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).
Conjugated protein-carbohydrate compounds including mucins, mucoid, and amyloid glycoproteins.
A 44-kDa highly glycosylated plasma protein that binds phospholipids including CARDIOLIPIN; APOLIPOPROTEIN E RECEPTOR; membrane phospholipids, and other anionic phospholipid-containing moieties. It plays a role in coagulation and apoptotic processes. Formerly known as apolipoprotein H, it is an autoantigen in patients with ANTIPHOSPHOLIPID ANTIBODIES.
Layers of protein which surround the capsid in animal viruses with tubular nucleocapsids. The envelope consists of an inner layer of lipids and virus specified proteins also called membrane or matrix proteins. The outer layer consists of one or more types of morphological subunits called peplomers which project from the viral envelope; this layer always consists of glycoproteins.
Platelet membrane glycoprotein complex essential for normal platelet adhesion and clot formation at sites of vascular injury. It is composed of three polypeptides, GPIb alpha, GPIb beta, and GPIX. Glycoprotein Ib functions as a receptor for von Willebrand factor and for thrombin. Congenital deficiency of the GPIb-IX complex results in Bernard-Soulier syndrome. The platelet glycoprotein GPV associates with GPIb-IX and is also absent in Bernard-Soulier syndrome.
Proteins which contain carbohydrate groups attached covalently to the polypeptide chain. The protein moiety is the predominant group with the carbohydrate making up only a small percentage of the total weight.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
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.
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.
Within a eukaryotic cell, a membrane-limited body which contains chromosomes and one or more nucleoli (CELL NUCLEOLUS). The nuclear membrane consists of a double unit-type membrane which is perforated by a number of pores; the outermost membrane is continuous with the ENDOPLASMIC RETICULUM. A cell may contain more than one nucleus. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)
Carbohydrates consisting of between two (DISACCHARIDES) and ten MONOSACCHARIDES connected by either an alpha- or beta-glycosidic link. They are found throughout nature in both the free and bound form.
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.
External envelope protein of the human immunodeficiency virus which is encoded by the HIV env gene. It has a molecular weight of 120 kDa and contains numerous glycosylation sites. Gp120 binds to cells expressing CD4 cell-surface antigens, most notably T4-lymphocytes and monocytes/macrophages. Gp120 has been shown to interfere with the normal function of CD4 and is at least partly responsible for the cytopathic effect of HIV.
Transmembrane envelope protein of the HUMAN IMMUNODEFICIENCY VIRUS which is encoded by the HIV env gene. It has a molecular weight of 41,000 and is glycosylated. The N-terminal part of gp41 is thought to be involved in CELL FUSION with the CD4 ANTIGENS of T4 LYMPHOCYTES, leading to syncytial formation. Gp41 is one of the most common HIV antigens detected by IMMUNOBLOTTING.
An envelope protein of the human immunodeficiency virus that is encoded by the HIV env gene. It has a molecular weight of 160,000 kDa and contains numerous glycosylation sites. It serves as a precursor for both the HIV ENVELOPE PROTEIN GP120 and the HIV ENVELOPE PROTEIN GP41.
Subpopulation of CD4+ lymphocytes that cooperate with other lymphocytes (either T or B) to initiate a variety of immune functions. For example, helper-inducer T-cells cooperate with B-cells to produce antibodies to thymus-dependent antigens and with other subpopulations of T-cells to initiate a variety of cell-mediated immune functions.
Purifying or cleansing agents, usually salts of long-chain aliphatic bases or acids, that exert cleansing (oil-dissolving) and antimicrobial effects through a surface action that depends on possessing both hydrophilic and hydrophobic properties.
A class of morphologically heterogeneous cytoplasmic particles in animal and plant tissues characterized by their content of hydrolytic enzymes and the structure-linked latency of these enzymes. The intracellular functions of lysosomes depend on their lytic potential. The single unit membrane of the lysosome acts as a barrier between the enzymes enclosed in the lysosome and the external substrate. The activity of the enzymes contained in lysosomes is limited or nil unless the vesicle in which they are enclosed is ruptured. Such rupture is supposed to be under metabolic (hormonal) control. (From Rieger et al., Glossary of Genetics: Classical and Molecular, 5th ed)
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.
A stack of flattened vesicles that functions in posttranslational processing and sorting of proteins, receiving them from the rough ENDOPLASMIC RETICULUM and directing them to secretory vesicles, LYSOSOMES, or the CELL MEMBRANE. The movement of proteins takes place by transfer vesicles that bud off from the rough endoplasmic reticulum or Golgi apparatus and fuse with the Golgi, lysosomes or cell membrane. (From Glick, Glossary of Biochemistry and Molecular Biology, 1990)
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).
Antigens on surfaces of cells, including infectious or foreign cells or viruses. They are usually protein-containing groups on cell membranes or walls and may be isolated.
Established cell cultures that have the potential to propagate indefinitely.
Development of neutralizing antibodies in individuals who have been exposed to the human immunodeficiency virus (HIV/HTLV-III/LAV).
Any of several carnivores in the family CANIDAE, that possess erect ears and long bushy tails and are smaller than WOLVES. They are classified in several genera and found on all continents except Antarctica.
That branch of learning which brings together theories and studies on communication and control in living organisms and machines.
The outermost layer of a cell in most PLANTS; BACTERIA; FUNGI; and ALGAE. The cell wall is usually a rigid structure that lies external to the CELL MEMBRANE, and provides a protective barrier against physical or chemical agents.
Insect members of the superfamily Apoidea, found almost everywhere, particularly on flowers. About 3500 species occur in North America. They differ from most WASPS in that their young are fed honey and pollen rather than animal food.
Infections with viruses of the genus HANTAVIRUS. This is associated with at least four clinical syndromes: HEMORRHAGIC FEVER WITH RENAL SYNDROME caused by viruses of the Hantaan group; a milder form of HFRS caused by SEOUL VIRUS; nephropathia epidemica caused by PUUMALA VIRUS; and HANTAVIRUS PULMONARY SYNDROME caused by SIN NOMBRE VIRUS.
A plant genus of the family ORCHIDACEAE which depends on the fungus Armillaria mellea to complete its life cycle. It is an ingredient of Zhenxuanyin (DRUGS, CHINESE HERBAL).
The characteristic 3-dimensional shape and arrangement of multimeric proteins (aggregates of more than one polypeptide chain).
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
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.
A protein that accounts for more than half of the peripheral nervous system myelin protein. The extracellular domain of this protein is believed to engage in adhesive interactions and thus hold the myelin membrane compact. It can behave as a homophilic adhesion molecule through interactions with its extracellular domains. (From J Cell Biol 1994;126(4):1089-97)
Antibodies produced by a single clone of cells.
Technique using an instrument system for making, processing, and displaying one or more measurements on individual cells obtained from a cell suspension. Cells are usually stained with one or more fluorescent dyes specific to cell components of interest, e.g., DNA, and fluorescence of each cell is measured as it rapidly transverses the excitation beam (laser or mercury arc lamp). Fluorescence provides a quantitative measure of various biochemical and biophysical properties of the cell, as well as a basis for cell sorting. Other measurable optical parameters include light absorption and light scattering, the latter being applicable to the measurement of cell size, shape, density, granularity, and stain uptake.
Exclusive legal rights or privileges applied to inventions, plants, etc.
The property of antibodies which enables them to react with some ANTIGENIC DETERMINANTS and not with others. Specificity is dependent on chemical composition, physical forces, and molecular structure at the binding site.
Immunoglobulin molecules having a specific amino acid sequence by virtue of which they interact only with the ANTIGEN (or a very similar shape) that induced their synthesis in cells of the lymphoid series (especially PLASMA CELLS).
Written or other literary works whose subject matter is medical or about the profession of medicine and related areas.
A composition in prose or verse presenting in dialogue or pantomime a story involving various characters, usually intended to be acted on a stage and to be regarded as a form of entertainment. (From Random House Unabridged Dictionary, 2d ed)
The study of natural phenomena by observation, measurement, and experimentation.
The fourth planet in order from the sun. Its two natural satellites are Deimos and Phobos. It is one of the four inner or terrestrial planets of the solar system.
The presence of antibodies directed against phospholipids (ANTIBODIES, ANTIPHOSPHOLIPID). The condition is associated with a variety of diseases, notably systemic lupus erythematosus and other connective tissue diseases, thrombopenia, and arterial or venous thromboses. In pregnancy it can cause abortion. Of the phospholipids, the cardiolipins show markedly elevated levels of anticardiolipin antibodies (ANTIBODIES, ANTICARDIOLIPIN). Present also are high levels of lupus anticoagulant (LUPUS COAGULATION INHIBITOR).
Three or more consecutive spontaneous abortions.
Autoantibodies directed against phospholipids. These antibodies are characteristically found in patients with systemic lupus erythematosus (LUPUS ERYTHEMATOSUS, SYSTEMIC;), ANTIPHOSPHOLIPID SYNDROME; related autoimmune diseases, some non-autoimmune diseases, and also in healthy individuals.
Antiphospholipid antibodies found in association with systemic lupus erythematosus (LUPUS ERYTHEMATOSUS, SYSTEMIC;), ANTIPHOSPHOLIPID SYNDROME; and in a variety of other diseases as well as in healthy individuals. The antibodies are detected by solid-phase IMMUNOASSAY employing the purified phospholipid antigen CARDIOLIPIN.

A single membrane-embedded negative charge is critical for recognizing positively charged drugs by the Escherichia coli multidrug resistance protein MdfA. (1/3809)

The nature of the broad substrate specificity phenomenon, as manifested by multidrug resistance proteins, is not yet understood. In the Escherichia coli multidrug transporter, MdfA, the hydrophobicity profile and PhoA fusion analysis have so far identified only one membrane-embedded charged amino acid residue (E26). In order to determine whether this negatively charged residue may play a role in multidrug recognition, we evaluated the expression and function of MdfA constructs mutated at this position. Replacing E26 with the positively charged residue lysine abolished the multidrug resistance activity against positively charged drugs, but retained chloramphenicol efflux and resistance. In contrast, when the negative charge was preserved in a mutant with aspartate instead of E26, chloramphenicol recognition and transport were drastically inhibited; however, the mutant exhibited almost wild-type multidrug resistance activity against lipophilic cations. These results suggest that although the negative charge at position 26 is not essential for active transport, it dictates the multidrug resistance character of MdfA. We show that such a negative charge is also found in other drug resistance transporters, and its possible significance regarding multidrug resistance is discussed.  (+info)

Overexpression of the multidrug resistance-associated protein (MRP1) in human heavy metal-selected tumor cells. (2/3809)

Cellular and molecular mechanisms involved in the resistance to cytotoxic heavy metals remain largely to be characterized in mammalian cells. To this end, we have analyzed a metal-resistant variant of the human lung cancer GLC4 cell line that we have selected by a step-wise procedure in potassium antimony tartrate. Antimony-selected cells, termed GLC4/Sb30 cells, poorly accumulated antimony through an enhanced cellular efflux of metal, thus suggesting up-regulation of a membrane export system in these cells. Indeed, GLC4/Sb30 cells were found to display a functional overexpression of the multidrug resistance-associated protein MRP1, a drug export pump, as demonstrated by Western blotting, reverse transcriptase-polymerase chain reaction and calcein accumulation assays. Moreover, MK571, a potent inhibitor of MRP1 activity, was found to markedly down-modulate resistance of GLC4/Sb30 cells to antimony and to decrease cellular export of the metal. Taken together, our data support the conclusion that overexpression of functional MRP1 likely represents one major mechanism by which human cells can escape the cytotoxic effects of heavy metals.  (+info)

Influence of tangeretin on tamoxifen's therapeutic benefit in mammary cancer. (3/3809)

BACKGROUND: Tamoxifen and the citrus flavonoid tangeretin exhibit similar inhibitory effects on the growth and invasive properties of human mammary cancer cells in vitro; furthermore, the two agents have displayed additive effects in vitro. In this study, we examined whether tangeretin would enhance tamoxifen's therapeutic benefit in vivo. METHODS: Female nude mice (n = 80) were inoculated subcutaneously with human MCF-7/6 mammary adenocarcinoma cells. Groups of 20 mice were treated orally by adding the following substances to their drinking water: tamoxifen (3 x 10(-5) M), tangeretin (1 x 10(-4) M), tamoxifen plus tangeretin (3 x 10(-5) M plus 1 x 10(-4) M), or solvent. RESULTS AND CONCLUSIONS: Oral treatment of mice with tamoxifen resulted in a statistically significant inhibition of tumor growth compared with solvent treatment (two-sided P = .001). Treatment with tangeretin did not inhibit tumor growth, and addition of this compound to drinking water with tamoxifen completely neutralized tamoxifen's inhibitory effect. The median survival time of tumor-bearing mice treated with tamoxifen plus tangeretin was reduced in comparison with that of mice treated with tamoxifen alone (14 versus 56 weeks; two-sided P = .002). Tangeretin (1 x 10(-6) M or higher) inhibited the cytolytic effect of murine natural killer cells on MCF-7/6 cells in vitro, which may explain why tamoxifen-induced inhibition of tumor growth in mice is abolished when tangeretin is present in drinking water. IMPLICATIONS: We describe an in vivo model to study potential interference of dietary compounds, such as flavonoids, with tamoxifen, which could lead to reduced efficacy of adjuvant therapy. In our study, the tumor growth-inhibiting effect of oral tamoxifen was reversed upon addition of tangeretin to the diet. Our data argue against excessive consumption of tangeretin-added products and supplements by patients with mammary cancer during tamoxifen treatment.  (+info)

Multidrug resistance (MDR1) P-glycoprotein enhances esterification of plasma membrane cholesterol. (4/3809)

Class I P-glycoproteins (Pgp) confer multidrug resistance in tumors, but the physiologic function of Pgp in normal tissues remains uncertain. In cells derived from tissues that normally express Pgp, recent data suggest a possible role for Pgp in cholesterol trafficking from the plasma membrane to the endoplasmic reticulum. We investigated the esterification of plasma membrane cholesterol under basal conditions and in response to sphingomyelinase treatment in transfected and drug-selected cell lines expressing differing amounts of functional class I Pgp. Compared with parental NIH 3T3 fibroblasts, cells transfected with human multidrug resistance (MDR1) Pgp esterified more cholesterol both without and with sphingomyelinase. Esterification also was greater in drug-selected Dox 6 myeloma cells than parental 8226 cells, which express low and non-immunodetectable amounts of Pgp, respectively. However, no differences in total plasma membrane cholesterol were detected. Transfection of fibroblasts with the multidrug resistance-associated protein (MRP) did not alter esterification, showing that cholesterol trafficking was not generally affected by ATP-binding cassette transporters. Steroidal (progesterone, dehydroepiandrosterone) and non-steroidal antagonists (verapamil, PSC 833, LY335979, and GF120918) were evaluated for effects on both cholesterol trafficking and the net content of 99mTc-Sestamibi, a reporter of drug transport activity mediated by Pgp. In Pgp-expressing cells treated with nonselective and selective inhibitors, both the kinetics and efficacy of inhibition of cholesterol esterification differed from the antagonism of drug transport mediated by Pgp. Thus, although the data show that greater expression of class I Pgp within a given cell type is associated with enhanced esterification of plasma membrane cholesterol in support of a physiologic function for Pgp in facilitating cholesterol trafficking, the molecular mechanism is dissociated from the conventional drug transport activity of Pgp.  (+info)

GR-891: a novel 5-fluorouracil acyclonucleoside prodrug for differentiation therapy in rhabdomyosarcoma cells. (5/3809)

