-FL at low pH. Reporter assays, siRNA knockdown, and ChIP revealed a functional HNF4α binding motif in the proximal region of the SLCO2B1 1e promoter.. The expression of the alternative OATP2B1 variants in intestine and kidney was previously reported (Pomari et al., 2009). We confirm that the OATP2B1 exon 1b transcription variant has a broad expression pattern consistent with previous reports ...
Drug Transporters: The Final Frontier for Drug Interactions—Part 2Drug Transporters: The Final Frontier for Drug Interactions—Part 2
The second in a pair of articles on drug transporters, this article focuses on uptake transporters that actively pump drugs into cells.
Organic anion-transporting polypeptide 14 | definition of Organic anion-transporting polypeptide 14 by Medical dictionaryOrganic anion-transporting polypeptide 14 | definition of Organic anion-transporting polypeptide 14 by Medical dictionary
Looking for online definition of Organic anion-transporting polypeptide 14 in the Medical Dictionary? Organic anion-transporting polypeptide 14 explanation free. What is Organic anion-transporting polypeptide 14? Meaning of Organic anion-transporting polypeptide 14 medical term. What does Organic anion-transporting polypeptide 14 mean?
Pachydermoperiostosis Publications and Abstracts | PubFacts.comPachydermoperiostosis Publications and Abstracts | PubFacts.com
Solute carrier organic anion transporter family member 2A1 (OATP2A1, encoded by the SLCO2A1 gene), which was initially identified as prostaglandin transporter (PGT), is expressed ubiquitously in tissues and mediates the distribution of prostanoids, such as PGE, PGF, PGDand TxB. It is well known to play a key role in the metabolic clearance of prostaglandins, which are taken up into the cell by OATP2A1 and then oxidatively inactivated by 15-ketoprostaglandin dehydrogenase (encoded by HPGD); indeed, OATP2A1-mediated uptake is the rate-limiting step of PGEcatabolism. Consequently, since OATP2A1 activity is required for termination of prostaglandin signaling via prostanoid receptors, its inhibition can enhance such signaling. Read More ...
Transport of estrone 3-sulfate mediated by organic anion transporter OATP4C1: Estrone 3-sulfate binds to the different...Transport of estrone 3-sulfate mediated by organic anion transporter OATP4C1: Estrone 3-sulfate binds to the different...
Fingerprint Dive into the research topics of Transport of estrone 3-sulfate mediated by organic anion transporter OATP4C1: Estrone 3-sulfate binds to the different recognition site for digoxin in OATP4C1. Together they form a unique fingerprint. ...
Kyushu University [UMENO JUNJI (Assistant Professor) Kyushu University Hospital, Department of Gastroenterology]Kyushu University [UMENO JUNJI (Assistant Professor) Kyushu University Hospital, Department of Gastroenterology]
Junji Umeno, Tadakazu Hisamatsu, Motohiro Esaki, Atsushi Hirano, Takayuki Matsumoto, Kitazono T, A Hereditary Enteropathy Caused by Mutations in the SLCO2A1 Gene, Encoding a Prostaglandin Transporter., e1005581, 2015.11, Previously, we proposed a rare autosomal recessive inherited enteropathy characterized by persistent blood and protein loss from the small intestine as chronic nonspecific multiple ulcers of the small intestine (CNSU). By whole-exome sequencing in five Japanese patients with CNSU and one unaffected individual, we found four candidate mutations in the SLCO2A1 gene, encoding a prostaglandin transporter. The pathogenicity of the mutations was supported by segregation analysis and genotyping data in controls. By Sanger sequencing of the coding regions, 11 of 12 other CNSU patients and 2 of 603 patients with a diagnosis of Crohns disease were found to have homozygous or compound heterozygous SLCO2A1 mutations. In total, we identified recessive SLCO2A1 mutations located at seven ...
Hepatic fatty acid translocase CD36 upregulation is associated with insulin resistance, hyperinsulinaemia and increased...Hepatic fatty acid translocase CD36 upregulation is associated with insulin resistance, hyperinsulinaemia and increased...
Results Compared with NL, hepatic mRNA and protein levels of FAT/CD36 were significantly higher in patients with NAS (median fold increase 0.84 (range 0.15-1.61) and 0.66 (range 0.33-1.06), respectively); NASH (0.91 (0.22-1.81) and 0.81 (0.38-0.92), respectively); HCV G1 without steatosis (0.30 (0.17-1.59) and 0.33 (0.29-0.52), respectively); and HCV G1 with steatosis (0.85 (0.15-1.98) and 0.87 (0.52-1.26), respectively). In contrast to NL, FAT/CD36 was predominantly located at the plasma membrane of hepatocytes in patients with NAFLD and HCV G1 with steatosis. A significant correlation was observed between hepatic FAT/CD36 expression index and plasma insulin levels, insulin resistance (HOMA-IR) and histological grade of steatosis in patients with NASH (r=0.663, r=0.735 and r=0.711, respectively) and those with HCV G1 with steatosis (r=0.723, r=0.769 and r=0.648, respectively). ...
Human Renal Organic Anion Transporter 4 Operates as an Asymmetric Urate Transporter | American Society of NephrologyHuman Renal Organic Anion Transporter 4 Operates as an Asymmetric Urate Transporter | American Society of Nephrology
Figure 6. [3H]PAH efflux studies on X. laevis oocytes that were injected with water (mock) or hOAT4-cRNA. Three days after cRNA or water injection, 46 nl of a 200-μM [3H]PAH solution was injected into the oocytes, and efflux of [3H]PAH was measured, providing oocyte Ringers solution, chloride-free oocyte Ringers solution, and chloride-free oocyte Ringers solution plus 500 μM ES. The efflux was calculated as percentage of 3H content recovered in the supernatant compared with the sum of total radioactivity recovered in the medium and that remaining in the oocytes at the conclusion of a 30-min efflux period at room temperature, where hOAT4-expressing oocytes in oocyte Ringers solution were set to 100%, Data are means ± SEM or three independent experiments with five to seven oocytes each. **P , 0.01. ...
Organic Anion Transporters, Sodium-Independent | Semantic ScholarOrganic Anion Transporters, Sodium-Independent | Semantic Scholar
A subclass of ORGANIC ANION TRANSPORTERS that do not rely directly or indirectly upon sodium ion gradients for the transport of organic ions.
SLCO1B1 variants and statin-induced myopathy--a genomewide study. - Nuffield Department of Population HealthSLCO1B1 variants and statin-induced myopathy--a genomewide study. - Nuffield Department of Population Health
BACKGROUND: Lowering low-density lipoprotein cholesterol with statin therapy results in substantial reductions in cardiovascular events, and larger reductions in cholesterol may produce larger benefits. In rare cases, myopathy occurs in association with statin therapy, especially when the statins are administered at higher doses and with certain other medications. METHODS: We carried out a genomewide association study using approximately 300,000 markers (and additional fine-mapping) in 85 subjects with definite or incipient myopathy and 90 controls, all of whom were taking 80 mg of simvastatin daily as part of a trial involving 12,000 participants. Replication was tested in a trial of 40 mg of simvastatin daily involving 20,000 participants. RESULTS: The genomewide scan yielded a single strong association of myopathy with the rs4363657 single-nucleotide polymorphism (SNP) located within SLCO1B1 on chromosome 12 (P=4x10(-9)). SLCO1B1 encodes the organic anion-transporting polypeptide OATP1B1, which has
anti-Solute Carrier Family 22 (Organic Anion Transporter), Member 8 (SLC22A8) antibody (Alexa Fluor 488) ABIN909357 from...anti-Solute Carrier Family 22 (Organic Anion Transporter), Member 8 (SLC22A8) antibody (Alexa Fluor 488) ABIN909357 from...
