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33 results about "Efflux transporters" patented technology
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Method for augmentation of intraepithelial and systemic exposure of therapeutic agents having substrate activity for cytochrome P450 enzymes and membrane efflux systems following vaginal and oral cavity administration
InactiveUS20070036834A1Improve bioavailabilityImprove drug solubilityBiocidePowder deliveryWhole bodyMedicine
A vaginal or buccal delivery of therapeutic agents having a substrate affinity for metabolic cytochrome P-450 enzymes and membrane efflux transporter systems. A method for augmentation of systemic exposure to the therapeutic agents having a substrate affinity for cytochrome P-450 enzymes and membrane efflux transporter systems, by delivering said agents to the systemic circulation through vaginal or buccal mucosa.
Owner:FEMINA PHARMA +1
Methods and compositions for treating pain
InactiveUS20070087977A1Sufficient amountReduce central nervous system effectBiocideNervous disorderMedicineEfflux transporters
Methods and compositions are described for the modulation of central nervous system and / or fetal effects of substances. Methods and compositions are described for the modulation of efflux transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide for the increase of efflux transporter activity at blood-brain, blood-CSF and placental-maternal barriers to increase the efflux of drugs and other compounds from physiological compartments, including central nervous system and fetal compartments.
Owner:LIMERICK BIOPHARMA INC
Methods and compositions for treating pain
InactiveUS20060111307A1Sufficient amountReduce central nervous system effectBiocideSenses disorderMedicineCompound (substance)
Methods and compositions are described for the modulation of central nervous system and / or fetal effects of substances. Methods and compositions are described for the modulation of efflux transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide for the increase of efflux transporter activity at blood-brain, blood-CSF and placental-maternal barriers to increase the efflux of drugs and other compounds from physiological compartments, including central nervous system and fetal compartments.
Owner:LIMERICK NEUROSCI
Efflux inhibitor compositions and methods of treatment using the same
InactiveUS20140235631A1Improve blood-brain barrier permeabilityBiocidePowder deliveryIntestinal structureHematopoietic cell
The present invention relates to efflux inhibitor compositions and methods of using these agents for treating conditions where the activity of efflux transporter proteins (e.g., Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP)) inhibit effective delivery of a therapeutic agent to a target tissue (e.g., brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, and / or stem cells).
Owner:IZUMI TECH +1
Methods and compositions for therapeutic treatment
InactiveUS20090325906A1Reduce and eliminate hyperglycemiaBiocideAntipyreticAcute hyperglycaemiaTherapeutic treatment
Methods and compositions are described for the modulation of hyperglycemia and / or one or more symptoms of hyperglycemia. Methods and compositions are described for the modulation of efflux transporter activity to increase the efflux of calcineurin inhibitors out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide for the increase of efflux transporter activity to increase the efflux of calcineurin inhibitor from physiological compartments.
Owner:LIMERICK BIOPHARMA INC
Method for augmentation of intraepithelial and systemic exposure of therapeutic agents having substrate activity for cytochrome P450 enzymes and membrane efflux systems following vaginal and oral cavity administration
A vaginal or buccal delivery of therapeutic agents having a substrate affinity for metabolic cytochrome P-450 enzymes and membrane efflux transporter systems. A method for augmentation of systemic exposure to the therapeutic agents having a substrate affinity for cytochrome P-450 enzymes and membrane efflux transporter systems, by delivering said agents to the systemic circulation through vaginal or buccal mucosa.
Owner:FEMINA PHARMA +1
Methods and compositions for therapeutic treatment
InactiveUS20060111308A1Reduce and eliminate effectTherapeutic effectBiocideSenses disorderMedicineCompound (substance)
Methods and compositions are described for the modulation of central nervous system and / or fetal effects of substances. Methods and compositions are described for the modulation of efflux transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide for the increase of efflux transporter activity at blood-brain, blood-CSF and placental-maternal barriers to increase the efflux of drugs and other compounds from physiological compartments, including central nervous system and fetal compartments.
Owner:LIMERICK NEUROSCI
Soluble pyrone analogs methods and compositions
InactiveUS20090082400A1Reduce appetiteWeaken energyBiocideAntipyreticQuercetin derivativesCyclodextrin
Methods and compositions are described that comprise pyrone analogs such as flavonoids and cyclodextrins including quercetin and quercetin derivatives and sulfoalkyl ether cyclodextrins. In some cases the compounds of the invention are administered with a therapeutic agent such as an analgesic. In some cases, treatment with the compositions of the invention can result in the modulation of central nervous system and / or fetal effects of substances. Methods and compositions are described for the modulation of efflux transporter activity to increase the efflux of drugs and other compositions out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide for the increase of efflux transporter activity at blood-brain, blood-CSF and placental-maternal barriers to increase the efflux of drugs and other compositions from physiological compartments, including central nervous system and fetal compartments.
