Reversal of resistance in multidrug resistance protein (MRP1)-overexpressing cells by LY329146

  • Bioorg Med Chem Lett. 1999 Dec 6;9(23):3381-6. doi: 10.1016/s0960-894x(99)00610-1.
B H Norman  1 ,  A H Dantzig ,  J S Kroin ,  K L Law ,  L B Tabas ,  R L Shepard ,  A D Palkowitz ,  K L Hauser ,  M A Winter ,  J P Sluka ,  J J Starling
Affiliations
  • 1. Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.
PMID: 10612603 DOI: 10.1016/s0960-894x(99)00610-1
Abstract

The benzothiophene LY329146 reverses the drug resistance phenotype in multidrug resistance protein (MRP1)-overexpressing cells when dosed in combination with MRP1-associated oncolytics doxorubicin and vincristine. Additionally, LY329146 inhibited MRP1-mediated uptake of the MRP1 substrate LTC4 into membrane vesicles prepared from MRP1-overexpressing cells.