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TitleCryo-EM structure of P-glycoprotein bound to triple elacridar inhibitor molecules.
Journal, issue, pagesBiochem Biophys Res Commun, Vol. 709, Page 149855, Year 2024
Publish dateMay 21, 2024
AuthorsNorie Hamaguchi-Suzuki / Naruhiko Adachi / Toshio Moriya / Satoshi Yasuda / Masato Kawasaki / Kano Suzuki / Satoshi Ogasawara / Naohiko Anzai / Toshiya Senda / Takeshi Murata /
PubMed AbstractP-glycoprotein (P-gp) is an ATP-binding cassette transporter known for its roles in expelling xenobiotic compounds from cells and contributing to cellular drug resistance through multidrug efflux. ...P-glycoprotein (P-gp) is an ATP-binding cassette transporter known for its roles in expelling xenobiotic compounds from cells and contributing to cellular drug resistance through multidrug efflux. This mechanism is particularly problematic in cancer cells, where it diminishes the therapeutic efficacy of anticancer drugs. P-gp inhibitors, such as elacridar, have been developed to circumvent the decrease in drug efficacy due to P-gp efflux. An earlier study reported the cryo-EM structure of human P-gp-Fab (MRK-16) complex bound by two elacridar molecules, at a resolution of 3.6 Å. In this study, we have obtained a higher resolution (2.5 Å) structure of the P-gp- Fab (UIC2) complex bound by three elacridar molecules. This finding, which exposes a larger space for compound-binding sites than previously acknowledged, has significant implications for the development of more selective inhibitors and enhances our understanding of the compound recognition mechanism of P-gp.
External linksBiochem Biophys Res Commun / PubMed:38579618
MethodsEM (single particle)
Resolution2.49 - 2.54 Å
Structure data

38986

8y6h

EMDB-38986, PDB-8y6h:
P-glycoprotein in complex with UIC2 Fab and triple elacridar molecules in LMNG detergent
Method: EM (single particle) / Resolution: 2.49 Å

38987

8y6i

EMDB-38987, PDB-8y6i:
P-glycoprotein in complex with UIC2 Fab and triple elacridar molecules in nanodisc
Method: EM (single particle) / Resolution: 2.54 Å

Chemicals

ChemComp-R0Z:
elacridar

ChemComp-CLR:
CHOLESTEROL / Cholesterol

ChemComp-3PE:
1,2-Distearoyl-sn-glycerophosphoethanolamine / phospholipid*YM / Phosphatidylethanolamine

Source
  • homo sapiens (human)
  • mus musculus (house mouse)
KeywordsMEMBRANE PROTEIN / ABC transporter / elacridar / P-glycoprotein

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