Differentiation therapy provides an alternative treatment of cancer that overcomes the undesirable effects of classical chemotherapy, i.e. cytotoxicity and resistance to drugs. This new approach to cancer therapy focuses on the development of specific agents designed to selectively engage the process of terminal differentiation, leading to the elimination of tumorigenic cells and recovery of normal cell homeostasis. A series of new anti-cancer pyrimidine acyclonucleoside-like compounds were designed and synthesized by structural modifications of 5-fluorouracil, a drug which causes considerable cell toxicity and morbidity, and we evaluated their applicability for differentiation therapy in human rhabdomyosarcoma cells. We tested the pyrimidine derivative GR-891, (RS)-1-[[3-(2-hydroxyethoxy)-1-isopropoxy]propyl]-5-fluorouracil, an active drug which shows low toxicity in vivo and releases acrolein which is an aldehyde with anti-tumour activity. Both GR-891 and 5-fluorouracil caused time- and dose-dependent growth inhibition in vitro; however, GR-891 showed no cytotoxicity at low doses (22.5 micromol l(-1) and 45 micromol l(-1)) and induced terminal myogenic differentiation in RD cells (a rhabdomyosarcoma cell line) treated for 6 days. Changes in morphological features and in protein organization indicated re-entry in the pathway of muscular maturation. Moreover, GR-891 increased adhesion capability mediated by the expression of fibronectin, and did not induce overexpression of P-glycoprotein, the mdr1 gene product, implicated in multidrug resistance. New acyclonucleoside-like compounds such as GR-891 have important potential advantages over 5-fluorouracil because of their lower toxicity and their ability to induce myogenic differentiation in rhabdomyosarcoma cells. Our results suggest that this drug may be useful for differentiation therapy in this type of tumour.  (+info)

Induction of MDR1 gene expression by anthracycline analogues in a human drug resistant leukaemia cell line. (6/3809)

The effects of 4-demethoxydaunorubicin (idarubicin, IDA) and MX2, a new morpholino-anthracycline, on up-regulation of the MDR1 gene in the low-level multidrug resistant (MDR) cell line CEM/A7R were compared at similar concentrations (IC10, IC50 and IC90) over a short time exposure (4 and 24 h). The chemosensitivity of each drug was determined by a 3-day cell growth inhibition assay. Compared with epirubicin (EPI), IDA and MX2 were 17- and eightfold more effective in the CEM/A7R line respectively. No cross-resistance to 5-FU was seen in the CEM/A7R line. Verapamil (5 microM) and PSC 833 (1 microM), which dramatically reversed resistance to EPI in the CEM/A7R line, had no sensitizing effect on the resistance of this line to MX2, but slightly decreased resistance to IDA. The sensitivity to 5-FU was unchanged by these modulators. The induction of MDR1 mRNA expression by IDA, MX2 and 5-FU was analysed by Northern blotting and semiquantitatively assessed by scanning Northern blots on a phosphorimager. The relative level of MDR1 expression was expressed as a ratio of MDR1 mRNA to the internal RNA control glyceraldehyde-3-phosphate dehydrogenase (GAPDH). IDA, MX2 and 5-FU differentially up-regulated MDR1 mRNA in the CEM/A7R line in a dose-dependent manner. Both IDA and MX2 induced MDR1 expression within 4 h. 5-FU up-regulated MDR1 expression only when drug exposure was prolonged to 24 h. Based on MRK 16 binding, flow cytometric analysis of P-glycoprotein (Pgp) expression paralleled the increase in MDR1 mRNA levels. For the three anthracyclines, the increase in MDR1 expression was stable in cells grown in the absence of drug for more than 3 weeks after drug treatment. The induction of MDR1 expression by 5-FU was transient, associated with a rapid decrease in the increased Pgp levels which returned to baseline 72 h after the removal of 5-FU. This study demonstrates that MDR1 expression can be induced by analogues of anthracyclines not pumped by Pgp, and that this induction appears to be stable despite a 3-week drug-free period.  (+info)

Transport of rhodamine 123, a P-glycoprotein substrate, across rat intestine and Caco-2 cell monolayers in the presence of cytochrome P-450 3A-related compounds. (7/3809)

Effects of cytochrome P-450 3A- and P-glycoprotein (P-gp)-related compounds, erythromycin, midazolam, ketoconazole, verapamil, and quinidine, on transport of rhodamine 123 (Rho-123), a P-gp substrate, were studied in rat intestine and in Caco-2 cells. Ileum was mainly used in rat studies because this segment showed greater P-gp-mediated Rho-123 transport. In an in vitro everted rat ileum, all the compounds examined significantly inhibited the transport of Rho-123 from serosal to mucosal surfaces across the intestine, with different inhibitory potencies among these compounds. In an in vivo rat study, the exsorption of Rho-123 from blood to the intestinal lumen, which was evaluated as exsorption clearance of Rho-123 under a steady-state plasma concentration of Rho-123, was also inhibited when these compounds were added to the intestinal lumen. Similarly, transepithelial transport of Rho-123 from the basolateral to apical side across Caco-2 cell monolayers was inhibited by these compounds. A linear relationship was observed in their inhibitory potencies on Rho-123 transport between in vitro and in vivo studies using rat ileum and between studies with rat ileum and Caco-2 cells. P-gp-mediated transport across the intestine was found to be inhibited not only by P-gp-related but also by all the cytochrome P-450 3A-related compounds examined. Within experimental error, the relative inhibitory potencies were the same between the studies with rat ileum (in vivo, in vitro) and those with Caco-2 cells. Thus, it is suggested that the function of P-gp and its sensitivity to these drugs may be similar in rat intestine and Caco-2 cells.  (+info)

Stimulation of P-glycoprotein-mediated drug transport by prazosin and progesterone. Evidence for a third drug-binding site. (8/3809)

P-glycoprotein is a plasma membrane protein of mammalian cells that confers multidrug resistance by acting as a broad-specificity, ATP-dependent efflux transporter of diverse lipophilic neutral or cationic compounds. Previously, we identified two positively cooperative drug-binding sites of P-glycoprotein involved in transport [Shapiro, A. B. & Ling, V. (1997) Eur. J. Biochem. 250, 130-137]. The H site is selective for Hoechst 33342 and colchicine. The R site is selective for rhodamine 123 and anthracyclines. Substrate binding to one site stimulates transport by the other. In this paper, we show that prazosin and progesterone stimulate the transport of both Hoechst 33342 and rhodamine 123. Rhodamine 123 and prazosin (or progesterone) in combination stimulate Hoechst 33342 transport in an additive manner. In contrast, Hoechst 33342 and either prazosin or progesterone interfere with each other, so that the stimulatory effect of the combination on rhodamine 123 transport is less than that of each individually. Non-P-glycoprotein-specific effects of prazosin on membrane fluidity and permeability were excluded. These results indicate the existence of a third drug-binding site on P-glycoprotein with a positive allosteric effect on drug transport by the H and R sites. This allosteric site appears to be one of the sites of photoaffinity labeling of P-glycoprotein by [125I]iodoarylazidoprazosin [Safa, A. R., Agresti, M., Bryk, D. & Tamai, I. (1994) Biochemistry 33, 256-265] and is likely not to be capable of drug transport.  (+info)