anti-Solute Carrier Family 22 (Organic Anion Transporter), Member 8 (SLC22A8) antibody (Alexa Fluor 488) ABIN909357 from antibodies-online
Experimental non-alcoholic fatty liver disease results in decreased hepatic uptake transporter expression and function in ratsExperimental non-alcoholic fatty liver disease results in decreased hepatic uptake transporter expression and function in rats
Non-alcoholic fatty liver disease (NAFLD) encompasses a spectrum of diagnoses ranging from simple fatty liver (SFL), to non-alcoholic steatohepatitis (NASH). This study aimed to determine the effect of moderate and severe NAFLD on hepatic transporter expression and function in vivo. Rats were fed a …
KAKEN - Researchers | INATOMI Jun (00311960)KAKEN - Researchers | INATOMI Jun (00311960)
Affiliation：The University of Tokyo,Faculty of Medicine,Research Associate,医学部附属病院,助手, Research Field：応用薬理学・医療系薬学,General pharmacology,Kidney internal medicine,Pediatrics,Pediatrics, Keywords：エストロン硫酸,Na^+,近位尿細管性アシドーシス,パラアミノ馬尿酸,rBAT,オクラトキシンA,organic anion transporter2,organic anion transporter3,organic anion transporter1,BAT1, # of Research Projects：8, # of Research Products：9
Vesicular uptake and exocytosis of L-aspartate is independent of sialin.Vesicular uptake and exocytosis of L-aspartate is independent of sialin.
The mechanism of release and the role of l-aspartate as a central neurotransmitter are controversial. A vesicular release mechanism for l-aspartate has been difficult to prove, as no vesicular l-aspartate transporter was identified until it was found that sialin could transport l-aspartate and l-glutamate when reconstituted into liposomes. We sought to clarify the release mechanism of l-aspartate and the role of sialin in this process by combining l-aspartate uptake studies in isolated synaptic vesicles with immunocyotchemical investigations of hippocampal slices. We found that radiolabeled l-aspartate was taken up into synaptic vesicles. The vesicular l-aspartate uptake, relative to the l-glutamate uptake, was twice as high in the hippocampus as in the whole brain, the striatum, and the entorhinal and frontal cortices and was not inhibited by l-glutamate. We further show that sialin is not essential for exocytosis of l-aspartate, as there was no difference in ATP-dependent l-aspartate uptake in ...
Directional trans-epithelial transport of organic anions in porcine LLC-PK1 cells that co-express human OATP1B1 (OATP-C) and...Directional trans-epithelial transport of organic anions in porcine LLC-PK1 cells that co-express human OATP1B1 (OATP-C) and...
The transcellular transport of many compounds, which cannot readily cross the lipid bilayer, is mediated by drug uptake and efflux transporters. Human OATP1B1 and MRP2 have been implicated in the hepato-biliary transport of many endogenous and exogenous compounds. Here, we have established epithelia …
Localization of organic anion transporting polypeptide 3 (oatp3) in mouse brain parenchymal and capillary endothelial cells<...Localization of organic anion transporting polypeptide 3 (oatp3) in mouse brain parenchymal and capillary endothelial cells<...
TY - JOUR. T1 - Localization of organic anion transporting polypeptide 3 (oatp3) in mouse brain parenchymal and capillary endothelial cells. AU - Ohtsuki, Sumio. AU - Takizawa, Takuya. AU - Takanaga, Hitomi. AU - Hori, Satoko. AU - Hosoya, Ken Ichi. AU - Terasaki, Tetsuya. PY - 2004/8/1. Y1 - 2004/8/1. N2 - Organic anion transporting polypeptide 3 (oatp3) transports various CNS-acting endogenous compounds, including thyroid hormones and prostaglandin E2, between extra- and intracellular spaces, suggesting a possible role in CNS function. The purpose of this study was to clarify the expression and localization of oatp3 in the mouse brain. RT-PCR analysis revealed that oatp3 mRNA is expressed in brain capillary-rich fraction, conditionally immortalized brain capillary endothelial cells, choroid plexus, brain and lung, but not in liver or kidney, where oatp1, 2 and 5 mRNAs were detected. Immunohistochemical analysis with anti-oatp3 antibody suggests that oatp3 protein is localized at the ...
AID 682056 - TP TRANSPORTER: uptake (pH 5.0) of Estrone-3-sulfate at a concentration of 5.43 nM in OATP-B-expressing HEK293...AID 682056 - TP TRANSPORTER: uptake (pH 5.0) of Estrone-3-sulfate at a concentration of 5.43 nM in OATP-B-expressing HEK293...
BioAssay record AID 682056 submitted by ChEMBL: TP_TRANSPORTER: uptake (pH 5.0) of Estrone-3-sulfate at a concentration of 5.43 nM in OATP-B-expressing HEK293 cells.
Drug Transporter (DT) Information | VARIDT: Variability of Drug Transporter DatabaseDrug Transporter (DT) Information | VARIDT: Variability of Drug Transporter Database
This Na(+)-independent transporter mediates the organic anions such as the thyroid hormones thyroxine (T4) and rT3 and may play a signifiant role in regulating T4 flux into and out of the brain. Other potential substrates, such as triiodothyronine (T3), 17-beta-glucuronosyl estradiol, estrone-3-sulfate and sulfobromophthalein (BSP) are transported with much lower efficiency ...
OPUS 4 | Untersuchungen zur Expression und Funktion von OATP-Transportern in Blutzellen und der Blut-Hirn-SchrankeOPUS 4 | Untersuchungen zur Expression und Funktion von OATP-Transportern in Blutzellen und der Blut-Hirn-Schranke
Aus pharmakologischer Sicht sind unter den Aufnahmetransportern Vertreter der organic anion transporting polypeptide-Familie (OATPs) von besonderem Interesse. Transporter dieser Familie besitzen nicht nur ein breites Substratspektrum endogener und exogener Substanzen, sondern sind auch in zahlreichen Geweben exprimiert. Gut untersucht ist dabei vor allem die Leber mit den vorwiegend hepatisch exprimierten Vertretern OATP1B1 und OATP1B3, während zur Expression und Funktion der OATPs in weiteren pharmakologischen Zielstrukturen, wie beispielsweise den Blutzellen oder auch der Blut-Hirn-Schranke, weit weniger bekannt ist. Ziel dieser Arbeit war es daher, ausgewählte OATP-Transporter hinsichtlich ihrer Expression, ihrem Interaktionspotential und der Funktion in der Blut-Hirn-Schranke und zwei Blutzellpopulationen zu charakterisieren. Dabei konnte zunächst die Expression des OATP2B1 und OATP1A2 in der Blut-Hirn-Schranke bestätigt und deren funktionelle Interaktion mit ausgewählten Dopaminrezeptor
Cara Mencari Jodoh Sekota di Dunia Maya Dengan WOO - shitliciousCara Mencari Jodoh Sekota di Dunia Maya Dengan WOO - shitlicious
Ramuan tradisional untuk obat asam urat adalah obat yang banyak dicari oleh wanita, dan pria yang berumur di atas 30 tahun, karena banyak yang terkena penyakit asam urat. bahkan sekarang di bawah umur 30 tahun sudah terkena asam urat akut. jika penyakit sudah parah akan mengakibatkan persendian tidak bisa bergerak. tetapi anda tidak usah khawatir, karena sekarang sudah muncul obat untuk asam urat herbal tradisional berkhasiat tinggi. obat asam urat yang alami ampuh dari dulu tradisional ini adalah salah satu obat herbal asam urat dan kolesterol menahun tradisional berkhasiat tinggi, dan obat asam urat herbal tradisional terbaik alami ampuh dari dulu. tidak hanya bisa dijadikan untuk obat asam urat dan testimoni penderita asam urat, tetapi bisa juga mengobati kolesterol tinggi ...
