• A novel human hepatic organic anion transporting polypeptide (OATP2). (wikipedia.org)
  • In study B, 23 patients with castration-resistant prostate cancer received probes for CYP3A4 (midazolam), CYP2C9 (warfarin), CYP2C19 (omeprazole), and CYP2C8 (pioglitazone), and transporter substrates for P-glycoprotein (P-gp) (fexofenadine) and breast cancer resistance protein (BCRP)/organic anion transporting polypeptide (OATP) 1B1 (rosuvastatin) at baseline and after repeat once-daily administration of apalutamide 240 mg to steady state. (springer.com)
  • Transporters such as organic anion-transporting polypeptide 1A2, P-glycoprotein, human organic cation transporter 1, and multidrug and toxin extrusion protein 1 are involved in the pharmacokinetics of LVX. (dovepress.com)
  • We examined expression levels of organic anion-transporting polypeptide (OATP)1B1, OATP1B3, OATP1B7, and organic anion transporter (OAT)1 as solute carrier transporters and multidrug resistance-associated protein (MRP)1 and MRP2 as ATP-binding cassette transporters, using real-time polymerase chain reaction and accumulation of 3 H-MTX in cancer cells after 10-Gy irradiation, assuming stereotactic body radiotherapy. (frontiersin.org)
  • Hepatic uptake of cholephilic organic compounds is mediated by members of the organic anion-transporting polypeptide (OATP) family. (nih.gov)
  • Impact of organic anion transporting polypeptide, P-glycoprotein, and breast cancer resistance protein transporters on observed tamoxifen and endoxifen concentration and adverse effects. (cdc.gov)
  • PURPOSE: Recent in vitro studies demonstrated that dasatinib inhibits organic cation transporter 2 (OCT2), multidrug and toxin extrusion proteins (MATEs), and organic anion transporting polypeptide 1B1/1B3 (OATP1B1/1B3). (bvsalud.org)
  • We cloned Xenopus monocarboxylate transporter 8 (mct8) and organic anion-transporting polypeptide 1C1 (oatpc1c1), focusing on these two transporters given their importance for vertebrate brain development. (researcher-app.com)
  • BSEP, Na+-taurocholate cotransporting polypeptide, and organic anion transporting polypeptide B were downregulated with most cholestatic and some noncholestatic drugs, whereas deregulation of multidrug resistance-associated proteins was more variable, probably mainly reflecting secondary effects. (hal.science)
  • The overall homology with human LST-1 was 60.2%, which is the highest among all known organic anion transporters. (nih.gov)
  • rlst-1 is a counterpart of human LST-1 and is one of the important transporters in rat liver for the clearance of bile acid. (nih.gov)
  • For instance, DTG decreases the renal clearance of metformin by inhibiting organic cation transporters in renal tubular cells. (medscape.com)
  • Protein expression and function of organic anion transporters in short-term and long-term cultures of Huh7 human hepatoma cells. (cancerindex.org)
  • In our studies on neurotransmitter metabolism we have focused our efforts on transporters, a functional class of proteins that move neurotransmitters and other small molecules across membranes in cells. (stanford.edu)
  • We functionally characterized the two transporters using a radiolabeled hormones in vitro uptake assay in COS-1 cells. (researcher-app.com)
  • Transport of 16 substrates was measured for each individual human OATP in complementary RNA-injected Xenopus laevis oocytes. (nih.gov)
  • OATP-B also transported estrone-3-sulfate but not bile salts. (nih.gov)
  • OATP-B, OATP-C, and OATP8 account for the major part of sodium-independent bile salt, organic anion, and drug clearance of human liver. (nih.gov)
  • Recently, we isolated a new complementary DNA (cDNA) encoding human liver-specific organic anion transporter (LST-1), representing the multispecificity of human liver. (nih.gov)
  • Protein alignment and bootstrap analysis showed that Xenopus mct8 and oatp1c1 are closer to their mammalian orthologs than their teleost counterparts. (researcher-app.com)
  • Xenopus mct8 was found to actively transport both T3 and T4 bidirectionally. (researcher-app.com)
