ABCMdb

PMID: 22497316

Mo W, Qi J, Zhang JT
Different roles of TM5, TM6, and ECL3 in the oligomerization and function of human ABCG2.
Biochemistry. 2012 May 1;51(17):3634-41. Epub 2012 Apr 19., [PubMed]

Sentences

No. Mutations Sentence Comment

175 ABCG2 p.Arg482Gly However, their oligomerization activities do not appear to depend on the hydrophobicity of these TM segments, which is different from the TM segments involved in ABCC1 dimerization.15 While the exact drug-binding sites in ABCG2 are unknown, early studies have suggested that the interactions of the substrate with ABCG2 involve multiple binding sites in the protein.25 For example, Arg482 has been shown to affect substrate specificity.26 All our constructs have the same R482G mutation that provides a gain of function in recognition of more substrates. Login to comment 178 ABCG2 p.Leu554Pro For example, it has been shown that the L554P mutation in TM5 reduces the drug resistance function of ABCG2.27 TM5 has also been found to contain a steroid binding element,28 further suggesting that TM5 may be important in substrate recognition and binding. Login to comment