What does ABCG2 do?
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 pumps?
ATP-binding cassette (ABC), sub-family G, isoform 2 protein (ABCG2, also known as breast cancer resistance protein, BCRP) is a drug efflux pump and an important member of the ABC transporter superfamily. ABCG2 was identified independently by three separate groups in 1998 and 1999 [3–5].
Where is ABCG2 located?
10.26. ABCG2 is located on human chromosome 4q22 (Allikmets et al., 1998); the gene spans approximately 66 kb and has 16 exons, encoding 655 amino acid residues (Bailey-Dell et al., 2001). BCRP shares about 25% amino acid identity with ABCG5 and ABCG8.
What is the full name of BCRP?
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 does ABCB1 gene do?
ABCB1 is an environment susceptible gene that codes for P-glycoprotein (P-gp). P-gp is responsible for multidrug resistance during chemotherapy of breast cancer. Six different non-synonymous Single Nucleotide Polymorphism (nsSNPs) of human ABCB1 gene were found in COSMIC database.
What drugs are P glycoprotein inhibitors?
Some common pharmacological inhibitors of P-glycoprotein include: amiodarone, clarithromycin, ciclosporin, colchicine, diltiazem, erythromycin, felodipine, ketoconazole, lansoprazole, omeprazole and other proton-pump inhibitors, nifedipine, paroxetine, reserpine, saquinavir, sertraline, quinidine, tamoxifen, verapamil.
What are BCRP inhibitors?
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 …
Is pantoprazole a BCRP inhibitor?
In Sf9-BCRP vesicles, pantoprazole and omeprazole inhibited MTX transport (IC50 13 microm and 36 microm, respectively).
How does ABCB1 work?
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.
Which is an important substrate specificity for ABCG2?
ABCG2 has a broad substrate specificity and is one of the most important efflux proteins modulating pharmacokinetics of drugs, nutrients and toxicokinetics of toxicants. ABCG2 is an important player in transporter-mediated drug-drug interactions (tDDI). Areas covered: The aims of the review are i) t …
How is ABCG2 overexpression related to cancer treatment?
ABCG2 overexpression can render the cancer cells resistant to the ABCG2 substrate chemotherapy agents, such as mitoxantrone, doxorubicin, SN-38, and several TKIs. To the best of our knowledge, no published clinical trial has ever succeeded in reversing the ABCG2-mediated MDR.
Where is ABCG2 found in the human body?
Moreover, in the normal tissues, ABCG2 is expressed on the apical membranes and plays a pivotal role in tissue protection against various xenobiotics. For this reason, ABCG2 is recognized to be an important determinant of the pharmacokinetic characteristics of its substrate drugs.
Which is an exogenous substrate of ABCG2 efflux pump?
As an efflux pump exhibiting a broad substrate specificity localized on cellular plasma membrane, ABCG2 excretes a variety of endogenous and exogenous substrates including chemotherapeutic agents, such as mitoxantrone and several tyrosine kinase inhibitors.