Owner:LIMERICK BIOPHARMA INC
Methods and compositions for treating pain
InactiveUS20090076053A1Reduce central nervous system effectEliminate central nervous system effectBiocideSenses disorderMedicineEfflux transporters
Methods and compositions are described for the modulation of central nervous system and / or fetal effects of substances. Methods and compositions are described for the modulation of efflux transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide for the increase of efflux transporter activity at blood-brain, blood-CSF and placental-maternal barriers to increase the efflux of drugs and other compounds from physiological compartments, including central nervous system and fetal compartments.
Owner:LIMERICK BIOPHARMA INC
Methods and compositions for therapeutic treatment
InactiveCN101573109AOrganic active ingredientsNervous disorderTherapeutic treatmentEfflux transporters
Owner:LIMERICK BIOPHARMA INC
Flavonoid Dimers and Methods of Making and Using Such
ActiveUS20090197943A1Reduce multidrug resistanceDelay drug resistanceBiocideOrganic chemistryCytotoxicityDrug accumulation
Multidrug resistance (MDR) is a major problem in cancer chemotherapy. The best characterized resistance mechanism is the one mediated by the over-expression of drug efflux transporters, permeability-glycoprotein (P-gp), which pump a variety of anticancer drugs out of the cells, resulting in lowered intracellular drug accumulation. A series of flavonoid dimers are developed in this invention, which are linked together by linker groups of various lengths. These flavonoid dimers are found to be efficient P-gp modulators that increase cytotoxicity of anticancer drugs in vitro and dramatically enhance their intracellular drug accumulation. It is found that the flavonoid dimers of this invention is also useful in reducing drug resistance in treating parasitic diseases.
Owner:THE HONG KONG POLYTECHNIC UNIV +1
Sorghum aluminum tolerance gene, SbMATE
InactiveUS7582809B2Improve toleranceImprove abilitiesBryophytesSugar derivativesCITRATE ESTERHigh level expression
The major aluminum tolerance gene, the SbMATE gene, encodes a root citrate efflux transporter that is Al-inducible at the level of gene transcription and is also Al-activated at the level of protein function. High level of expression of the SbMATE gene and the protein was found in roots. SbMATE orthologs with high degree of sequence homology were found in other higher plants, including rice. Successful transformation of Arabidopsis provides strong evidence that SbMATE can work across species to enhance tolerance to Al in other important crops grown in localities worldwide where Al3+ cations are present in acid soils and are toxic to plants.
Owner:US SEC AGRI +1
Efflux inhibitor compositions and methods of treatment using the same
InactiveUS20190167630A1Improve blood-brain barrier permeabilityPowder deliveryOrganic active ingredientsHematopoietic cellSpinal cord
The present invention relates to efflux inhibitor compositions and methods of using these agents for treating conditions where the activity of efflux transporter proteins (e.g., Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP)) inhibit effective delivery of a therapeutic agent to a target tissue (e.g., brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, and / or stem cells).
Owner:IZUMI TECH
Method for increasing yield of L-alanyl-L-glutamine from recombinant escherichia coli
InactiveCN105543155AImprove conversion rateIncrease productionBacteriaMicroorganism based processesEscherichia coliL-alanyl-l-glutamine
The invention discloses a method for improving activity of an L-alanyl-L-glutamine biosynthesis system containing recombinant DNA. A recombinant plasmid of the recombinant escherichia coli comprises an amino-acid ester acyltransferase encoding gene (SAET) which can catalyze L-glutamine and L-alanine methyl ester hydrochloride to generate L-alanyl-L-glutamine, and a multidrug efflux transporter protein encoding gene (ydeE) which can transporting L-alanyl-L-glutamine outside cells from cells, and due to co-expression of the two encoding genes, stability of a bacterium can be effectively improved, and the yield and the transformation rate of the bacterium can be increased. The recombinant plasmid is obtained by recombining SAET and ydeE with the same plasmid, or by co-transforming two recombinant plasmids with different resistances of two genes respectively. The yield of L-alanyl-L-glutamine of the recombinant bacterium can be increased by 3.33 times when compared with a conventional yield.
Owner:JIANGNAN UNIV
Pathogen resistant plant cells and methods of making
InactiveUS20150037893A1Cell receptors/surface-antigens/surface-determinantsPlant peptidesPlant cellGene Modification
The present invention relates to genetically modified plant cells that have reduced expression or activity of at least one amino acid efflux transporter and / or at least one mineral efflux transporter compared to levels of expression or activity of the at least one amino acid efflux transporter or mineral efflux transporter in an unmodified plant cell. The present invention also relates to genetically modified plant cells that have increased expression or activity of at least one amino acid influx transporter and / or at least one mineral influx transporter compared to levels of expression or activity of the at least one amino acid influx transporter or mineral influx transporter in an unmodified plant cell.
