MDR Assay Kit (Fluorometric)
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(7 Publications)
MDR Assay Kit ab112142 uses a fluorescent MDR indicator for assaying MDR pump activity. The hydrophobic fluorescent dye molecule rapidly penetrates cell membranes and becomes trapped after action by cellular enzymes. MDR transporters will expel the dye from the cell, decreasing the cellular fluorescence intensity. Readout is by fluorometric plate reader (Ex/Em 490/525 nm).
View Alternative Names
CD243, MDR1, PGY1, ABCB1, ATP-dependent translocase ABCB1, ATP-binding cassette sub-family B member 1, Multidrug resistance protein 1, P-glycoprotein 1, Phospholipid transporter ABCB1
- FuncS
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Functional Studies - MDR Assay Kit (Fluorometric) (AB112142)
Effect of Cyclosporin A on the inhibition of P-gp pump in MCF7/ADR cells. The increased concentration of Cyclosporin A resulted in an increase in fluorescence signal caused by the inhibition of P-gp pump which enhanced the intracellular accumulation of MDR indicator dye. The EC50 = 2.4 µM (measured with the kit) is similar to the value reported in the literature.
Product details
Multi drug resistance (MDR) is a major factor in the failure of many forms of chemotherapy. In the past few years it has become widely accepted that the resistance to chemotherapy correlates with the overexpression of at least two ATP dependent drug efflux pumps. These cell membrane proteins, called P-glycoprotein (Pgp, MDR1), and multidrug resistance associated protein (MRP1) are members of the ABC transporter family. Abcam's Fluorimetric MDR Assay Kits use a fluorescent MDR indicator for assaying these two MDR pump activities. This hydrophobic fluorescent dye molecule rapidly penetrates cell membranes and becomes trapped in cells. Following a short incubation, the intracellular free dye concentration can increase significantly. In the MDR1 and/or MRP1-expressing cells this dye is extruded by the MDR transporters, thus decreasing the cellular fluorescence intensity. However, when its extrusion is blocked by an agent that interferes with the MDR1 and/or MRP1 pump-activity, its cellular fluorescence intensity increases significantly. Abcam's Fluorimetric MDR Assay Kits are ideal for high throughput screening of MDR pump inhibitors or identifying the cells that have high level of MDR pump activities.
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Biological function summary
MDR1 plays a major role in protecting tissues by limiting drug penetration and facilitating the excretion of xenobiotics. It is part of the ATP-binding cassette (ABC) transporter family which forms a complex infrastructure of proteins responsible for the transport of molecules across cellular membranes. Its ability to pump out chemotherapy drugs significantly impacts treatment efficacy especially in certain cancer types where overexpression can lead to multidrug resistance.
Pathways
MDR1 interacts closely within the drug metabolism and transport pathways. It plays a vital role in the pharmacokinetic properties of drugs affecting both their distribution and elimination processes. MDR1 works in concert with other proteins in the ABC transporter family like MRP1 and BCRP which also contribute to drug resistance and excretion. The balance and activity of these transporters directly influence therapeutic outcomes and toxicity of cancer chemotherapeutic agents.
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Publications (7)
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Molecular oncology 18:386-414 PubMed37842807
2023
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Pharmaceutics 12: PubMed32545588
2020
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ACS nano 14:6947-6955 PubMed32383849
2020
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RSC advances 9:5362-5376 PubMed35515894
2019
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Oncotarget 8:87860-87877 PubMed29152126
2017
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Scientific reports 7:8419 PubMed28827665
2017
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PloS one 9:e97512 PubMed24830744
2014
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