TY - JOUR. T1 - Interaction of the P-glycoprotein multidrug transporter (MDR1) with high affinity peptide chemosensitizers in isolated membranes, reconstituted systems, and intact cells. AU - Sharom, Frances J.. AU - Yu, Xiaohong. AU - Lu, Peihua. AU - Liu, Ronghua. AU - Chu, Joseph W K. AU - Szabó, Katalin. AU - Müller, M.. AU - Hose, Curtis D.. AU - Monks, Anne. AU - Váradi, A.. AU - Seprődi, J.. AU - Sarkadi, B.. PY - 1999/8/15. Y1 - 1999/8/15. N2 - P-Glycoprotein-mediated multidrug resistance can be reversed by the action of a group of compounds known as chemosensitizers. The interactions with P-glycoprotein of two novel hydrophobic peptide chemosensitizers (reversins 121 and 205) have been studied in model systems in vitro, and in a variety of MDR1-expressing intact tumor cells. The reversins bound to purified P-glycoprotein with high affinity (77-154 nM), as assessed by a quenching assay using fluorescently labeled purified protein. The peptides modulated P-glycoprotein ATPase activity ...
TY - JOUR. T1 - Expression of a human multidrug resistance gene in human ovarian carcinoma cell lines. AU - Sekiya, S.. AU - Nunoyama, T.. AU - Shirasawa, H.. AU - Kimura, H.. AU - Kawata, M.. AU - Iijima, N.. AU - Sugimoto, Y.. AU - Tsuruo, T.. AU - Takamizawa, H.. PY - 1992/6. Y1 - 1992/6. N2 - To investigate the possible role of the multidrug resistance phenotype to chemoresistance in human ovarian carcinoma, we have analyzed human multidrug resistance gene (mdr 1) expression in 8 human ovarian adenocarcinoma cell lines. An increase in P-glycoprotein level specific to multidrug-resistant tumor cells was not apparently associated with the increase in resistance to vincristine (VCR) or doxorubicin (Adriamycin). Mdr 1 transcripts (4.5 kilobases) were observed in the RNA preparation obtained from only one cell line (SHIN-3) that showed the highest resistance to both drugs in vitro and in vivo. No cell lines showed mdr 1 DNA amplification. These results suggest that the insensitivity of human ...
TY - JOUR. T1 - Inhibition of human P-glycoprotein transport and substrate binding using a galantamine dimer. AU - Namanja, Hilda A.. AU - Emmert, Dana. AU - Pires, Marcos M.. AU - Hrycyna, Christine A.. AU - Chmielewski, Jean. PY - 2009/10/30. Y1 - 2009/10/30. N2 - The human multidrug resistance transporter P-glycoprotein (P-gp) prevents the entry of compounds into the brain by an active efflux mechanism at the blood-brain barrier (BBB). Treatment of neurodegenerative diseases, therefore, has become a challenge and the development of new reversible inhibitors of P-gp is pertinent to overcome this problem. We report the design and synthesis of a crosslinked agent based on the Alzheimers disease treatment galantamine (Gal-2) that inhibits P-gp-mediated efflux from cultured cells. Gal-2 was found to inhibit the efflux of the fluorescent P-gp substrate rhodamine 123 in cancer cells that over-express P-gp with an IC50 value of approximately 0.6 μM. In addition, Gal-2 was found to inhibit the ...
TY - JOUR. T1 - P-glycoprotein expression and multidrug resistance in adrenocortical carcinoma. AU - Flynn, Stuart D. AU - Murren, J. R.. AU - Kirby, W. M.. AU - Honig, J.. AU - Kan, L.. AU - Kinder, B. K.. PY - 1992. Y1 - 1992. N2 - Background. The response of adrenocortieal carcinoma (ACC) to adjuvant chemotherapy has been disappointing with no significant impact on survival. The normal adrenal cortex has very high levels of P-glycoprotein, an energy-dependent efflux pump of a variety of structurally unrelated chemotherapeutic agents. P-glycoprotein has been implicated as a cause of multidrug resistance in a variety of neoplasms. The purpose of this study was to evaluate P-glycoprotein expression in ACC. Methods. Eleven patients with ACC had paraffin-em bedded tumor evaluated for P-glycoprotein expression. These were analyzed by immunohistochemistry assay with a battery of four anti-P-glycoprotein antibodies (MRK-16, JSB-1, UIC-2, MDR). Results. All eleven cases showed intense, predominantly ...
This study was aimed at evaluating the influence of 5637-conditioned medium (5637-CM) and human recombinant cytokines on both expression and function of P-glycoprotein (P-gp) in TF-1, a GM-CSF/IL-3-dependent acute myeloid leukemia cell line which constitutively expresses functional P-gp. P-gp expression was measured by flow cytometry using MRK16 monoclonal antibody. P-gp function was measured by rhodamine 123 (Rh 123) efflux kinetics. When TF-1 cells were cultured with 5637-CM (50% v/v), both P-gp expression and P-gp efflux capacity were increased in a time-dependent manner with a 4-fold increase in P-gp expression level at day 6 whereas TF-1 cell differentiation status remained unchanged as assessed by morphological studies, phenotypical and cytochemistry analysis. Recombinant cytokines including GM-CSF, G-CSF, IL-1 beta, IL-6, stem cell factor, LIF, erythropoietin, and IL-3 had no effect on P-gp expression whereas TNF alpha induced dose- and time-dependent P-gp and mdr-1 gene overexpression. However,
How to Cite: Karunaratne, D.N. and Audus, K.L., 2007. Use of fluorescent probes to monitor the efflux transporters P-Glycoprotein and MRP1 in Bewo cells. Journal of the National Science Foundation of Sri Lanka, 35(1), pp.19-27. DOI: http://doi.org/10.4038/jnsfsr.v35i1.3658 ...
P‐glycoprotein (Pgp) is a 170 kDa phosphorylated glycoprotein encoded by human MDR1 gene. It is responsible for the systemic disposition of numerous structurally and pharmacologically 1unrelated lipophilic and amphipathic drugs, carcinogens, toxins, and other xenobiotics in many organs, such as the intestine, liver, kidney, and brain. Like cytochrome P450s (CYP3A4), Pgp is vulnerable to inhibition, activation, or induction by herbal constituents. This was demonstrated by using an ATPase assay, purified Pgp protein or intact Pgp‐expressing cells, and proper probe substrates and inhibitors. Curcumin, ginsenosides, piperine, some catechins from green tea, and silymarin from milk thistle were found to be inhibitors of Pgp, while some catechins from green tea increased Pgp‐mediated drug transport by heterotropic allosteric mechanism, and St. Johns wort induced the intestinal expression of Pgp in vitro and in vivo. Some components (e.g., bergamottin and quercetin) from grapefruit juice were reported to
DI-fusion, le Dépôt institutionnel numérique de lULB, est loutil de référencementde la production scientifique de lULB.Linterface de recherche DI-fusion permet de consulter les publications des chercheurs de lULB et les thèses qui y ont été défendues.
P-glycoprotein (P-gp) overexpression is the most frequently observed cause of multidrug resistance in neoplastic cells. In our experiments, P-gp was expressed in L1210 mice leukemia cells (S cells) by selection with vincristine (R cells) or transfection with the gene encoding human P-gp (T cells). Remodeling of cell surface sugars is associated with P-gp expression in L1210 cells as a secondary cellular response. In this study, we monitored the alteration of cell surface saccharides by Sambucus nigra agglutinin (SNA), wheat germ agglutinin (WGA) and Maackia amurensis agglutinin (MAA). Sialic acid is predominantly linked to the surface of S, R and T cells via α-2,6 branched sugars that tightly bind SNA. The presence of sialic acid linked to the cell surface via α-2,3 branched sugars was negligible, and the binding of MAA (recognizing this branch) was much less pronounced than SNA. WGA induced greater cell death than SNA, which was bound to the cell surface and agglutinated all three L1210 cell-variants
The purpose of this work was to investigate if P-glycoprotein (Pgp) efflux pump activity could be inhibited in the sub-bronchial epithelial cell line, Calu-3, by glucocorticosteroids and β-ligands. The Pgp modulation efficiency of each compound was determined by its ability to increase the accumulation of the Pgp substrate rhodamine 123 (Rh123) accumulation in these cells. Pgp inhibition was observed at ≥ 100 μM steroids and β-ligand. The modulation effectiveness of the β-ligands increased with increasing hydrophobicity (log Poctanol/aqueous) whereas an obvious correlation was not obtained with the complete set of steroids tested. Steroidal Pgp substrates did not affect Rh123 accumulation (e.g., aldosterone, dexamethasone, 11β, 17α, 21-OH progesterone). In contrast, two hydrophobic non P-gp steroidal substrates (testosterone and progesterone) displayed different effects on Rh123 accumulation, with progesterone being the more potent modulator. The most hydrophobic β-ligand, propranolol, ...
TY - JOUR. T1 - Estradiol regulation of P-glycoprotein expression in mouse kidney and human tubular epithelial cells, implication for renal clearance of drugs. AU - Kanado, Yuki. AU - Tsurudome, Yuya. AU - Omata, Yuji. AU - Yasukochi, Sai. AU - Kusunose, Naoki. AU - Akamine, Takahiro. AU - Matsunaga, Naoya. AU - Koyanagi, Satoru. AU - Ohdo, Shigehiro. PY - 2019/11/12. Y1 - 2019/11/12. N2 - P-glycoprotein (P-gp/ABCB1) is an ATP-binding cassette drug efflux transporter expressed in a variety of tissues that affects the pharmacokinetic disposition of many drugs. Although several studies have reported gender-dependent differences in the expression of P-gp, the role of sex hormones in regulating the expression of P-gp and its transport activity has not been well understood. In this study, we demonstrated that 17β-estradiol has the ability to induce the expression of P-pg in mouse kidneys and cultured human renal proximal tubular epithelial cells. After intravenous injection of a typical P-gp ...
OBJECTIVE: In vitro and animal experiments suggest that P-glycoprotein forms a functional barrier between maternal and fetal blood circulation in the placenta, thus protecting the fetus from exposure to xenobiotics during pregnancy. In this study we aimed to characterize the role of P-glycoprotein in the blood-placental barrier by use of dually perfused human placenta. METHODS: Twenty-eight human placentas were obtained after delivery, and both the maternal side and the fetal side were perfused for 2 hours. Saquinavir was used as a probe drug for P-glycoprotein-dependent active transfer, and PSC833 (valspodar) or GG918 was used as an inhibitor of P-glycoprotein function in a maternal-to-fetal and fetal-to-maternal perfusion setting. Genotyping for ABCB1 (C3435T and G2677A/T) polymorphism and quantification of P-glycoprotein expression were done for each placenta. RESULTS: The fetal-to-maternal transfer of saquinavir was 108-fold higher (P = .003) compared with transfer from the maternal to the ...
Drug resistance is a major problem in cancer chemotherapy. Treatment protocols generally include a number of different cytotoxic drugs given in combination. Therefore, drug resistance in the tumor is likely to result from the coexpression of several cellular activities able to prevent cell killing by any of the drugs used. In this study we have measured several potential drug resistance mechanisms consisting of the multidrug resistance gene product P-glycoprotein, glutathione, glutathione-transferase and -peroxidase, and the DNA repair enzyme O6-alkylguanine-DNA-alkyltransferase in samples of colon carcinoma and normal adjacent mucosa from 23 untreated patients. All of these, with the exception of P-glycoprotein, showed significant increases in tumor tissue levels when compared with normal tissue from the same patient. The significance was highest for glutathione peroxidase (P less than or equal to 0.0005). Individual patients, however, showed very different patterns, with none, several, or all ...
P-glycoprotein (P-gp) is a member of the ATP-Binding Cassette transporter superfamily and mediates transmembrane efflux of many drugs. Since it is involved in multi-drug resistance activity in various cancer cells, the development of P-gp inhibitor is one of the major concerns in anticancer therapy. Human P-gp protein has at least two functional drug binding sites that are called H site and R site, hence it has multi-binding-specificities. Though the amino acid residues that constitute in drug binding pockets have been proposed by previous experimental evidences, the shapes and the binding poses are not revealed clearly yet. In this study, human P-gp structure was built by homology modeling with available crystal structure of mouse P-gp as a template and docking simulations were performed with inhibitors such as verapamil, hoechst33342, and rhodamine123 to construct the interaction between human P-gp and its inhibitors. The docking simulations were performed 500 times for each inhibitor, and
Inhibition of intestinal P-glycoprotein might enhance the absorption of orally administered P-glycoprotein substrate drugs. We show here a 10-fold increased oral bioavailability of paclitaxel in mice treated with the P-glycoprotein blocker SDZ PSC 833. These results encourage further research on the …
Phospho-glycoprotein (P-gP) is a polytopic plasma membrane protein whose overexpression causes multidrug resistance (MDR) responsible for the failure of cancer chemotherapy. P-gp 170 is a member of the ATP-binding cassette (ABC) transporter superfamily and has two potentially interesting regions for drugs interfering with its efflux function, namely the oligosaccharides on the first extracellular loop with unknown function and the two intracellular ATP-binding regions providing the energy for drug efflux function. The polylactoseamine oligosaccharides on the first loop can specifically bind the tomato lectin (TL). The P-gp efflux activities of TL-pre-treated MDR resistant cells were measured in the presence of structurally unrelated resistance modifiers such as phenothiazines, terpenoids and carotenoids. The inhibition of efflux activity was measured via the increased rhodamine uptake by mouse lymphoma cells transfected in human MDR1 gene and in human brain capillary endothelial cells. The ...
TY - JOUR. T1 - Topological folding and proteolysis profile of P-glycoprotein in membranes of multidrug-resistant cells. T2 - Implications for the drug-transport mechanism. AU - Zhang, Mei. AU - Wang, Guichun. AU - Shapiro, Adam. AU - Zhang, Jian-Ting. PY - 1996. Y1 - 1996. N2 - P-glycoprotein (Pgp)1 is a polytopic membrane protein and functions as an energy-dependent drug efflux pump. It is responsible for multidrug resistance (MDR) in cancer cell lines. Recently, the topological structure of Pgp has been investigated. However, the results are in dispute. A major question concerning the Pgp topology is the membrane orientation of the loop linking TM4 and TM5 (loop 4) and the loop linking TM8 and TM9 (loop 8). In this study, we generated polyclonal antibodies specific to these two loops. In combination with a panel of other well-characterized site-specific polyclonal and monoclonal antibodies of Pgp, we tested the membrane orientation of these two loops of Pgp in multidrug-resistant cells using ...
The ATP-binding cassette (ABC) transporter ABCB1, encoded by the multidrug resistance gene MDR1, is expressed on brain microvascular endothelium and several types of epithelium, but not on endothelia outside the CNS. It is an essential component of the blood-brain barrier. The aim of this study was to identify cell-specific controls on the transcription of MDR1 in human brain endothelium. Reporter assays identified a region of 500bp around the transcription start site that was optimally active in brain endothelium. Chromatin immunoprecipitation identified Sp3 and TFIID associated with this region and EMSA (electrophoretic mobility shift assays) confirmed that Sp3 binds preferentially to an Sp-target site (GC-box) on the MDR1 promoter in brain endothelium. This result contrasts with findings in other cell types and with the colon carcinoma line Caco-2, in which Sp1 preferentially associates with the MDR1 promoter. Differences in MDR1 transcriptional control between brain endothelium and Caco-2 ...
Expression of the multidrug transporter P-glycoprotein (P-gp) is one of the major causes of multidrug resistance in cancer cells. P-gp is a 170-kDa membrane protein encoded by the MDR1 gene in humans. Based on its sequence and domain organization, P-gp is classified as a member of ATP binding cassette superfamily; it consists of two symmetrical halves, each half containing six transmembrane (TM) domains and a cytoplasmic nucleotide binding domain. Although most members of the ABC transporter family have stringent substrate specificities, P-gp recognizes many compounds, including anthracyclines (e.g., doxorubicin and daunomycin), vinca alkaloids (e.g., vincristine and vinblastine), antibiotics (e.g., actinomycin D), circular and toxic peptides (e.g., valinomycin and gramicidin), and relatively noncytotoxic agents such as verapamil, azidopine, quinidine, and cyclosporin A. These P-gp substrates have no common chemical structure. They are all low-molecular-weight nonanionic hydrophobic or ...
TY - JOUR. T1 - Progesterone interacts with P-glycoprotein in multidrug-resistant cells and in the endometrium of gravid uterus. AU - Yang, C. P.H.. AU - DePinho, S. G.. AU - Greenberger, L. M.. AU - Arceci, R. J.. AU - Horwitz, S. B.. PY - 1989. Y1 - 1989. N2 - P-glycoprotein (P-GP) plays a pivotal role in maintaining the multidrug-resistant (MDR) phenotype. This membrane glycoprotein is overproduced in MDR cells and the endometrium of the mouse gravid uterus (Arceci, R.J., Croop, J.M., Horwitz, S.B., and Housman, D. (1988) Proc. Natl. Acad. Sci. U.S.A. 85, 4350-4354). This latter observation and an interest in endogenous substrates for P-GP led to a study of the interaction of steroids with P-GP found in the endometrium of the mouse gravid uterus and in MDR cells derived from the murine macrophage-like cell J774.2. [3H]Azidopine labeling of P-GP from these two sources was inhibited by various steroids, particularly progesterone. Progesterone also markedly inhibited [3H]vinblastine binding to ...
Good Morning David, Ive done several years of Multi Drug Resistance Protein work. It was a tough nut to crack back a few years ago. We use JSB-1 primary antibody [far superior to C219] and the procedure is long... weve added extra IgG fragments to give the DAB some extra places to bind. Its really a nice, clean, amplified method. I can send you the worksheet for the procedure if youd like. Please find the related publications below (methods paper is #2). I think #3 may be of special interest to you. 1)Toth, K., Vaughan, M.M., Slocum, H.K., Fredericks, W.J., Chen, Y., Arredondo, M.A., Harstrick, A., Karakousis, C., Baker, R.M., Rustum, Y.M. Comparison of an Immunoperoxidase sandwich Staining Method and Western Blot Detection of P-glycoprotein in Human Cell Lines and Sarcomas. Amer. J. Path. 140:1009-1016, 1992. 2)Toth, K., Vaughan, M.M., Slocum, H.K., Arredondo, M.A., Takita, H., Baker, R.M., Tsuro, T., and Rustum, Y.M. New Immunohistochemical Sandwich Staining Method for MDR1 ...
