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A Salt Bridge in Intracellular Loop 2 is Essential for Folding of Human P-glycoprotein"


Biochemistry. 2013 May 1;


Authors: Loo TW, Clarke DM


Abstract

There is no high-resolution structure of the human P-glycoprotein (P-gp; ABCB1) drug pump. Homology models based on the crystal structures of mouse and C. elegans P-gps show extensive contacts between ICL2 (in the first transmembrane domain) and the second nucleotide-binding domain. Human P-gp modeled on these P-gp structures yield different ICL2 structures. Only the model based on the C. elegans P-gp structure predicts the presence of a salt bridge. We show that the Glu256-Arg276 salt bridge was critical for P-gp folding.

PMID: 23634976 [PubMed - as supplied by publisher]