ABCMdb

PMID: 17318783

Fong WF, Wan CK, Zhu GY, Chattopadhyay A, Dey S, Zhao Z, Shen XL
Schisandrol A from Schisandra chinensis reverses P-glycoprotein-mediated multidrug resistance by affecting Pgp-substrate complexes.
Planta Med. 2007 Mar;73(3):212-20. Epub 2007 Feb 22., [PubMed]

Sentences

No. Mutations Sentence Comment

67 ABCB1 p.Phe983Ala ABCB1 p.Phe983Ala Baculovirus-mediated expression of human Pgp and photoaffinity labeling of Pgp with [125 I]IAAP High Five insect cells were transfected with a recombinant baculovirus harboring either the wild type {BV-MDR1-(H6)} [14] or the F983A mutant {BV-MDR1-F983A-(H6)} [15] human MDR1 cDNA [16]. Login to comment 123 ABCB1 p.Phe983Ala To investigate the effect of SCH on Pgp substrate recognition, we performed photoaffinity labeling studies with [125 I]IAAP in insect cells transfected with either wild type or the F983A mutated Pgp. Login to comment 127 ABCB1 p.Phe983Ala The inhibitory effect of SCH on [125 I]IAAP binding was unaltered in the F983A mutatant Pgp, indicating that this specific allosteric regulatory site was not involved in the inhibitory action of SCH. Login to comment 157 ABCB1 p.Phe983Ala Lastly, SCH showed some inhibitory effects on [125 I]IAAP photo-labelling of Fig. 9 Effect of SCH on [125 I]IAAP binding to wild-type and to the F983A mutant of Pgp. Login to comment 158 ABCB1 p.Phe983Ala Membrane preparations (15 mg of protein) containing wild-type Pgp (A) or the F983A mutant (B) were photoaffinity labeled with 5nM [125 I]IAAP in the presence of varying concentrations (0±100 mM) of SCH. Login to comment