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Reversal of breast cancer resistance protein–mediated drug resistance by tryprostatin A

✍ Scribed by Holger Woehlecke; Hiroyuki Osada; Andreas Herrmann; Hermann Lage

Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
391 KB
Volume
107
Category
Article
ISSN
0020-7136

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✦ Synopsis

Abstract

MDR in human cancers is one of the major causes of failure of chemotherapy. A member of the superfamily of ABC transporters, BCRP, was demonstrated to confer an atypical MDR phenotype to tumor cells. To overcome the BCRP‐mediated drug resistance, the fungal secondary metabolite TPS‐A, a diketopiperazine, was analyzed with regard to its potency to reverse the BCRP‐mediated drug‐resistant phenotype. At concentrations of 10–50 μM, TPS‐A reversed a mitoxantrone‐resistant phenotype and inhibited the cellular BCRP‐dependent mitoxantrone accumulation in the human gastric carcinoma cell line EPG85‐257RNOV, the human breast cancer cell line MCF7/AdrVp (both exhibiting acquired BCRP‐mediated MDR) and the BCRP cDNA‐transfected breast cancer cell line MCF‐7/BCRP clone 8. No cytotoxicity was seen at effective concentrations. These data indicate that TPS‐A is a novel BCRP inhibitor. © 2003 Wiley‐Liss, Inc.

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