Structure-Activity Relationships for Interaction with Multidrug Resistance Protein 2 (ABCC2/MRP2): The Role of Torsion Angle for a Series of Biphenyl-Substituted Heterocycles

2007 ◽  
Vol 35 (6) ◽  
pp. 937-945 ◽  
Author(s):  
Yurong Lai ◽  
Li Xing ◽  
Gennadiy I. Poda ◽  
Yiding Hu
Keyword(s):  
Multidrug Resistance ◽  
Torsion Angle ◽  
Multidrug Resistance Protein ◽  
Structure Activity Relationships ◽  
Multidrug Resistance Protein 2 ◽  
Structure Activity ◽  
Resistance Protein

scholarly journals Role of Glutathione in the Regulation of Cisplatin Resistance in Cancer Chemotherapy

2010 ◽  
Vol 2010 ◽  
pp. 1-7 ◽  
Author(s):  
Helen H. W. Chen ◽  
Macus Tien Kuo
Keyword(s):  
Multidrug Resistance ◽  
Mammalian Cells ◽  
Cisplatin Resistance ◽  
Multidrug Resistance Protein ◽  
Transfected Cells ◽  
High Affinity ◽  
Multidrug Resistance Protein 2 ◽  
Resistance Protein ◽  
Rate Limiting

Three mechanisms have been proposed for the role of glutathione (GSH) in regulating cisplatin (CDDP) sensitivities that affects its ultimate cell-killing ability: (i) GSH may serve as a cofactor in facilitating multidrug resistance protein 2- (MRP2-) mediated CDDP efflux in mammalian cells, since MRP2-transfected cells were shown to confer CDDP resistance; (ii) GSH may serve as a redox-regulating cytoprotector based on the observations that many CDDP-resistant cells overexpress GSH and γ-glutamylcysteine synthesis (γ-GCS), the rate-limiting enzyme for GSH biosynthesis; (iii) GSH may function as a copper (Cu) chelator. Elevated GSH expression depletes the cellular bioavailable Cu pool, resulting in upregulation of the high-affinity Cu transporter (hCtr1) which is also a CDDP transporter. This has been demonstrated that overexpression of GSH by transfection with γ-GCS conferred sensitization to CDDP toxicity. This review describes how these three models were developed and critically reviews their importance to overall CDDP cytotoxicity in cancer cell treatments.

scholarly journals Multidrug Resistance Protein 2 Implicates Anticancer Drug-Resistance to Sorafenib

2011 ◽  
Vol 34 (3) ◽  
pp. 433-435 ◽  
Author(s):  
Yoshihiko Shibayama ◽  
Kou Nakano ◽  
Hiroshi Maeda ◽  
Miyuki Taguchi ◽  
Ryuji Ikeda ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Multidrug Resistance ◽  
Anticancer Drug ◽  
Multidrug Resistance Protein ◽  
Multidrug Resistance Protein 2 ◽  
Resistance Protein ◽  
Anticancer Drug Resistance
Sign in / Sign up

Export Citation Format

Share Document