Our study demonstrated that rIL2, administered at 9 MIU/kg twice a day intraperitoneally for 4 days in mice, induces a 2-fold decrease in the protein expression of intestinal Pgp. This lower Pgp protein expression led to a 1.6-fold decrease in Pgp activity measured in vitro with everted gut sacs. This decreased Pgp activity was associated with increased digoxin and saquinavir bioavailabilities in mice pretreated with rIL2. This is the first in vivo report where a decrease in intestinal Pgp activity is shown to be induced by a decrease in Pgp protein expression.. In the present study, we have developed a new in vitro model to study the intestinal Pgp function of mice. Rat everted gut sacs have already been used, especially with rhodamine 123 as Pgp substrate (Yumoto et al., 1999; Veau et al., 2001). Conversely, mouse intestine had never been used in the same model until now. The secretion of rhodamine 123 across everted mouse intestine was strongly inhibited by verapamil and cyclosporin A, both ...
[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
This Application Note demonstrates how to measure P-glycoprotein (Pgp) Inhibition fast and simple on a Microplate Reader. Read more.
HIV-1 is shed in genital secretions which increase the risk of transmission between sexual partners and from mother to infant. Antiretroviral medication taken prior to exposure to HIV-1 can prevent viral transmission from a mother to her infant. Raltegravir (RAL), by blocking integration of viral cDNA into the hosts genome, makes an excellent candidate for preventing HIV-1 infection. RAL is licensed for treatment with twice-daily dosing based on plasma trough concentrations; however, intracellular concentrations of RAL which are relevant to blocking infection of cells have not been previously studied. P-glycoprotein pumps, which are involved in regulating drug absorption and metabolism, can influence intracellular drug concentrations. P-glycoprotein concentrations appear to vary with menstrual cycle suggesting it may affect intracellular drug concentration of RAL in women.. Women will be enrolled in the study and followed during the course of a menstrual cycle while taking a dose of 400mg PO ...
HIV-1 is shed in genital secretions which increase the risk of transmission between sexual partners and from mother to infant. Antiretroviral medication taken prior to exposure to HIV-1 can prevent viral transmission from a mother to her infant. Raltegravir (RAL), by blocking integration of viral cDNA into the hosts genome, makes an excellent candidate for preventing HIV-1 infection. RAL is licensed for treatment with twice-daily dosing based on plasma trough concentrations; however, intracellular concentrations of RAL which are relevant to blocking infection of cells have not been previously studied. P-glycoprotein pumps, which are involved in regulating drug absorption and metabolism, can influence intracellular drug concentrations. P-glycoprotein concentrations appear to vary with menstrual cycle suggesting it may affect intracellular drug concentration of RAL in women.. Women will be enrolled in the study and followed during the course of a menstrual cycle while taking a dose of 400mg PO ...
The activity of P-glycoprotein (Pgp/MDR1/ABCB1) and multidrug resistance proteins (MRP/ABCC) influence the pharmacokinetics and bioavailability of many drugs. Few suitable cell lines for the study of drug transport exist. Additional non-human cell lines may help clarify species differences and contribute to the current knowledge of drug transport. The aim of the present study was to characterize three rat epithelial cell lines for transporter expression and activity. Transporter expression was assessed in intestinal IEC-6 and renal GERP and NRK-52E cells using RT-PCR and Western blot analysis. Pgp and Mrp transport activity were analyzed by measuring calcein accumulation and glutathione-S-bimane efflux, respectively. The three cell lines showed Pgp expression and Pgp-dependent transport, both decreasing with culture time after reaching confluency. Besides Pgp, cells expressed Mrp1, Mrp3, Mrp4, and Mrp5, while Mrp2 and Mrp6 were absent. In addition, they showed temperature- and Mrp-dependent ...
Supplementary Materialsmolecules-24-00707-s001. in a standard human being jejunum and were already validated for the testing of Axitinib tyrosianse inhibitor P-gp inducers and activators [5,21,26,27]. Open in a separate window Number 1 Chemical constructions of the oxygenated xanthones OX 1C6 investigated in this study. Additionally, using everted intestinal sacs of Wistar-Han rats, the effect of the most promising compound on P-gp activity was evaluated < 0.01; **** < 0.0001 vs. control (0 M)]. 2.4. Evaluation of P-Glycoprotein Transport Activity P-gp activity was evaluated using two different protocols: The first approach, by evaluating the accumulation of Rhodamine 123 (Rho 123) in the presence of the OXs (20.0 M) during the 60-min accumulation phase of the fluorescent P-gp substrate (Figure 4); and the second approach, by evaluating the accumulation of Rho 123 after pre-exposure of Caco-2 cells to the OXs (20.0 M) for 24 h (Figure 5). The first assay aims to evaluate the potential immediate ...
CUL4A encodes a core component of a cullin-based E3 ubiquitin ligase complex that regulates many critical processes such as cell cycle progression, DNA replication, DNA repair and chromatin remodeling by targeting a variety of proteins for ubiquitination and degradation. In the research described in this report we aimed to clarify whether CUL4A participates in multiple drug resistance (MDR) in breast cancer cells. We first transfected vectors carrying CUL4A and specific shCUL4A into breast cancer cells and corresponding Adr cells respectively. Using reverse transcription polymerase chain reactions and western blots, we found that overexpression of CUL4A in MCF7 and MDA-MB-468 cells up-regulated MDR1/P-gp expression on both the transcription and protein levels, which conferred multidrug resistance to P-gp substrate drugs, as determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assays. On the other hand, silencing CUL4A in MCF7/Adr and MDA-MB-468/Adr cells led to the opposite
5416 The proteasome inhibitor bortezomib has been approved for single-agent treatment of multiple myeloma and is being evaluated in other malignancies. Two prominent effects of bortezomib are inhibition of nuclear factor-kappa-B activation and stabilization of p53, both of which may affect the cellular response to cytotoxic drugs. The purpose of the present study was to assess efficacy of bortezomib in acute myeloid leukemia (AML) by determining its activity as a single agent in AML cell lines with wt (ML-1) and inactive (HL60) p53 and against cells overexpressing MDR proteins prevalent in AML, including P-glycoprotein (Pgp), multidrug resistance protein-1 (MRP-1), breast cancer resistance protein (BCRP) and lung resistance protein (LRP). In addition, interactions between bortezomib and chemotherapy drugs with activity in AML were studied. Cells were cultured for four days in 96-well microculture assays with bortezomib and the chemotherapy drugs Ara-C, DNR, Dox or Ida individually, ...
TY - JOUR. T1 - Generation of multidrug resistant lymphoma cell lines stably expressing P-glycoprotein. AU - Pop, Iliodora. AU - Pop, Laurentiu. AU - Vitetta, Ellen S.. AU - Ghetie, Maria Ana. PY - 2008/4/1. Y1 - 2008/4/1. N2 - The objective of this study was to generate new P-glycoprotein (P-gp)-expressing multidrug resistant (MDR) cell lines by drug selection. Since our previous studies have been carried out with cells infected with a P-gp-containing vector, it was important to confirm our findings in cells generated by drug selection. In this report, we describe three B-lymphoma cell lines which became drug-resistant by stepwise exposure to vincristine (VCR): Raji cells resistant to 18 nM VCR (R18V), Namalwa cells resistant to 21 nM VCR (N21V) and DHL-4 cells resistant to 12 nM VCR (DHL-41/12V). Cells overexpressed P-gp and continued to express CD19, CD20 and CD22, all of which are targets for monoclonal antibody (MAb) therapy. The P-gp pump in these new cells was functional as determiped by ...
Chitosan (CS), a nature-derived polysaccharide, is a promising nano-carrier material with good biocompatibility and biodegradability. However, the biomedical applications of CS are hindered because of its poor aqueous solubility. To circumvent this drawback, a series of Brij-grafted-chitosan copolymers (BCs) with various grafting degree of Brij-S20 were first developed and reported. The results indicated that the water solubility of BCs (from 9.13 to 9.54 mg/mL) were much higher than that of CS (0.32 mg/mL), due to the broken intra- and/or inter-molecular hydrogen bonds and the decreased initial crystallinity in BCs. The amphiphilic structure of BCs presented lower critical micelle concentration (0.116-0.376 mg/mL) thus facilitating its self-aggregation into micelles for drug encapsulation. Moreover, BCs markedly enhanced the intracellular uptake of rhodamine-123 in MDCK-MDR1 cells. This inhibition on Pgp-mediated efflux was also confirmed by confocal microscopy. In conclusion, BCs could be ...
The interactions between the human P-glycoprotein (Pgp) and two different types of immunosuppressant drugs known to modulate multidrug resistance in tumor cells have been directly investigated using our newly developed drug-stimulated ATPase assay for Pgp function. The macrolides FK506 and FK520 stimulate the Pgp-ATPase activity with affinities in the 100 nM range, nearly 10 times higher than that of verapamil, a well known Pgp substrate. On the other hand, the cyclic peptides cyclosporin A and dihydrocyclosporin C do not stimulate the Pgp-ATPase activity at all. They do, however, act as potent competitive inhibitors of verapamil-stimulated Pgp-ATPase activity, with affinity constants in the 20-25 nM range. Thus, although these two classes of immunosuppressant drugs affect the Pgp in different ways, they both probably interact with high affinity at the transported drug binding site(s) of the Pgp, which would explain their ability to resensitize multidrug-resistant cells to the killing action of ...
The application of most agents with the capacity to reverse multidrug resistance (MDR) via modulation of the multidrug transporter P-glycoprotein (Pgp) was shown to be associated with toxic side-effects. For this reason, we have investigated the effect of combinations of suboptimal concentrations of …
P-glycoprotein (P-gp) is an efflux pump involved in the protection of tissues of several organs by influencing xenobiotic disposition. P-gp plays a key role in multidrug resistance and in the progression of many neurodegenerative diseases. The development of new and more effective therapeutics targeting P-gp thus represents an intriguing challenge in drug discovery. P-gp inhibition may be considered as a valid approach to improve drug bioavailability as well as to overcome drug resistance to many kinds of tumours characterized by the over-expression of this protein. This study aims to develop classification models from a unique dataset of 59 compounds for which there were homogeneous experimental data on P-gp inhibition, ATPase activation and monolayer efflux. For each experiment, the dataset was split into a training and a test set comprising 39 and 20 molecules, respectively. Rational splitting was accomplished using a sphere-exclusion type algorithm. After a two-step (internal/external) ...
Changes in P-glycoprotein and ABCG2 densities may play a role in amyloid-beta accumulation in Alzheimers disease. However, previous studies report conflicting results from different brain regions, without correcting for changes in vessel density. We developed an automated method to measure transporter density exclusively within the vascular space, thereby correcting for vessel density. We then examined variability in transporter density across brain regions, matter, and disease using two cohorts of post-mortem brains from Alzheimers disease patients and age-matched controls. Changes in transporter density were also investigated in capillaries near plaques and on the mRNA level. P-glycoprotein density varied with brain region and matter, whereas ABCG2 density varied with brain matter. In temporal cortex, P-glycoprotein density was 53% lower in Alzheimers disease samples than in controls, and was reduced by 35% in capillaries near plaque deposits within Alzheimers disease samples. ABCG2 ...
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Supplementary Materialsijms-21-02443-s001. demonstrate how the treatments targeted tumor cells over the standard breast cells. The recognition of energy rate of metabolism alteration could start strategies of enhancing chemotherapy for malignant breasts cancer. strong course=kwd-title Keywords: caffeine, cisplatin, phasor-FLIM, energy rate of metabolism, breast tumor 1. Introduction Based on the Country wide Breast Cancer Basis, breast cancer may be the most common tumor diagnosed in ladies, and one in eight women will be diagnosed with breast Rabbit Polyclonal to MEN1 cancer in their lifetime [1]. A subtype of breast cancer is basal-like breast cancer, also known as triple-negative breast cancer (TNBC). Given its lack of estrogen receptors (ER), SB 203580 reversible enzyme inhibition progesterone receptors (PR), and low expression of human epidermal growth factor receptor 2 (HER2), there is no effective biological targeted therapy [2]. MDA-MB-231 is a known representative of triple-negative ...
Thiosemicarbazone-related compounds are well-known to have active antiviral, antibacterial, antimalarial, and antihypertensive properties (42), as well as antitumor activity that can overcome resistance to chemotherapeutics (19, 43). Recently, we reported that the small-molecule thiosemicarbazone NSC73306 is significantly more cytotoxic to cells that overexpress P-glycoprotein than to cells that do not, and this unique property is directly proportional to functional P-glycoprotein protein expression (19). Therefore, we proposed that NSC73306 could be used to resensitize P-glycoprotein-expressing multidrug resistant carcinoma cells to chemotherapy. However, in addition to P-glycoprotein, the presence of MRPs and ABCG2 is well documented in numerous types of the cancer cells (4) and has been shown to play a major role in the development of MDR in cancer cells (16, 18, 44, 45). For example, ABCG2 and MRP1 are known to transport numerous anticancer chemotherapeutics, whereas MRP4 and MRP5 can ...
Background At least four major categories of invasive breast cancer have been reproducibly identified by gene expression profiling: luminal A, luminal B, HER2-type and basal-like. growth factor receptor 2 (HER2), cytokeratin 5/6 (CK5/6), and epidermal growth factor receptor (EGFR). Using immunostain results in combination with histologic grade, cases were grouped into molecularly defined XL647 subtypes. We used Cox proportional hazards models to estimate hazard ratios (HRs) and 95% confidence intervals (CIs). Results We observed differences in the association between risk factors and subtypes of breast cancer. In general, many reproductive factors were most strongly associated with the luminal A subtype, although these differences were not statistically significant. Weight gain since age 18 showed significant differences in its association with molecular subtypes (p-heterogeneity=0.05) and was most strongly associated with the luminal B subtype (p-trend 0.001). Although there was not significant ...
TY - JOUR. T1 - Modulators of the multidrug-transporter, P-glycoprotein, exist in the human plasma. AU - Ichikawa, Misako. AU - Yoshimura, Akihiko. AU - Furukawa, Tatsuhiko. AU - Sumizawa, Tomoyuki. AU - Akiyama, Shin ichi. PY - 1990/1/15. Y1 - 1990/1/15. N2 - P-glycoprotein (P-gp) is thought to mediate the transport of anticancer drugs and to be responsible for the multidrug-resistant (MDR) phenotype. P-gp is also expressed in normal human tissues, such as the adrenal gland, kidney, liver, colon and capillary endothelium of the brain. However, the function and transporting substrates of P-gp in normal tissues are still not understood. This paper explains that some compounds in the human plasma can modulate the transporting activity of P-gp. A partially purified fraction from the human plasma enhanced the accumulation of anti-cancer agents in MDR cells. This fraction inhibited the efflux of vinblastine from MDR cells, and also inhibited the photoaffinity labeling of P-gp with azidopine as ...
P-glycoprotein belongs to the family of ATP-binding cassette proteins which hydrolyze ATP to catalyse the translocation of their substrates through membranes. This protein extrudes a large range of components out of cells, especially therapeutic agents causing a phenomenon known as multidrug resistance. Because of its clinical interest, its activity and transport function have been largely characterized by various biochemical studies. In the absence of a high-resolution structure of P-glycoprotein, homology modeling is a useful tool to help interpretation of experimental data and potentially guide experimental studies. We present here three-dimensional models of two different catalytic states of P-glycoprotein that were developed based on the crystal structures of two bacterial multidrug transporters. Our models are supported by a large body of biochemical data. Measured inter-residue distances correlate well with distances derived from cross-linking data. The nucleotide-free model features a large
had a profound effect on the tissue distribution and especially the brain accumulation of a range of drugs frequently used in humans, including dexamethasone, digoxin, cyclosporin A, ondansetron, domperidone, and loperamide. All drugs were shown to be excellent substrates of the murine ABCB1A P-glycoprotein and its human counterpart, the MDR1 P-glycoprotein, ABCB1. We found that the ability of ABCB1 to prevent accumulation of some drugs in the brain is a prerequisite for their clinical use, as absence of the transporter led to severe toxicity or undesired CNS pharmacodynamic effects. Subsequent work has fully confirmed the profound effect of the drug-transporting ABCB1 P-glycoprotein on the pharmacokinetics of drugs in humans. In fact, every new drug is now screened for transport by ABCB1, as this limits oral availability and penetration into sanctuaries protected by ABCB1, such as the brain. ...
