Please use this identifier to cite or link to this item: http://scholarbank.nus.edu.sg/handle/10635/15016
Title: Effects of novel purine analogs and the role of aromatic amino acids on MRP4 functions
Authors: YANG FEI
Keywords: MRP, MRP4, bimane-GS efflux, resistance to 6-TG, aromatic amino acid
Issue Date: 11-Nov-2005
Source: YANG FEI (2005-11-11). Effects of novel purine analogs and the role of aromatic amino acids on MRP4 functions. ScholarBank@NUS Repository.
Abstract: Multidrug resistance proteins (MRPs) are membrane glycoproteins that mediate the ATP-dependent export of organic anions, including cytotoxic and antiviral drugs, from cells. The MRPs that have been functionally characterized so far share the property of ATP-dependent export pumps for conjugates with glutathione, glucuronate or sulfate. Multidrug resistance protein 4 (MRP4) is a member of MRP family. Like other MRPs, MRP4 is organic anion transporter, but it has the unique ability to transport cyclic nucleotides and some nucleoside monophosphate analogs.This study was carried out to screen for inhibitors of MRP4 as well as to determine the contribution of conserved aromatic amino acid residues (Trp216, Trp230 and Phe 324) to the activity of MRP4.Our data showed that purine or azapurine analogs are able to inhibit MRO4 activity. In addition, mutations of the conserved aromatic amino residues led to the loss of transport activity as well as the loss of resistance to nucleoside analog.
URI: http://scholarbank.nus.edu.sg/handle/10635/15016
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