What is the ABCG2 gene?
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 is a BCRP inhibitor?
BCRP inhibitors include, among others, fumitremorgin C (FTC), the FTC analogue Ko143, the acridone carboxamide derivative GF120918, anti-HIV protease inhibitors nelfinavir and ritonavir, the dietary flavonoids chrysin and biochanin A, the tyrosine kinase inhibitors gefitinib and imatinib [5, 16, 36], and herb extracts …
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 | ||
| View/Edit Human View/Edit Mouse |
What is the role of BCRP?
BCRP physiologically functions as a part of a self-defense mechanism for the organism; it enhances elimination of toxic xenobiotic substances and harmful agents in the gut and biliary tract, as well as through the blood-brain, placental, and possibly blood-testis barriers.
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 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 human MDR1?
The human MDR1 gene encodes an integral membrane protein, P glycoprotein (Pgp), whose function is the energy dependent export of substances from the inside of cells, and from membranes, to the outside. Its physiological role is the protection of cells from toxic substances or metabolites.
Where is ABCA1 located?
The ABCA1 protein is produced in many tissues, with high amounts found in the liver and in immune system cells called macrophages. This protein moves cholesterol and certain fats called phospholipids across the cell membrane to the outside of the cell.
Where is BCRP found?
The highest BCRP expression and function were found in stem-like CD34+/CD38− cells in both normal and AML marrows.
What does BCRP stand for?
ABCG2, more commonly referred to as BCRP (Breast Cancer Resistance Protein), is an efflux transporter that serves two major drug transport functions. Firstly, it restricts the distribution of its substrates into organs such as the brain, testes, placenta, and across the gastrointestinal tract (GIT).
What drugs are P gp inhibitors?
Examples of drugs that are substrates of P-gp efflux pump include: Apixaban, colchicine, cyclosporine, dabigatran, digoxin, edoxaban, rivaroxaban, and tacrolimus. The degree of effect on P-gp substrate serum concentration may be altered by dose and timing of orally administered P-gp inhibitor or inducer.
What is ABCB1 transporter?
The ATP-binding cassette (ABC) transporter protein ABCB1 (P-glycoprotein) is known for its involvement in multidrug resistance (MDR) of tumor cells by preventing intracellular accumulation of cytotoxic drugs.
What is the function of MDR1?
What does CD34+ and CD38+ mean?
Cells observed as CD34+ and CD38- are of an undifferentiated, primitive form; i.e., they are multipotential hemopoietic stem cells. Thus, because of their CD34+ expression, such undifferentiated cells can be sorted out. In tumors, CD34 is found in alveolar soft part sarcoma, preB-ALL (positive in 75%), AML (40%),…
What is the function of CD33?
Function. CD33 can be stimulated by any molecule with sialic acid residues such as glycoproteins or glycolipids. Upon binding, the immunoreceptor tyrosine-based inhibition motif (ITIM) of CD33, present on the cytosolic portion of the protein, is phosphorylated and acts as a docking site for Src homology 2…
What is CD157 and CD38?
CD38 is a paralog of CD157, which is also located on chromosome 4 (4p15) in humans. CD38 was first identified in 1980 as a surface marker ( cluster of differentiation) of thymus cell lymphocytes. In 1992 it was additionally described as a surface marker on B cells, monocytes, and natural killer cells (NK cells).
What is the tissue distribution of CD34+ cells?
Tissue distribution. Cells expressing CD34 (CD34 + cell) are normally found in the umbilical cord and bone marrow as hematopoietic cells, or in mesenchymal stem cells, endothelial progenitor cells, endothelial cells of blood vessels but not lymphatics (except pleural lymphatics), mast cells, a sub-population of dendritic cells…