33 results about "Efflux transporters" patented technology

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.

Methods and compositions are described for the modulation of central nervous system and / or fetal effects of calcineurin inhibitors. 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 at Blood-Tissue, blood-CSF and placental-maternal barriers to increase the efflux of calcineurin inhibitor from physiological compartments, including central nervous system and fetal compartments.

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.

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).

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.

Homologs of the E. coli proteins orf353, bacterial lg-like domain (group 1) protein (orf405), flu antigen 43 (orfl 364), NodT-family outer-membrane-factor-lipoprotein efflux transporter (orfl 767), gspK (orf3515), gspJ (orf3516), toriB-dependent siderophore receptor (orO597), fibrial protein (orf3613), upec-948, upec- 1232. A chain precursor of the type- 1 fimbria! protein (upec- 1875), yapH homolog (upec-2820), hemolysin A (recp-3768), and Sel l repeat-containing protein (upec-521 1 ) from several pathogenic strains of E. coli have been identified with regions within the proteins that are conserved across all E. coli. Fragments corresponding to the conserved regions, especially immunogenic fragments such a linear B-epitopes, are provided.; In addition, variants of the bacterial lg-l ike domain (group 1 ) protein (orf405), yapH homolog (upec2820) and two different fragments of hemolysin A (recp3768) are provided herein that have increased solubility as compared to the native protein where the variants still raise a substantially similar immune response in a subject as the corresponding native protein.

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.

Described are compounds and methods useful in measuring membrane permeability and efflux transporter activity in bacteria, including multidrug resistance Gram negative bacteria.

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.

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.