Cara Mencari Jodoh Sekota di Dunia Maya Dengan WOO - shitliciousCara Mencari Jodoh Sekota di Dunia Maya Dengan WOO - shitlicious
Ramuan tradisional untuk obat asam urat adalah obat yang banyak dicari oleh wanita, dan pria yang berumur di atas 30 tahun, karena banyak yang terkena penyakit asam urat. bahkan sekarang di bawah umur 30 tahun sudah terkena asam urat akut. jika penyakit sudah parah akan mengakibatkan persendian tidak bisa bergerak. tetapi anda tidak usah khawatir, karena sekarang sudah muncul obat untuk asam urat herbal tradisional berkhasiat tinggi. obat asam urat yang alami ampuh dari dulu tradisional ini adalah salah satu obat herbal asam urat dan kolesterol menahun tradisional berkhasiat tinggi, dan obat asam urat herbal tradisional terbaik alami ampuh dari dulu. tidak hanya bisa dijadikan untuk obat asam urat dan testimoni penderita asam urat, tetapi bisa juga mengobati kolesterol tinggi ...
Little Friends Photo: Taping of THE INSIDER with Debbie MatenopoulosLittle Friends Photo: Taping of THE INSIDER with Debbie Matenopoulos
Ramuan tradisional untuk obat asam urat adalah obat yang banyak dicari oleh wanita, dan pria yang berumur di atas 30 tahun, karena banyak yang terkena penyakit asam urat. bahkan sekarang di bawah umur 30 tahun sudah terkena asam urat akut. jika penyakit sudah parah akan mengakibatkan persendian tidak bisa bergerak. tetapi anda tidak usah khawatir, karena sekarang sudah muncul obat untuk asam urat herbal tradisional berkhasiat tinggi. obat asam urat yang alami ampuh dari dulu tradisional ini adalah salah satu obat herbal asam urat dan kolesterol menahun tradisional berkhasiat tinggi, dan obat asam urat herbal tradisional terbaik alami ampuh dari dulu. tidak hanya bisa dijadikan untuk obat asam urat dan testimoni penderita asam urat, tetapi bisa juga mengobati kolesterol tinggi ...
Little Friends Photo: Taping of THE INSIDER with Debbie MatenopoulosLittle Friends Photo: Taping of THE INSIDER with Debbie Matenopoulos
Ramuan tradisional untuk obat asam urat adalah obat yang banyak dicari oleh wanita, dan pria yang berumur di atas 30 tahun, karena banyak yang terkena penyakit asam urat. bahkan sekarang di bawah umur 30 tahun sudah terkena asam urat akut. jika penyakit sudah parah akan mengakibatkan persendian tidak bisa bergerak. tetapi anda tidak usah khawatir, karena sekarang sudah muncul obat untuk asam urat herbal tradisional berkhasiat tinggi. obat asam urat yang alami ampuh dari dulu tradisional ini adalah salah satu obat herbal asam urat dan kolesterol menahun tradisional berkhasiat tinggi, dan obat asam urat herbal tradisional terbaik alami ampuh dari dulu. tidak hanya bisa dijadikan untuk obat asam urat dan testimoni penderita asam urat, tetapi bisa juga mengobati kolesterol tinggi ...
Little Friends Photo: Taping of THE INSIDER with Debbie MatenopoulosLittle Friends Photo: Taping of THE INSIDER with Debbie Matenopoulos
Ramuan tradisional untuk obat asam urat adalah obat yang banyak dicari oleh wanita, dan pria yang berumur di atas 30 tahun, karena banyak yang terkena penyakit asam urat. bahkan sekarang di bawah umur 30 tahun sudah terkena asam urat akut. jika penyakit sudah parah akan mengakibatkan persendian tidak bisa bergerak. tetapi anda tidak usah khawatir, karena sekarang sudah muncul obat untuk asam urat herbal tradisional berkhasiat tinggi. obat asam urat yang alami ampuh dari dulu tradisional ini adalah salah satu obat herbal asam urat dan kolesterol menahun tradisional berkhasiat tinggi, dan obat asam urat herbal tradisional terbaik alami ampuh dari dulu. tidak hanya bisa dijadikan untuk obat asam urat dan testimoni penderita asam urat, tetapi bisa juga mengobati kolesterol tinggi ...
SLCO3A1 purified MaxPab mouse polyclonal antibody (B01P) - (H00028232-B01P) - Products - AbnovaSLCO3A1 purified MaxPab mouse polyclonal antibody (B01P) - (H00028232-B01P) - Products - Abnova
Mouse polyclonal antibody raised against a full-length human SLCO3A1 protein. SLCO3A1 (ABM82880.1, 1 a.a. ~ 692 a.a) full-length human protein. (H00028232-B01P) - Products - Abnova
Industry Transporters on SteamIndustry Transporters on Steam
An economic simulation where you build up production chains as effectively as possible on a large scale terrain. You can choose from a large variety of wares and buildings to build up your production chain and use up to 4 types of transportation ...
S, the measurement of overall level of carbonyls of plasma proteins | URAT1 inhibitor urat1inhibitor.comS, the measurement of overall level of carbonyls of plasma proteins | URAT1 inhibitor urat1inhibitor.com
S, the measurement of overall level of carbonyls of plasma proteins may be used as a surrogate marker of oxidative modification of VWF, as shown in the present
Hardly any impact [82].The absence of an association of survival with | URAT1 inhibitor urat1inhibitor.comHardly any impact [82].The absence of an association of survival with | URAT1 inhibitor urat1inhibitor.com
Hardly any effect .The absence of an association of buy GW0742 survival together with the far more frequent variants (like CYP2D6*4) prompted these
Habbatussauda plus mengkudu - Herbal CirebonHabbatussauda plus mengkudu - Herbal Cirebon
Herbal Online , Grosir Herbal Cirebon , Jual obat herbal , Madu , Habbatussauda , Minyak zaitun , Herbal Asam Urat , Obat Herbal ...
Sodium-independent organic anion transporter E | definition of Sodium-independent organic anion transporter E by Medical...Sodium-independent organic anion transporter E | definition of Sodium-independent organic anion transporter E by Medical...
Looking for online definition of Sodium-independent organic anion transporter E in the Medical Dictionary? Sodium-independent organic anion transporter E explanation free. What is Sodium-independent organic anion transporter E? Meaning of Sodium-independent organic anion transporter E medical term. What does Sodium-independent organic anion transporter E mean?
Functional analysis of rat renal organic anion transporter OAT-K1: Bidirectional methotrexate transport in apical membrane<...Functional analysis of rat renal organic anion transporter OAT-K1: Bidirectional methotrexate transport in apical membrane<...
TY - JOUR. T1 - Functional analysis of rat renal organic anion transporter OAT-K1. T2 - Bidirectional methotrexate transport in apical membrane. AU - Masuda, Satohiro. AU - Takeuchi, Ayako. AU - Saito, Hideyuki. AU - Hashimoto, Yukiya. AU - Inui, Ken Ichi. PY - 1999/10/1. Y1 - 1999/10/1. N2 - Renal organic anion transporter OAT-K1 was stably transfected in MDCK cells and examined for its transport characteristics and membrane localization. OAT-K1 mediated both uptake and efflux of methotrexate in the apical membranes. Immunoblotting showed that the apparent molecular mass of the expressed OAT-K1 was 50 kDa, which was comparable to that found in the rat renal brush-border membranes. The OAT-K1-mediated methotrexate transport was significantly inhibited in the presence of several organic anions such as folate and sulfobromophthalein. These findings suggest that OAT-K1 mediates bidirectional methotrexate transport across the apical membranes, and may be involved in the renal handling of ...