  • Again similar to humans, Xenopus oatp1c1 transported T4 but not T3, MIT, or DIT. (researcher-app.com)
  • We applied a recently developed in vitro-in vivo extrapolation method, including hepatic metabolism and transport processes, herein referred to as the Extended Clearance Concept Classification System (ECCCS). (degruyter.com)
  • 6. Camenisch G, Umehara K. Predicting human hepatic clearance from in vitro drug metabolism and transport data: a scientific and pharmaceutical perspective for assessing drug-drug interactions. (degruyter.com)
  • Human-derived hepatic cell lines are a valuable alternative to primary hepatocytes for drug metabolism, transport and toxicity studies. (cancerindex.org)
  • Overall goal was to isolate an anion transport protein found in proximal convoluted tubule cells of rat kidney nephron. (bepress.com)
  • Cleared renally - 50% of the administered dose is eliminated in this way, mainly by active secretion via the OAT organic anion transport proteins in the proximal convoluted tubule. (derangedphysiology.com)
  • To evaluate the structural features of GSH required for interaction with the protein, we investigated the ability of a series of GSH analogs to enhance GSH stimulatable transport of [ 3 H]estrone 3-sulfate (E 1 SO 4 ). (aspetjournals.org)
  • Transports dehydroepiandrosterone sulfate, estrone-3-sulfate, and pregnenolone sulfate with Km values of 30, 12 and 11 μM, respectively. (tcdb.org)
  • γ-Glu-Leu-Gly was 1.6-fold more effective than GSH in stimulating E 1 SO 4 uptake, and kinetic analysis indicated this was due to an increased V max . (aspetjournals.org)
  • Importantly, both hOAT1 and rat renal organic anion transporter 1 (rROAT1) mediated saturable, probenecid-sensitive uptake of cidofovir, adefovir, and other nucleoside phosphonate antivirals. (aspetjournals.org)
  • Evodiamine enhanced the uptake (from 154.85 ± 23.17 to 198.48 ± 26.31 pmol/mg protein) and distribution (from 736.61 ± 108.07 to 911.89 ± 124.64 ng/g tissue) of pravastatin in NASH rat liver. (bvsalud.org)
  • It is capable of transporting a variety organic anions and mediates sodium-independent uptake of bile in the liver. (nih.gov)
  • 14C-TEA uptake in hOCT1 plasmid DNA-transfected HeLa cells was trans-stimulated by unlabeled TEA and 1-methyl-4-phenyl-pyridinium. (drugbank.com)
  • Pombrio JM, Giangreco A, Li L, Wempe MF, Anders MW, Sweet DH, Pritchard JB, Ballatori N. Mercapturic acids (N-acetylcysteine S-conjugates) as endogenous substrates for the renal organic anion transporter-1. (ucdenver.edu)
  • A cDNA clone was isolated from a human renal library and designated human organic anion transporter 1 (hOAT1). (aspetjournals.org)
  • This keynote address will describe new drugs emerging from studies of the VHL tumor suppressor protein (pVHL), which is usually defective in clear cell renal cell carcinomas (ccRCCs). (aspet.org)
  • MDR1/ABCB1, MRP2/ABCC2, and breast cancer resistance protein (BCRP)/ABCG2 are expressed in the liver and intestine and contribute to the disposition of many drugs. (aspetjournals.org)
  • The present study was designed to determine whether rosuvastatin is transported by MDR1, MRP2, and BCRP. (aspetjournals.org)
  • The ABCC2 gene provides instructions for producing a protein called multidrug resistance protein 2 (MRP2). (medlineplus.gov)
  • MRP2 also transports a substance called bilirubin out of liver cells and into bile (a digestive fluid produced by the liver). (medlineplus.gov)
  • Most of the mutations change single protein building blocks (amino acids) in MRP2. (medlineplus.gov)
  • The accumulation of other substances that usually get transported out of tissues by the MRP2 protein can cause additional signs and symptoms in people with Dubin-Johnson syndrome, but these features usually do not cause health problems. (medlineplus.gov)
  • Structure and function of the MRP2 (ABCC2) protein and its role in drug disposition. (medlineplus.gov)
