What are BCRP substrates?
BCRP SUBSTRATES Substrates of BCRP initially were reported to be a wide range of chemotherapeutics such as mitoxantrone, camptothecin derivates, flavopiridol, and methotrexate (1). Notably, several TKIs such as imatinib, gefitinib, and nilotinib are BCRP substrates (1,13).
What does ABCG2 do?
The ABCG2 gene belongs to a group of genes called the ATP-binding cassette family; genes in this family provide instructions for making proteins that transport molecules across cell membranes. In the intestines, the ABCG2 protein helps release (secrete) a substance called urate into the urine.
What are ABCG2 pump inhibitors?
A natural flavonoid found in foods and natural supplement products. An estrogen used to treat perimenopausal and postmenopausal symptoms. An HIV protease inhibitor used in combination with other antiretroviral agents for the treatment of HIV-1 with advanced immunodeficiency.
What is ABCG2 transporter?
ABCG2 is a constitutively expressed ATP-binding cassette (ABC) transporter that protects many tissues against xenobiotic molecules. Its activity affects the pharmacokinetics of commonly used drugs and limits the delivery of therapeutics into tumour cells, thus contributing to multidrug resistance.
Where is ABCG2 located?
ABCG2 is a translocation protein used to actively pump drugs and other compounds against their concentration gradient using the bonding and hydrolysis of ATP as the energy source….
| ABCG2 | ||
|---|---|---|
| Location (UCSC) | Chr 4: 88.09 – 88.23 Mb | Chr 6: 58.56 – 58.67 Mb |
| PubMed search | ||
| Wikidata | ||
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Where is ABCG2 expressed?
In normal human tissues, ABCG2 is prominently expressed in placental syncytiotrophoblasts, epithelium of small intestine and colon, liver canalicular membranes, and ducts and lobules of mammary tissue [23].
How do ABC transporters move molecules?
One of the largest classes of transporters is the ABC (ATP binding cassette) transporter superfamily8–10. These transporters use the binding and hydrolysis of ATP to power the translocation of a diverse assortment of substrates, ranging from ions to macromolecules, across membranes.
What is another name for ABCA1?
ABCA1, also known as cholesterol efflux regulatory protein (CERP), functions as a cholesterol membrane transporter involved in the regulation of cellular cholesterol and phospholipid homeostasis. It has been shown that ABCA1 mediates the traffic of lipids between Golgi and cell membrane.
What is OATP1B1 substrate?
OATP1B1 is an uptake transporter exclusively expressed on the sinusoidal side of hepatocytes. It is responsible for the hepatic uptake of drugs and endogenous compounds from the blood. OATP1B1 substrates often, but by no means always, contain a carboxylic acid moiety.
What are SLCO1B1 drugs?
SLCO1B1 (solute carrier organic anion transporter family member 1B1) is a drug transporter that helps the body get rid of certain medicines through the liver.