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Urate transport in the kidney proximal tubule is a bidirectional process. Although the urate reabsorption pathway has been elucidated recently, there is little knowledge about the excretory route. The basolateral organic anion transporters OAT1 and OAT3 presumably mediate uptake from blood into the cell, but for apical export from the cell into urine no candidate transporter has been identified. In this study, we show that the apical organic anion transporter MRP4 mediates ATP-dependent urate transport in isolated membrane vesicles and exports urate from transfected cells. Furthermore, the complex interaction pattern of urate with the MRP4 substrates MTX, cAMP, and cGMP indicates that MRP4 is an organic anion transporter with multiple allosteric binding sites.. Isolated apical and basolateral membrane vesicles from kidney proximal tubule have been used widely to study organic anion transport mechanisms, mainly using PAH or urate as a substrate (31). In contrast to basolateral membrane vesicles, ...
Molecular characterization of the renal organic anion transporter 1 | Springer for Research & DevelopmentMolecular characterization of the renal organic anion transporter 1 | Springer for Research & Development
Organic anions of diverse chemical structures are secreted in renal proximal tubules. The first step in secretion, uptake of organic anions across the basolateral membrane of tubule cells, is...
Assessment of Amino Acid/Drug Transporters for Renal Transport of [18F]Fluciclovine (anti-[18F]FACBC) in Vitro - Semantic...Assessment of Amino Acid/Drug Transporters for Renal Transport of [18F]Fluciclovine (anti-[18F]FACBC) in Vitro - Semantic...
[18F]Fluciclovine (trans-1-amino-3-[18F]fluorocyclobutanecarboxylic acid; anti-[18F]FACBC), a positron emission tomography tracer used for the diagnosis of recurrent prostate cancer, is transported via amino acid transporters (AATs) with high affinity (Km: 97-230 μM). However, the mechanism underlying urinary excretion is unknown. In this study, we investigated the involvement of AATs and drug transporters in renal [18F]fluciclovine reuptake. [14C]Fluciclovine (trans-1-amino-3-fluoro[1-14C]cyclobutanecarboxylic acid) was used because of its long half-life. The involvement of AATs in [14C]fluciclovine transport was measured by apical-to-basal transport using an LLC-PK1 monolayer as model for renal proximal tubules. The contribution of drug transporters herein was assessed using vesicles/cells expressing the drug transporters P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), multidrug resistance-associated protein 4 (MRP4), organic anion transporter 1 (OAT1), organic anion transporter 3
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OAT1 is a multispecific organic anion transporter exclusively located on the basolateral membrane of the middle proximal tubule, S2 segment (Tojo et al., 1999). PAH is a high-affinity substrate of OAT1 (Km = 14.3 μM), and OAT1-mediated PAH transport was inhibited by a variety of anionic drugs (Sekine et al., 1997). OAT1 is an organic anion/dicarboxylate exchanger; preloaded glutarate trans-stimulates the uptake of PAH via OAT1 (Sekine et al., 1997). From these findings, we inferred that OAT1 is the major renal organic anion transporter at the basolateral membrane of the proximal tubule. However, the contribution of OAT1 in the renal excretion of organic anions remains to be elucidated. In fact, we have already identified several isoforms of OAT1 (Sekine et al., 1998), one of which shows higher affinity to PCG.. This study demonstrated the inhibition of PAH transport via OAT1 by all the penicillins and cephalosporins tested and OAT1-mediated transport of [3H]PCG and [14C]cephaloridine (Fig. 3). ...
Regulatory mechanisms of gamma-aminobutyric acid transporter 1 in the rat brain :: University of Southern California...Regulatory mechanisms of gamma-aminobutyric acid transporter 1 in the rat brain :: University of Southern California...
Chemical synapses are the principal locations where signals are transmitted between neurons. The transmission of this chemical signal is largely influenced by the action of neurotransmitter transporters which contribute to synaptic transmission by removing neurotransmitters from the synaptic cleft and thus terminating the synaptic signal. Abnormal activities of neurotransmitter transporters are associated with a variety of brain disorders. Therefore, drugs targeting neurotransmitter transporters play an important role in treating these diseases.; Since only the neurotransmitter transporters present on the plasma membrane are able to take up synaptically localized transmitters, it is critical to maintain a proper number of surface transporters. Recent advances in transporter biochemistry and molecular biology have provided substantial insights into transporter structure and function, intracellular transporter trafficking, and the association of transporters with other cellular proteins. All of ...
Regulatory mechanisms of gamma-aminobutyric acid transporter 1 in the rat brain :: University of Southern California...Regulatory mechanisms of gamma-aminobutyric acid transporter 1 in the rat brain :: University of Southern California...
Chemical synapses are the principal locations where signals are transmitted between neurons. The transmission of this chemical signal is largely influenced by the action of neurotransmitter transporters which contribute to synaptic transmission by removing neurotransmitters from the synaptic cleft and thus terminating the synaptic signal. Abnormal activities of neurotransmitter transporters are associated with a variety of brain disorders. Therefore, drugs targeting neurotransmitter transporters play an important role in treating these diseases.; Since only the neurotransmitter transporters present on the plasma membrane are able to take up synaptically localized transmitters, it is critical to maintain a proper number of surface transporters. Recent advances in transporter biochemistry and molecular biology have provided substantial insights into transporter structure and function, intracellular transporter trafficking, and the association of transporters with other cellular proteins. All of ...
JCI - Phenotypic and pharmacogenetic evaluation of patients with thiazide-induced hyponatremiaJCI - Phenotypic and pharmacogenetic evaluation of patients with thiazide-induced hyponatremia
Thiazide diuretics are among the most widely used treatments for hypertension, but thiazide-induced hyponatremia (TIH), a clinically significant adverse effect, is poorly understood. Here, we have studied the phenotypic and genetic characteristics of patients hospitalized with TIH. In a cohort of 109 TIH patients, those with severe TIH displayed an extended phenotype of intravascular volume expansion, increased free water reabsorption, urinary prostaglandin E2 excretion, and reduced excretion of serum chloride, magnesium, zinc, and antidiuretic hormone. GWAS in a separate cohort of 48 TIH patients and 2,922 controls from the 1958 British birth cohort identified an additional 14 regions associated with TIH. We identified a suggestive association with a variant in SLCO2A1, which encodes a prostaglandin transporter in the distal nephron. Resequencing of SLCO2A1 revealed a nonsynonymous variant, rs34550074 (p.A396T), and association with this SNP was replicated in a second cohort of TIH cases. TIH ...
Determination of the external loops and the cellular orientation of the N- and the C-termini of the human organic anion...Determination of the external loops and the cellular orientation of the N- and the C-termini of the human organic anion...
The OAT (organic anion transporter) family mediates the absorption, distribution and excretion of a diverse array of environmental toxins and clinically important drugs. OAT dysfunction significantly contributes to renal, hepatic, neurological and fetal toxicity and disease. As a first step to establish the topological model of hOAT1 (human OAT1), we investigated the external loops and the cellular orientation of the N- and the C-termini of this transporter. Combined approaches of immunofluorescence studies and site-directed chemical labelling were used for such purpose. Immunofluorescence microscopy of Myc-tagged hOAT1 expressed in cultured cells identified that both the N- and the C-termini of the transporter were located in the cytoplasm. Replacement of Lys59 in the predicted extracellular loop I with arginine resulted in a mutant (K59R), which was largely inaccessible for labelling by membrane-impermeable NHS (N-hydroxysuccinimido)-SS (dithio)-biotin present in the extracellular medium. This ...
A Phase 1, Randomized, Open-label, Crossover Study to Evaluate the Effect of the Organic Anion Transporter Inhibitor Probenecid...A Phase 1, Randomized, Open-label, Crossover Study to Evaluate the Effect of the Organic Anion Transporter Inhibitor Probenecid...
