Sandbox Reserved 1606

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===Cavities and Leucine Plug===
===Cavities and Leucine Plug===
[[Image:Map_leucine_plug.png|200 px|right|thumb|Figure 2. Locations of Cavities 1 and 2 and the Leucine Plug in ABCG2. The above protein is in the open, unbound ATP conformation.]]
[[Image:Map_leucine_plug.png|200 px|right|thumb|Figure 2. Locations of Cavities 1 and 2 and the Leucine Plug in ABCG2. The above protein is in the open, unbound ATP conformation.]]
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Substrates are transported through ABCG2 via two cavities separated by a leucine plug. <scene name='83/832932/Cavity_1_zoom_out/1'>Cavity 1</scene> acts as the multidrug binding pocket and is formed by the interface of the TMDs from each dimer.
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Substrates are transported through ABCG2 via two cavities separated by a leucine plug. <scene name='83/832932/Cavity_1_zoom_out/1'>Cavity 1</scene> acts as the multidrug binding pocket and is formed by the interface of the TMDs from each dimer. Substrates, such as estrone 3-sulfate (E_1S),
<scene name='83/832932/Cavity_1_-_use2/1'>Cavity 1</scene>
<scene name='83/832932/Cavity_1_-_use2/1'>Cavity 1</scene>
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<scene name='83/832932/Cavity_1_zoom_out/1'>Cavity 1 (zoom out)</scene>
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<scene name='83/832932/Lysine_plug_use/1'>Leucine Plug</scene>
<scene name='83/832932/Lysine_plug_use/1'>Leucine Plug</scene>

Revision as of 01:31, 5 April 2020

This Sandbox is Reserved from Jan 13 through September 1, 2020 for use in the course CH462 Biochemistry II taught by R. Jeremy Johnson at the Butler University, Indianapolis, USA. This reservation includes Sandbox Reserved 1598 through Sandbox Reserved 1627.
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ABCG2 Multidrug Transporter

ABCG2 Multidrug Transporter

Drag the structure with the mouse to rotate

References

[1] [2] [3] [4]

  1. ↑ 1.0 1.1 1.2 1.3 Taylor NMI, Manolaridis I, Jackson SM, Kowal J, Stahlberg H, Locher KP. Structure of the human multidrug transporter ABCG2. Nature. 2017 Jun 22;546(7659):504-509. doi: 10.1038/nature22345. Epub 2017 May, 29. PMID:28554189 doi:http://dx.doi.org/10.1038/nature22345
  2. ↑ 2.0 2.1 2.2 Manolaridis I, Jackson SM, Taylor NMI, Kowal J, Stahlberg H, Locher KP. Cryo-EM structures of a human ABCG2 mutant trapped in ATP-bound and substrate-bound states. Nature. 2018 Nov;563(7731):426-430. doi: 10.1038/s41586-018-0680-3. Epub 2018 Nov, 7. PMID:30405239 doi:http://dx.doi.org/10.1038/s41586-018-0680-3
  3. ↑ 3.0 3.1 Robey RW, Pluchino KM, Hall MD, Fojo AT, Bates SE, Gottesman MM. Revisiting the role of ABC transporters in multidrug-resistant cancer. Nat Rev Cancer. 2018 Jul;18(7):452-464. doi: 10.1038/s41568-018-0005-8. PMID:29643473 doi:http://dx.doi.org/10.1038/s41568-018-0005-8
  4. ↑ Jackson SM, Manolaridis I, Kowal J, Zechner M, Taylor NMI, Bause M, Bauer S, Bartholomaeus R, Bernhardt G, Koenig B, Buschauer A, Stahlberg H, Altmann KH, Locher KP. Structural basis of small-molecule inhibition of human multidrug transporter ABCG2. Nat Struct Mol Biol. 2018 Apr;25(4):333-340. doi: 10.1038/s41594-018-0049-1. Epub, 2018 Apr 2. PMID:29610494 doi:http://dx.doi.org/10.1038/s41594-018-0049-1

Student Contributors

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