Owner:THE GENERAL HOSPITAL CORP +1
Assay and kit for drug efflux transporter activity
The present invention relates to high-throughput cell-based assays for real-time monitoring of multi-resistant drug protein activity. The present invention is an improvement over existing assays in that in addition to a fluorescent drug efflux probe as an indicator of MDR protein activity, the instant assays provide an o-tolidine-based dye for quenching extracellular fluorescence of the probe.
Owner:BOARD OF RGT UNIV OF NEBRASKA
Novel conditionally immortalized human proximal tubule cell line expressing functional influx and efflux transporters
InactiveUS20130130223A1Genetically modified cellsArtificial cell constructsMicroorganismPharmacology toxicology
The invention relates to the field of biology and medicine. In particular, the invention relates to the field of pharmaceutical research and drug development, and especially to means for physiological, pharmacological and toxicological research. More in particular, the invention provides renal cell lines with proximal tubular characteristics including multiple influx and efflux transporters. These cell lines are termed ciPTEC. Four representative examples have been deposited at the Deutsche Sammlung von Mikroorganismen and Zellkulturen GmbH (DSMZ or German Collection of Microorganisms and Cell Cultures) at Inhoffenstrasse 7 B, 38124 Braun-schweig, Germany under accession number DSM ACC3019, DSM AC-C3020, DSM ACC3021 and DSM ACC3022.
Owner:STICHTING KATHOLIEKE UNIV
Compositions and methods related to silicon transport
InactiveUS20110154532A1Improve the immunityIncreased and decreased silicon transportImmunoglobulinsFermentationNucleotideSilicon uptake
Based on our identification of silicon influx and efflux transporter genes in plants known to take up silicon efficiently including wheat, horsetail, oat, sorghum, and barley, the present invention features polynucleotides encoding silicon transporters; vectors, cells, and plants including such polynucleotides, and methods for making such plants. The invention also features silicon transporter polypeptides and fragments thereof. Plants expressing heterologous silicon transporters may exhibit both increased silicon uptake and increased resistance to biotic and abiotic stresses. In particular, plants such as soybean expressing silicon transporters may exhibit increased resistance to pathogens such as rust.
Owner:UNIV LAVAL
Flavonoid dimers and methods of making and using such
ActiveUS8710097B2Delay drug resistanceReduce resistanceBiocideOrganic chemistryCytotoxicityDrug accumulation
Multidrug resistance (MDR) is a major problem in cancer chemotherapy. The best characterized resistance mechanism is the one mediated by the over-expression of drug efflux transporters, permeability-glycoprotein (P-gp), which pump a variety of anticancer drugs out of the cells, resulting in lowered intracellular drug accumulation. A series of flavonoid dimers are developed in this invention, which are linked together by linker groups of various lengths. These flavonoid dimers are found to be efficient P-gp modulators that increase cytotoxicity of anticancer drugs in vitro and dramatically enhance their intracellular drug accumulation. It is found that the flavonoid dimers of this invention is also useful in reducing drug resistance in treating parasitic diseases.
Owner:THE HONG KONG POLYTECHNIC UNIV +1
Conserved escherichia coli immunogens
Owner:NOVARTIS AG
Pharmaceutical oral dose formulation and composition of matter
An apparatus and method for formulating low solubility, low permeability and / or p-glycoprotein efflux transporter substrate drugs or herbal extracts for increased intestinal absorption. The method utilizes a supercritical fluid, such as carbon dioxide to complex a low solubility, low permeability and / or p-glycoprotein efflux transporter substrate drug or herbal extract, the p-glycoprotein inhibitors quercitin and piperine, with a carbohydrate. The result is a micro-emulsion of the drug or herbal extract which has both higher solubility and permeability than if dosed alone; as well as resistance to p-glycoprotein mediated efflux, once absorbed into the intestinal lumen.
Owner:THROWER DAVID W
Compositions and methods related to silicon transport
Based on our identification of silicon influx and efflux transporter genes in plants known to take up silicon efficiently, including wheat, horsetail, oat, sorghum, and barley, the present invention features polynucleotides encoding silicon transporters; vectors, cells, and plants including such polynucleotides, and methods for making such plants. The invention also features silicon transporter polypeptides and fragments thereof. Plants expressing heterologous silicon transporters may exhibit both increased silicon uptake and increased resistance to biotic and abiotic stresses. In particular, plants such as soybean expressing silicon transporters may exhibit increased resistance to pathogens such as rust.