The purpose of this study is to evaluate the effect of multiple-dose administration of probenecid on the pharmacokinetics of JNJ-63549109 and JNJ-64167896
SLC22A8 - WikipediaSLC22A8 - Wikipedia
Solute carrier family 22 member 8, or organic anion transporter 3 (OAT3), is a protein that in humans is encoded by the SLC22A8 gene. OAT3 is involved in the transport and excretion of organic ions some of which are drugs (e.g., penicillin G (benzylpenicillin), methotrexate (MTX), indomethacin (an NSAID), and ciprofloxacin (a fluoroquinolone antibiotic)) and some of which are pure toxicants. SLC22A8 (OAT3) is indirectly dependent on the inward sodium gradient, which is a driving force for reentry of dicarboxylates into the cytosol. Dicarboxylates, such as alpha-ketoglutarate generated within the cell, or recycled from the extracellular space, are used as exchange substrates to fuel the influx of organic anions against their concentration gradient. The encoded protein is an integral membrane protein and appears to be localized to the basolateral membrane of renal proximal tubule cells. GRCh38: Ensembl release 89: ENSG00000149452 - Ensembl, May 2017 GRCm38: Ensembl release 89: ENSMUSG00000063796 - ...
Abstract 15784: Impact of SLCO1B1 Genotype on Pediatric Simvastatin Pharmacokinetics | CirculationAbstract 15784: Impact of SLCO1B1 Genotype on Pediatric Simvastatin Pharmacokinetics | Circulation
Background: Simvastatin (SV) is administered as a lactone prodrug requiring hydrolysis to its active moiety, simvastatin acid (SA), to disrupt hepatic cholesterol biosynthesis. In adults, allelic variation of SLCO1B1 encoding the liver-specific organic anion transporting polypeptide (OATP1B1) drug uptake transporter reduces statin cellular uptake. As a consequence, concentrations at the site of action are lower compromising efficacy and circulating plasma concentrations are increased, placing patients at higher risk for adverse events. Expression of OATPs in mice changes during development, raising the question of whether in humans the genotype-phenotype relationship observed in adults is relevant in the developing child.. Methods: Participants (8-21 years) with at least one allelic variant of SLCO1B1 c.521 T,C (521TC; n=12, 521CC; n=2) and wild type controls (521TT; n=12) completed a single oral dose pharmacokinetics (PK) study. SV, SA, and metabolites were quantified by liquid chromatography ...
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Tomato plants (Lycopersicon esculentum L. var. Ailsa Craig) were grown in water culture in nutrient solution in a series of 10 increasing levels of nitrate nutrition. Using whole plant data derived from analytical and yield data of individual plant parts, the fate of anion charge arising from increased NO3 assimilation was followed in its distribution between organic anion accumulation in the plant and OH− efflux into the nutrient solution as calculated by excess anion over cation uptake. With increasing NO3 nutrition the bulk of the anion charge appeared as organic anion accumulation in the plants. OH− efflux at a maximum accounted for only 20% of the anion charge shift. The major organic anion accumulated in response to nitrate assimilation was malate. The increase in organic anion accumulation was paralleled by an increase in cation concentration (K+, Ca2+, Mg2+, Na+). Total inorganic anion levels (NO3−, SO42−, H2PO4−, Cl−) were relatively constant. The effect of increasing NO3 ...
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Dicarboxylate (succinate, fumarate, malate) transporter, vcINDY. The 3-d structure is known to 3.2 Å resolution with citrate and Na+ bound (Mancusso et al. 2012). May also transport citrate and glutamate with low affinity. Can use Na+ or Li+ as the cotransported cation. MtrF (TC#2.A.68.1.2) and YdaH (TC# 2.A.68.1.4) have been shown to have similar 3-d folds as vcINDY (Vergara-Jaque et al. 2015), confirming the assignment of these two families to the same superfamily (Prakash et al. 2003 ...
Hyperglycemic Modification to Classical Two-Vessel Occlusion for Inducing Transient Cerebral Ischemia in Sprague-Dawley Rats |...Hyperglycemic Modification to Classical Two-Vessel Occlusion for Inducing Transient Cerebral Ischemia in Sprague-Dawley Rats |...
This Review article will introduce organic anion transporting polypeptides which recognize endo- and exogenous organic anionic compounds and recent findings about their upregulation in cancer cells.
Difference between revisions of Lee:JC - OpenWetWareDifference between revisions of "Lee:JC" - OpenWetWare
Maeda T, Irokawa M, Arakawa H, Kuraoka E, Nozawa T, Tateoka R, Itoh Y, Nakanishi T, and Tamai I. Uptake transporter organic anion transporting polypeptide 1B3 contributes to the growth of estrogen-dependent breast cancer. J Steroid Biochem Mol Biol 2010 Oct; 122(4) [http://www.sciencedirect.com/science?_ob=MImg&_imagekey=B6T8X-50G6962-1-C&_cdi=5098&_user=16764&_pii=S0960076010002888&_origin=search&_coverDate=10%2F31%2F2010&_sk=998779995&view=c&wchp=dGLbVlW-zSkzS&md5=4e61be9c7a06b0a1c489bad90ac1d2c4&ie=/sdarticle.pdf 180-5](10/7/10 ...
KEGG ORTHOLOGY: K08747KEGG ORTHOLOGY: K08747
Organic anion transporting polypeptides of the OATP/ SLC21 family: phylogenetic classification as OATP/ SLCO superfamily, new nomenclature and molecular/functional properties ...
Transporter Screening ServiceTransporter Screening Service
Profacgen provides various transporter cell models and customized transporter screening service for the identification of novel transporter-targeted therapeutics.
Multidrug resistance-associated protein 2Multidrug resistance-associated protein 2
Epithelial polarityEpithelial polarity
SLC22A8SLC22A8
SLC17A3SLC17A3
SLCO1A2SLCO1A2
SLCO3A1SLCO3A1
SLC22A9SLC22A9
SLC22A12SLC22A12
SLC22A10SLC22A10
SLCO2A1SLCO2A1
CitrininCitrinin
KCNK3KCNK3
PAX1PAX1
SLC22A4SLC22A4
SLCO1B3SLCO1B3
SLCO4A1SLCO4A1
SLCO2B1SLCO2B1
ABCC3ABCC3
OATP4C1OATP4C1
SLCO1B1SLCO1B1
SLC22A11SLC22A11
SLC22A7SLC22A7
ProbenecidProbenecid
SafinamideSafinamide
Bromopyruvic acidBromopyruvic acid
SLC22A25SLC22A25
Major facilitator superfamilyMajor facilitator superfamily
ABCC5ABCC5
Slc22a21Slc22a21
ABCC1ABCC1
Alkali metalAlkali metal
Coomassie Brilliant BlueCoomassie Brilliant Blue
DiureticDiuretic
HomeostasisHomeostasis
Mitochondrial thiamine pyrophosphate carrierMitochondrial thiamine pyrophosphate carrier
AntioxidantAntioxidant
ATP-binding cassette transporterATP-binding cassette transporter
Natrium bahasa Indonesia, ensiklopedia bebasNatrium bahasa Indonesia, ensiklopedia bebas
Cationic amino acid transporter 2Cationic amino acid transporter 2
Monosodium glutamateMonosodium glutamate
Glutamic acidGlutamic acid
Chloride channelChloride channel
Adenosine triphosphateAdenosine triphosphate
Lactic acidLactic acid
SLC30A8SLC30A8
FerroportinFerroportin
GLUT1GLUT1
SLC22A1SLC22A1
Štítna žľaza - WikipédiaŠtítna žľaza - Wikipédia
StatinStatin
AntinutrientAntinutrient
MicrodialysisMicrodialysis
GlycolysisGlycolysis
