Sandbox Reserved 1613: Difference between revisions
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ABCG2 transports a variety of <scene name='83/832939/Mz29/1'>substrates</scene>, particularly flat, hydrophobic, and/or polycylic molecules. It is found in different biological membranes, such as the blood-brain barrier (BBB), blood-testis barrier, and the blood-placental barrier. It is thought to help protect those tissues and many others from cytotoxins. In addition to cytotoxin protection, ABCG2 secretes endogenous substrates in the adrenal gland, excretes toxins in the liver and kidneys, and regulates absorption of substrates. | ABCG2 transports a variety of <scene name='83/832939/Mz29/1'>substrates</scene>, particularly flat, hydrophobic, and/or polycylic molecules. It is found in different biological membranes, such as the blood-brain barrier (BBB), blood-testis barrier, and the blood-placental barrier. It is thought to help protect those tissues and many others from cytotoxins. In addition to cytotoxin protection, ABCG2 secretes endogenous substrates in the adrenal gland, excretes toxins in the liver and kidneys, and regulates absorption of substrates. | ||
<ref name="Fetsch">PMID:15990223</ref> | <ref name="Fetsch">PMID:15990223</ref> | ||
== Relevance == | |||
By utilizing certain binders (<scene name='83/832939/5d3-fab/2'>5D3</scene>), it is able to be stabilized for crystallographic imaging.<ref name="Taylor">PMID:28554189</ref> This has allowed researchers in the past decade to make advances based upon the greater understanding of its structure. Using these advances, inhibitors have been found to stop effluxion by ABCG2. Completely inhibiting this function, however, has residual effects on the excretory system. One such effect is decreased uric acid excretion in both the kidneys and the gut, which causes hyperuricemia. This results in an increased risk of uric acid crystal build-up, known as tophi formation, which causes a type of arthritis known as gout. Balancing the inhibition of ABCG2 will determine how to lessen these effects while continuing to combat cancer resistivity.<ref name="Cleophas">PMID:28461764</ref> See also: | |||
*[https://en.wikipedia.org/wiki/Hyperuricemia Hyperuricemia at Wikipedia] | |||
*[https://en.wikipedia.org/wiki/Gout Gout at Wikipedia] | |||
*[https://en.wikipedia.org/wiki/Tophus Tophus at Wikipedia] | |||
== Disease == | == Disease == | ||
One of the causes for multidrug resistant cancers is the excretion of cancer drugs out of the cell, thereby decreasing the effective intracellular concentration. ABCG2, also known as the breast cancer resistance protein (BCRP), effluxes multiple chemotherapeutic agents such as mitoxantrone and camptothecin analogies, making the cancerous breast cells resistant to chemotherapy. Competitive inhibitors, such as <scene name='83/832939/Abcg2_bound_to_mz29/3'>MZ29</scene>, that shut down ABCG2 to stop the efflux of cancer drugs in order to combat the resistivity of breast cancer. <ref>[ https://en.wikipedia.org/wiki/ABCG2 "ABCG2 -." Wikipedia, the Free Encyclopedia. Web. 20 Apr. 2020].</ref><ref name=”Jackson”>PMID:29610494</ref> See also: | |||
*[https://en.wikipedia.org/wiki/Mitoxantrone Mitoxantrone at Wikipedia] | |||
*[https://en.wikipedia.org/wiki/Camptothecin Camptothecin at Wikipedia] | |||
== 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]] | ||
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</StructureSection> | </StructureSection> | ||
==References== | ==References== | ||
<References/> | <References/> | ||
==Student Contributors== | ==Student Contributors== | ||