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Dofequidar, also known as MS-209, is a quinolone-derived sphingomyelin synthase inhibitor that blocks P-glycoprotein and multidrug resistance-associated protein-1, is under development by Schering for the potential treatment of multidrug resistant tumors. Dofequidar was found to sensitizes cancer stem-like side population cells to chemotherapeutic drugs by inhibiting ABCG2/BCRP-mediated drug export.
TY - JOUR. T1 - P-glycoprotein retains function when reconstituted into a sphingolipid- and cholesterol-rich environment. AU - Modok, Szabolcs. AU - Heyward, Catherine. AU - Callaghan, Richard. PY - 2004/10/1. Y1 - 2004/10/1. N2 - P-glycoprotein (P-gp) appears to be associated within specialized raftlike membrane microdomains. The activity of P-gp is sensitive to its lipid environment, and a functional association hi raft microdomains will require that P-gp retains activity in the microenvironment. Purified hamster P-gp was reconstituted in liposomes comprising sphingomyelin and cholesterol, both highly enriched in membrane microdomains and known to impart a liquid-ordered phase to bilayers. The activity of P-gp was compared with that of proteoliposomes composed of crude egg phosphatidylcholine (unsaturated) or dipalmitoyl phosphatidylcholine (saturated) in the presence or absence of cholesterol. The maximal rate of ATP hydrolysis was not significantly altered by the nature of the lipid species. ...
BioAssay record AID 150617 submitted by ChEMBL: Concentration required for 50% inhibition (racemic) at binding site of human P-Glycoprotein (P-gp) in one-affinity model.
Overexpression of adenosine triphosphate-binding cassette (ABC) transport proteins is emerging seeing that a crucial contributor to anticancer medication level of resistance. assays. eIF4G mRNA degradation was accelerated in cells transfected with miR-503 mimics. Furthermore, it had been demonstrated that eIF4G and ABC translation protein were downregulated in MCF-7/ADR cells after transfection with miR-503 significantly. It was discovered that miR-503 mimics could sensitize the cells to treatment with ADM, TAX and TAM. These findings confirmed for the very first time that eIF4G acted as an integral element in MCF-7/ADR cells, and Riociguat could end up being a competent agent for preventing and reversing multi-drug resistance in breast malignancy. (11) determinded that cisplatin-resistance cells upregulated MRP1 when compared with sensitive MCF-7 cells. The eukaryotic initiation factor (eIF) 4F complex consists of three proteins: cap-binding protein eIF4E, scaffolding protein eIF4G and ...
KAMISAKO, T. and OGAWA, H. (2005), Alteration of the expression of adenosine triphosphate-binding cassette transporters associated with bile acid and cholesterol transport in the rat liver and intestine during cholestasis. Journal of Gastroenterology and Hepatology, 20: 1429-1434. doi: 10.1111/j.1440-1746.2005.03950.x ...
ORCID: 0000-0002-6804-3897, Najlah, M. and Demanuele, Antony (2009) A polyamidoamine (PANAM) dendrimer-based drug delivery system to bypass the P-glycoprotein efflux transporter. Journal of Pharmacy and Pharmacology, 61 (Supple). p. 101. Full text not available from this repository. ...
TY - JOUR. T1 - Intestinal P-glycoprotein expression is multimodally regulated by intestinal ischemia-reperfusion. AU - Terada, Yusuke. AU - Ogura, Jiro. AU - Tsujimoto, Takashi. AU - Kuwayama, Kaori. AU - Koizumi, Takahiro. AU - Sasaki, Shunichi. AU - Maruyama, Hajime. AU - Kobayashi, Masaki. AU - Yamaguchi, Hiroaki. AU - Iseki, Ken. PY - 2014/6/2. Y1 - 2014/6/2. N2 - Purpose. Reactive oxygen species (ROS) have multiple physiological effects that are amount-dependent. ROS are one of the causes of intestinal ischemia-reperfusion (I/R) injury. In this study, we investigated whether the amount of ROS and the degree of intestinal I/R injury affect the expression level of P-glycoprotein (P-gp). Methods. We used hydrogen peroxide (H2O2) as ROS in in vitro experiments. Intestinal I/R model rats, which were subjected 15-min ischemia (I/R-15), were used in in vivo experiments. Results. P-gp expression in Caco-2 cells was increased in response to 1 μM of H2O2 but decreased upon exposure to 10 mM of ...
Overactivity of the multidrug efflux transporter P-glycoprotein (P-gp) at the blood-brain barrier (BBB) is believed to play an important role in resistance to central nervous system drug treatment. (R)-[11C]verapamil (VPM) PET can be used to measure the function of P-gp at the BBB, but low brain uptake of VPM hampers the mapping of regional differences in cerebral P-gp function and expression. The aim of this study was to evaluate the dose-response relationship of two potent P-gp inhibitors and to investigate if increased brain uptake of VPM mediated by P-gp inhibition can be used to assess regional differences in P-gp activity. Two groups of Sprague-Dawley rats (n = 12) underwent single VPM PET scans at 120 min after administration of different doses of the P-gp inhibitors tariquidar and elacridar. In an additional six rats, paired VPM PET scans were performed before and after administration of 3 mg/kg tariquidar. Inhibitor administration resulted in an up to 11-fold increase in VPM brain distribution
Pgp (P-glycoprotein, MDR1, ABCB1) is an energy-dependent drug efflux pump that is a member of the ATP-binding cassette (ABC) family of proteins. Preliminary studies have reported that nonspecific inhibitors of Pgp affect synthesis and esterification of cholesterol, putatively by blocking trafficking of cholesterol from the plasma membrane to the endoplasmic reticulum, and that relative increases in Pgp within a given cell type are associated with increased accumulation of cholesterol. Several key efflux proteins involved in the cholesterol metabolic pathway are transcriptionally regulated by the nuclear hormone liver X receptor (LXR). Therefore, to examine the interplay between P-glycoprotein and the cholesterol metabolic pathway, we utilized a high fat, normal cholesterol diet to upregulate LXRα without affecting dietary cholesterol. Our research has demonstrated that mice lacking in P-glycoprotein do not exhibit alterations in hepatic total cholesterol storage, circulating plasma total cholesterol
J. Clin. Invest.104:147-153 (1999). In our 1999 JCI article, we reported that the rate and extent of absorption of orally administered digoxin is determined by the level of intestinal P-glycoprotein (P-gp) expression. Rifampin treatment reduced digoxin plasma concentrations substantially after oral administration and, to a lesser extent, after intravenous (i.v.) administration. Moreover, rifampin increased intestinal P-gp content 3.5 ± 2.1-fold which correlated significantly with the area under the plasma concentration curve under pharmacokinetic calculations up to 144 hours (AUC0-144h) after oral digoxin.. Based on these findings, we concluded that intestinal P-gp affects the extent of digoxin biovailability and that the decreasing oral digoxin bioavailability during rifampin is caused by induction of intestinal P-gp.. Two issues were brought to our attention by Win L. Chiou, Sang M. Chung and Ta C. Wu (College of Pharmacy at the University of Illinois at Chicago). Chiou et al. had requested ...
BioAssay record AID 354662 submitted by ChEMBL: Inhibition of p-glycoprotein expressing human MCF7 cells assessed as [3H]vinblastine accumulation.
TY - JOUR. T1 - Genomic structure, gene expression, and promoter analysis of human multidrug resistance-associated protein 7. AU - Kao, Hsin Hsin. AU - Chang, Ming Shi. AU - Cheng, Jan Fang. AU - Huang, Jin Ding. PY - 2003/2/13. Y1 - 2003/2/13. N2 - The multidrug resistance-associated protein (MRP) subfamily transporters associated with anticancer drug efflux are attributed to the multidrug-resistance of cancer cells. The genomic organization of human multidrug resistance-associated protein 7 (MRP7) was identified. The human MRP7 gene, consisting of 22 exons and 21 introns, greatly differs from other members of the human MRP subfamily. A splicing variant of human MRP7, MRP7A, expressed in most human tissues, was also characterized. The 1.93-kb promoter region of MRP7 was isolated and shown to support luciferase activity at a level 4- to 5-fold greater than that of the SV40 promoter. Basal MRP7 gene expression was regulated by 2 regions in the 5′-flanking region at -1,780-1,287 bp, and at -611 ...
GF120918 has a high inhibitory effect on P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). We developed [11C]GF120918 as a positron emissi
BACKGROUND AND PURPOSE The expression of P-glycoprotein (P-gp), encoded by the multidrug resistance 1 (MDR1) gene, is associated with the emergence of the MDR phenotype in cancer cells. We investigated whether metformin (1,1-dimethylbiguanide hydrochloride) down-regulates MDR1 expression in MCF-7/adriamycin (MCF-7/adr) cells. EXPERIMENTAL APPROACH MCF-7 and MCF-7/adr cells were incubated with metformin and changes in P-gp expression were determined at the mRNA, protein and functional level. Transient transfection assays were performed to assess its gene promoter activities, and immunoblot analysis to study its molecular mechanisms of action. KEY RESULTS Metformin significantly inhibited MDR1 expression by blocking MDR1 gene transcription. Metformin also significantly increased the intracellular accumulation of the fluorescent P-gp substrate rhodamine-123. Nuclear factor-kappa B (NF-kappa B) activity and the level of I kappa B degradation were reduced by metformin treatment. Moreover, ...
The pharmacogenetic evaluation of several genes implicated in drug pharmacokinetics should provide efficient tools for individualizing drug therapy by optimizing drug dosage. This would both improve drug efficacy and prevent adverse effects (19). Such evaluation may be particularly useful for drugs characterized by a narrow therapeutic index and/or significant toxicity, such as the calcineurin inhibitors tacrolimus and cyclosporine. In this study, we demonstrated that several polymorphisms of the MDR1 gene partly explain the variability of tacrolimus dose requirement in renal transplant recipients.. Abundantly expressed in the enterocytes, P-gp, the MDR1 gene product, may play an important role in the variability of tacrolimus absorption (7,20-23⇓⇓⇓⇓). Thus, interindividual variations in P-gp expression and/or function may explain the interindividual variability of tacrolimus bioavailability among individuals. Genetic polymorphisms related to the intestinal expression of P-gp therefore ...
XR9051 is as a potent modulator of P-glycoprotein-mediated multidrug resistance (MDR) following a synthetic chemistry programme based on a natural product lead compound. XR9051 was shown to be a potent inhibitor of the binding of the cytotoxic to P-glycoprotein (EC50 = 1.4 +/- 0.5 nM). XR9051 reverses the MDR phenotype through direct interaction with P-glycoprotein.
TY - JOUR. T1 - Expression of P-glycoprotein in high grade osteosarcomas with special emphasis on chondroblastic subtype. AU - Radig, K.. AU - Hackel, C.. AU - Herting, J.. AU - Oda, Y.. AU - Mittler, U.. AU - Neumann, W.. AU - Roessner, A.. PY - 1997/3/15. Y1 - 1997/3/15. N2 - The development of chemoresistance is one of the major clinical problems in the therapy of malignant bone tumors in childhood. The expression of membrane-bound P-glycoprotein turned out to be an essential factor in the evidence of resistant tumor cells. To investigate the significance of multidrug resistance in the prognosis of highly malignant osteosarcomas, the immunohistologic expression of P-glycoprotein was investigated in the tumor tissue of 52 patients under special consideration of the histologic subtype. The data were compared with the histologic regression grade in the resection specimen and correlated with clinical data. Formalin-fixed, paraffin-embedded tissue and, additionally, fresh frozen material taken ...
inproceedings{1250504, articleno = {abstract O1}, author = {Van der Heyden, S and Daminet, Sylvie and Waelbers, Tim and Paepe, Dominique and Hesta, Myriam and Ducatelle, Richard}, booktitle = {JOURNAL OF COMPARATIVE PATHOLOGY}, issn = {0021-9975}, language = {eng}, location = {Belgrade, Serbia}, number = {4}, pages = {abstract O1:342--abstract O1:342}, title = {Evaluation of mucosal P-glycoprotein expression in the small intestine of dogs with lymphoplasmacytic enteritis}, url = {http://dx.doi.org/10.1016/j.jcpa.2010.09.140}, volume = {143}, year = {2010 ...
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TY - JOUR. T1 - P-glycoproteins in pathology. T2 - The multidrug resistance gene family in humans. AU - Weinstein, Ronald S. AU - Kuszak, Jerome R.. AU - Kluskens, Larry F.. AU - Coon, John S.. PY - 1990. Y1 - 1990. N2 - Many cancers do not respond to chemotherapy on primary exposure to drugs, thus manifesting intrinsic drug resistance. Other cancers that do initially respond subsequently become resistant to the same drugs and simultaneously to other drugs to which the patient has had no previous exposure. This is a form of acquired drug resistance. There is a pressing need to better understand the mechanisms of drug resistance and to use this information to develop strategies for the chemosensitization of drug-resistant tumors. A goal of the pathology laboratory is to offer chemosensitivity tests that identify intrinsic or acquired resistance of tumors to specific drugs or classes of drugs to enable the clinician to tailor therapy to the biology of cancers in individual patients. Multidrug ...
Sofosbuvir and velpatasvir have a medium to high potential for interactions with antiretrovirals. Sofosbuvir is a substrate of the important drug transporters P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), though it is not a substrate for the critical CYP or UGT-1A1 antiretroviral-metabolizing enzymes. The sofosbuvir metabolite GS-331007 is not a substrate of P-gp, BCRP, or other transporters. Velpatasvir is a substrate of P-gp, BCRP, organic anion transport polypeptide (OATP)-1B, and the important metabolizing enzymes CYP3A4, CYP2B6, and CYP2C8. Velpatasvir inhibits P-gp, BCRP, and OATP1B ...
The development of resistance to microtubule-interacting drugs is a multifactorial process. Induction of P-glycoprotein that maintains intracellular drug concentrations below cytotoxic levels is one mechanism involved in Taxol resistance. Interest in epothilone partly relates to the observation that the drug is active in Taxol-resistant cell lines and tumors expressing P-glycoprotein (6, 8), indicating that it is not a substrate for P-glycoprotein. The present study further shows that EpoB neither induces MDR1 expression nor causes the expression of other drug efflux pumps even in a highly EpoB-resistant cell line, EpoB480 (Fig. 1).. The introduction of mutations in drug-targeted proteins is another mechanism of drug resistance. The unusual phenotype of Taxol/epothilone dependence has been described as cancer cells develop resistance to Taxol or the epothilones (15-19). Because abnormal microtubule dynamics impair mitotic spindle function and inhibit normal cell proliferation, it has been ...
One patient died because of massive upper gastrointestinal bleeding. The incidence rate increases with age and the time passing from first symptoms to diagnosis tends to be long. Excitatory amino acid-induced excitation of dopamine-containing neurons in the rat substantia nigra: modulation by kynurenic acid. Spectrum sharing among multiple end-to-content paths of different requests can greatly improve resource efficiency. Thyroid hormone receptor-beta is associated with coronary angiogenesis during pathological cardiac hypertrophy.. This paper describes a method using a programmable calculator to determine generic cialis india intravenous nutritional requirements of severely ill patients. Although minor elevations in WBC count can occur after SE of any type, pleocytosis should not be attributed to SE alone unless all other causes have been eliminated. As demonstrated by indirect immunofluorescence, antigen to this antibody is present on the surface of all three bovine cell lines tested. The ...
Following is the transcript of The Bodys live chat on multidrug resistance, which took place on July 10, 2006, at 3:30 p.m. Eastern Time. The chat was ...
TY - JOUR. T1 - Communication between the nucleotide binding domains of P-glycoprotein occurs via conformational changes that involve residue 508. AU - Gabriel, Mark P.. AU - Storm, Janet. AU - Rothnie, Alice. AU - Taylor, Andrew M.. AU - Linton, Kenneth J.. AU - Kerr, Ian D.. AU - Callaghan, Richard. PY - 2003/6/6. Y1 - 2003/6/6. N2 - Our aim is to provide molecular understanding of the mechanisms underlying the (i) interaction between the two nucleotide binding domains (NBDs) and (ii) coupling between NBDs and transmembrane domains within P-glycoprotein (Pgp) during a transport cycle. To facilitate this, we have introduced a number of unique cysteine residues at surface exposed positions (E393C, S452C, I500C, N508C, and K578C) in the N-terminal NBD of Pgp, which had previously been engineered to remove endogenous cysteines. Positions of the mutations were designed using a model based on crystallographic features of prokaryotic NBDs. The single cysteine mutants were expressed in insect cells ...
TY - JOUR. T1 - Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents. AU - Wang, Xiao. AU - Ren, Qian wen. AU - Liu, Xian xuan. AU - Yang, Yan ting. AU - Wang, Bing hua. AU - Zhai, Rong. AU - Qi, Jia Grace. AU - Tian, Jing wei. AU - Wang, Hong bo. AU - Bi, Yi. PY - 2019/1/1. Y1 - 2019/1/1. N2 - Hederagenin is a naturally occurring pentacyclic triterpenoids compound with multiple pharmacological activities. We recently showed that H6, a synthetic derivative of hederagenin, could enhance the anticancer activity of paclitaxel in drug-resistant cells in vitro and in vivo, but showed poor solubility. With the aim of improving the drug resistant reversal activity of H6, here we designed and synthesized a series of novel H6 analogues. Our results showed that compound 10 at the concentration of 5 μM significantly enhanced the cytotoxicity of paclitaxel to drug-resistant KBV cells and sensitized cells to paclitaxel in arresting cells in G2/M phase and inducing ...
