ABCG2: Difference between revisions

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{{Short description|An article about the ABCG2 protein}}
{{DISPLAYTITLE:ABCG2}}
{{DISPLAYTITLE:ABCG2}}


==ABCG2==
== Overview ==
[[File:ABCG2 with plasma membrane.jpg|thumb|right|ABCG2 protein embedded in the plasma membrane]]
[[File:ABCG2_with_plasma_membrane.jpg|thumb|right|Diagram of ABCG2 in the plasma membrane]]
'''ABCG2''' (ATP-binding cassette sub-family G member 2) is a protein that in humans is encoded by the '''ABCG2''' gene. It is a member of the [[ATP-binding cassette transporter]] family, which is involved in the transport of various molecules across extra- and intracellular membranes.


'''ABCG2''', also known as the '''ATP-binding cassette sub-family G member 2''', is a protein that in humans is encoded by the ''ABCG2'' gene. It is a member of the [[ATP-binding cassette transporter|ATP-binding cassette (ABC) transporter]] family, which is involved in the transport of various molecules across extra- and intracellular membranes.
== Structure ==
ABCG2 is a half-transporter, meaning it consists of a single [[transmembrane domain]] and a single [[nucleotide-binding domain]]. It functions as a homodimer or homotetramer to transport substrates across the [[cell membrane]].


==Structure==
== Function ==
ABCG2 is a half-transporter, meaning it consists of a single [[transmembrane domain]] and a single [[nucleotide-binding domain]]. It functions as a homodimer, with two identical ABCG2 proteins associating to form a functional transporter. The protein is embedded in the [[plasma membrane]], where it plays a crucial role in the efflux of substrates out of the cell.
ABCG2 plays a critical role in the [[efflux]] of xenobiotics and endogenous substrates from cells. It is known to transport a wide variety of substrates, including [[drugs]], [[metabolites]], and [[lipids]]. This transporter is highly expressed in the [[placenta]], [[liver]], [[intestine]], and [[blood-brain barrier]], where it contributes to the protection of tissues from toxic substances.


==Function==
== Clinical Significance ==
ABCG2 is known for its role in the [[multidrug resistance]] phenomenon, where it actively transports a variety of drugs and xenobiotics out of cells, thereby reducing their intracellular concentrations. This function is particularly important in [[cancer]] cells, where overexpression of ABCG2 can lead to resistance to chemotherapy drugs.
ABCG2 is associated with [[multidrug resistance]] in cancer therapy. Overexpression of ABCG2 in cancer cells can lead to decreased intracellular accumulation of chemotherapeutic agents, resulting in treatment failure. It is also involved in the pharmacokinetics of various drugs, affecting their absorption, distribution, and elimination.


In addition to its role in drug resistance, ABCG2 is involved in the transport of physiological substrates, including [[heme]], [[porphyrins]], and [[steroid hormone|steroid hormones]]. It is expressed in various tissues, including the [[liver]], [[intestine]], [[placenta]], and [[blood-brain barrier]], where it contributes to the protection of tissues from toxic substances.
== Genetic Variants ==
Several [[single nucleotide polymorphisms]] (SNPs) in the ABCG2 gene have been identified, which can influence the function of the transporter. These genetic variants can affect drug response and toxicity, making ABCG2 an important consideration in [[personalized medicine]].


==Clinical significance==
== Research ==
Mutations in the ''ABCG2'' gene can lead to altered function of the protein, which may result in various clinical conditions. For example, certain polymorphisms in ''ABCG2'' are associated with increased risk of [[gout]], due to impaired excretion of [[uric acid]].
Ongoing research is focused on understanding the regulation of ABCG2 expression and function, as well as its role in drug resistance and [[pharmacogenomics]]. Inhibitors of ABCG2 are being investigated as potential adjuvants in cancer therapy to overcome drug resistance.


ABCG2 is also a target for overcoming drug resistance in cancer therapy. Inhibitors of ABCG2 are being investigated as potential adjuvants to chemotherapy, aiming to increase the effectiveness of anticancer drugs by preventing their efflux from cancer cells.
== Related Pages ==
 
==Research==
Ongoing research is focused on understanding the detailed mechanisms of substrate recognition and transport by ABCG2, as well as its regulation and expression in different tissues. Structural studies using techniques such as [[X-ray crystallography]] and [[cryogenic electron microscopy]] are providing insights into the conformational changes that occur during the transport cycle.
 
==Related pages==
* [[ATP-binding cassette transporter]]
* [[ATP-binding cassette transporter]]
* [[Multidrug resistance]]
* [[Multidrug resistance]]
* [[Cancer therapy]]
* [[Pharmacogenomics]]
* [[Drug metabolism]]
* [[Cell membrane]]


[[Category:Transport proteins]]
[[Category:Genes on human chromosome 4]]
[[Category:ATP-binding cassette transporters]]
[[Category:ATP-binding cassette transporters]]
[[Category:Membrane proteins]]
[[Category:Human proteins]]

Latest revision as of 11:59, 15 February 2025


Overview[edit]

File:ABCG2 with plasma membrane.jpg
Diagram of ABCG2 in the plasma membrane

ABCG2 (ATP-binding cassette sub-family G member 2) is a protein that in humans is encoded by the ABCG2 gene. It is a member of the ATP-binding cassette transporter family, which is involved in the transport of various molecules across extra- and intracellular membranes.

Structure[edit]

ABCG2 is a half-transporter, meaning it consists of a single transmembrane domain and a single nucleotide-binding domain. It functions as a homodimer or homotetramer to transport substrates across the cell membrane.

Function[edit]

ABCG2 plays a critical role in the efflux of xenobiotics and endogenous substrates from cells. It is known to transport a wide variety of substrates, including drugs, metabolites, and lipids. This transporter is highly expressed in the placenta, liver, intestine, and blood-brain barrier, where it contributes to the protection of tissues from toxic substances.

Clinical Significance[edit]

ABCG2 is associated with multidrug resistance in cancer therapy. Overexpression of ABCG2 in cancer cells can lead to decreased intracellular accumulation of chemotherapeutic agents, resulting in treatment failure. It is also involved in the pharmacokinetics of various drugs, affecting their absorption, distribution, and elimination.

Genetic Variants[edit]

Several single nucleotide polymorphisms (SNPs) in the ABCG2 gene have been identified, which can influence the function of the transporter. These genetic variants can affect drug response and toxicity, making ABCG2 an important consideration in personalized medicine.

Research[edit]

Ongoing research is focused on understanding the regulation of ABCG2 expression and function, as well as its role in drug resistance and pharmacogenomics. Inhibitors of ABCG2 are being investigated as potential adjuvants in cancer therapy to overcome drug resistance.

Related Pages[edit]