Owner:UNIV LAVAL
Fluorescent probes for drug permeability in gram negative bacteria
ActiveUS20200018705A1Fluorescence enhancementControl concentrationCompound screeningOrganic chemistryFluoProbesMembrane permeability
Described are compounds and methods useful in measuring membrane permeability and efflux transporter activity in bacteria, including multidrug resistance Gram negative bacteria.
Owner:SAINT LOUIS UNIVERSITY +1
A kind of pharmaceutical composition and its preparation method and application
ActiveCN107158070BImprove solubilityImprove permeabilityOrganic active ingredientsCardiovascular disorderPuerarinPharmaceutical drug
The invention relates to a pharmaceutical composition, and a preparation method and application thereof. The pharmaceutical composition disclosed in the invention contains puerarin and Ligusticum wallichii extract used as active components; preferably, the pharmaceutical composition does not contain other active components. The Ligusticum wallichii extract in the pharmaceutical composition can improve the dissolving capability of puerarin, enhance the intestinal permeability of puerarin, reduce the influence of intestinal efflux transport protein P-gp on efflux of puerarin, improve the oral absorption of puerarin from a plurality of links and enhance the oral bioavailability of puerarin, so synergistic effect is exerted on treatment of cardiovascular and cerebrovascular diseases.
Owner:SOUTHERN MEDICAL UNIVERSITY
Compositions and methods for the treatment of aud
PendingUS20220125816A1Increase in liabilityIncreased toxicityOrganic active ingredientsNervous disorderAlcohol abuse disorderEfflux transporters
Provided herein are methods to improve transport or uptake of an avermectin compound in a cell or tissue expressing an efflux transporter P-glycoprotein (Pgp) by co-administering an effective amount of the avermectin compound and a Ppg inhibitor to the cell or tissue. The method also provides improved efficiency transport or uptake of an avermectin compound in the cell or tissue. The methods can be used therapeutically to treat Alcohol Use Disorder.
Owner:UNIV OF SOUTHERN CALIFORNIA
Assay and kit for drug efflux transporter activity
Owner:BOARD OF RGT UNIV OF NEBRASKA
Fluorescent probes for drug permeability in gram negative bacteria
ActiveUS11092549B2Fluorescence enhancementControl concentrationCompound screeningOrganic chemistryFluoProbesMembrane permeability
Owner:SAINT LOUIS UNIVERSITY +1
Deuterated analogs of elacridar
ActiveUS11504366B2Organic active ingredientsIsotope introduction to heterocyclic compoundsHematopoietic cellBiliary tract
The present invention relates to efflux inhibitor compounds, compositions, and methods of using the same. More specifically, the instant invention comprises deuterated analogs of elacridar with superior pharmacokinetic properties such that it is now possible to facilitate accumulation and distribution of therapeutic agents to effective levels in cells or compartments protected by efflux transporter proteins such as Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP). Such transporter protected compartments include brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, stem cells, and solid tumors. In other embodiments, the present invention comprises methods of using the instant deuterated analogs.
Owner:IZUMI TECH
Pharmaceutical Oral Dose Formulation and Composition of Matter
InactiveUS20180071214A1Low systemic bioavailabilityPrevents intestinal uptakePowder deliveryHydroxy compound active ingredientsQuercitrinEnterosorption
A method of formulating low solubility, low permeability and / or p-glycoprotein efflux transporter substrate drugs or herbal extracts for increased intestinal absorption and a composition of matter for said drugs or herbal extracts. The method utilizes a water, alcohol or organic solvent to complex a low solubility, low permeability and / or p-glycoprotein efflux transporter substrate drug or herbal extract, the p-glycoprotein inhibitors quercitin and piperine, with a carbohydrate. The result is a microemulsion of the drug or herbal extract which has both higher solubility and permeability than if dosed alone; as well as resistance to p-glycoprotein mediated efflux, once absorbed into the intestinal lumen.
Owner:THROWER DAVID W
Application of a kind of Boai capsule as liver transporter inhibitor
ActiveCN104352632BImprove efficacyDecreased hepatic clearanceOrganic active ingredientsCapsule deliveryWestern medicineDisease
The invention relates to an application of a cacumen platyclad-folium artemisiae argyi capsule as a liver transporter inhibitor. Particularly, the cacumen platyclad-folium artemisiae argyi capsule plays an inhibiting role on the liver transporter (comprising an uptake transporter and an efflux transporter), so that the cacumen platyclad-folium artemisiae argyi capsule can be combined with western medicines in use for preventing or treating diseases, for example, the cacumen platyclad-folium artemisiae argyi capsule used as the liver transporter inhibitor is combined with irbesartan in use for preventing and treating hypertension.
Owner:YANGTZE RIVER PHARMA GRP BEIJING HAIYAN PHARMA +1
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