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

B H Norman; 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

doi:10.1016/s0960-894x(99)00610-1

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.

Authors

B H Norman¹, 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

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.

MeSH terms

ATP-Binding Cassette Transporters / antagonists & inhibitors*
Antineoplastic Agents / pharmacology
Biological Transport
Cell Membrane / metabolism
Drug Resistance, Multiple / genetics*
HL-60 Cells
HeLa Cells
Humans
Leukotriene C4 / antagonists & inhibitors
Leukotriene C4 / metabolism
Multidrug Resistance-Associated Proteins
Sulfonamides / pharmacology*
Thiophenes / pharmacology*

Substances

ATP-Binding Cassette Transporters
Antineoplastic Agents
Multidrug Resistance-Associated Proteins
Sulfonamides
Thiophenes
Leukotriene C4
LY 329146