ABCMdb

PMID: 18094074

Velamakanni S, Janvilisri T, Shahi S, van Veen HW
A functional steroid-binding element in an ATP-binding cassette multidrug transporter.
Mol Pharmacol. 2008 Jan;73(1):12-7., [PubMed]

Sentences

No. Mutations Sentence Comment

18 ABCG2 p.Arg482Gly The R482G replacement does not significantly affect the interactions of ABCG2 with Hoechst 33342 and steroid hormones (Robey et al., 2003; Janvilisri et al., 2005; Ozvegy-Laczka et al., 2005). Login to comment 22 ABCG2 p.Arg482Gly ABCG2 mutants were generated with the QuikChange method (Stratagene, La Jolla, CA) using pGEM-BCRP R482G This study was supported by the Medical Research Council and Association for International Cancer Research. Login to comment 28 ABCG2 p.Leu558Ala ABCG2 p.Ser552Met ABCG2 p.Gly553Arg Mutations in the ABCG2R482G gene were introduced using the forward primer 5b18;-TTT TTT CAC GTC TGT TGG TCA ATC TCA C-3b18; and the reverse primer 5b18;-ATT GAC CAA CAG ACG TGA AAA AAT CAT C-3b18; for G553R, the forward primer 5b18;-GAT GAT TTT TAT GGG TCT GTT GGT CAA TCT CAC-3b18; and reverse primer 5b18;-CCA ACA GAC CCA TAA AAA TCA TCA TAA ACA C-3b18; for S552M, and the forward primer 5b18;-GGT CTG GGG GTC AAT GGC ACA ACC ATT GCA TCT TGG-3b18; and reverse primer 5b18;- ATG GTT GTG CCA TTG ACC CCC AGA CCT GAA AAA ATC-3b18; for L555A L558A. Login to comment 64 ABCG8 p.Gly575Arg A G575R substitution at the start of this element in ABCG8 is associated with a dysfunction of ABCG5/8, causing sitosterolemia (Berge et al., 2000). Login to comment 69 ABCG8 p.Gly574Arg By analogy to the sitosterolemia-associated G574R substitution in ABCG8, Gly553 in the SxxLxxL motif was replaced by arginine (GR mutant). Login to comment 83 ABCG2 p.Ser552Met The Ser552 to methionine substitution (as observed in hERॷ) did not alter protein expression (Fig. 2A and SM mutant) or the interaction of ABCG2R482G with PG (Fig. 2D) but decreased the apparent Kd value for ED 6-fold (from 4.7 afe; 0.3 òe;M for ABCG2R482G to 0.8 afe; 0.2 òe;M for SM mutant), whereas the Bmax was unaffected (106.6 afe; 7.4 nmol/mg of protein for ABCG2R482G versus 104.2 afe; 5.5 Fig. 2. Login to comment 86 ABCG2 p.Arg482Gly B, ABCG2 R482G -ATPase activity in inside-out membrane vesicles without substrate (basal) or with 25 òe;M ED, 10 òe;M PG, 10 òe;M daunomycin, or 10 òe;M cholesterol. Login to comment