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Full-Text Articles in Life Sciences
Characterization Of Cucurbitacin-Inspired Estrone Analogues As Novel Inhibitors Of Human Atp- Binding Cassette Proteins (Abcb1 And Abcc1), Jennifer Kyeremateng
Characterization Of Cucurbitacin-Inspired Estrone Analogues As Novel Inhibitors Of Human Atp- Binding Cassette Proteins (Abcb1 And Abcc1), Jennifer Kyeremateng
Electronic Theses and Dissertations
ATP-binding cassette (ABC) transporters are a large class of integral membrane proteins that contribute to key physiological functions in all organisms by utilizing ATP binding and hydrolysis to transport diverse substrates across membrane barriers. P-glycoprotein (P-gp/ ABCB1) and Multidrug Resistance protein 1 (MRP1/ABCC1) are widely reported ABC transporters associated with multidrug resistance in cancer. Multidrug resistance (MDR) mediated by P-gp and MRP1 is responsible for treatment failures of many metastatic cancers as a result of reduced accumulation, bioavailability and diminished potency of anticancer drugs. Currently, known P-gp and MRP1 inhibitors are limited due to toxicity, lack of selectivity and low …
Identification And Characterization Of Modulators Of Human Mrp1 (Abcc1) And Human Mrp2 (Abcc2) Expression, Vivian Osei Poku
Identification And Characterization Of Modulators Of Human Mrp1 (Abcc1) And Human Mrp2 (Abcc2) Expression, Vivian Osei Poku
Electronic Theses and Dissertations
ATP-binding cassette (ABC) transporters are known to play a critical role in conferring multidrug resistance (MDR) in various cancers. Several retrospective analyses of chemotherapy results have reported high expression of Multidrug Resistance Protein 1 (MRP1) and Multidrug Resistance Protein 2 (MRP2) in tumor cells exhibiting the MDR phenotype. High MRP1 and MRP2 expression in cancer patients predict a higher risk of treatment failure, resulting in relapse and disease recurrence as well as shortened survival rates. The key role of MRP1 and MRP2 play in the development of MDR makes them important therapeutic targets that hold a great promise for addressing …
Discovery And Characterization Of Novel Substrate Selective Inhibitors Of Human Mrp1 (Abcc1), Angelina Sampson
Discovery And Characterization Of Novel Substrate Selective Inhibitors Of Human Mrp1 (Abcc1), Angelina Sampson
Electronic Theses and Dissertations
Multidrug resistance protein 1 (MRP1/ABCC1) actively transports a variety of drugs, toxic molecules and important physiological substrates across the plasma membrane. It can confer broad-spectrum drug resistance and can decrease the bioavailability of many important drugs such as anti-cancer agents, antibiotics, antivirals, antidepressants and antiinflammatory drugs. Calcein-AM, a fluorescent reporter commonly used for studying compound interactions with MRP1 was recently used in the development of a high content imaging-based assay by our group. This assay was robust and had better sensitivity than fluorescent plate readouts. The assay identified 12 MRP1 inhibitors after screening an anticancer library of 386 compounds. Due …
Engineering Of Two-Color Atp-Binding Cassette Biosensor Proteins For Discovery Of Novel Substrates And Modulators, Bremansu Osa-Andrews
Engineering Of Two-Color Atp-Binding Cassette Biosensor Proteins For Discovery Of Novel Substrates And Modulators, Bremansu Osa-Andrews
Electronic Theses and Dissertations
ATP-binding cassette (ABC) transporter proteins are a vast, ubiquitous superfamily of proteins most of which unlock the energy from ATP-binding and hydrolysis to influx or efflux a wide spectrum of structurally dissimilar substrates across cell membranes. All eukaryotic ABC transporters including P-gp and MRP1 only exist as efflux pumps whose prominent expression in cells is associated with multidrug resistance of antiretrovirals, antiepileptics, antimalarials and anticancer agents. P-gp and MRP1 reduce the bioavailability and efficacy of chemotherapeutic drugs by actively pumping out these drugs, thereby, leading to poor clinical outcomes during chemotherapy. Due to their clinical importance, profiling of the interaction …