重組細胞
expressed in baculovirus infected Sf9 cells
形狀
liquid
濃度
5 mg/mL
顏色
off-white
UniProt登錄號
運輸包裝
dry ice
儲存溫度
−70°C
基因資訊
human ... ABCC1(4363)
一般說明
Membrane Preparations for ATPase Assays are suitable for drug-efflux transporter interaction studies based on ATPase activity determination, and could be used for differentiation between transporter substrates and inhibitors.
應用
The ATPase assay is an in vitro membrane assay designed to indicate the nature of the interaction between the compound and the transporter. By measuring ATPase activity, both activation and inhibition of transporters can be investigated using membranes from baculovirus-infected insect cells or mammalian cell membranes containing high levels of human or rodent wild-type transporters. ABC transporters mediate the transport of substrates against a concentration gradient using energy derived from ATP hydrolysis, which is proportional to the transporter activity and could easily be detected with a colorimetric method.
To assess activation, ABC transporter-rich membranes are incubated with various (typically in 8) concentrations of the test article and the effect on basal ATPase activity is measured. Compounds that stimulate ATPase are generally considered substrates for the transporter. To assess inhibition, a test article′ ability to modify the activity of a given ABC transporter stimulated with its prototypical substrates is examined. The activation and inhibition tests are complementary assays.
Stimulation detected in the activation assay indicate that the compound is a transported substrate of the transporter, while interactions detected in the inhibition test indicate interaction of the test compounds with the transporter, but do not give information on the nature (substrate or inhibitor) of the interaction. In some cases inhibitors or slowly transported compounds may inhibit the baseline transporter ATPase activity as well.
Slowly transported substrates often do not stimulate the ATPase activity in a detectable extent; however the existing interaction can be identified in the inhibition assay.
To assess activation, ABC transporter-rich membranes are incubated with various (typically in 8) concentrations of the test article and the effect on basal ATPase activity is measured. Compounds that stimulate ATPase are generally considered substrates for the transporter. To assess inhibition, a test article′ ability to modify the activity of a given ABC transporter stimulated with its prototypical substrates is examined. The activation and inhibition tests are complementary assays.
Stimulation detected in the activation assay indicate that the compound is a transported substrate of the transporter, while interactions detected in the inhibition test indicate interaction of the test compounds with the transporter, but do not give information on the nature (substrate or inhibitor) of the interaction. In some cases inhibitors or slowly transported compounds may inhibit the baseline transporter ATPase activity as well.
Slowly transported substrates often do not stimulate the ATPase activity in a detectable extent; however the existing interaction can be identified in the inhibition assay.
外觀
Supplied as frozen membrane vesicles, containing 5 mg/ml membrane protein, labeled with volume, catalog number (transporter) and date of production.
法律資訊
Distributed for SOLVO Biotechnology, Inc.
儲存類別代碼
12 - Non Combustible Liquids
水污染物質分類（WGK）
WGK 1
閃點（°F）
Not applicable
閃點（°C）
Not applicable
S-M He et al.
Current medicinal chemistry, 18(3), 439-481 (2010-12-15)
Multidrug ABC transporters such as P-glycoprotein (P-gp/MDR1/ABCB1) and multidrug resistance protein 1 (MRP1/ABCC1) play an important role in the extrusion of drugs from the cell and their overexpression can be a cause of failure of anticancer and antimicrobial chemotherapy. Recently
Eva Bakos et al.
Pflugers Archiv : European journal of physiology, 453(5), 621-641 (2006-12-26)
MRP1 (ABCC1) is a peculiar member of the ABC transporter superfamily for several aspects. This protein has an unusually broad substrate specificity and is capable of transporting not only a wide variety of neutral hydrophobic compounds, like the MDR1/P-glycoprotein, but
J H Hooijberg et al.
FEBS letters, 469(1), 47-51 (2000-03-10)
The transport mechanism by which the multidrug resistance protein 1 (MRP1) effluxes cytotoxic agents out of cells is still not completely understood. However, the cellular antioxidant glutathione (GSH) has been shown to have an important role in MRP1-mediated drug transport.
Roger G Deeley et al.
Physiological reviews, 86(3), 849-899 (2006-07-04)
Multidrug Resistance Proteins (MRPs), together with the cystic fibrosis conductance regulator (CFTR/ABCC7) and the sulfonylurea receptors (SUR1/ABCC8 and SUR2/ABCC9) comprise the 13 members of the human "C" branch of the ATP binding cassette (ABC) superfamily. All C branch proteins share
Cornelius F H Mueller et al.
Circulation research, 97(7), 637-644 (2005-08-27)
Glutathione (GSH) is the major source of intracellular sulfhydryl groups. Oxidized GSH (GSSG) can be recycled to GSH by the GSH reductase or exported from the cell. The mechanism by which GSSG is exported and the consequence of its export
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