PMID: 16456713

Loo TW, Clarke DM
Recent progress in understanding the mechanism of P-glycoprotein-mediated drug efflux.
J Membr Biol. 2005 Aug;206(3):173-85., [PubMed]
Sentences
No. Mutations Sentence Comment
96 ABCB1 p.Pro223Ala
X
ABCB1 p.Pro223Ala 16456713:96:25
status: NEW
view ABCB1 p.Pro223Ala details
ABCB1 p.Phe335Ala
X
ABCB1 p.Phe335Ala 16456713:96:157
status: NEW
view ABCB1 p.Phe335Ala details
For example, mutation of Pro223 to alanine in TM 4 decreased the affinity of P-gp for colchicine but not vinblastine (Loo & Clarke, 1993b) while mutation of Phe335 to alanine decreased the affinity of P-gp for vinblastine but not for colchicine (Loo & Clarke, 1993a, 1994b). Login to comment
200 ABCB4 p.Leu975Cys
X
ABCB4 p.Leu975Cys 16456713:200:202
status: NEW
view ABCB4 p.Leu975Cys details
During ATP hydrolysis, conformational changes between TM6 and TM12 were detected by disulfide cross-linking between cysteines introduced at the extracellular ends of these TMs (residue L332C in TM6 and L975C in TM12) (Loo & Clarke, 1996a, 1997b). Login to comment
201 ABCB4 p.Leu975Cys
X
ABCB4 p.Leu975Cys 16456713:201:28
status: NEW
view ABCB4 p.Leu975Cys details
Cross-linking between L332C/L975C prevented conformational changes during ATP hydrolysis, resulting in inhibition of ATPase activity. Login to comment