Open Access. Powered by Scholars. Published by Universities.®
Articles 1 - 2 of 2
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 …
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 …