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Introduction
Function
[1]
ABCG2 transports a variety of substrates, 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.
Disease
Relevance
Structural highlights
Nature_Structural_&_Molecular_Biology_Vol_25
[2]
Multidrug Transporter ABCG2 is a that consists of two cavities separated by a . Cavity 1 is a binding pocket open to the cytoplasm and the inner leaflet of the plasma membrane. Its shape is suitable to bind flat, hydrophobic and polycyclic substrates. Many of its amino acids residues form hydrophobic interactions with the bound substrate, as shown in green in Figure 1. Cavity 2 is located above the leucine plug. It is empty until a are bound to ABCG2. promote the release of the substrate from the cavity into the extracellular space.