Sandbox Reserved 1606: Difference between revisions
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===Cavities and Leucine Plug=== | ===Cavities and Leucine Plug=== | ||
[[Image: | [[Image:Cavities_and_leucine_plug_abcg2.png|250 px|right|thumb|Figure 2. Locations of Cavities 1 and 2 and the Leucine Plug in ABCG2. The protein is in the inward-facing conformation with Cavity 1 open to the cytosol for substrate recruitment, the Leucine Plug is intact, and Cavity 2 is completely occluded. [https://www.rcsb.org/structure/5NJ3 (5NJ3)]]] | ||
Substrates are transported through ABCG2 via two cavities separated by a leucine plug (Figure 2). <scene name='83/832932/Cavity_1_zoom_out/2'>Cavity 1</scene> acts as a multidrug binding pocket and is formed by helices at the interface of the monomers in the TMD. When ATP is not bound to the NBDs, Cavity 1 is <scene name='83/832932/Overall_structure_cavity_1hel/3'>open to the cytosol</scene> in order to recruit substrates for transport. Cavity 1 is <scene name='83/832932/Cavity_1_narrow_surface/4'>narrow</scene> and full of nonpolar, hydrophobic residues and, as a result, prefers nonpolar, hydrophobic substrates, particularly flat, polycyclic molecules. Substrates, such as estrone sulfate, <scene name='83/832932/Cavity_1_-_use2/4'>form hydrogen bonds and stacking interactions</scene> with residues from each subunit in Cavity 1.<ref name="Taylor"/> | Substrates are transported through ABCG2 via two cavities separated by a leucine plug (Figure 2). <scene name='83/832932/Cavity_1_zoom_out/2'>Cavity 1</scene> acts as a multidrug binding pocket and is formed by helices at the interface of the monomers in the TMD. When ATP is not bound to the NBDs, Cavity 1 is <scene name='83/832932/Overall_structure_cavity_1hel/3'>open to the cytosol</scene> in order to recruit substrates for transport. Cavity 1 is <scene name='83/832932/Cavity_1_narrow_surface/4'>narrow</scene> and full of nonpolar, hydrophobic residues and, as a result, prefers nonpolar, hydrophobic substrates, particularly flat, polycyclic molecules. Substrates, such as estrone sulfate, <scene name='83/832932/Cavity_1_-_use2/4'>form hydrogen bonds and stacking interactions</scene> with residues from each subunit in Cavity 1.<ref name="Taylor"/> | ||
