Sandbox Reserved 1613
From Proteopedia
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== Relevance == | == Relevance == | ||
- | Due to ABCG2 excreting xenobiotics from the cell, they also transport essential cancer drugs out of the cell. By utilizing certain inhibitors (5D3 and MZ29), it is possible to shut down these transporters in order to get cancer drugs to remain in and apoptosis the cell. However, this could have residual effects on the excretory system as ABCG2 would no longer be able to excrete anything from the cell, including those detrimental to the body. | + | Due to ABCG2 excreting xenobiotics from the cell, they also transport essential cancer drugs out of the cell. By utilizing certain inhibitors (5D3 and <scene name='83/832939/Abcg2_bound_to_mz29/2'>MZ29</scene>), it is possible to shut down these transporters in order to get cancer drugs to remain in and apoptosis the cell. However, this could have residual effects on the excretory system as ABCG2 would no longer be able to excrete anything from the cell, including those detrimental to the body. |
== Structural highlights == | == Structural highlights == | ||
[[Image:Ligand_Interactions_6ffc.png|400 px|right|thumb|Figure 2]] | [[Image:Ligand_Interactions_6ffc.png|400 px|right|thumb|Figure 2]] |
Revision as of 21:12, 6 April 2020
ABCG2 Transporter Protein
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References
- ↑ 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
- ↑ 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
- ↑ 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
- ↑ Fetsch PA, Abati A, Litman T, Morisaki K, Honjo Y, Mittal K, Bates SE. Localization of the ABCG2 mitoxantrone resistance-associated protein in normal tissues. Cancer Lett. 2006 Apr 8;235(1):84-92. doi: 10.1016/j.canlet.2005.04.024. Epub, 2005 Jun 28. PMID:15990223 doi:http://dx.doi.org/10.1016/j.canlet.2005.04.024
Student Contributors
Samuel Sullivan, Jaelyn Voyles, Shelby Skaggs