  • Keitel V, Nies AT, Brom M, Hummel-Eisenbeiss J, Spring H, Keppler D. A common Dubin-Johnson syndrome mutation impairs protein maturation and transport activity of MRP2 (ABCC2). (medlineplus.gov)
  • rlst-1 encodes 652 amino acids, predicting at least 11 transmembrane regions. (nih.gov)
  • E 1 SO 4 transport activity surpassed GSH-stimulated levels in the presence of tripeptides in which Cys was substituted with the hydrophobic amino acids Leu, Phe, and homo-Phe. (aspetjournals.org)
  • Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). (drugbank.com)
  • The Ki values of several compounds in interacting with hOCT1 differed substantially from the corresponding values for the rat organic cation transporter, rOCT1, and the human kidney-specific organic cation transporter, hOCT2, determined in previous studies. (drugbank.com)
  • Transiently transfected HeLa cells represent a useful tool in studying the interactions and kinetics of organic cations and other xenobiotics with hOCT1 and in understanding the molecular events involved in organic cation transport. (drugbank.com)
  • This protein is one of a family of multidrug resistance proteins involved in the transport of substances out of cells. (medlineplus.gov)
  • Some substances, such as phenytoin and calcium, are bound extensively to proteins such as albumin. (ashp.org)
  • Solute carrier organic anion transporter family member 1B1 is a protein that in humans is encoded by the SLCO1B1 gene. (wikipedia.org)
  • BOPTA transport by multidrug resistance associated protein 2 induced an aquaporin-mediated water transport, whereas MEB transport did not. (aspetjournals.org)
  • Figure 9.1 Overview of bilirubin metabolism and transport. (projecttulip.org)
  • The primary defect in Dubin-Johnson syndrome is a mutation in an apical canalicular membrane protein responsible for the excretion of bilirubin and other nonbile salt organic anions. (medscape.com)
  • In addition, the transport of certain MRP1 substrates is stimulated by the presence of GSH. (aspetjournals.org)
  • An Eadie-Hofstee analysis suggested that there were two transport sites in BCRP, with an apparent K m of 10.8 μM for the high affinity site and 307 μM for the low affinity site. (aspetjournals.org)
  • These data demonstrate that rosuvastatin is transported efficiently by BCRP and suggest that BCRP plays a significant role in the disposition of rosuvastatin. (aspetjournals.org)
  • It mediates the coupled exchange of alpha-ketoglutarate with organic ions such as P-AMINOHIPPURIC ACID. (ucdenver.edu)
  • We have previously shown that the multi-drug resistance protein (MRP) mediates the ATP-dependent membrane transport of glutathione S-conjugates and additional amphiphilic organic anions. (silverchair.com)
  • Thesis Objectives: Prepared organic compounds in an organic synthesis laboratory. (bepress.com)
  • The gills play a role in the excretion of some organic compounds (log P (astm.org)
  • We tested the interaction of an array of organic cations and other compounds with hOCT1 by determining Ki values in inhibiting 14C-tetraethylammonium (TEA) transport in the transfected cells. (drugbank.com)
  • Arsenic compounds exist in a number of inorganic and organic forms. (cdc.gov)
  • Other inorganic arsenic compounds may vary somewhat in relative toxicity, and organic arsenic compounds appear to be essentially nontoxic. (cdc.gov)
  • Some organic arsenic compounds may be used as pesticides or as additives in animal feed. (cdc.gov)
  • However, polar compounds, which account for most drug metabolites, cannot diffuse back into the circulation and are excreted unless a specific transport mechanism exists for their reabsorption (eg, as for glucose, ascorbic acid , and B vitamins). (msdmanuals.com)
  • The apparent permeability value for rosuvastatin across MDR1-Madin-Darby canine kidney cells was low (∼8 nm/s), and no directional transport was observed. (aspetjournals.org)
  • Rosuvastatin transport occurred into an osmotically sensitive space and was saturable. (aspetjournals.org)