Synthesis of carbon-11-labeled tariquidar derivatives as new PET agents for imaging of breast cancer resistance protein (ABCG2). Appl Radiat Isot. 2010 Jun; 68(6):1098-103 ...
In this study we demonstrate that the placental drug-transporting P-gp can profoundly limit the passage of various potentially toxic or therapeutically beneficial P-gp substrate drugs into the fetus. We further show that this placental P-gp can be completely blocked by orally administered PSC833 or GG918, resulting in greatly increased transplacental passage of drugs into the fetus. Previously, Lankas et al. showed that the absence of Mdr1a P-gp in the placenta of naturally occurring Mdr1a mutant fetuses is associated with increased fetal accumulation and toxicity of the pesticide avermectin (13). Taken together, the data demonstrate that the mouse Mdr1a P-gp makes a major contribution to yet another biologically important protective barrier. The list now includes the blood-brain barrier, the blood-nerve barrier, the blood-testis barrier, the maternal-fetal barrier, and the intestinal barrier (10, 12, 13, 25-28). Thus, P-gp activity protects the central blood circulation and a range of tissue ...
P-glycoprotein (ABCB1) is an ATP-Binding Cassette (ABC) transporter that effluxes anticancer drugs out of the cell. Homology model of human P-gp based on crystal structure of C. elegans P-gp suggests that residues in ICL1 (D164) and ICL3 (D805) interact with NBDs via ball-and-socket joint thus creating a more extensive network surface between TMDs and NBDs (Jin et. al., 2012). It was observed that D164C/D805C mutant when expressed in HeLa cells led to misprocessing of P-gp and failed to transport all tested drug substrates. The misprocessed protein is trapped intracellularly and associates more with chaperone Hsp70.This misfolded protein could be rescued to cell surface by growing at lower temperature (27°C), treatment with substrates (cyclosporine A), modulators (tariquidar) or small corrector molecules for 4-18 hrs. The homology model of human P-gp based on crystal structure of mouse P-gp shows SNPs D800N, V801M and D1088N are located spatially close to Asp805 and all these residues together ...
Buy (S)-(-)-Verapamil Hydrochloride (CAS 36622-29-4), an isomer that inhibits the p-glycoprotein efflux pump in MDR tumor cell lines, from Santa Cruz.
Jeffrey Penny carried out a PhD at the University College of Wales investigating mechanisms and regulation of intestinal and renal transporter proteins. His research continued at the Department of Surgery, University of Dundee investigating the cytoprotective role of the P-glycoprotein efflux transporter against dietary and environmental carcinogen. Collaborative research at the University of Dundee addressed isolation of intestinal stem cells and characterisation of transporter and enzyme activities in nascent tissue grafts. Whilst at the Division of Cell and Molecular Sciences, St. Georges Hospital Medical School, London he studied the expression and characterisation of novel transporter proteins as potential drug targets. He then took up a joint School of Pharmacy/Medicine Fellowship at the University of Manchester to investigate the role of intestinal drug transporters in relation to prediction of therapeutic-drug absorption. He is currently an academic at the School of Pharmacy and leads ...
Zosuquidar (LY335979) is a potent negative modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. - Mechanism of Action & Protocol.
Multidrug resistance (MDR) is a common phenomenon in clinical oncology and is a major obstacle to cancer chemotherapy. Many nanoparticle (NP)-based drug delivery systems have been developed to overcome MDR depending on increasing intracellular drug concentrations via increased cellular uptake and rapid drug Journal of Materials Chemistry B HOT Papers
Table 1. Pharmacokinetic parameters of carbamazepine (200 mg single oral dose) before and after 10 days of honey administration Pharmacokinetic parameters C max (µg.ml -1) AUC (0-72) (µg.h.ml -1) Values are shown as mean ± SEM. (n =12) 68 oducts on the P-gp activity has also been studied. In 108 xin intake, seizures and drug allergy were also ex- in vitro study using various fruit extracts, it was hat extracts of strawberry, orange, apricot and Study de t inhibited the intestinal P-gp [ 13]. In another in vi-111 On day 1, single oral dose of 200 mg carbamazepine study using rat small intestine, extracts of grapefruit rital, Novartis [India] Limited) and 0.5 mg digoxin 73 uice and orange juice inhibited the transport activity of oxin, Burroughs Wellcome, [India] Limited) were 74 gp [ 14]. In a study done in humans, grapefruit juice inistered to the volunteers at 7 AM who were fasted 75 ad no effect on P-gp activity [ 15]. Another human rnight. They were not allowed to take food for fur- 76 ...
A drug-resistant human small cell lung cancer cell line, H209/V6, selected in the presence of increasing concentrations of 9-(4,6-O-ethylidene-β-d-glucopyranosyl)-4′-demethylepipodophyllotoxin (VP-16) from parental H209 cells, is 22-, 9-, and 4-fold resistant to VP-16, 4′-(9-acridinylamino)methanesulfon-m-anisidide, and doxorubicin, respectively, but not cross-resistant to 1,4-dihydroxy-5,8-bis({2-[(2-hydroxyethyl)amino]ethyl}-amino)-9,10-anthracenedione. These cells do not overexpress P-glycoprotein or the multidrug resistance-associated protein. Immunoblotting demonstrates that H209 cells contain the Mr 170,000 isoform of topoisomerase II (topo II), while H209/V6 cells have a Mr 160,000 enzyme but none of the Mr 170,000 isoform. The cell lines have equal amounts of topo IIβ. The H209/V6 cells have a 5-fold decrease in total immunoreactive topo IIα. The catalytic and VP-16-induced DNA cleavage activities of the topo II present in 0.35 m NaCl nuclear extracts are decreased 2- to 3-fold in ...
Sequence requirements of the ATP-binding site within the C-terminal nucleotide-binding domain (NBD2) of mouse P-glycoprotein were investigated by using two recombinantly expressed soluble proteins of different lengths and photoactive ATP analogues, 8-azidoadenosine triphosphate (8N(3)-ATP) and 2,3,4-O-(2,4,6-trinitrophenyl)-8-azidoadenosine triphosphate (TNP-8N(3)-ATP). The two proteins, Thr(1044)-Thr(1224) (NBD2(short)) and Lys(1025)-Ser(1276) (NBD2(long)), both incorporated the four consensus sequences of ABC (ATP-binding cassette) transporters, Walker A and B motifs, the Q-loop, and the ABC signature, while differing in N-terminal and C-terminal extensions. Radioactive photolabeling of both proteins was characterized by hyperbolic dependence on nucleotide concentration and high-affinity binding with K(0.5)(8N(3)-ATP) = 36-37 microM and K(0.5)(TNP-8N(3)-ATP) = 0.8-2.6 microM and was maximal at acidic pH. Photolabeling was strongly inhibited by TNP-ATP (K(D) = 0.1-5 microM) and ATP (K(D) = 0.5-2.7
Background: Treatment failure in leukemia is due to either pharmacokinetic resistance or cell resistanceto drugs. Materials and Methods: Gene expression of multiple drug resistance protein (MDR-1), multidrugresistance-related protein (MRP) and low resistance protein (LRP) was assessed in 45 pediatric ALL cases and 7healthy controls by real time PCR. The expression was scored as negative, weak, moderate and strong. Results:The male female ratio of cases was 2.75:1 and the mean age was 5.2 years. Some 26/45 (58%) were in standardrisk, 17/45(38%) intermediate and 2/45 (4%) in high risk categorie, 42/45 (93%) being B-ALL and recurrenttranslocations being noted in 5/45 (11.0%). Rapid early response (RER) at day 14 was seen in 37/45 (82.3%)and slow early response (SER) in 8/45 (17.7%) cases. Positive expression of MDR-1, LRP and MRP was notedin 14/45 (31%), 15/45 (33%) and 27/45 (60%) cases and strong expression in 3/14 (21%), 11/27 (40.7%) and 8/15(53.3%) cases respectively. Dual or more gene positivity was
The analogs showed a different behavior toward cells with acquired resistance against the normal product disorazole C1 , which owe their resistance phenotype at the least in part to overexpression in the ABCB1 p glycoprotein pump. All agents have been subnanomolar inhibitors of wild kind HeLa cells. Paclitaxel and vinblastine had been 1395 and 502 fold much less active, respectively, during the resistant cells . Knockdown of the Pglycoprotein pump, ABCB1, restored most, of their activity . In contrast, the HeLa DZR cells showed only small cross resistance to the dictyostatin analogs that was thoroughly reversed by ABCB1 knockdown. The information propose that the dictyostatins may perhaps be only weak substrates for ABCB1. Additionally, as the HeLa DZR cells have been generated by just one exposure on the mutagen ethyl methane sulfonate followed by a stepwise improved disorazole C1 exposure, its possible that resistance mechanisms apart from elevated ABCB1 exist, but these never seem to ...
Alzheimers disease (AD), the most common form of neurodegenerative disorder, is characterized by deposition of amyloid-β (Aβ) plaques in the brain. Aβ monomer undergoes nucleation to form oligomers, then soluble aggregates, then fibrils which make up the plaques. Aβ oligomer species are believed to be the most neurotoxic aggregate species. Currently under investigation is a mechanism for Aβ removal from the brain, across the blood-brain barrier (BBB). P-glycoprotein (P-gp) is a membrane-bound efflux protein located on the apical, or blood, side of the BBB, which transports a wide variety of substrates. Further complicating this potential clearance mechanism is the reduction of P-gp cell surface expression in arteries exhibiting cerebral amyloid angiopathy (CAA), or the buildup of amyloid plaques around the arteries. P-gp has been suggested as a potential Aβ clearance mechanism based on its ability to transport a wide variety of amphipathic substrates even though experimental evidence of Aβ
Paritaprevir, ritonavir, and dasabuvir were predicted to inhibit intestinal P-gp, whereas only ritonavir and dasabuvir were predicted to inhibit P-gp in the liver and kidney (Table 4). Only a minimal increase in the exposure (similar magnitude increase for both Cmax and AUC) of digoxin was observed, suggesting that this interaction may have only occurred in the intestine. However, previous reports suggested the lack of sensitivity of digoxin to intestinal P-gp inhibition (Shi et al., 2011; Nader and Foster, 2014), and overprediction of the observed DDI by the static models may be explained in part by some of the assumptions in the calculations. For example, the static model assumes that the compounds are fully soluble in 250 ml and, unlike the PBPK model, static modeling does not account for parameters such as permeability, transit time in the intestine, or compound solubility or dissolution. PBPK modeling significantly improved the DDI predictions of the 3D regimen with digoxin, where the ...
BACKGROUND: The ABC transporter P-glycoprotein (P-gp) is recognized as a site for drug-drug interactions and provides a mechanistic explanation for clinically relevant pharmacokinetic interactions with digoxin. The question of whether several P-gp inhibitors may have additive effects has not yet been addressed. METHODS: We evaluated the effects on serum concentrations of digoxin (S-digoxin) in 618 patients undergoing therapeutic drug monitoring. P-gp inhibitors were classified as Class I, with a known effect on digoxin kinetics, or Class II, showing inhibition in vitro but no documented effect on digoxin kinetics in humans. Mean S-digoxin values were compared between groups of patients with different numbers of coadministered P-gp inhibitors by a univariate and a multivariate model, including the potential covariates age, sex, digoxin dose and total number of prescribed drugs. RESULTS: A large proportion (47%) of the digoxin patients undergoing therapeutic drug monitoring had one or more P-gp ...
P-glycoprotein (Pgp) is expressed in various tissues such as brain, liver, kidney, and intestine (Cordon-Cardo et al., 1990; Brady et al., 2002) and plays an important role in defining the pharmacokinetics of many drugs. Pgp functions as a drug efflux pump and exports hydrophobic, bulky drugs such as anticancer agents, cardiac glycosides, β-blockers, calcium channel blockers, and immunosuppressants. Since Pgp has a broad substrate recognition, the concomitant administration of drugs often causes drug interactions by inhibiting Pgp-mediated transport (Yu, 1999). For example, inhibition of digoxin transport in cultured epithelial cell lines expressing Pgp by various drugs such as quinidine (Tanigawara et al., 1992; Fromm et al., 1999), verapamil (Tanigawara et al., 1992), and cyclosporin A (Okamura et al., 1993) has been reported. We have also demonstrated that the renal clearance of digoxin was decreased in patients receiving a concomitant administration of clarithromycin and, accordingly, the ...
Author: Ebinger, M. et al.; Genre: Journal Article; Published in Print: 2005-09; Title: Is testosterone a substrate of P-glycoprotein in abcb1ab knock out mice?
description of : ABCB4 , anti ABCB4 products, ABC21 anti-GBD1 anti-ICP3 anti-MDR2 anti-MDR2/3 anti-MDR3 anti-PFIC-3 anti-PGY3 and related products to ABCB4, ABC21, GBD1, ICP3, MDR2, MDR2/3, MDR3, PFIC-3, PGY3
Glycoprotein-41 (gp41) and glycoprotein-120 (gp120) are HIV viral coat proteins. Soluble glycoproteins often show a high ... Glycoproteins are important for white blood cell recognition.[citation needed] Examples of glycoproteins in the immune system ... Other examples of glycoproteins include: gonadotropins (luteinizing hormone a follicle-stimulating hormone) glycoprotein IIb/ ... One example of glycoproteins found in the body is mucins, which are secreted in the mucus of the respiratory and digestive ...
Glycoprotein 100, gp100 or Melanocyte protein PMEL is 661 amino acids long and is a type I transmembrane glycoprotein enriched ...
glycoprotein. glycoprotein glī˝kōprō´tēn [key], organic compound composed of both a protein and a carbohydrate joined together ... One set of glycoproteins also carry the blood group determinants. The carbohydrate portion of a glycoprotein is usually a small ... Salivary mucus contains the glycoprotein called mucin. Among other glycoproteins, one particularly interesting example is ... Solutions of glycoproteins usually exhibit high viscosity, an observation explaining the highly viscous character of egg white ...
Envelope glycoprotein GP120 (or gp120) is a glycoprotein exposed on the surface of the HIV envelope. It was discovered by ... Human Immunodeficiency Virus Glycoprotein 120 Vashistha H, Husain M, Kumar D, Singhal PC (2009). "Tubular cell HIV-1 gp120 ... A conserved region in the gp120 glycoprotein that is involved in the metastable attachment of gp120 to CD4 has been identified ... Gp120 is anchored to the viral membrane, or envelope, via non-covalent bonds with the transmembrane glycoprotein, gp41. Three ...
Structure of the chlorovirus PBCV-1 major capsid glycoprotein determined by combining crystallographic and carbohydrate ...
Glycoprotein VI deficiency is a bleeding disorder associated with a decreased ability to form blood clots. Explore symptoms, ... Glycoprotein VI deficiency can be caused by mutations in the GP6 gene, which provides instructions for making a protein called ... Some cases of glycoprotein VI deficiency are not caused by GP6 gene mutations; instead these cases are acquired, which means ... The prevalence of glycoprotein VI deficiency is unknown. At least 15 cases have been described in the scientific literature. ...
Dairpoosh wrote: , Im looking for a method for isolation of Glycoproteins , from plant cells.I would be very grateful if ... Glycoprotein. Dr Engelbert Buxbaum via methods%40net.bio.net (by engelbert_buxbaum from hotmail.com). Fri Apr 6 10:17:07 EST ... Now since you are talking about glycoproteins I presume that you are dealing with a transmembrane protein. To isolate those, ...
Structure Of a zinc-binding domain in the Junin virus envelope glycoprotein. J Biol Chem. 2011;286:1528-36.CrossRefPubMedGoogle ... Unusual molecular architecture of the machupo virus attachment glycoprotein. J Virol. 2009;83:8259-65.PubMedPubMedCentral ... Acidic Ph-induced conformations and Lamp1 binding of the Lassa virus glycoprotein spike. PLoS Pathog. 2016;12:E1005418.PubMed ... Arenavirus Z-glycoprotein association requires Z myristoylation but not functional ring or late domains. J Virol. 2007;81:9451- ...
The HIV envelope glycoprotein is a challenging protein to study by X-ray crystallography as it sits in a membrane, it is ... Because the envelope glycoprotein is critical for infection, it is an obvious target for HIV therapy and thus the subject of ... Ebola glycoprotein, a previous featured structure, serves the same function to recognise host cells and internalise the virus. ... If the body can produce antibodies to the envelope glycoprotein, the virus can be prevented from binding to, and infecting ...
Epididymal Sperm Sperm Plasma Membrane Late Spermatid Major Glycoprotein Epididymal Epithelium These keywords were added by ... Hamilton D.W., Wenstrom J.C., Moore A. (1986) Characterization of a Sperm Membrane Glycoprotein. In: Dhindsa D.S., Bahl O.P. ( ... Brown, C. R., von Glos, K. I., and Jones, R., 1983, Changes in plasma membrane glycoproteins of rat spermatozoa during ... van Lenten, L., and Ashwell, G., 1971, Studies on the chemical and enzymatic modification of glycoproteins, J. Biol. Chem., 246 ...
Amyloidogenic glycoprotein, extracellular (IPR008154). Short name: Amyloid_glyco_extra Overlapping homologous superfamilies * ... This entry represents an extracellular domain that is usually found at the N-terminal of amyloidogenic glycoproteins such as ...
Purchase Glycoprotein and Proteoglycan Techniques, Volume 16 - 1st Edition. Print Book & E-Book. ISBN 9780444806529, ... Glycoprotein and Proteoglycan Techniques, Volume 16 1st Edition. 0.0 star rating Write a review ... 2. Glycoproteins and proteoglycans. 3. Isolation and fractionation. 4. Physico-chemical characterisation. 5. Analysis of ... The past two decades have seen an expansion of interest in glycoproteins. From being a borderline area between carbohydrate and ...
