Fumitremorgin C reverses multidrug resistance in cells transfected with the breast cancer resistance protein.

Abstract

Fumitremorgin C (FTC) is a potent and specific chemosensitizing agent in cell lines selected for resistance to mitoxantrone that do not overexpress P-glycoprotein or multidrug resistance protein. The gene encoding a novel transporter, the breast cancer resistance protein (BCRP), was recently found to be overexpressed in a mitoxantrone-selected human colon cell line, S1-M1-3.2, which was used to identify FTC. Because the drug-selected cell line may contain multiple alterations contributing to the multidrug resistance phenotype, we examined the effect of FTC on MCF-7 cells transfected with the BCRP gene. We report that FTC almost completely reverses resistance mediated by BCRP in vitro and is a pharmacological probe for the expression and molecular action of this transporter.

• Authors: S K Rabindran, D D Ross, L A Doyle, W Yang, L M Greenberger
• Journal: Cancer research (Cancer Res) Vol. 60 Issue 1 Pg. 47-50 (Jan 01 2000) ISSN: 0008-5472 [Print] United States
• PMID: 10646850 (Publication Type: Journal Article, Research Support, U.S. Gov't, Non-P.H.S.)

Chemical References

• ABCG2 protein, human
• ATP Binding Cassette Transporter, Subfamily G, Member 2
• ATP-Binding Cassette Transporters
• Antineoplastic Agents
• Indoles
• Neoplasm Proteins
• tryptoquivaline

Topics

• ATP Binding Cassette Transporter, Subfamily G, Member 2
• ATP-Binding Cassette Transporters (drug effects, genetics)
• Antineoplastic Agents (pharmacology)
• Breast Neoplasms (metabolism)
• Drug Resistance, Multiple
• Drug Resistance, Neoplasm
• Female
• Humans
• Indoles (pharmacology)
• Neoplasm Proteins (drug effects, genetics)
• Transfection
• Tumor Cells, Cultured (drug effects)