ABCG2 requires a single aromatic amino acid to "clamp" substrates and inhibitors into the binding pocket.
Gose T, Shafi T, Fukuda Y, Das S, Wang Y, Allcock A, Gavan McHarg A, Lynch J, Chen T, Tamai I, Shelat A, Ford RC, Schuetz JD.
Gose T, et al.
FASEB J. 2020 Apr;34(4):4890-4903. doi: 10.1096/fj.201902338RR. Epub 2020 Feb 17.
FASEB J. 2020.
PMID: 32067270
Free PMC article.
Structural studies indicate that substrate and inhibitor (ligands) binding to ABCG2 can be differentiated quantitatively by the number of amino acid contacts, with inhibitors displaying more contacts. Although binding is the obligate initial step in the transport cycle, th …
Structural studies indicate that substrate and inhibitor (ligands) binding to ABCG2 can be differentiated quantitatively by the number of …