Recombinant Glycoprotein Expression. Product Listing Application Overview Recombinant expression of glycoproteins is of great ... Recombinant Glycoprotein Expression includes these areas of focus: Expression Systems. FAQs for Recombinant Glycoprotein ... Yeast primarily modifies glycoproteins with only high mannose N-glycans.. *Plant and insect cell lines can modify N-glycans ... Some mammalian cell lines can add the non-human epitopes Gal α1-3 Gal or N-glycolylneuraminic acid (NGNA) to glycoproteins. ...
... Mauricio Cesar Palmieri mcpalmie at FOX.CCE.USP.BR Fri Apr 8 07:26:47 EST 1994 *Previous message: How do you ...
... , P-Glycoprotein Inhibitor, P-Glycoprotein Substrate, P-Glycoprotein Inducer, P-gp. ... P Glycoproteins, P-Glycoproteins, P GLYCOPROTEIN Z, P-Glycoproteins [Chemical/Ingredient], p glycoproteins, p-glycoprotein, p- ... P-Glycoprotein. Aka: P-Glycoprotein, P-Glycoprotein Inhibitor, P-Glycoprotein Substrate, P-Glycoprotein Inducer, P-gp ... P-Glycoprotein [Chemical/Ingredient], p-glycoprotein, p glycoprotein, p-gp, glycoprotein p, ATP-Binding Cassette, Sub-Family B ...
Glycoprotein Ib-IX-V complex. The GPIb-IX-V complex is an abundant membrane receptor complex originating in megakaryocytes and ... University of NottinghamResearchGroupsStructural BiologyResearch projectsGlycoprotein GP Ib IX-V ...
The monoclonal antibody has a continuous amino acid sequence, and a binding affinity for the P-glycoprotein which manifests in ... A monoclonal antibody that recognises a structurally continuous and extracellularly-located epitope of human P-glycoprotein is ... Glycoprotein P is a plasma membrane protein which is over-expressed on the surfaces of cell lines or human tumour cells that ... The monoclonal antibody has a continuous amino acid sequence, and a binding affinity for the P-glycoprotein which manifests in ...
... column packed with amide 1.7 lm sorbent was applied to the characterization of glycoprotein digests. Due to the impact of the ... Characterization of glycoprotein digests with hydrophilic interaction chromatography and mass spectrometry. *Gilar M ... column packed with amide 1.7 lm sorbent was applied to the characterization of glycoprotein digests. Due to the impact of the ...
What is P-Glycoprotein?. P-glycoprotein (P-gp) is a plasma membrane protein which acts as a localized drug transport mechanism ...
Glycoprotein glycosylation and cancer progression.. Dennis JW1, Granovsky M, Warren CE. ... Glycosylation of glycoproteins and glycolipids is one of many molecular changes that accompany malignant transformation. GlcNAc ... beta-1,4-mannosyl-glycoprotein beta-1,4-N-acetylglucosaminyltransferase. *alpha-1,6-mannosylglycoprotein beta 1,6-N- ...
tr,P89961,P89961_9HEPC Envelope glycoprotein E1 (Fragment) OS=Hepacivirus C OX=11103 PE=4 SV=1 ...
P-glycoprotein 1 (permeability glycoprotein, abbreviated as P-gp or Pgp) also known as multidrug resistance protein 1 (MDR1) or ... Wikimedia Commons has media related to P-glycoprotein.. *P-Glycoprotein at the US National Library of Medicine Medical Subject ... Increased intestinal expression of P-glycoprotein can reduce the absorption of drugs that are substrates for P-glycoprotein. ... P-gp is a glycoprotein that in humans is encoded by the ABCB1 gene.[4] P-gp is a well-characterized ABC-transporter (which ...
A system for functional analysis of Ebola virus glycoprotein. Ayato Takada, Clinton Robison, Hideo Goto, Anthony Sanchez, K. ... A system for functional analysis of Ebola virus glycoprotein. Ayato Takada, Clinton Robison, Hideo Goto, Anthony Sanchez, K. ... reported the incorporation of foreign glycoproteins (i.e., cellular CD4 or measles virus glycoproteins) into VSV particles. In ... glycoprotein;. GFP,. green fluorescent protein;. ResGP,. Reston GP;. FCS,. fetal calf serum. ...
I think this glycoproteins may be destroyed by Enzymes. Pineaple and papaya contains enzymes. ... A virus has glycoprotein antigen molecules on its surface that bind to surface protein and/or glycoprotein molecules on the ... HIV contains Glycoprotein 120 envelope on its cluster. I think this glycoproteins may be destroyed by Enzymes. Pineaple and ... How cooking beans destroy the glycoprotein structure and function. ?. Asked by Wiki User ...
Antifreeze GlycoProtein Mimetic Polymers. Dal 2015-06-01 al 2020-05-31, progetto in corso ... glyco)proteins (AFGPs) which have several antifreeze effects, including ice recrystallization inhibition (IRI) - they slow ...
Membrane glycoprotein synonyms, Membrane glycoprotein pronunciation, Membrane glycoprotein translation, English dictionary ... definition of Membrane glycoprotein. n. Any of a group of conjugated proteins having a carbohydrate as the nonprotein component ... glycoprotein. (redirected from Membrane glycoprotein). Also found in: Thesaurus, Medical, Encyclopedia. gly·co·pro·tein. (glī′ ... The classic form of MDR is due to an increased activity of P-glycoprotein (P-gp), a 170 kDa plasma membrane glycoprotein. P-gp ...
Arenaviruses are comprised of two RNA genome segments and four proteins, the polymerase L, the envelope glycoprotein GP, the ... Burri, D.J.; Palma, J.R.D.; Kunz, S.; Pasquato, A. Envelope Glycoprotein of Arenaviruses. Viruses 2012, 4, 2162-2181. ... Arenaviruses are comprised of two RNA genome segments and four proteins, the polymerase L, the envelope glycoprotein GP, the ... Burri DJ, Palma JRD, Kunz S, Pasquato A. Envelope Glycoprotein of Arenaviruses. Viruses. 2012; 4(10):2162-2181. ...
... when a beta-2 glycoprotein 1 antibodies test is ordered; and what the results of the test might mean ... Describes how a beta-2 glycoprotein 1 antibodies test is used to help diagnose antiphospholipid syndrome (APS), determine the ... Beta-2 glycoprotein 1 antibody tests are primarily used along with cardiolipin antibody and lupus anticoagulant testing to help ... Beta-2 glycoprotein 1 antibody is an autoantibody that is associated with inappropriate blood clotting. This test detects and ...
  • N-linked protein glycosylation (N-glycosylation of N-glycans) at Asn residues (Asn-x-Ser/Thr motifs) in glycoproteins. (wikipedia.org)
  • glycoprotein glī˝kōprō´tēn [ key ] , organic compound composed of both a protein and a carbohydrate joined together in covalent chemical linkage. (infoplease.com)
  • Glycoprotein VI deficiency can be caused by mutations in the GP6 gene, which provides instructions for making a protein called glycoprotein VI (GPVI). (medlineplus.gov)
  • As a result, there is a shortage (deficiency) of functional GPVI protein on the surface of platelets, which leads to bleeding problems characteristic of glycoprotein VI deficiency. (medlineplus.gov)
  • Now since you are talking about glycoproteins I presume that you are dealing with a transmembrane protein. (bio.net)
  • So, I am wondering whether all of the proteins eluted from lectin chromatography were glycoprotein or a part of the protein was non-glycoprotein. (bio.net)
  • The HIV envelope glycoprotein is a challenging protein to study by X-ray crystallography as it sits in a membrane, it is heavily glycosylated and conformationally heterogenous. (ebi.ac.uk)
  • This entry represents an extracellular domain that is usually found at the N-terminal of amyloidogenic glycoproteins such as amyloid-beta precursor protein (APP, or A4). (ebi.ac.uk)
  • The protein is an ATP-dependent, transmembrane transport/efflux pump glycoprotein that is expressed in liver, kidney, small intestine and brain. (fpnotebook.com)
  • P-glycoprotein (P-gp) is a plasma membrane protein which acts as a localized drug transport mechanism, actively exporting drugs out of the cell. (thebody.com)
  • Monosaccharides commonly found in eukaryotic glycoproteins include: The sugar group(s) can assist in protein folding, improve proteins' stability and are involved in cell signalling. (wikipedia.org)
  • P-glycoprotein 1 (permeability glycoprotein, abbreviated as P-gp or Pgp ) also known as multidrug resistance protein 1 ( MDR1 ) or ATP-binding cassette sub-family B member 1 ( ABCB1 ) or cluster of differentiation 243 ( CD243 ) is an important protein of the cell membrane that pumps many foreign substances out of cells. (wikipedia.org)
  • A 2015 review of polymorphisms in ABCB1 found that "the effect of ABCB1 variation on P-glycoprotein expression (messenger RNA and protein expression) and/or activity in various tissues (e.g. the liver, gut and heart) appears to be small. (wikipedia.org)
  • The surface glycoprotein (GP) is expressed from the fourth of the seven structural protein genes ( 3 , 6 ). (pnas.org)
  • Full-length cDNAs encoding the Ebola Reston virus glycoprotein (ResGP) ( 14 ), VSV G protein ( 15 ), and influenza A/turkey/Ireland/1378/83 (H5N8) virus hemagglutinin ( 16 ) were cloned into a mammalian expression vector, pCAGGS ( 17 ), and designated pCResGP, pCVSVG, and pCTH, respectively. (pnas.org)
  • Arenaviruses are comprised of two RNA genome segments and four proteins, the polymerase L, the envelope glycoprotein GP, the matrix protein Z, and the nucleoprotein NP. (mdpi.com)
  • Glycoprotein 100, gp100 or Melanocyte protein PMEL is 661 amino acids long and is a type I transmembrane glycoprotein enriched in melanosomes, which are the melanin-producing organelles in melanocytes. (wikipedia.org)
  • P-glycoprotein (P-gp) is a transmembrane protein associated with a phenotype of cross resistance to certain anticancer agents. (nih.gov)
  • Researchers at FDA developed an efficacious Filovirus subunit vaccine based on a recombinant protein consisting of the extracellular domain of the Filovirus glycoprotein fused to an Fc Fragment of human immunoglobulin (FiloGP-Fc). (fda.gov)
  • The FiloGP-Fc fusion protein resembles the native glycoprotein expressed at the surface of cells and viral particles. (fda.gov)
  • Ebola virus glycoprotein Fc fusion protein confers protection against lethal challenge in vaccinated mice" Vaccine 2011 Apr. (fda.gov)
  • Glycoproteins are a form of protein that contain sugar residue. (reference.com)
  • The protein part of the glycoprotein is created on the surface by other amino acids. (reference.com)
  • Perturbation of ER-associated functions such as disturbed ER glycoprotein quality control, protein glycosylation and protein folding results in activation of an ER stress coping response. (mdpi.com)
  • Glycoproteins are molecules containing sugar and protein, which permit healthy cell-to-cell communication in the human body. (livestrong.com)
  • Basically, glycoprotein is a biomolecule composed of a protein and a carbohydrate (an oligosaccharide). (wikidoc.org)
  • The removal of one or more alpha 1,2-linked mannose residues from a mannosylated protein that occurs as part of glycoprotein ER-associated glycoprotein degradation (gpERAD). (yeastgenome.org)
  • It is a glycoprotein with a 42-kDa core protein with extensive N-linked glycosylation. (atlasgeneticsoncology.org)
  • Zinc-alpha2-glycoprotein (ZAG), a 43-kDa protein, is overexpressed in certain human malignant tumors and acts as a lipid-mobilizing factor to stimulate lipolysis in adipocytes leading to cachexia in mice implanted with ZAG-producing tumors. (anabolicminds.com)
  • Loss of adipose tissue in cancer cachexia has been associated with tumour production of a lipid-mobilizing factor (LMF) which has been shown to be homologous with the plasma protein zinc-alpha(2)-glycoprotein (ZAG). (anabolicminds.com)
  • Glyco" means "sugar", so glycoproteins are a type of protein linked to a sugar. (paulaschoice.com)
  • On the other hand, glycosylation is a pre-requisite for proper protein folding, which in case of diagnostic and therapeutic glycoproteins should ideally not include immu-nogenic residues. (innovations-report.com)
  • Their cognate GPH receptors (GPHRs) are type A leucine-rich repeat (LRR)-containing G-protein-coupled receptors (LGR) with a large glycoprotein extracellular domain (ECD). (frontiersin.org)
  • Modified C-reactive protein interacts with platelet glycoprotein Ibα. (biomedsearch.com)
  • A conserved region in the gp120 glycoprotein that is involved in the metastable attachment of gp120 to CD4 has been identified and targeting of invariant region has been achieved with a broadly neutralising antibody, IgG1-b12. (wikipedia.org)
  • A monoclonal antibody that recognises a structurally continuous and extracellularly-located epitope of human P-glycoprotein is described. (google.com)
  • 1. A monoclonal antibody that recognizes a structurally continuous and extracellularly-located epitope of human P-glycoprotein consisting of a continuous amino acid sequence, and which has a binding affinity for P-glycoprotein such that it is capable of staining greater than 90% of live CEM-VBL10 cells when tested in a flow cytometry experiment. (google.com)
  • 2. A monoclonal antibody of claim 1 in which the said amino acid sequence is located on the fourth extracellular loop of human P-glycoprotein. (google.com)
  • 9. A method of claim 8 in which a peptide corresponding to a structurally continuous extracellular domain of human P-glycoprotein or a part thereof is used to screen for the desired monoclonal antibody. (google.com)
  • 11. An immunological diagnostic kit containing as specific reagent a monoclonal antibody according to either of claims 1, 2, 3, 4, 5, 6, or 7 for the detection of human multidrug-resistant cells or human P-glycoprotein. (google.com)
  • Beta-2 glycoprotein 1 antibody is an autoantibody that is associated with inappropriate blood clotting. (labtestsonline.org)
  • Beta-2 glycoprotein antibody is considered one of the primary autoantibodies called antiphospholipid antibodies that mistakenly target the body's own lipid-proteins (phospholipids) found in the outermost layer of cells (cell membranes) and platelets. (labtestsonline.org)
  • A Fab fragment of the chimeric monoclonal antibody 7E3 and inhibitor of the glycoprotein (GP) IIb/IIIa receptor, that blocks platelet aggregation. (fpnotebook.com)
  • Because antibody-dependent cell-mediated cytotoxicity (ADCC) exists as an example of glycan function in glycoproteins, there have been many studies of glycan remodeling of antibodies. (go.jp)
  • Antibody cross-competition analysis of the human immunodeficiency virus type 1 gp120 exterior envelope glycoprotein. (semanticscholar.org)
  • Each Heartland Virus Glycoprotein 1 Antibody is fully covered by our Guarantee+, to give you complete peace of mind and the support when you need it. (novusbio.com)
  • Ebola glycoprotein, a previous featured structure , serves the same function to recognise host cells and internalise the virus. (ebi.ac.uk)
  • To circumvent this problem, we developed a novel complementation system for functional analysis of Ebola virus glycoproteins. (pnas.org)
  • Herein we show that Ebola Reston virus glycoprotein (ResGP) is efficiently incorporated into VSV particles. (pnas.org)
  • Chemical modification of cells to alter their surface proteins markedly reduced their susceptibility to VSVΔG*-ResGP but not to VSVΔG*-G. These findings suggest that cell surface glycoproteins with N-linked oligosaccharide chains contribute to the entry of Ebola viruses, presumably acting as a specific receptor and/or cofactor for virus entry. (pnas.org)
  • Jeremy Luban, Aaron Lin, and Ted Diehl join the TWiV team to discuss their work on identifying a single amino acid change i n the Ebola virus glycoprotein from the West African outbreak that increases infectivity in human cells. (virology.ws)
  • Ebola virus (EBOV) entry requires the surface glycoprotein (GP) to initiate attachment and fusion of viral and host membranes. (shapeways.com)
  • As with many viruses targeted by host factors, Ebola virus employs a tetherin antagonist, the viral glycoprotein (EboGP), to counteract restriction and promote virus release. (mdpi.com)
  • Fusing the EboGP msd to a normally secreted form of the glycoprotein effectively promotes Ebola virus particle release. (mdpi.com)
  • 2015. "Requirements within the Ebola Viral Glycoprotein for Tetherin Antagonism" Viruses 7, no. 10: 5587-5602. (mdpi.com)
  • The study showed that CD205, a trans membrane glycoprotein , is robustly expressed in a variety of solid malignancies, such as pancreatic and bladder tumors, as well as triple negative breast cancer (TNBC). (thefreedictionary.com)
  • The IHC study of CD-99 (a cell membrane glycoprotein ) and intranuclear FLI-1 (a DNA-binding transcription factor) is important to diagnose ES. (thefreedictionary.com)
  • NASDAQ: RCKT), is developing its first adeno-associated viral vector -based gene therapy, RP-A501, that is designed to restore the lysosome-associated membrane glycoprotein 2 (LAMP-2) gene which is defective in patients afflicted with Danon disease, the company said. (thefreedictionary.com)
  • Lattice structures forming between LacNAc repeats on N-glycan branches, and galectins determine plasma membrane glycoprotein residency time by inhibiting endocytosis of them (31,34). (thefreedictionary.com)
  • At the beginning of this century, a number of researchers conducted systematic reviews on the association of platelet membrane glycoprotein polymorphisms and risk of CAD. (thefreedictionary.com)
  • Platelet glycoprotein 4 (CD36) (or fatty acyl translocase [FAT], or scavenger receptor class B, member 3 [SCARB3]) is an essential cell surface and skeletal muscle outer mitochondrial membrane glycoprotein involved in multiple functions in the body. (mdpi.com)
  • EboV infection is initiated by the fusion between viral and host cell membranes, which is mediated by the viral membrane glycoprotein (GP) ( 2 , 3 ). (sciencemag.org)
  • Glycoproteins are proteins which contain oligosaccharide chains ( glycans ) covalently attached to amino acid side-chains. (wikipedia.org)
  • Carbohydrates are attached to some proteins to form glycoproteins. (wikipedia.org)
  • Glycoproteins are also often important integral membrane proteins , where they play a role in cell-cell interactions. (wikipedia.org)
  • Many proteins released by cells to the blood and other fluids are glycoproteins. (infoplease.com)
  • Electron microscopy is better placed to study proteins with these characteristics and the image in our calendar is based on the cryoEM map of the envelope glycoprotein solved by Sriram Subramaniam's group. (ebi.ac.uk)
  • A subfamily of transmembrane proteins from the superfamily of ATP-BINDING CASSETTE TRANSPORTERS that are closely related in sequence to P-GLYCOPROTEIN. (fpnotebook.com)
  • 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. (fpnotebook.com)
  • Glycoprotein-41 (gp41) and glycoprotein-120 (gp120) are HIV viral coat proteins. (wikipedia.org)
