Abstract:
:Drug substrates stimulate ATPase activity of the P-glycoprotein (P-gp) ATP-binding cassette drug pump by an unknown mechanism. Cross-linking analysis was performed to test if drug substrates stimulate P-gp ATPase activity by altering cross-talk at the first transmission interface linking the drug-binding [intracellular loop 4 (S909C)] and first nucleotide-binding domains [NBD1 (V472C or L443C)]. In the absence of lipid (inactive P-gp), only V472C/S909C showed cross-linking. Drugs blocked V472C/S909C cross-linking. In the presence of lipids (active P-gp), drug substrates promoted only L443C/S909C cross-linking. This suggests that drug substrates stimulate ATPase activity through a conformational change that shifts Ser909 away from Val472 and toward Leu443.
journal_name
Biochemistryjournal_title
Biochemistryauthors
Loo TW,Clarke DMdoi
10.1021/acs.biochem.6b00233subject
Has Abstractpub_date
2016-05-24 00:00:00pages
2817-20issue
20eissn
0006-2960issn
1520-4995journal_volume
55pub_type
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