SodiumSodium
VasopressinVasopressin
Lithium-ion batteryLithium-ion battery
Antioxidante - Wikipédia, a enciclopédia livreAntioxidante - Wikipédia, a enciclopédia livre
AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesDisciplines and OccupationsInformation Science
Organic Anion Transporters, Sodium-IndependentOrganic Anion TransportersOrganic Anion Transport Protein 1p-Aminohippuric AcidAnion Transport ProteinsAnionsProbenecidUricosuric AgentsOrganic Anion Transport Polypeptide CEstroneBiological TransportSulfobromophthaleinOrganic Cation Transport ProteinsOrganic Anion Transporters, Sodium-DependentOchratoxinsMultidrug Resistance-Associated ProteinsOrganic Anion Transporters, ATP-DependentCarrier ProteinsATP-Binding Cassette TransportersGlutaratesKidneyTaurocholic AcidKidney Tubules, ProximalMembrane Transport ProteinsDicarboxylic AcidsXenopus laevisDicarboxylic Acid TransportersRNA, ComplementaryUnithiolBile CanaliculiPhenolsulfonphthaleinSodium-Phosphate Cotransporter Proteins, Type IOocytesChoroid PlexusRenal AgentsOrganic Cation Transporter 1Leukotriene C4SymportersHyperbilirubinemia, HereditaryBiological Transport, ActiveLLC-PK1 CellsIndicanPenicillin GHyperbilirubinemia2,4-Dichlorophenoxyacetic AcidSulfinpyrazoneIodopyracetCatecholamine Plasma Membrane Transport ProteinsCefotiamFlounderKineticsMolecular Sequence DataJaundice, Chronic IdiopathicIon TransportMethotrexateLiverMercury IsotopesCimetidineRats, Mutant StrainsDehydroepiandrosterone SulfateRats, Sprague-DawleyCell MembraneCell LineRats, Inbred LECP-GlycoproteinRNA, MessengerTissue DistributionAmino Acid SequenceBileCephaloridineDNA, ComplementarySulfuric Acid EstersPharmaceutical PreparationsAminopterinPravastatinTransfectionSteviaGlutathioneBiotinylationDrug InteractionsPhysiological ProcessesUric AcidP-GlycoproteinsLiddle SyndromeAntiportersXanthurenatesCloning, MolecularHepatocytesSalicylatesKetoglutaric AcidsPropionatesDose-Response Relationship, DrugBlood-Brain BarrierSubstrate SpecificityDrug Resistance, MultipleCOS CellsBile Acids and SaltsCyclic P-OxidesXenobioticsFurosemideBiliary TractCells, CulturedXenopusAnion Exchange Protein 1, ErythrocyteRats, WistarBlotting, NorthernKidney CortexPharmacokineticsKidney TubulesMembrane ProteinsAdenosine TriphosphateDogsGlucuronidesChloridesTritiumToxins, BiologicalSequence Homology, Amino AcidReverse Transcriptase Polymerase Chain ReactionBase SequenceMonocarboxylic Acid TransportersBlotting, WesternGlucose Transporter Type 1CHO CellsCholestasisOrganophosphonatesSodiumHEK293 CellsFolic Acid AntagonistsBilirubinChloride-Bicarbonate AntiportersImmunohistochemistryMonosaccharide Transport ProteinsSerotonin Plasma Membrane Transport ProteinsHepatocyte Nuclear Factor 1-alpha4,4'-Diisothiocyanostilbene-2,2'-Disulfonic AcidGene Expression RegulationMice, KnockoutMetabolic Clearance RateDopamine Plasma Membrane Transport ProteinsCercopithecus aethiopsHistamine H2 AntagonistsAdenineImmunoblottingMercuryCricetulusGene ExpressionRecombinant ProteinsExcitatory Amino Acid Transporter 2Protein BindingCarbon RadioisotopesSulfatesCricetinaeMutagenesis, Site-DirectedDiureticsQuinolinesExcitatory Amino Acid Transporter 3BicarbonatesKillifishesAmino Acid Transport System X-AGModels, BiologicalDNA PrimersBinding SitesHydrogen-Ion ConcentrationMicroinjectionsExcitatory Amino Acid Transporter 1IsoquinolinesBenzbromaroneMolecular StructureNorepinephrine Plasma Membrane Transport ProteinsBrainAmino Acid SubstitutionTime FactorsCarboxylic AcidsFluorescent DyesCation Transport ProteinsGlycocholic AcidStructure-Activity RelationshipCationsAmino Acid Transport SystemsFluoresceinGlucose Transporter Type 3GABA Plasma Membrane Transport ProteinsSex CharacteristicsAmino Acid Transport Systems, NeutralEpithelial CellsAnti-Inflammatory Agents, Non-SteroidalMicrovilliRabbitsGlucose Transporter Type 4FluoresceinsCaco-2 CellsAntiviral AgentsMembrane Transport ModulatorsChromatography, High Pressure LiquidGlycosylationSwineMice, Inbred C57BLMalpighian TubulesEstradiolGlucose Transporter Type 2Digoxin
Solute carrier organic anion transporter family member 1B3 - DrugBankSolute carrier organic anion transporter family member 1B3 - DrugBank
Solute carrier organic anion transporter family member 1B3 - Molecular Target Profile - BCIQSolute carrier organic anion transporter family member 1B3 - Molecular Target Profile - BCIQ
SLCO2A1 Gene - GeneCards | SO2A1 Protein | SO2A1 AntibodySLCO2A1 Gene - GeneCards | SO2A1 Protein | SO2A1 Antibody
SLCO1B3 Gene - GeneCards | SO1B3 Protein | SO1B3 AntibodySLCO1B3 Gene - GeneCards | SO1B3 Protein | SO1B3 Antibody
Solute Carrier Organic Anion Transporter Family Member 1B1 (SLCO1B1) Genotype, Statin, Varies - Mayo Clinic Laboratories |...Solute Carrier Organic Anion Transporter Family Member 1B1 (SLCO1B1) Genotype, Statin, Varies - Mayo Clinic Laboratories |...
SLCO1A2 - wikidocSLCO1A2 - wikidoc
anti-SLCO1A2 antibody | GeneTexanti-SLCO1A2 antibody | GeneTex
Drug Transporters: The Final Frontier for Drug Interactions-Part 2Drug Transporters: The Final Frontier for Drug Interactions-Part 2
Anika Dzierlenga, PhD | College of Pharmacy - University of ArizonaAnika Dzierlenga, PhD | College of Pharmacy - University of Arizona
Membrane & Intracellular Transport | The EMBO JournalMembrane & Intracellular Transport | The EMBO Journal
Organic anion transporter polypeptide (IPR004156) | InterPro | EMBL-EBIOrganic anion transporter polypeptide (IPR004156) | InterPro | EMBL-EBI
Organic anion transporter 4 - WikipediaOrganic anion transporter 4 - Wikipedia
Organic anion transporter 1 - WikipediaOrganic anion transporter 1 - Wikipedia
The multispecific organic anion transporter (OAT) family. - PubMed - NCBIThe multispecific organic anion transporter (OAT) family. - PubMed - NCBI
Organic anion transporter family: current knowledge. - PubMed - NCBIOrganic anion transporter family: current knowledge. - PubMed - NCBI
Identifying the hepatic organic anion transporter: One of many? - Weinman - 2005 - Hepatology - Wiley Online LibraryIdentifying the hepatic organic anion transporter: One of many? - Weinman - 2005 - Hepatology - Wiley Online Library
ABCC3 - Canalicular multispecific organic anion transporter 2 - Homo sapiens (Human) - ABCC3 gene & proteinABCC3 - Canalicular multispecific organic anion transporter 2 - Homo sapiens (Human) - ABCC3 gene & protein
Solute carrier organic anion transporter family member 2B1 - DrugBankSolute carrier organic anion transporter family member 2B1 - DrugBank
Slco2b1 - Solute carrier organic anion transporter family member - Mus musculus (Mouse) - Slco2b1 gene & proteinSlco2b1 - Solute carrier organic anion transporter family member - Mus musculus (Mouse) - Slco2b1 gene & protein
Figure 4 | Active Hydrophilic Components of the Medicinal Herb Salvia miltiorrhiza (Danshen) Potently Inhibit Organic Anion...Figure 4 | Active Hydrophilic Components of the Medicinal Herb Salvia miltiorrhiza (Danshen) Potently Inhibit Organic Anion...