  • [ 1 ] This rare autosomal recessive condition is characterized by conjugated hyperbilirubinemia with normal liver transaminases, a unique pattern of urinary excretion of heme metabolites (coproporphyrins), and the deposition of a pigment that gives the liver a characteristic black color (see the image below). (medscape.com)
  • Our results indicate that the absence of Mrp or an isoform of Mrp from the canalicular membrane is the basis for the hereditary defect of the hepatobiliary excretion of anionic conjugates by the transport-deficient hepatocyte. (silverchair.com)
  • The ECCCS represents a powerful tool to anticipate the DDI potential of victim drugs based on in vitro drug metabolism and transport data. (degruyter.com)
  • This review attempts to summarize the effects of inorganic, organometallic, and organic pollutants on gill physiology, biochemistry, and histopathology. (astm.org)
  • Inorganic anions also appear to affect ionoregulation. (astm.org)
  • The responsible nonsense mutation affects the protein product of ank, resulting in diminished production of extracellular inorganic pyrophosphate, an important inhibitor of nucleation and of the growth of apatite crystals. (biomedcentral.com)
  • The ank gene product is one of several cell membrane proteins, including ectonucleoside triphosphate pyrophosphohydrolase enzymes and alkaline phosphatase, that regulate extracellular inorganic pyrophosphate levels and thereby regulate mineralization. (biomedcentral.com)
  • A landmark investigation into the genetic basis of murine progressive ankylosis has clarified the physiologic role of extracellular inorganic pyrophosphate (ePPi) in suppressing pathologic deposition of basic calcium phosphate (BCP) (an inclusive term for hydroxyapatite, octacalcium phosphate, and tricalcium phosphate) in articular tissue [ 1 ]. (biomedcentral.com)
  • A number of endogenous systems, such as the aerobic metabolism and electron transport chains, generate highly reactive molecules with important biological functions known as reactive oxygen species (ROS), including superoxide and hydrogen peroxide (H2O2). (bvsalud.org)
  • 1] "Cloning and functional characterization of human sodium-dependent organic anion transporter (SLC10A6). (tcdb.org)
  • However, their relevance for investigations of drug-drug and drug-organic anion (e.g., bile acid, steroid hormone) interactions at the transporter level remains to be established. (cancerindex.org)
  • In addition, this tripeptide was shown to be a competitive inhibitor of apigenin-stimulated GSH transport ( K i value of 14 μM), confirming that it either interacts with the same site on MRP1 as GSH or that the binding of the two tripeptides is mutually exclusive. (aspetjournals.org)
  • Filgotinib, an oral Janus kinase-1 preferential inhibitor, is approved in Europe and Japan for adults with rheumatoid arthritis. (bvsalud.org)
  • Cotreatment with ROCK inhibitor Y-27632 [4-(1-aminoethyl)-N-(4-pyridyl) cyclohexanecarboxamide dihydrochloride] and MLCK activator calmodulin reduced bile canaliculi constriction and dilatation, respectively, confirming the role of these pathways in drug-induced intrahepatic cholestasis. (hal.science)
  • BMC research notes 2022 3 15 (1): 104. (cdc.gov)
  • Pharmacogenetics and genomics 2022 11 33 (1): 10-18. (cdc.gov)
  • 60(1): 359-373, 2022 Dec. (bvsalud.org)
  • In vitro transcription-translation Proteins were synthesised by in vitro transcription/translation using the PURESYSTEM kit (NEB). (icem2012.org)
  • Additionally, TCTP has been ascribed a role in DNA damage sensing and restoration, forming complexes with ATM and the DNA binding subunits Ku70 and Ku80 of DNA-dependent protein kinase [16]. (icem2012.org)
  • Signaling mechanisms involved in the regulation of ePPi formation are poorly understood, but adenylyl cyclase activation decreases and protein kinase C activation increases the accumulation of ePPi in media surrounding cartilage or chondrocyte cultures [ 7 ]. (biomedcentral.com)
  • The human multidrug resistance protein 1 (MRP1) is a primary active transporter of reduced (GSH) and oxidized glutathione, as well as GSH-, glucuronate-, and sulfate-conjugated organic anions. (aspetjournals.org)