  • Myelin Oligodendrocyte Glycoprotein (MOG) is one of the proteins in myelin , a fatty insulating substance found in the white matter of the central nervous system . (mult-sclerosis.org)
  • Glycoproteins are proteins that contain oligosaccharide chains ( glycans ) covalently attached to their polypeptide backbones. (wikidoc.org)
  • CandyCane glycoprotein molecular weight standards separate into alternating bands of glycosylated and nonglycosylated proteins during polyacrylamide gel electrophoresis. (thermofisher.com)
  • The P-glycoproteins (Pgps) are a small family of transport proteins associated with the multidrug resistance phenotype of cell lines selected for growth in cytotoxic drugs. (aacrjournals.org)
  • If the body can produce antibodies to the envelope glycoprotein, the virus can be prevented from binding to, and infecting human cells. (ebi.ac.uk)
  • Human broadly neutralizing antibodies to the envelope glycoprotein complex of hepatitis C virus. (semanticscholar.org)
  • N-linked, glycosylation can prevent proper glycoprotein folding and full inhibition can be toxic to an individual cell. (wikipedia.org)
  • Vaccines could aid in raising antibodies, but unfortunately, the envelope glycoprotein is extremely variable due to the high mutation rate of the virus, and also masked by extensive glycosylation, both features which make raising antibodies difficult. (ebi.ac.uk)
  • Glycoprotein glycosylation and cancer progression. (nih.gov)
  • Glycosylation of glycoproteins and glycolipids is one of many molecular changes that accompany malignant transformation. (nih.gov)
  • P-gp is a 170 kDa transmembrane glycoprotein , which includes 10-15 kDa of N-terminal glycosylation. (wikipedia.org)
  • This creates glycoproteins when sugar is added to polypeptides in a process called glycosylation. (reference.com)
  • Recombinant expression of glycoproteins is of great interest, particularly in the production of therapeutic glycoproteins such as immunoglobulins and hormones for the biopharmaceutical market. (neb.com)
  • Recombinant glycoprotein E produced in mammalian cells in large-scale as an antigen for varicella-zoster-virus serology. (gu.se)
  • A recombinant glycoprotein E (gE) from varicella-zoster virus (VZV) was generated and produced in Chinese Hamster Ovary (CHO) cells, in the development of a specific antigen for analysis of IgG antibodies to VZV. (gu.se)
  • Juliano R.L., Ling V.A. A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants. (wikidoc.org)
  • Gp120 is anchored to the viral membrane, or envelope, via non-covalent bonds with the transmembrane glycoprotein, gp41. (wikipedia.org)
  • A 170-kDa transmembrane glycoprotein from the superfamily of ATP-BINDING CASSETTE TRANSPORTERS. (fpnotebook.com)
  • Human p-glycoprotein-1 (1280 aa, 141 kDa) is encoded by the human ATP-binding cassette, sub-family B (MDR/TAP), member 1 (ABCB1) gene. (fpnotebook.com)
  • P-gp is a glycoprotein that in humans is encoded by the ABCB1 gene. (wikipedia.org)
  • They also found 11 different missense mutations in the PMM2 gene in 16 patients suffering from the carbohydrate-deficient glycoprotein type Ia syndrome. (bmj.com)
  • Utilizing low stringency screening, we have identified a novel gene closely related to the Pgps expressed in the pig and other mammalian liver which we have called Sister of P-glycoprotein ( spgp ). (aacrjournals.org)
  • Other examples of glycoproteins include: gonadotropins (luteinizing hormone a follicle-stimulating hormone) glycoprotein IIb/IIIa, an integrin found on platelets that is required for normal platelet aggregation and adherence to the endothelium. (wikipedia.org)
  • Elevated intrathecal myelin oligodendrocyte glycoprotein antibodies in multiple sclerosis. (biomedsearch.com)
  • HIV-1 entry depends on the sequential interaction of the gp120 exterior envelope glycoprotein with the receptors on the cell, CD4 and members of the chemokine receptor family. (nih.gov)
  • ATP-binding cassette (ABC) transporters, in particular P-glycoprotein (encoded by ABCB1), are important and selective elements of the blood-brain barrier (BBB), and they actively contribute to brain homeostasis. (hindawi.com)
  • P-glycoprotein (P-gp/Abcb1), Abcc2, and Abcc3 determine the pharmacokinetics of etoposide. (webmd.com)
  • glycoprotein IIb/IIIa , an integrin found on platelets that is required for normal platelet aggregation and adherence to the endothelium . (wikipedia.org)
  • These images are a random sampling from a Bing search on the term "Glycoprotein IIB/IIIA Inhibitor. (fpnotebook.com)
  • Eptifibatide selectively and reversibly binds to and blocks the platelet glycoprotein IIb/IIIa receptor. (fpnotebook.com)
  • In medicine , glycoprotein IIb/IIIa ( GPIIb/IIIa , also known as integrin α IIb β 3 ) is an integrin complex found on platelets . (wikidoc.org)
  • Defects in glycoprotein IIb/IIIa cause Glanzmann's thrombasthenia . (wikidoc.org)
  • Glycoprotein IIb/IIIa inhibitors can be used to prevent blood clots in an effort to decrease the risk of heart attack or stroke . (wikidoc.org)
  • Without GPVI binding to collagen, platelets cannot come together efficiently to form a clot, leading to the bleeding problems associated with glycoprotein VI deficiency. (medlineplus.gov)
  • The carbohydrate portion of a glycoprotein is usually a small sugar or no more than 8 to 10 individual monosaccharide units. (infoplease.com)
  • A series of chaperones, folding enzymes, glucosidases, and carbohydrate transferases support glycoprotein synthesis and processing. (mdpi.com)
  • A new family of cognate glycoproteins with chitinase-sensitive carbohydrate moiety, chitinoproteins (ChiP) has been detected in Drosophila melanogaster and other insects. (europa.eu)
  • Four types of carbohydrate-deficient glycoprotein syndrome have been described, and the cause of two of them has been found. (bmj.com)
  • 1 Four types of carbohydrate-deficient glycoprotein syndrome have been recognised, depending on the isoelectric focusing pattern of serum sialotransferrins. (bmj.com)
  • Although a heterogenous group of disorders many of the clinical findings of the carbohydrate-deficient glycoprotein syndromes are characteristic, the presentation varies with age and type. (bmj.com)
  • The commonest variety of the carbohydrate-deficient glycoprotein syndromes is type Ia, and in most instances a deficiency of phosphomannomutase has been recognised. (bmj.com)
  • Glycoproteins produced by cultured cells generally have heterogeneous glycans, so it is unclear which glycan is associated with the function of the glycoprotein. (go.jp)
  • To solve this problem, transgenic cells have been developed to produce homogeneous glycoproteins through control of the biosynthetic pathway, but it is difficult to prepare glycoproteins with various kinds of homogeneous glycan by using this approach. (go.jp)
  • Our results indicate the successful in vitro synthesis of a glycoprotein with a GlcNAc2Man5 glycan. (aiche.org)
  • Additionally, we find that a glycoprotein construct, which mimics the cathepsin-activated species by proteolytic removal of the EboGP glycan cap and mucin domains, is unable to counteract tetherin. (mdpi.com)
  • The unique saccharide-binding properties of plant lectins, such as Concanavalin A (Con A) have made them useful for the labeling and isolation of glycan-presenting cells and glycoproteins in serum and cell lysate. (polysciences.com)
  • Some mammalian cell lines can add the non-human epitopes Gal α1-3 Gal or N-glycolylneuraminic acid (NGNA) to glycoproteins. (neb.com)
  • [8] In 2009, the first structure of a mammalian P-glycoprotein was solved (3G5U). (wikipedia.org)
  • Thus, our VSV system should be useful for investigating the functions of glycoproteins from highly pathogenic viruses or those incapable of being cultured in vitro . (pnas.org)
  • What Are the Functions of Glycoproteins? (reference.com)
  • This review summarizes developments and understanding relating to characteristics, synthesis, and functions of prokaryotic glycoproteins. (nih.gov)
  • There are three different types of glycoproteins that are determined differentiated through their synthesis mechanism and structure. (reference.com)
  • Therefore we have developed a cell-free expression system for the synthesis of glycoproteins. (aiche.org)
  • Yeast primarily modifies glycoproteins with only high mannose N-glycans. (neb.com)
  • Unusual molecular architecture of the machupo virus attachment glycoprotein. (springer.com)
  • Filovirus GP is a type I glycoprotein, containing both N-linked and O-linked carbohydrates ( 2 , 8 , 9 ), which contribute to considerably larger molecular weights than those predicted from deduced amino acid sequences. (pnas.org)
  • It is helpful and often necessary to include glycoproteins as standards and/or molecular weight markers. (sigmaaldrich.com)
  • Overexpression of this glycoprotein is associated with multidrug resistance (see DRUG RESISTANCE, MULTIPLE). (fpnotebook.com)
  • Reversal of P-glycoprotein-mediated multidrug resistance and phar. (ingentaconnect.com)
  • Beyer WR, Popplau D, Garten W, Von Laer D, Lenz O. Endoproteolytic processing of the lymphocytic choriomeningitis virus glycoprotein by the subtilase Ski-1/S1p. (springer.com)
  • We offer Heartland Virus Glycoprotein 1 Antibodies for use in common research applications: ELISA. (novusbio.com)
  • Our Heartland Virus Glycoprotein 1 Antibodies can be used in a variety of model species: Virus. (novusbio.com)
  • Choose from our Heartland Virus Glycoprotein 1 polyclonal antibodies. (novusbio.com)
  • Many people make sure to include glycoproteins in their diet as a way to boost their immune systems and prevent or delay the spread of cancer. (livestrong.com)
  • Found in dengue virus and many related viruses, dimers of these viral glycoproteins lie flat on the viral membrane, and are comprised largely of beta-strands. (virology.ws)
  • Furthermore, vesicular stomatitis viruses with HAP2 in place of the viral glycoprotein cannot enter cells. (virology.ws)
  • Babies receive glycoproteins from their mothers' milk that hinder bacteria, viruses and even cancer cells. (livestrong.com)
  • We found that the infection of African green monkey kidney (Vero) cells by vesicular stomatitis viruses bearing the EboV glycoprotein (GP) requires the activity of endosomal cysteine proteases. (sciencemag.org)
  • structural glycoproteins, which occur in connective tissue . (wikipedia.org)
  • One of the three structural glycoproteins of classical swine fever virus (CSFV) is E0, a disulfide-bonded homodimer that induces virus-neutralizing antibodies and occurs in a virion-bound as well as a secreted form. (sciencemag.org)
  • The A33 glycoprotein is a member of the immunoglobulin superfamily and contains three distinct structural domains: a 213 amino acid extracellular region containing two immunoglobulin-like domains (a C2-type domain and a v-type domain), a 23 amino acid hydrophobic transmembrane domain, and a 62 amino acid highly polar intracellular tail containing four consecutive cysteine residues (Heath et al. (atlasgeneticsoncology.org)
  • Synthetic peptide corresponding to a region within amino acids 249 - 311 of Human Oligodendrocyte myelin glycoprotein. (abcam.com)
  • O-Linked glycoproteins often become part of an extracellular matrix after it is secreted by the cell. (reference.com)
  • This extracellular matrix surrounds the O-linked glycoproteins. (reference.com)
  • Towards an understanding of the dystrophin-glycoprotein complex: linkage between the extracellular matrix and the membrane cytoskeleton in muscle fibers. (semanticscholar.org)
  • Glycoproteins change the plasma membrane permeability making it easier for the attraction of eggs to the sperm cells. (reference.com)
  • P-glycoprotein (permeability glycoprotein , abbreviated as P-gp or Pgp ) is a well-characterized ABC-transporter of the MDR / TAP subfamily. (thefullwiki.org)
  • it gives a good, broad perspective on the variable and yet ordered structures shown by glycoproteins and proteoglycans, and a thorough chemical overview of what can and cannot be done to the intact glycoproteins and their isolated glycopeptides. (elsevier.com)
  • To purify glycoproteins or glycopeptides that bind the particular lectin used. (wikidoc.org)
  • Among other glycoproteins, one particularly interesting example is isolated from certain antarctic fishes who survive near-freezing water temperatures as a result of freezing-point depression of their blood serum by a globular glycoprotein. (infoplease.com)
  • Intended for the in vitro quantitative measurement of antibodies directed to β2-Glycoprotein I in human serum and plasma to aid in the diagnosis of antiphospholipid syndrome (APS) and to evaluate the thrombotic risk in patients with systemic lupus erythematosus (SLE). (fishersci.com)
  • OBJECTIVE: To evaluate antibodies to myelin oligodendrocyte glycoprotein (MOG) in the serum and cerebrospinal fluid (CSF) of patients with multiple sclerosis (MS) and control individuals. (biomedsearch.com)
  • Your search returned 44 Glycoprotein M6A ELISA ELISA Kit across 2 suppliers. (biocompare.com)
  • The TWiVirions reveal bacteriophage genes that control eukaryotic reproduction, and the biochemical basis for increased Ebolavirus glycoprotein activity during the recent outbreak. (virology.ws)
  • Although widely distributed in eukaryotic cells glycoproteins appear to be rare in prokaryotic organisms. (nih.gov)
  • We previously developed a first-generation vaccine antigen called DS-Cav1, comprising a prefusion-stabilized form of the fusion (F) glycoprotein, which elicits high-titer protective responses against respiratory syncytial virus (RSV) in mice and macaques. (nature.com)
  • If present in the patient's specimen, antibodies to β2-Glycoprotein I bind to their specific antigen. (fishersci.com)
  • P-glycoprotein (abbreviated as P-gp or Pgp ) is a well characterized human ABC-transporter of the MDR / TAP subfamily. (wikidoc.org)
  • Your search returned 223 envelope glycoprotein Antibodies across 13 suppliers. (biocompare.com)
  • Salivary mucus contains the glycoprotein called mucin. (infoplease.com)
  • P-glycoprotein has also recently been designated CD243 ( cluster of differentiation 243). (thefullwiki.org)
  • Miraculin, is a glycoprotein extracted from Synsepalum dulcificum a berry which alters human tongue receptors to recognize sour foods as sweet. (wikipedia.org)
  • Human vaccine trials, using the cross-reactive glycoproteins B and D, have shown no protection against genital HSV-2 infection or disease. (gu.se)
  • Synthetic peptide within Human P Glycoprotein (C terminal). (abcam.com)
  • The purpose of this research study is to determine the effects of ritonavir and efavirenz on the activity of P-glycoprotein in human brain. (clinicaltrials.gov)
  • Stabilization of the soluble, cleaved, trimeric form of the envelope glycoprotein complex of human immunodeficiency virus type 1. (semanticscholar.org)
  • A human cytomegalovirus glycoprotein complex designated gC-II is a major heparin-binding component of the envelope. (semanticscholar.org)
  • Cell surface heparan sulfate is a receptor for human herpesvirus and interacts with envelope glycoprotein K8.1," Journal of Virology , vol. 75, no. 23, pp. 11583-11593, 2001. (hindawi.com)
  • The processing and function of EboV GP are analogous to those of other type-I envelope glycoproteins, such as Env of the human immunodeficiency virus (HIV) and HA of the influenza virus ( 4 , 7 , 10 - 12 ). (sciencemag.org)
  • Neutralizing antibodies, by contrast, must access the functional envelope glycoprotein complex and typically recognize conserved or variable epitopes near the receptor-binding regions. (nih.gov)
  • The knowledge pertaining to the functional aspects of prokaryotic glycoproteins is rather scarce. (nih.gov)
  • The HIV-1 envelope glycoprotein (Env) functional spike has evolved multiple immune evasion strategies, and only a few broadly neutralizing determinants on the assembled spike are accessible to Abs. (iavi.org)
  • The fusion loop of the dengue virus E glycoprotein cannot substitute for the HAP2 sequence. (virology.ws)
  • There are many structures in the PDB of fragments of glycoprotein bound to antibodies, in efforts to understand the their interaction. (ebi.ac.uk)
  • Interaction of endocytic signals from the HIV-1 envelope glycoprotein complex with members of the adaptor medium chain family. (semanticscholar.org)
  • Some of these N-linked glycoproteins contain carbohydrates. (reference.com)
  • The carbohydrates that are inside the glycoprotein are modified by enzymes that also takes away some of the sugars. (reference.com)
  • A group of metabolic disorders characterised by a defect in the modification of glycoproteins by carbohydrates was first recognised in the early 1980s. (bmj.com)
  • In 1995, a subpopulation of CF-1™ mice with deficient expression of mdr1a P-glycoprotein (PGP) was identified by the department of Safety Assessment, Merck Research Laboratories, West Point, PA. (criver.com)
  • Of course, standard glycoprotein, fetuin was stained well. (bio.net)
  • Last two decades of structure-function studies performed in numerous laboratories provided substantial progress in understanding basic science, physiological, pathophysiological, pharmacological, and comparative aspects of glycoprotein hormones (GPHs) and their cognate receptors. (frontiersin.org)
  • The family of glycoprotein hormones (GPHs) consists of luteinizing hormone (LH), chorionic gonadotropin (CG), follicle-stimulating hormone (FSH), and thyroid-stimulating hormone (TSH), which are heterodimers formed by the non-covalent association of a common alpha (α) and a hormone-specific beta (β) subunit. (frontiersin.org)
  • Eight sugars commonly found in glycoproteins. (wikipedia.org)
  • It then attaches other sugars so that it forms new glycoproteins. (reference.com)
  • The eight sugars contained in glycoproteins. (wikidoc.org)
  • Identifies sugars that the glycoprotein contains and their stoichiometry. (wikidoc.org)
  • this obstacle is mainly due to the overexpression of P-glycoprotein (P-gp). (ingentaconnect.com)
  • During the arenavirus life cycle, processing of the viral envelope glycoprotein precursor (GPC) by the cellular subtilisin kexin isozyme-1 (SKI-1)/site-1 protease (S1P) is crucial for productive infection. (springer.com)
  • 13 ) reported the incorporation of foreign glycoproteins (i.e., cellular CD4 or measles virus glycoproteins) into VSV particles. (pnas.org)

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