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Showing 1 to 20 of 162 for “"Multidrug resistance"”.
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4-ISOXAZOLYL-1,4-DIHYDROPYRIRINES BIND THE MULTIDRUG-RESISTANCE TRANSPORTER
<p>The development of multidrug resistance in tumor cells has been recognized as a major obstacle to successful cancer treatment. Tumor cells in vitro and in vivo can develop multidrug resistance (MDR) to the lethal effects of a variety of cytotoxic drugs used to treat cancerous tumor cells. The …
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4-ISOXAZOLYL-1,4-DIHYDROPYRIRINES BIND THE MULTIDRUG-RESISTANCE TRANSPORTER
<p>The development of multidrug resistance in tumor cells has been recognized as a major obstacle to successful cancer treatment. Tumor cells in vitro and in vivo can develop multidrug resistance (MDR) to the lethal effects of a variety of cytotoxic drugs used to treat cancerous tumor cells. The …
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Multidrug resistance-associated protein 2 (MRP2) and oxaliplatin transport
… We hypothesized that the efflux transporter multidrug resistance protein-2 (MRP2), encoded for by the ABCC2 gene, may play a role in determining cellular sensitivity to oxaliplatin by transporting oxaliplatin-derived platinum. Human MRP2-expressing inside-out membrane vesicles prepared from …
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The nucleotide binding domains of multidrug resistance-p-glycoproteins
Bibliography: leaves 116-128.
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Engineering membrane-selective antibiotic peptides to combat multidrug resistance
Antibiotic resistance is a global health emergency that mandates new drug development strategies. Natural antimicrobial peptides (AMPs) have been long-recognized as a potential source of bacteriolytic drugs, but the shortcomings of non-specific membrane toxicity, proteolytic instability, and in …
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Broad Ligand Specificity in the Small Multidrug Resistance Transporter EmrE
<p>EmrE, an <italic>E. coli</italic> small multidrug resistance transporter, effluxes a diverse range of toxic polyaromatic cations, thus imparting resistance to drug compounds of this type. Transporters must interconvert between inward- and outward-facing structures during the transport cycle to …
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Subcellular Localization and Activity of the Multidrug Resistance Protein 1
<p>Multi-drug resistance or MDR is a major impediment to the successful administration of chemotherapy. Broadly defined, the term MDR applies to any mechanism the cell uses to counter the effects of chemotherapeutic agents, protecting the cell at once against the toxicity of many, structurally …
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Nanomaterials and Block Copolymers for Overcoming Multidrug Resistance in Cancer
The development of multidrug resistance in cancer is one of the leading causes for decreased chemotherapy efficacy and is particularly threatening to aggressive cancers such as that of the pancreas. In cancers where chemotherapy is amongst the few treatment options, it is crucial to develop …
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Modulation of the Expression of Multidrug Resistance Proteins by Sulforaphane and Erucin
Sulforaphane increases gene expression through binding of the Nrf2 transcription factor to the antioxidant response element (ARE) in the promoter region of target genes. Because SF and ER increased MRP1 expression at the mRNA level, we investigated the impact of these compounds on MRP1 …
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Structural and Mechanistic Studies of Multidrug Resistance Efflux Pumps in Multiple Families
Multidrug resistance, whereby pathogens develop resistance to several antimicrobial agents, is a large and growing public health concern globally. In order to combat its continued spread, a better understanding of resistance mechanisms is necessary. One recurring mechanism of multidrug resistance …
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Characterization and Inhibition of the Dimer Interface in Bacterial Small Multidrug Resistance Proteins
As one of the mechanisms of antibiotic resistance, bacteria use several families of membrane-embedded α-helical transporters to remove cytotoxic molecules from the cell. The small multidrug resistance protein family (SMR) is one such group of drug transporters that because of their relative small …
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Ritonavir - A Novel Multidrug Resistance Modulator in Cancer Chemotherapy and Ocular Neovascular Diseases
Multidrug resistance (MDR), a clinical outcome characterized by subtherapeutic intracellular drug concentration, is one of the predominant factors limiting effective cancer chemotherapy. Several possible mechanisms and molecular alterations have been implicated in the development of MDR, including …
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Mechanisms of multidrug resistance in bladder cancer: the role of the nuclear membrane
Multidrug resistance (MDR) describes the phenomenon whereby cancer cells<br/>exposed to a single cytotoxic drug develop cross resistance to numerous other<br/>structurally unrelated chemotherapeutics. The development of MDR is a major<br/>cause of cancer chemotherapy treatment failure in all types …
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Expression profile of multidrug resistance genes and proteins in cancerous and stem cells
… cells and discover their association with multidrug resistance (MDR) related genes, i.e. multiple drug resistance I (mdrl) gene and anti-apoptotic gene (bcl-2) in human glioma compared to normal brain tissues and cell lines. Glioma and normal astrocyte cell lines have been employed for …
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Development of novel strategies to combat multidrug resistance mediated by efflux transporters and intracellular bacteria
<p>Multidrug resistance (MDR) is the condition where cancer cells or microorganisms cease to respond to multiple drugs. MDR conferred by efflux transporters, that deprive the bioavailability of drugs at their site of action, are a threat to cancer and malarial chemotherapy. Specifically, the …
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The Evaluation of Conserved Amino Acids that Influence Polysubstrate Specificity in the Multidrug Resistance Transporter, EmrE
… mechanism of substrate recognition/binding by multidrug resistance transporters has taken different approaches. I have utilized a PCR-driven site-directed mutagenesis analysis to alter conserved amino acid residues within the Escherichia coli small multidrug transporter, EmrE. The EmrE variants …
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Multidrug resistance proteins (MRP) transport the cytokine/nuclear protein High Mobility Group Box 1 (HMGB1) across membranes
… Iysosomes, and the direct involvement of Multidrug Resistance Proteins (MRP/ABCC) in the transport process. I started with the observation that HMGB1 and IL-1 beta, another leaderless cytokine, do colocalize inside secretory Iysosomes in macrophages, and that a pharmacological inhibitor of …
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Mechanism of sarcoplasmic reticulum Ca-ATPase and multidrug resistance P-glycoprotein probed by Pi-HOH oxygen exchange
Bibliography: leaves 135-146.
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The Role of Astrocyte-Derived Factors in the Regulation of Multidrug Resistance at the Developing Blood-Brain Barrier
P-glycoprotein (P-gp; encoded by Abcb1) at the blood-brain barrier (BBB) plays an important role in regulating the movement of exogenous and endogenous substrates into the developing brain. P-gp levels in brain endothelial cells (BECs), which form the capillaries of the BBB, increase dramatically …
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