  • The transport function of the mrp gene-encoded conjugate export pump was assayed in plasma membrane vesicles with leukotriene C4 as a high-affinity glutathione S-conjugate substrate. (silverchair.com)
  • While SOD catalyzes the dismutation of superoxide anion (O2') to H2O2, catalase and glutathione (peroxidase, reductase) system reduce cellular toxicity degrading peroxides into oxygen and water 9 . (bvsalud.org)
  • The aim of this study was to isolate a rat counterpart of human LST-1 and examine the expression regulation of its messenger RNA (mRNA) to clarify the molecular basis of cholestasis. (nih.gov)
  • rlst-1 also belongs to the same new gene family as human LST-1, located between the organic anion transporter family and the prostaglandin transporter. (nih.gov)
  • What does this gene/protein do? (cancerindex.org)
  • These diseases are the result of a defect in transport of sialic acid across lysosomal membranes and are associated with mutations in the gene encoding the sialic acid transporter sialin. (stanford.edu)
  • Expression of the MRP gene-encoded conjugate export pump in liver and its selective absence from the canalicular membrane in transport-deficient mutant hepatocytes. (silverchair.com)
  • Organic Anion Transport Protein 1" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (ucdenver.edu)
  • Serotonin Plasma Membrane Transport Proteins" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (musc.edu)
  • Double immunofluorescence microscopy of livers from transport-deficient TR- mutant rats localized Mrp only to the lateral but not to the canalicular membrane. (silverchair.com)
  • 2019;381(1):13-24. (springer.com)
  • RARITAN, N.J., September 17, 2019 - The Janssen Pharmaceutical Companies of Johnson & Johnson announced today multiple data presentations from its prostate cancer and solid tumor portfolios will be featured at the European Society for Medical Oncology (ESMO) Annual Congress 2019, taking place September 27 to October 1 in Barcelona, Spain. (jnj.com)
  • Wagner F, Kunz TC, Chowdhury SR, Thiede B, Fraunholz M , Eger D, Kozjak-Pavlovic V. Armadillo repeat-containing protein 1 is a dual localization protein associated with mitochondrial intermembrane space bridging complex. (uni-wuerzburg.de)
  • The inhibition of influx is due in large part to the binding of metal ions to sulphydryl groups on transport proteins (ATPases), while the stimulation of efflux appears to be governed by the displacement of calcium from the intercellular tight junctions of the epithelial cells. (astm.org)
  • The parotid gland has serous cells in abundance, which produce a salivary secretion with abundant water and electrolytes responsible for the buffering capacity and protection of dental surface 1 . (bvsalud.org)
  • The proteins synthesized by parotid acinar cells are stored in large secretory granules whose composition includes α-amylase, leucine-rich parotid secretory protein (PSP), and proline-rich proteins (PRPs), in addition to multiple minor components 2-3 related to digestive and protective functions. (bvsalud.org)
  • This protein is also identified as an ovarian-tumor-specific antigen. (childrensmercy.org)
  • Introduction TCTP, also known as Fortilin/Histamine Releasing Element (HRF), was first discovered over two decades ago as a growth promoting factor in Ehrlich ascites tumor [1]. (icem2012.org)
  • The elaboration of ePPi by chondrocytes is a bioregulable process, enhanced by transforming growth factor β, ascorbate, retinoic acid, bone morphogenetic protein, transglutaminase, and thyroid hormones and diminished by parathyroid-hormone-related peptide isoforms, insulin-like growth factor-1, tumor necrosis factor α, and interleukin 1. (biomedcentral.com)
  • A polyspecific transporter for organic cations found primarily in the kidney. (ucdenver.edu)
  • The expression of rlst-1 may be under feedback regulation of cholestasis by biliary obstruction and/or sepsis. (nih.gov)