Article
ABCG2 harboring the Gly482 mutation confers high-level resistance to various hydrophilic antifolates.
Cancer research - 15 Sept 2005
Shafran Assaf, Ifergan Ilan, Bram Eran, Jansen Gerrit, Kathmann Ietje, Peters Godefridus J, Robey Robert W, Bates Susan E, Assaraf Yehuda G
Abstract excerpt
ABCG2 is an ATP-binding cassette transporter that confers resistance to various chemotherapeutic agents. Recent studies have established that an Arg (wild-type) to Gly mutation at amino acid 482 in ABCG2 alters substrate specificity. Here, we explored the role of this G482 mutation in antifolate resistance using a clinically relevant 4-hour drug exposure. Stable transfectants overexpressing the mutant G482...
Topics
- ATP Binding Cassette Transporter, Subfamily G, Member 2
- ATP-Binding Cassette Transporters
- Cell Line
- Cell Membrane
- Doxorubicin
- Drug Resistance, Neoplasm
- Folic Acid Antagonists
- Humans
- Methotrexate
- Mutation
- Neoplasm Proteins
- Polyglutamic Acid