Slco1a5 MGI Mouse Gene Detail - MGI:1351865 - solute carrier organic anion transporter family, member 1a5Slco1a5 MGI Mouse Gene Detail - MGI:1351865 - solute carrier organic anion transporter family, member 1a5
Organic anion transporter F | definition of Organic anion transporter F by Medical dictionaryOrganic anion transporter F | definition of Organic anion transporter F by Medical dictionary
SLCO4A1 (solute carrier organic anion transporter family member 4A1)SLCO4A1 (solute carrier organic anion transporter family member 4A1)
SLCO5A1 (solute carrier organic anion transporter family member 5A1)SLCO5A1 (solute carrier organic anion transporter family member 5A1)
Characterization of Methotrexate Transport and Its Drug Interactions with Human Organic Anion Transporters | Journal of...Characterization of Methotrexate Transport and Its Drug Interactions with Human Organic Anion Transporters | Journal of...
Potential Drug Interactions Mediated by Renal Organic Anion Transporter OATP4C1 | Journal of Pharmacology and Experimental...Potential Drug Interactions Mediated by Renal Organic Anion Transporter OATP4C1 | Journal of Pharmacology and Experimental...
Sodium-independent organic anion transporter E | definition of Sodium-independent organic anion transporter E by Medical...Sodium-independent organic anion transporter E | definition of Sodium-independent organic anion transporter E by Medical...
Human Metabolome Database: Showing Protein Canalicular multispecific organic anion transporter 1 (HMDBP01658)Human Metabolome Database: Showing Protein Canalicular multispecific organic anion transporter 1 (HMDBP01658)
Molecular characterization of the renal organic anion transporter 1 | Springer for Research & DevelopmentMolecular characterization of the renal organic anion transporter 1 | Springer for Research & Development
Solute Carrier Organic Anion Transporter Family Member 1b1 - Semantic ScholarSolute Carrier Organic Anion Transporter Family Member 1b1 - Semantic Scholar
Human Metabolome Database: Showing Protein Solute carrier organic anion transporter family member 2A1 (HMDBP05558)Human Metabolome Database: Showing Protein Solute carrier organic anion transporter family member 2A1 (HMDBP05558)
A Human Canalicular Multispecific Organic Anion Transporter (cMOAT) Gene Is Overexpressed in Cisplatin-resistant Human Cancer...A Human Canalicular Multispecific Organic Anion Transporter (cMOAT) Gene Is Overexpressed in Cisplatin-resistant Human Cancer...
anti-Solute Carrier Family 22 (Organic Anion Transporter), Member 8 (SLC22A8) antibody (Alexa Fluor 488) ABIN909357 from...anti-Solute Carrier Family 22 (Organic Anion Transporter), Member 8 (SLC22A8) antibody (Alexa Fluor 488) ABIN909357 from...
Function of both sinusoidal and canalicular transporters controls the concentration of organic anions within hepatocytes |...Function of both sinusoidal and canalicular transporters controls the concentration of organic anions within hepatocytes |...
Flavonoids Are Inhibitors of Human Organic Anion Transporter 1 (OAT1)-Mediated Transport | Drug Metabolism & DispositionFlavonoids Are Inhibitors of Human Organic Anion Transporter 1 (OAT1)-Mediated Transport | Drug Metabolism & Disposition
FUNCTIONAL ANALYSIS OF AN α-HELICAL REGION IN THE HUMAN MULTIDRUG AND ORGANIC ANION TRANSPORTER MRP1FUNCTIONAL ANALYSIS OF AN α-HELICAL REGION IN THE HUMAN MULTIDRUG AND ORGANIC ANION TRANSPORTER MRP1
Human Renal Organic Anion Transporter 4 Operates as an Asymmetric Urate Transporter | American Society of NephrologyHuman Renal Organic Anion Transporter 4 Operates as an Asymmetric Urate Transporter | American Society of Nephrology
Proton Pump Inhibitors Inhibit Methotrexate Transport by Renal Basolateral Organic Anion Transporter hOAT3 | Drug Metabolism &...Proton Pump Inhibitors Inhibit Methotrexate Transport by Renal Basolateral Organic Anion Transporter hOAT3 | Drug Metabolism &...
AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesDisciplines and OccupationsInformation Science
Organic Anion Transporters, Sodium-IndependentOrganic Anion TransportersOrganic Anion Transport Protein 1p-Aminohippuric AcidAnion Transport ProteinsAnionsProbenecidUricosuric AgentsOrganic Anion Transport Polypeptide CEstroneBiological TransportSulfobromophthaleinOrganic Cation Transport ProteinsOrganic Anion Transporters, Sodium-DependentOchratoxinsMultidrug Resistance-Associated ProteinsOrganic Anion Transporters, ATP-DependentCarrier ProteinsATP-Binding Cassette TransportersGlutaratesKidneyTaurocholic AcidKidney Tubules, ProximalMembrane Transport ProteinsDicarboxylic AcidsXenopus laevisDicarboxylic Acid TransportersRNA, ComplementaryUnithiolBile CanaliculiPhenolsulfonphthaleinSodium-Phosphate Cotransporter Proteins, Type IOocytesChoroid PlexusRenal AgentsOrganic Cation Transporter 1Leukotriene C4SymportersHyperbilirubinemia, HereditaryBiological Transport, ActiveLLC-PK1 CellsIndicanPenicillin GHyperbilirubinemia2,4-Dichlorophenoxyacetic AcidSulfinpyrazoneIodopyracetCatecholamine Plasma Membrane Transport ProteinsCefotiamFlounderKineticsMolecular Sequence DataJaundice, Chronic IdiopathicIon TransportMethotrexateLiverMercury IsotopesCimetidineRats, Mutant StrainsDehydroepiandrosterone SulfateRats, Sprague-DawleyCell MembraneCell LineRats, Inbred LECP-GlycoproteinRNA, MessengerTissue DistributionAmino Acid SequenceBileCephaloridineDNA, ComplementarySulfuric Acid EstersPharmaceutical PreparationsAminopterinPravastatinTransfectionSteviaGlutathioneBiotinylationDrug InteractionsPhysiological ProcessesUric AcidP-GlycoproteinsLiddle SyndromeAntiportersXanthurenatesCloning, MolecularHepatocytesSalicylatesKetoglutaric AcidsPropionatesDose-Response Relationship, DrugBlood-Brain BarrierSubstrate SpecificityDrug Resistance, MultipleCOS CellsBile Acids and SaltsCyclic P-OxidesXenobioticsFurosemideBiliary TractCells, CulturedXenopusAnion Exchange Protein 1, ErythrocyteRats, WistarBlotting, NorthernKidney CortexPharmacokineticsKidney TubulesMembrane ProteinsAdenosine TriphosphateDogsGlucuronidesChloridesTritiumToxins, BiologicalSequence Homology, Amino AcidReverse Transcriptase Polymerase Chain ReactionBase SequenceMonocarboxylic Acid TransportersBlotting, WesternGlucose Transporter Type 1CHO CellsCholestasisOrganophosphonatesSodiumHEK293 CellsFolic Acid AntagonistsBilirubinChloride-Bicarbonate AntiportersImmunohistochemistryMonosaccharide Transport ProteinsSerotonin Plasma Membrane Transport ProteinsHepatocyte Nuclear Factor 1-alpha4,4'-Diisothiocyanostilbene-2,2'-Disulfonic AcidGene Expression RegulationMice, KnockoutMetabolic Clearance RateDopamine Plasma Membrane Transport ProteinsCercopithecus aethiopsHistamine H2 AntagonistsAdenineImmunoblottingMercuryCricetulusGene ExpressionRecombinant ProteinsExcitatory Amino Acid Transporter 2Protein BindingCarbon RadioisotopesSulfatesCricetinaeMutagenesis, Site-DirectedDiureticsQuinolinesExcitatory Amino Acid Transporter 3BicarbonatesKillifishesAmino Acid Transport System X-AGModels, BiologicalDNA PrimersBinding SitesHydrogen-Ion ConcentrationMicroinjectionsExcitatory Amino Acid Transporter 1IsoquinolinesBenzbromaroneMolecular StructureNorepinephrine Plasma Membrane Transport ProteinsBrainAmino Acid SubstitutionTime FactorsCarboxylic AcidsFluorescent DyesCation Transport ProteinsGlycocholic AcidStructure-Activity RelationshipCationsAmino Acid Transport SystemsFluoresceinGlucose Transporter Type 3GABA Plasma Membrane Transport ProteinsSex CharacteristicsAmino Acid Transport Systems, NeutralEpithelial CellsAnti-Inflammatory Agents, Non-SteroidalMicrovilliRabbitsGlucose Transporter Type 4FluoresceinsCaco-2 CellsAntiviral AgentsMembrane Transport ModulatorsChromatography, High Pressure LiquidGlycosylationSwineMice, Inbred C57BLMalpighian TubulesEstradiolGlucose Transporter Type 2Digoxin
