TITLE

Flavonoid binding to a multi-drug-resistance transporter protein: an STD-NMR study

AUTHOR(S)
Nissler, Ludwig; Gebhardt, Rolf; Berger, Stefan
PUB. DATE
August 2004
SOURCE
Analytical & Bioanalytical Chemistry;Aug2004, Vol. 379 Issue 7/8, p1045
SOURCE TYPE
Academic Journal
DOC. TYPE
Article
ABSTRACT
Flavonoids are well known to inhibit the function of the multi-drug-resistance (mdr) transporter by interacting with their ATP binding domains. The precise orientation of these molecules inside the ATP binding pocket is still unclear. We applied the saturation transfer difference (STD) NMR technique to investigate the binding of the flavonoid luteolin and its 7-O-β-D- glycopyranoside to the recombinant nucleotide binding domain (NBD2) of mouse-mdr. First, this NMR technique confirmed binding of both ligands to NBD2, as was determined from tryptophan fluorescence-quenching experiments. Further, the results suggest binding of both luteolin and its 7-O-β-D-glycopyranoside by their polar groups at positions 4, 5, and 3' to the protein.
ACCESSION #
14281855

 

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