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Medicinal and Pharmaceutical Chemistry Commons™
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Full-Text Articles in Medicinal and Pharmaceutical Chemistry
Calcitriol And Calcipotriol Modulate Transport Activity Of Abc Transporters And Exhibit Selective Cytotoxicity In Mrp1-Overexpressing Cells, Kee W. Tan, Angelina Sampson, Bremansu Osa-Andrews, Surtaj H. Iram
Calcitriol And Calcipotriol Modulate Transport Activity Of Abc Transporters And Exhibit Selective Cytotoxicity In Mrp1-Overexpressing Cells, Kee W. Tan, Angelina Sampson, Bremansu Osa-Andrews, Surtaj H. Iram
Chemistry and Biochemistry Faculty Publications
Efflux transporters P-glycoprotein (P-gp/ABCB1), multidrug resistance protein 1 (MRP1/ABCC1), and breast cancer resistance protein (BCRP/ABCG2) can affect the efficacy and toxicity of a wide variety of drugs and are implicated in multidrug resistance (MDR). Eight test compounds, recently identified from an intramolecular FRET-based high throughput screening, were characterized for their interaction with MRP1. We report that the active metabolite of vitamin D3, calcitriol, and its analog calcipotriol are selectively cytotoxic to MRP1-overexpressing cells, besides inhibiting transport function of P-gp, MRP1, and BCRP. Calcitriol and calcipotriol consistently displayed a potent inhibitory activity on MRP1-mediated doxorubicin and calcein efflux in MRP1-overexpressing H69AR …
Development Of Novel Intramolecular Fret-Based Abc Transporter Biosensors To Identify New Substrates And Modulators, Bremansu Osa-Andrews, Kee W. Tan, Angelina Sampson, Surtaj H. Iram
Development Of Novel Intramolecular Fret-Based Abc Transporter Biosensors To Identify New Substrates And Modulators, Bremansu Osa-Andrews, Kee W. Tan, Angelina Sampson, Surtaj H. Iram
Chemistry and Biochemistry Faculty Publications
Multidrug resistance protein 1 (MRP1) can efflux a wide variety of molecules including toxic chemicals, drugs, and their derivatives out of cells. Substrates of MRP1 include anti-cancer agents, antibiotics, anti-virals, anti-human immunodeficiency virus (HIV), and many other drugs. To identify novel substrates and modulators of MRP1 by exploiting intramolecular fluorescence resonance energy transfer (FRET), we genetically engineered six different two-color MRP1 proteins by changing green fluorescent protein (GFP) insertion sites, while keeping the red fluorescent protein (RFP) at the C-terminal of MRP1. Four of six recombinant proteins showed normal expression, localization, and transport activity. We quantified intramolecular FRET using ensemble …