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• W3176642017 abstract "Multidrug resistance (MDR) has been linked to the failure of chemotherapy, and poor prognoses and reduced survival rates in patients in several cancer types. MDR cancers often become resistant to pharmacologically and structurally diverse drugs by overexpressing members of the family of ATP Binding Cassette (ABC) transporters. The breast cancer resistance protein (BCRP) is expressed in many tissues, including those with barrier or detoxifying functions such as blood-brain barrier, placenta, and is responsible for the active export of a wide variety of toxins across the plasma membrane. Given its role in MDR, inhibitors of BCRP have been studied for years. To search for BCRP inhibitors as potential leads for the development of co-therapeutics to combat MDR, we used high-throughput in silico ligand docking similar to studies performed previously in the search for inhibitors of the P-glycoprotein (Brewer et al., Mol. Pharmacol. 86, 716–726, 2014). A number of drug like molecules were identified that reversed multidrug resistance of a BCRP-overexpressing breast cancer cell line generated in our lab (Nanayakkara, unpublished). To understand the mechanism of inhibition of BCRP by these compounds, biochemical assays assessing ATP hydrolysis activity as well as other biochemical properties of BCRP are required. To obtain protein amounts that are large enough for biochemical and biophysical evaluation of inhibitor action, a gene for human BCRP was designed with optimized codon usage for translation and expression in P. pastoris. Maximum expression of BCRP in the PichiaPink™ system was observed after 9 hours of growth on a methanol based medium. Protein expression was confirmed by Western blot analysis using both BCRP and anti-His antibodies. ATP hydrolysis assays indicated that the protein expressed was catalytically active and that the ATP hydrolysis activity could be stimulated by the BCRP transport substrate, Hoechst 33342. Here we also report our attempts to purify BCRP from PichiaPink™ membranes and characterize the protein both as solubilized in mixed micelles as well as upon reconstitution into membrane nanodiscs Support or Funding Information This work is supported by NIH NIGMS [R15GM094771-02] to John G. Wise, SMU University Research Council, the SMU Center for Drug Discovery, Design and Delivery, Ms. Lynn McBee and New England Biolabs, the Communities Foundation of Texas, a private gift from Ms. Suzy Ruff of Dallas, Texas, as well as the Hamilton Undergraduate Research Scholarship the SMU Undergraduate Research Assistantship Programs. This abstract is from the Experimental Biology 2018 Meeting. There is no full text article associated with this abstract published in The FASEB Journal." @default.
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• W3176642017 date "2018-04-01" @default.
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• W3176642017 title "Optimization of Breast Cancer Resistance Protein (BCRP) Expression in the Yeast Pichia pastoris" @default.
• W3176642017 doi "https://doi.org/10.1096/fasebj.2018.32.1_supplement.531.15" @default.
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