2. Academic Validation
  3. Reversal of resistance in multidrug resistance protein (MRP1)-overexpressing cells by LY329146

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

Affiliation

  • 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.

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