PolypeptideSoluteEncodesLocalizationMultispecificCanalicularProteinTransmembrane transporterPolypeptidesHepatic organic anionOATPsProteinsOAT3MediatesKidneySuperfamilyMRP2CharacterizationSpecific Organic Anion TransporterExchangerMetabolismHOAT1 and hOAT3ProstaglandinPolypeptide 1B1Basolateral organic anionTransporting organic anion polypeptideDrug transporterHumanSubstrate specificityPharmacokineticsFunctionalMembrane transportersLiver-specificOATP2B1PolyspecificTransportCassette
Polypeptide1
Solute1
Encodes1
Localization1
Multispecific12
Canalicular1
Protein15
Transmembrane transporter2
Polypeptides3
Hepatic organic anion3
OATPs3
  • Since the numbering of different OATPs in particular species was based originally on the order of discovery, similarly numbered OATPs in humans and rats did not necessarily correspond in function, tissue distribution and substrate specificity (in spite of the name, some OATPs also transport organic cations and neutral molecules) so a scheme of using digits for rat OATPs and letters for human ones was introduced [ PMID: 10873595 ]. (ebi.ac.uk)
  • In addition, the methotrexate transporter OATK is closely related to OATPs. (ebi.ac.uk)
  • Such interactions may result in serious undesired effects and changed drug efficacy, therefore, some studies on interaction between botanical supplement ingredients and drug transporters such as P-gp and OATPs are described here, suggesting that the interaction between botanical supplements and the drug transporters is clinically significant. (mdpi.com)
Proteins10
OAT32
Mediates7
Kidney3
Superfamily4
MRP23
Characterization1
Specific Organic Anion Transporter1
Exchanger1
Metabolism2
HOAT1 and hOAT31
Prostaglandin3
Polypeptide 1B13
Basolateral organic anion1
Transporting organic anion polypeptide1
Drug transporter1
  • Services include evaluation of drug-transporter interactions using in vitro models expressing human and animal transporters from the ABC-binding cassette (ABC) and solute-linked carrier (SLC) superfamilies. (corning.com)
Human7
Substrate specificity1
Pharmacokinetics1
Functional5
Membrane transporters2
Liver-specific1
OATP2B11
Polyspecific2
Transport9
Cassette1
Multispecific Substrate Recognition of Kidney-Specific Organic Anion Transporters OAT-K1 and OAT-K2 | Journal of Pharmacology...
Multispecific Substrate Recognition of Kidney-Specific Organic Anion Transporters OAT-K1 and OAT-K2 | Journal of Pharmacology... (jpet.aspetjournals.org)
Aubagio (Teriflunomide Tablets): Side Effects, Interactions, Warning, Dosage & Uses
Aubagio (Teriflunomide Tablets): Side Effects, Interactions, Warning, Dosage & Uses (rxlist.com)
The Placental Barrier: the Gate and the Fate in Drug Distribution | SpringerLink
The Placental Barrier: the Gate and the Fate in Drug Distribution | SpringerLink (link.springer.com)
Effect of Gene-Mercury Interactions on Mercury Toxicokinetics and Neurotoxicity | SpringerLink
Effect of Gene-Mercury Interactions on Mercury Toxicokinetics and Neurotoxicity | SpringerLink (link.springer.com)
SLCO1B3 gene: MedlinePlus Genetics
SLCO1B3 gene: MedlinePlus Genetics (medlineplus.gov)
Characterization of Methotrexate Transport and Its Drug Interactions with Human Organic Anion Transporters | Journal of...
Characterization of Methotrexate Transport and Its Drug Interactions with Human Organic Anion Transporters | Journal of... (jpet.aspetjournals.org)
Potential Drug Interactions Mediated by Renal Organic Anion Transporter OATP4C1 | Journal of Pharmacology and Experimental...
Potential Drug Interactions Mediated by Renal Organic Anion Transporter OATP4C1 | Journal of Pharmacology and Experimental... (jpet.aspetjournals.org)
ADME-Enabling Technologies in Drug Design and Development | Analytical Chemistry | Chemistry | Subjects | Wiley
ADME-Enabling Technologies in Drug Design and Development | Analytical Chemistry | Chemistry | Subjects | Wiley (wiley.com)
Solute carrier organic anion transporter family member 2B1 - DrugBank
Solute carrier organic anion transporter family member 2B1 - DrugBank (drugbank.ca)
IJMS | Free Full-Text | Transcriptomic Analysis in Diabetic Nephropathy of Streptozotocin-Induced Diabetic Rats | HTML
IJMS | Free Full-Text | Transcriptomic Analysis in Diabetic Nephropathy of Streptozotocin-Induced Diabetic Rats | HTML (mdpi.com)
Antitargets and Drug Safety | Drug Discovery & Development | Pharmaceutical & Medicinal Chemistry | Chemistry | Subjects | Wiley
Antitargets and Drug Safety | Drug Discovery & Development | Pharmaceutical & Medicinal Chemistry | Chemistry | Subjects | Wiley (wiley.com)
Fycompa (Perampanel Tablets, for Oral Use): Side Effects, Interactions, Warning, Dosage & Uses
Fycompa (Perampanel Tablets, for Oral Use): Side Effects, Interactions, Warning, Dosage & Uses (rxlist.com)
Drug Delivery: Principles and Applications, 2nd Edition | Drug Formulation & Delivery | Pharmaceutical & Medicinal Chemistry |...
Drug Delivery: Principles and Applications, 2nd Edition | Drug Formulation & Delivery | Pharmaceutical & Medicinal Chemistry |... (wiley.com)
Isolation and characterization of a digoxin transporter and its rat homologue expressed in the kidney | PNAS
Isolation and characterization of a digoxin transporter and its rat homologue expressed in the kidney | PNAS (pnas.org)
Compound Report Card
Compound Report Card (ebi.ac.uk)
CHEMBL2106240 Compound Report Card
CHEMBL2106240 Compound Report Card (ebi.ac.uk)
Compound Report Card
Compound Report Card (ebi.ac.uk)
Compound Report Card
Compound Report Card (ebi.ac.uk)
Compound Report Card
Compound Report Card (ebi.ac.uk)
RCSB PDB - QUE Ligand Summary Page
RCSB PDB - QUE Ligand Summary Page (rcsb.org)
SLCO4A1 (solute carrier organic anion transporter family member 4A1)
SLCO4A1 (solute carrier organic anion transporter family member 4A1) (atlasgeneticsoncology.org)
Human Metabolome Database: Showing Protein Canalicular multispecific organic anion transporter 1 (HMDBP01658)
Human Metabolome Database: Showing Protein Canalicular multispecific organic anion transporter 1 (HMDBP01658) (hmdb.ca)
SLCO5A1 (solute carrier organic anion transporter family member 5A1)
SLCO5A1 (solute carrier organic anion transporter family member 5A1) (atlasgeneticsoncology.org)