ABCG2 p.Ser552Met
| Predicted by SNAP2: | A: N (82%), C: N (61%), D: D (59%), E: D (63%), F: D (71%), G: N (82%), H: D (75%), I: D (75%), K: D (63%), L: D (53%), M: D (71%), N: N (66%), P: D (63%), Q: D (53%), R: D (59%), T: N (72%), V: N (53%), W: D (85%), Y: D (75%), |
| Predicted by PROVEAN: | A: N, C: D, D: D, E: D, F: D, G: N, H: D, I: D, K: D, L: D, M: D, N: N, P: D, Q: D, R: D, T: N, V: D, W: D, Y: D, |
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[hide] A functional steroid-binding element in an ATP-bin... Mol Pharmacol. 2008 Jan;73(1):12-7. 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., [PMID:18094074]
Abstract [show]
The human breast cancer resistance protein is an ATP-binding cassette (ABC) multidrug transporter that affects the bioavailability of chemotherapeutic drugs and can confer drug resistance on cancer cells. It is the second member of the ABCG subfamily, other members of which are associated with human steroid disorders such as hypercholesterolemia, sitosterolemia, and atherosclerosis. The molecular bases of protein-steroid interactions in ABC transporters are unknown. Here, we identify a steroid-binding element in the membrane domain of ABCG2 with a similarity to steroid hormone/nuclear receptors. The element facilitates steroid hormone binding and mediates modulation of ABCG2 activity. The identification of this element might provide an opportunity for the development of new therapeutic ligands for ABCG2.
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No. Sentence Comment
28 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.
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ABCG2 p.Ser552Met 18094074:28:384
status: NEW83 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.
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ABCG2 p.Ser552Met 18094074:83:4
status: NEW