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ATP-Binding Cassette Subfamily G

ATP-binding cassette subfamily G (ABCG family) is a class of transport proteins that consist of a single ABC cassette in the amino-terminal followed by six putative transmembrane domains. There are five members: ABCG1, ABCG2, ABCG4, ABCG5, and ABCG8. To become functionally active, ABCG1, ABCG2, and ABCG4 form homodimers, and ABCG5 and ABCG8 form obligate heterodimers. They function as cholesterol transporters except for ABCG2. ABCG1 and ABCG4 are involved in the reverse cholesterol transport from macrophage to the liver and ABCG5 as well as ABCG8 regulate the biliary excretion of cholesterol. Although ABCG2 is not involved in the cholesterol transporters, it plays an essential role in the pharmacokinetics of drugs in the clearance organs and tissue barriers due to its broad substrate specificity to xenobiotic compounds.

The five members of the ABCG family is encoded by different genes, ABCG1, ABCG2, ABCG4, ABCG5 and ABCG8 respectively. Except for ABCG5, and ABCG8 (2p21), other members genes of ABCG family are located in different sites of the chromosome (ABCG1: 21q22.3; ABCG2: 4q22.1; ABCG4: 11q23.3). Hence, the five members of ABCG family present some differences in expression pattern and functions. The following table shows five members of ABCG family.

Human ABCG Family Members
ABCG1 ABCG2 ABCG4 ABCG5 ABCG8

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